i/r

(R)-CSN5i-3 is CSN5i-3 of the R configuration.

Carubicin is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis.

Notoginsenoside R1 (Sanchinoside R1) has been shown to exhibit antioxidant, antiapoptotic, anti-inflammatory, and immune-stimulatory properties.

Floctafenine (R-4318) is an orally available nonsteroidal anti-inflammatory compound that is a COX-I and COX-2 inhibitor and interferes with the antiplatelet effects of aspirin.Floctafenine has analgesic activity and is used in the study of pain.

Sinapinic Acid (Synapoic acid) protects the rat liver from CCl4-induced inflammation, most likely by acting as a free radical scavenger and modulator of NF-κB p65 activation and proinflammatory cytokine expression. Sinapic acid with antioxidant role protects cardiac cells and its functions from I/R induced oxidative stress. Sinapic acid is a potentially useful agent for the protection against liver fibrosis and cirrhosis. Sinapic acid prevents the alterations in the levels of lipids and lipoproteins by virtue of its anti-lipidaemic effect in isoproterenol induced myocardial infarcted rats. Sinapic acid ameliorates hyperglycemia through PLC-PKC signals to enhance the glucose utilization in diabetic rats.

Luteolinidin chloride is a natural product. It is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.

Polyphyllin D induces apoptosis via the mitochondrial apoptotic pathway as evidenced by decreased Bcl-2 expression levels, disruption of MMP and increased Bax, cytochrome C, and cleaved-caspase-3 levels. Polyphyllin D has an anti-angiogenic effect. Polyphyllin D has toxicity in human RBCs as well as its underlying mechanism for the hemolysis and eryptosis/erythroptosis. Polyphyllin D has strong anticancer activity, can overcome drug resistance in R-HepG2 cells and elicit programmed cell death via mitochondrial dysfunction.

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I/R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1/2, p38, and JNK1/2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

1. Vitexin has antinociceptive and antispasmodic activities. 2. Vitexin exhibits a prominent first-pass effect. 3. Vitexin has antioxidant, antimyeloperoxidase, and α-glucosidase inhibitory activities. 4. Vitexin can either inhibit or induce activities of

1-Heptadecanoyl-rac-glycerol is a monoacylglycerol that contains heptadecanoic acid at the sn-1 position. It is active against the bacteria E. aerogens, E. cloacae, P. mirabilis, and S. faecalis (MIC = 78 μg/ml for all).1 1-Heptadecanoyl-rac-glycerol has been found in T. africana, I. sonorae, and wheat bran.1,2,3 |1. Kuete, V., Metuno, R., Ngameni, B., et al. Antimicrobial activity of the methanolic extracts and compounds from Treculia africana and Treculia acuminata (Moraceae). S. Afr. J. Bot. 74(1), 111-115 (2008).|2. Fernández-Galicia, E., Calada, F., Roman-Romos, R., et al. Monoglycerides and fatty acids from Ibervillea sonorae root: Isolation and hypoglycemic activity. Planta Med. 73(3), 236-240 (2007).|3. Prinsen, P., Gutiérrez, A., Faulds, C.B., et al. Comprehensive study of valuable lipophilic phytochemicals in wheat bran. J. Agric. Food Chem. 62(7), 1664-1673 (2014).

C22 dihydro 1-Deoxyceramide (m18:0/22:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C22 dihydro 1-Deoxyceramide (m18:0/22:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found as the most prevalent dihydro deoxyceramide species in mouse brain, spinal cord, and sciatic nerve at one, three, and six months of age.4 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Alecu, I., Tedeschi, A., Behler, N., et al. Localization of 1-deoxysphingolipids to mitochondria induces mitochondrial dysfunction. J. Lipid. Res. 58(1), 42-59 (2017).|4. Schwartz, N.U., Mileva, I., Gurevich, M., et al. Quantifying 1-deoxydihydroceramides and 1-deoxyceramides in mouse nervous system tissue. Prostaglandins Other Lipid Mediat. 141, 40-48 (2019).

