MINA53 inhibitor (Compound 10) is an inhibitor of MINA53.

DCZ3301 is a novel aryl-guanidino inhibitor.

Compound 10w, a substituted pyrazolo[1,5-a]pyrimidinamide compound, is a ZSTK474 analog that shows anticancer activity against HeLa cells.

Terbogrel is an oral thromboxane A2 receptor antagonist (IC50 is about 10 nM) and thromboxane A2 synthase inhibitor (IC50 is about 10 nM). Terbogrel is an antiplatelet compound that inhibits platelet aggregation and is a potential compound for the prevention of blood clots.

Compound PDK0269, as 5-HT3 receptor agonists(3–100 μM, pEC50 5.05±0.06), acutely increased XII (hypoglossal) burst frequency and regularity, and decreased bursts/episode . Phenylbiguanide produced a dose-related (10-500 microM) increase in the release of dopamine (280-2000%). When nomifensine (5 microM) was included in the Ringer solution, the effect of Compound PDK0269 on the release of dopamine was ameliorated or inhibited.

Milataxel is an orally bioavailable taxane with potential antineoplastic activity. Upon oral administration, milataxel and its major active metabolite M-10 bind to and stabilize tubulin, resulting in the inhibition of microtubule depolymerization and cell division, cell cycle arrest in the G2/M phase, and the inhibition of tumor cell proliferation. Unlike other taxane compounds, milataxel appears to be a poor substrate for the multidrug resistance (MDR) membrane-associated P-glycoprotein (P-gp) efflux pump and may be useful for treating multidrug-resistant tumors. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).This compound is unstable in powder form and other related salt forms are recommended.

SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGFR2, IC50 = 27 nM), FGFR1 (IC50= 170

10-FTHF is a donor of formyl groups in anabolism used as a substrate in formyltransferase reactions, which is important in purine biosynthesis.This compound is unstable in powder form and other related salt forms are recommended.

NO-prednisolone (NCX-1015) is a compound that effectively stimulates the production of IL-10 in vivo. It is a Prednisolone derivative that releases nitric oxide (NO).

Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring NPM-ALK (IC50: 9 nM). X-376 also inhibits SY5Y neuroblastoma cells harboring ALK F1174L, MKN-45 gastric carcinoma cells harboring MET dependent, HepG2 cells and PC-9 lung cancer cell lines harboring EGFR exon 19 del with IC50s of 68 nM, 156 nM, 9.644 μM and 2.989 μM, respectively[1]. The effects of Ensartinib (X-396) in vivo against H3122 xenografts are examined. A pharmacokinetic study reveals that Ensartinib shows substantial bioavailability and moderate half-lives in vivo. Nude mice harboring H3122 xenografts are treated with Ensartinib at 25mg/kg bid. Ensartinib significantly delays the growth of tumors compared to vehicle alone. In the xenograft experiments, Ensartinib appears well-tolerated in vivo. Mouse weight is unaffected by Ensartinib treatment. Drug-treated mice appear healthy and do not display any signs of compound related toxicity. To further assess potential side effects of Ensartinib, additional systemic toxicity and toxico-kinetic studies are performed in Sprague Dawley (SD) rats. Following 10 days of repeated oral administration of Ensartinib at 20, 40, 80 mg/kg in SD rats, all animals survive to study termination. The no significant toxicity (NST) levels are determined to be 80mg/kg for Ensartinib. At NST levels, Ensartinib achieves an AUC of 66 μM×hr and a Cmax of 7.19 μM[1]. [1]. Lovly CM, et al. Insights into ALK-driven cancers revealed through development of novel ALK tyrosine kinaseinhibitors. Cancer Res. 2011 Jul 15;71(14):4920-31.

OAT1/3-IN-2 (compound 8) is a dual inhibitor of OAT1 and OAT3 that demonstrates potential protective effects against Cys-Hg toxicity in HEK-OAT1 cells (10 μM) and may safeguard renal function. This compound is useful for investigating mercury-induced nephrotoxicity [1].

Centellasaponin A (compound 10), a pentacyclic triterpene saponin, has been isolated from the methanolic extract of Centella asiatica [1].

Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). It has the capability to induce apoptosis and block cells at the G1/G0 phase, making it applicable in cancer research [1].

(4S)-10-Nor-calamenen-10-one (Compound 15), an eudesmane sesquiterpene sourced from Alpinia oxyphylla [1], amplifies LPS-induced nitric oxide (NO) production in microglial cells.

Compound 24f, an antifungal agent also known as 'Antifungal agent 85,' demonstrates potent antibacterial properties, exhibiting minimum inhibitory concentration (MIC) values ranging from 2.5 to 10 μM against diverse Gram-positive bacteria [1].

(S)-O-Methylencecalinol (compound 10), a calmodulin-targeting molecule, has been isolated from the aerial parts of Ageratina grandifolia [1].

Antiproliferative agent-26 (compound 4g) exhibits a broad spectrum of activity against leukemia, CNS cancers, melanoma, renal, and breast cancers at a concentration of 10 μM. It hinders colony formation and induces cell cycle arrest in the G1 phase at 5 μM, while arresting the cell cycle at the S phase at 25 μM [1].

Pomalidomide-PEG1-C2-N3 is a compound that has been synthesized as a conjugate of an E3 ligase ligand-linker. This compound incorporates the cereblon ligand based on Pomalidomide and a 1-unit PEG linker, which are commonly used in PROTAC technology. Utilizing Pomalidomide-PEG1-C2-N3, it is possible to design a selective CDK6 PROTAC degrader known as CP-10. CP-10 effectively induces the degradation of CDK6, displaying a DC50 value of 2.1 nM[1].

Pipernonaline is a useful organic compound for research related to life sciences. The catalog number is T124000 and the CAS number is 88660-10-0.

Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities, including antibacterial, anticancer, antiplatelet, and antioxidant properties.1,2,3,4It is active against Gram-positive (MICs = 5-160 µg/ml) and Gram-negative bacteria (MICs = 136-200 µg/ml), as well as yeasts (MICs = 10-20 µg/ml).1Ajoene is cytotoxic to mouse melanoma cells (IC50= 18 µM), as well as human colon, lung, mammary, and pancreatic cancer cells (IC50s = 7-41 µM).2It reduces tumor growth in a B16/BL6 mouse model of melanoma when administered at a dose of 25 mg/kg every other day and decreases the number of lung metastases when administered prior to tumor cell inoculation at doses ranging from 1-25 mg/kg. It inhibits ADP- or collagen-induced platelet aggregation in isolated baboon platelets when used at concentrations ranging from 75 to 150 µg/ml and in platelet-rich plasma isolated from baboons when administered at a dose of 25 mg/kg.3Ajoene (25 mg/kg) prevents thrombus formation on damaged arterial walls in heparinized pigs in anin situmodel of thrombogenesis.5It also reduces high-fat diet-induced hepatic steatosis, histopathological markers of liver damage, thiobarbituric acid reactive substances (TBARS) formation, and protein oxidation in a mouse model of non-alcoholic fatty liver disease (NAFLD).4 1.Naganawa, R., Iwata, N., Ishikawa, K., et al.Inhibition of microbial growth by ajoene, a sulfur-containing compound derived from garlicAppl. Environ. Microbiol.62(11)4238-4242(1996) 2.Taylor, P., Noriega, R., Farah, C., et al.Ajoene inhibits both primary tumor growth and metastasis of B16/BL6 melanoma cells in C57BL/6 miceCancer Lett.239(2)298-304(2006) 3.Teranishi, K., Apitz-Castro, R., Robson, S.C., et al.Inhibition of baboon platelet aggregation in vitro and in vivo by the garlic derivative, ajoeneXenotransplantation10(4)374-379(2003) 4.Han, C.Y., Ki, S.H., Kim, Y.W., et al.Ajoene, a stable garlic by-product, inhibits high fat diet-induced hepatic steatosis and oxidative injury through LKB1-dependent AMPK activationAntioxid. Redox Signal.14(2)187-202(2011) 5.Apitz-Castro, R., Badimon, J.J., and Badimon, L.A garlic derivative, ajoene, inhibits platelet deposition on severely damaged vessel wall in an in vivo porcine experimental modelThromb. Res.75(3)243-249(1994)

Compound 24, a 5-HT2 agonist-1, selectively activates 5-HT2A, 5-HT2B, and 5-HT2C receptors with IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. The free base form of this compound is utilized in research pertaining to depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headaches, PTSD, seizure disorders, and additional CNS disorders [1].