Carbazomycin A is a bacterial metabolite that has been found in Streptomyces and has diverse biological activities.1,2It is active againstS. aureus,T. asteroides, andT. mentagrophytes(MIC = 12.5 μg/ml for all), as well as the plant pathogenic fungusP. oryzae(MIC = 25 μg/ml). Carbazomycin A is cytotoxic to MCF-7, KB, NCI H187, and Vero cells (IC50s = 26.2, 30.1, 18.4, and 32.6 μg/ml, respectively).2 1.Sakano, K.-I., Ishimaru, K., and Nakamura, S.New antibiotics, carbazomycins A and B. I. Fermentation, extraction, purification and physico-chemical and biological propertiesJ Antibiot. (Tokyo)33(7)683-689(1980) 2.Intaraudom, C., Rachtawee, P., Suvannakad, R., et al.Antimalarial and antituberculosis substances from Streptomyces sp. BCC26924Tetrahedron67(39)7593-7597(2011)

3-hydroxy Palmitic acid methyl ester (3-hydroxy PAME) is an esterized long-chain fatty acid involved in quorum sensing in R. solanacearum, a bacteria that causes lethal wilting in plants. 3-hydroxy-PAME (175 nM) increases levels of PhcA-regulated virulence factors, greater than 20-, 30-, and 25-fold for EPS I, EGL, and PME, respectively, in the AW1-83 strain of R. solanacearum.

1-Deoxysphingosine (m18:1(4E)) is an atypical sphingolipid that contains a double bond at the 4E native position and is formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 Plasma levels of 1-deoxysphingosine (m18:1(4E)) are increased in patients with chronic idiopathic axonal neuropathy (CIAP) and diabetic distal symmetrical polyneuropathy (DSPN).3 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Hube, L., Dohrn, M.F., Karsai, G., et al. Metabolic syndrome, neurotoxic 1-deoxysphingolipids and nervous tissue inflammation in chronic idiopathic axonal polyneuropathy (CIAP). PLoS One 12(1):e0170583, (2017).

(S)-Salsolidine, a chemical compound, functions as a weak inhibitor of monoamine oxidase (MAO), exhibiting an inhibition constant (K i ) of 63 μM. R enantiomer demonstrating a greater efficacy than (S)-Salsolidine, boasting a K i value of 26 μM compared to the S form.

Echinatin exerts a protective effect against ischemia/reperfusion (I/R)-induced myocardial injury on hearts, this effect may be attributed to the antioxidant and anti-inflammatory activities of this compound. Echinatin can inhibit DNP-ATPase activity whil

Tricarbonyldichlororuthenium(II) dimer, a pharmacological CO donor, prevents ischemia/reperfusion (I/R)-induced oxidative damage to the gastric mucosa by enhancing gastric blood flow (GBF) and reducing DNA oxidation and systemic inflammatory response.

Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.

RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage. It alleviates acute kidney injury by attenuating Cisplatin- and I/R-induced kidney damage, along with associated inflammatory responses and necroptosis [1].

C24 dihydro 1-Deoxyceramide (m18:0/24:0) is a very long-chain atypical ceramide containing a 1-deoxysphinganine backbone. 1-Deoxysphingolipids are formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 C24 dihydro 1-Deoxyceramide (m18:0/24:0) has been found in mouse embryonic fibroblasts (MEFs) following application of 1-deoxysphinganine alkyne or 1-deoxysphinganine-d3.3 It has also been found in mouse brain, spinal cord, and sciatic nerve at one, three, and six months of age.4 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemical structure of native 1-deoxysphingosine. J. Lipid Res. 57(7), 1194-1203 (2016).|2. Alecu, I., Othman, A., Penno, A., et al. Cytotoxic 1-deoxysphingolipids are metabolized by a cytochrome P450-dependent pathway. J. Lipid Res. 58(1), 60-71 (2017).|3. Alecu, I., Tedeschi, A., Behler, N., et al. Localization of 1-deoxysphingolipids to mitochondria induces mitochondrial dysfunction. J. Lipid. Res. 58(1), 42-59 (2017).|4. Schwartz, N.U., Mileva, I., Gurevich, M., et al. Quantifying 1-deoxydihydroceramides and 1-deoxyceramides in mouse nervous system tissue. Prostaglandins Other Lipid Mediat. 141, 40-48 (2019).

Anti-MI/R injury agent 1 (compound 18), derived from Panaxatriol, represents an orally administered, potent agent against myocardial ischemia/reperfusion (MI/R) injury. It improves cell viability in cardiomyocytes subjected to oxygen-glucose deprivation and reperfusion (OGD/R)-induced injury. Furthermore, this compound significantly reduces myocardial infarction size, diminishes levels of circulating cardiac troponin I (cTnI), and mitigates cardiac tissue damage in rat models [1].

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan is an agent-linker conjugate for antibody-drug conjugates (ADCs), incorporating Exatecan, a DNA Topoisomerase I inhibitor (IC 50 = 2.2 μM) [1].

RSVA405 is an AMPK activator (EC50 = 1 μM), and is STAT3 inhibitor

Ipratropium bromide monohydrate (Ipratropium bromide hydrate) is a muscarinic antagonist structurally related to ATROPINE but often considered safer and more effective for inhalation use. It is used for various bronchial disorders, in rhinitis, and as an antiarrhythmic.

Harzianopyridone is an atpenin-like compound that functions as an inhibitor of mammalian and nematode mitochondrial complex II, also known as succinate:ubiquinone oxidoreductase (SQR), demonstrating IC50 values of 0.017, 0.2, and 2 μM against bovine, rat, and nematode complex II, respectively. Additionally, it inhibits nematode quinol-fumarate reductase (QFR) with an IC50 value of 0.36 μM. Significantly selective for complex II over complexes I and III in rats and cattle, as well as complex I in nematodes, with IC50 values exceeding 100 μM, it exhibits notable antibacterial and antifungal properties, with EC50 values of 35.9, 42.2, 60.4, and 50.2 μg/ml against R. solani, S. rolfsii, M. phaseolina, and F. oxysporum, respectively.

CU-32 is an inhibitor of cyclic GMP-AMP (cGAMP) synthase (cGAS; IC50= 0.45 μM).1It reduces DNA-, but not Sendai virus-, induced dimerization of IFN regulatory factor 3 in THP-1 cells, indicating selectivity for the cGAS DNA sensing pathway over the RIG-I-MAVS RNA sensing pathway. It is also selective for cGAS over toll-like receptors (TLRs) at 50 μM. CU-32 decreases IFN-stimulatory DNA-induced production of IFN-β in THP-1 cells when used at concentrations of 10, 30, and 100 μM. 1.Padilla-Salinas, R., Sun, L., Anderson, R., et al.Discovery of small-molecule cyclic GMP-AMP synthase inhibitorsJ. Org. Chem.85(3)1579-1600(2020)

5-HT7R antagonist 1 (free base) is a G protein-biased antagonist for the 5-HT 7 R receptor, with a dissociation constant (K i) of 6.5 nM.

R 59-022 hydrochloride (DKGI-I hydrochloride) is a 5-HT Receptor antagonist that activates protein kinase C (PKC).R 59-022 hydrochloride is a DGK inhibitor (IC50:2.8 µM) that inhibits the phosphorylation of OAG to OAPA.R 59-022 enhances thrombin-induced triglyceride production in platelets and inhibits the production of phosphatidic acid in neutrophils. R 59-022 enhances thrombin-induced diglyceride production in platelets and inhibits phosphatidic acid production in neutrophils.

Carbonic anhydrase inhibitor 8 (compound R-13) is a potent human carbonic anhydrase (hCA). Carbonic anhydrase inhibitor 8 shows K i values of 60.7 nM, 320.7 nM, 2298 nM for hCA I, hCA II, hCA IV, respectively.

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003). 3-Hydroxyterphenyllin is a p-terphenyl fungal metabolite originally isolated from A. candidus that has diverse biological activities, including antioxidant, antiproliferative, antibacterial, and antiviral properties.1,2,3,4 It has a 96% scavenging effect on 2,2-diphenyl-1-picrylhydrazyl radicals when used at a concentration of 100 μg/ml.2 3-Hydroxyterphenyllin inhibits the growth of HeLa cervical, A549 lung, and HepG2 liver cancer cells (IC50s = 23, 36, and 32 μM, respectively), as well as methicillin-resistant S. aureus (MRSA) and V. vulnificus bacteria (MIC = 31 μg/ml for both).3 It also inhibits HIV-1 integrase in both coupled and strand transfer assays (IC50s = 2.8 and 12.1 μM, respectively).4 References1. Kurobane, I., Vining, L.C., McInnes, A.G., et al. 3-Hydroxyterphenyllin, a new metabolite of Aspergillus candidus. Structure elucidation by 1H and 13C nuclear magnetic resonance spectroscopy. J. Antibiot. (Tokyo) 32(6), 559-564 (1979).2. Yen, G.-C., Chang, Y.-C., Sheu, F., et al. Isolation and characterization of antioxidant compounds from Aspergillus candidus broth filtrate. J. Agric. Food Chem. 49(3), 1426-1431 (2001).3. Wang, W., Liao, Y., Tang, C., et al. Cytotoxic and antibacterial compounds from the coral-derived fungus Aspergillus tritici SP2-8-1. Mar. Drugs 15(11), E348 (2017).4. Singh, S.B., Jayasuriya, H., Dewey, R., et al. Isolation, structure, and HIV-1-integrase inhibitory activity of structurally diverse fungal metabolites. J. Ind. Microbiol. Biotechnol. 30(12), 721-731 (2003).