Mollicellin I (compound 1), a depsidone, exhibits minimal growth inhibitory activity against human breast cancer (Bre04), human lung (Lu04), and human neuroma (N04) cell lines, with GI50 values exceeding 10 μg/mL [1].

Pedaliin 6''-acetate (compound 10), a natural product extracted from Dracocephalum tanguticum, exhibits antioxidative properties and a cytoprotective effect against doxorubicin (DOX)-induced toxicity in H9c2 cardiomyocytes, with an effective concentration (EC50) of 19.1 μM [1].

Gly-Gly-Arg, a tripeptide and pumping pheromone, is released from hatching eggs, stimulating pleopod pumping activity in subtidal crustaceans at a threshold concentration of 10 nM and eliciting a maximum response rate of 58.3%. Additionally, this compound plays a role in controlling larval release in these organisms [1].

mGluR5 antagonist-1 (compound 10) is a potent mGluR5 inhibitor exhibiting an IC50 of 11.5 nM and demonstrates antidepressant effects [1].

OAT1/3-IN-1 (compound 7), a dual inhibitor of OAT1 and OAT3, demonstrates the ability to mitigate the toxicity of Cys-Hg in HEK-OAT1 cells at a concentration of 10 μM and offers potential kidney protection. This compound is utilized in the investigation of mercury-induced renal damage [1].

Stigmast-5-ene-3,7-dione (Compound 10), isolated from the roots, leaves, and twigs of Penianthus longifolius [1], is a naturally occurring chemical entity.

G* peptide, also known as LVGRQLEEFL (mouse) TFA, is a segment corresponding to amino acids 113 to 122 ([113,122] apoJ) of apolipoprotein J. This compound possesses both anti-inflammatory and anti-atherogenic qualities. When combined with an apoJ mimetic, it constitutes the HM-10/10 peptide, a novel chimeric high-density lipoprotein mimetic peptide. The HM-10/10 peptide is notable for safeguarding retinal pigment epithelium (RPE) and photoreceptors from oxidant-induced cell death as referenced in sources [1] [2].

Prostaglandin D1 (PGD1) is the theoretical D-series metabolite of dihomo-γ-linolenic acid (DGLA), but to date it has not been isolated as a natural product. It is an inhibitor of ADP-induced platelet aggregation in humans with an IC50 value of 320 ng/ml, about 1/10 as potent as PGD2. 13,14-dihydro-15-keto Prostaglandin D1 (13,14-dihydro-15-keto PGD1) is the theoretical metabolite of PGD1 via the 15-hydroxy PG dehydrogenase metabolic pathway. No biological studies for this compound have been reported.

FLT3-IN-10 (2-Oxazolamine, 5-(4-fluorophenyl)-N-phenyl-) (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 shows the potential for the treatment of FLT3-mutated acute myeloid leukemia (AML).

ICMT-IN-10 (compound 32) serves as an inhibitor for ICMT, exhibiting potent activity with an IC50 value of 0.184 μM [1].

PAK4-IN-3 (compound 27e) is a PAK4 inhibitor exhibiting an IC50 of 10 nM and demonstrates antiproliferative effects on A549 cells with an IC50 of 0.61μM. It also induces concentration-dependent apoptosis in A549 cells and halts the cell cycle at the G0/G1 phase [1].

RIPK1/3-IN-1 (Compound 10) is a selective inhibitor of both RIPK1 and RIPK3, effectively preventing necroptosis by blocking the phosphorylation of RIPK1, RIPK3, and MLKL [1].

Antioxidant Agent-10 (Compound 3) demonstrates moderate DPPH scavenging activity, possessing an EC50 value of 33.2 μg/mL [1].