Nitrosoglutathione (GSNO) is an endogenous transnitrosation donor involved in S-nitrosation of a variety of cellular proteins. GSNO, an exogenous NO donor and substrate of rat alcohol dehydrogenase class III isoenzyme, inhibits cerebral angiotensin II-dependent and -independent AT1 receptor responses.

1. Methylophiopogonanone A has anti-inflammatory and anti-oxidative properties. 2. Methylophiopogonanone A has therapeutic potential against cerebral I/R injury through its ability to attenuate BBB disruption by regulating the expression of MMP-9 and tigh

Human carbonic anhydrase II-IN-24 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor. Human carbonic anhydrase II-IN-24 shows K i s of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively.

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.

Stipuleanoside R1 is a natural product for research related to life sciences. The catalog number is TN5997 and the CAS number is 96627-79-1.

ADRA1D receptor antagonist 1 (free base) antagonist ( K i =1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC 30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

Compound R-13, also known as hCAII-IN-7, is a powerful inhibitor of human carbonic anhydrase (hCA), exhibiting inhibition constants (Ki) of 60.7 nM for hCA I, 320.7 nM for hCA II, 2298 nM for hCA IV, and 35.2 nM for hCA IX, respectively [1].

Ipratropium Bromide (Sch 1000) is a synthetic anticholinergic agent that is used as an inhalant for treatment of acute bronchospasm due to chronic bronchitis and emphysema.

Pal-KTTKS is a lipidated pentapeptide consisting of a fragment of the type I collagen C-terminal propeptide conjugated to palmitic acid .1 It increases collagen production in human corneal and dermal fibroblasts when used at concentrations of 0.002, 0.004, and 0.008 wt%.2 Following topical administration, pal-KTTKS (50 μg/cm2) is found in the stratum corneum, epidermis, and dermis of isolated hairless mouse skin.1 It can self-assemble into flat tapes and extended fibrillar structures.3 Pal-KTTKS has been detected in anti-wrinkle creams.4 |1. Choi, Y.L., Park, E.J., Kim, E., et al. Dermal stability and in vitro skin permeation of collagen pentapeptides (KTTKS and palmitoyl-KTTKS). Biomol. Ther. (Seoul) 22(4), 321-327 (2014).|2. Jones, R.R., Castelletto, V., Connon, C.J., et al. Collagen stimulating effect of peptide amphiphile C16-KTTKS on human fibroblasts. Mol. Pharm. 10(3), 1063-1069 (2013).|3. Castelletto, V., Hamley, I.W., Whitehouse, C., et al. Self-assembly of palmitoyl lipopeptides used in skin care products. Langmuir 29(29), 9149-9155 (2013).|4. Chirita, R.-I., Chaimbbault, P., Archambault, J.-C., et al. Development of a LC-MS/MS method to monitor palmitoyl peptides content in anti-wrinkle cosmetics. Anal. Chim. Acta 641(1-2), 95-100 (2009).

MC1742 is an inhibitor of class I histone deacetylases (HDACs; IC50s = 0.1, 0.11, 0.02, and 0.61 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 7 and 40 nM for HDAC6 and HDAC10, respectively).1 It is selective for class I and class IIb over class IIa HDACs (IC50s = >50 μM for HDAC4, -5, -7, and -9). MC1742 reduces proliferation of HOS, MG-63, RD, A204, SK-ES-1, and A673 sarcoma cancer stem cells (CSCs). It increases levels of acetylated histone H3 and acetylated tubulin and induces apoptosis in MG-63 CSCs when used at a concentration of 2 μM. MC1742 also reactivates HIV-1 in JLAT 10.6 latently infected cells (EC50 = 350 nM).2 |1. Di Pompo, G., Salerno, M., Rotili, D., et al. Novel histone deacetylase inhibitors induce growth arrest, apoptosis, and differentiation in sarcoma cancer stem cells. J. Med. Chem. 58(9), 4073-4079 (2015).|2. Heffern, E.F.W., Ramani, R., Marshall, G., et al. Identification of isoform-selective hydroxamic acid derivatives that potently reactivate HIV from latency. J. Virus Erad. 5(2), 84-91 (2019).

Barlerin (8-O-Acetylshanzhiside methyl ester) has potential against cerebral ischemic injury, and its protective effect on oxygen-glucose deprivation-induced injury might be due to the suppression of intracellular Ca2+ elevation and caspase-3 activity, and improvement of mitochondrial energy metabolism.8-O-Acetylshanzhiside methylester can increase angiogenesis and improve functional recovery after stroke.8-O-Acetylshanzhiside methylester has protective effects on experimental myocardial ischemia injury, the effects might be due to block of myocardial inflammatory cascades through an HMGB1-dependent NF-κB signaling pathway.8-O-Acetylshanzhiside methylester protects diabetic brain against I/R injury by alleviating diabetic cerebral I/R injury and attenuating blood–brain barrier (BBB) breakdown, and its protective effects may involve HMGB-1 and NF-κB signalling pathway.

GSK598809 is a selective D(3)R antagonist recently progressed in Phase I trials. GSK-598809 may decrease the rewarding effects of contextual cues associated with drug intake preclinically, which may reduce drug craving in humans.

Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic transmission[2]. Rp-cAMPS (10 μM, 15 min) decreases the monosynaptic EPSCs evoked at the PB-CeLC and BLA-CeLC synapses in slices from arthritic rats but not in control neurons from normal animals. The inhibitory effect of Rp-cAMPS is significant compared to predrug (ACSF) control values obtained in the same neurons[2]. [1]. R J de Wit, et al. Inhibitory action of certain cyclophosphate derivatives of cAMP on cAMP-dependent protein kinases. Eur J Biochem. 1984 Jul 16;142(2):255-60. [2]. Rothermel JD, et al. A mechanistic and kinetic analysis of the interactions of the diastereoisomers of adenosine 3’,5’-(cyclic)phosphorothioate with purified cyclic AMP-dependent protein kinase. Biochem J. 1988 May 1;251(3):757-62.[3]. Fu Y, et al. PKA and ERK, but not PKC, in the amygdala contribute to pain-related synaptic plasticity and behavior. Mol Pain. 2008 Jul 16;4:26.[4]. Kuriyama S, et al. Isoproterenol inhibits rod outer segment phagocytosis by both cAMP-dependent and independent pathways. Invest Ophthalmol Vis Sci. 1995 Mar;36(3):730-6.[5]. Dostmann WR, et al. Probing the cyclic nucleotide binding sites of cAMP-dependent protein kinases I and II with analogs of adenosine 3’,5’-cyclic phosphorothioates. J Biol Chem. 1990 Jun 25;265(18):10484-91.[6]. Van Haastert PJ, et al. Competitive cAMP antagonists for cAMP-receptor proteins. J Biol Chem. 1984 Aug 25;259(16):10020-4.

(R)-ND-336 is a highly potent and selective MMP-9 inhibitor, displaying a K i value of 19 nM. It also exhibits inhibitory activity against MMP-2 (K i = 127 nM) and MMP-14 (K i =119 nM). With its significant potential, (R)-ND-336 is being investigated in the field of diabetic foot ulcers (DFUs) research [1].

UNC0006 is a beta-inhibitory protein biased D(2)R ligand, and is also an antagonist of G(i)-regulated cAMP production and a partial agonist of D(2)R/beta-arrestin-2 interaction. It has antipsychotic activity and is used in the study of neurological disorders.

4'-Acetyl chrysomycin A is a bacterial metabolite and derivative of chrysomycin A that has been found inStreptomycesand has antibacterial and anticancer activities.1It is active against strains of methicillin-resistantS. aureus(MRSA) and vancomycin-resistant strains ofE. faecalisandE. faecium(MICs = 0.5-2 μg/ml for all). 4'-Acetyl chrysomycin A is cytotoxic against a panel of human cancer cell lines, including doxorubicin-sensitive or -resistant cells (IC50s = 0.085-0.26 and 3.4-16 ng/ml, respectively). 1.Wada, S.-I., Sawa, R., Iwanami, F., et al.Structures and biological activities of novel 4'-acetylated analogs of chrysomycins A and BJ. Antibiot. (Tokyo)70(11)1078-1082(2017)

MC-Gly-Gly-Phe-Gly-(S)-Cyclopropane-Exatecan is a agent-linker conjugates for ADC , consisting Exatecan . Exatecan is a DNA Topoisomerase I inhibitor (IC 50 =2.2 μM) [1] .

Clometocillin is a penicillin that can active penicillin to pen-I or pen-R pneumococci.

(R)-SLV 319 is a potent and selective antagonist of cannabinoid receptor 1 (CB1), with a K i value of 894 nM. (R)-SLV 319 is a dextrorotatory counterpart of SLV 319 [1]