Aloeresin J (compound 10) is a chromone isolated from the ethanol extract of Aloe vera leaf bark.

10-Phenyl-[12]-cytochalasins Z16 (Compound 5), a member of the cytochalasins, exhibits inhibition of wheat root elongation with an IC50 of 17.35 μM [1].

Keap1-Nrf2-IN-10 (compound 15) is a potent inducer of NQO1 and efficaciously mitigates oxidative stress in gamma-irradiated mice by reducing MDA and ROS levels, as well as NQO1 in the liver, which enhances the survival rate of these mice [1].

DNA gyrase B-IN-2 (Compound E), a 2-aminobenzothiazole derivative, serves as a potent inhibitor of DNA gyrase B with substantial efficacy against ESKAPE pathogens. The compound exhibits potent nanomolar-range inhibition (IC 50 < 10 nM) and a broad-spectrum antibacterial effect, with minimum inhibitory concentrations below 0.03 μg/mL for most Gram-positive species and between 4–16 μg/mL for Gram-negative species including E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa, and Klebsiella pneumoniae. DNA gyrase B-IN-2 is applicable in infection research [1].

USP1-IN-5 (compound 10) is a potent inhibitor of both USP1, with an IC50 of less than 50 nM, and MDA-MB-436 cells, where it also exhibits an IC50 of less than 50 nM [1].

PLM-101 is an anticancer compound orally active against acute myeloid leukemia by targeting FLT3 and RET. It impedes RET function, promoting autophagic breakdown of FLT3, and suppresses the PI3K and Ras/ERK pathways, contributing to its anti-leukemic effects. The compound's antitumor efficacy is demonstrated in both a mouse MV4-11 flank xenograft model (doses of 3 and 10 mg/kg; po) and an allogeneic xenograft mouse model (dose of 40 mg/kg; po) [1].

Compound 11, labeled as a weak Hepatoprotective agent-1, is a naturally occurring substance extracted from the fruits of Arctium lappa L. It demonstrates modest hepatoprotective effects when applied at a concentration of 10 μM [1].

NLRP3-IN-22 (Compound II-4) is an inhibitor of NLRP3, exhibiting a 67% inhibition rate at a concentration of 10 μM [1].

MMP-9-IN-8 (Compound 3), an MMP-9 inhibitor, exhibits inhibitory activities of 42.16% at 10 μM and 58.28% at 50 μM. Additionally, MMP-9-IN-8 demonstrates anti-cancer properties, inducing apoptosis in MCF-7 cells with an IC50 value of 23.42 μM [1].

Antitumor agent-49 (Compound 10), a harmine derivative-furoxan hybrid featuring nitric oxide (NO) donating properties, exhibits cytotoxic effects against HepG2 cells, achieving an IC50 value of 1.79 µM and inducing significant NO production in vitro [1].

Laserine oxide is a useful organic compound for research related to life sciences. The catalog number is T124156 and the CAS number is 82433-10-1.

Geodin hydrate is a useful organic compound for research related to life sciences. The catalog number is T125050 and the CAS number is 3209-10-7.

Aspyrone is a polyketide fungal metabolite that has been found inAspergillusand has diverse biological activities.1,2It is active against a panel of 13 fungi when used at a concentration of 20 μg/ml and a panel of 21 bacteria in a disc assay when used at a concentration of 100 μg per disc.1Aspyrone (10-1,000 mg/L) is nematocidal againstP. penetrans.2 1.Torres, M., Balcells, M., Sala, N., et al.Bactericidal and fungicidal activity of Aspergillus ochraceus metabolites and some derivativesPestic. Sci.53(1)9-14(1999) 2.Kimura, Y., Nakahara, S., and Fujioka, S.Aspyrone, a nematicidal compound isolated from the fungus, Aspergillus melleusBiosci. Biotech. Biochem.60(8)1375-1376(1996)

The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2. LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4-EA was a potent antagonist with about three times greater affinity for the receptor than LTB4 (Ki = 1.22 nM versus 3.88 nM). LTB4-EA antagonizes the LTB4-induced contractions of guinea pig lung parenchyma with an EC50 of 10 nM. LTB4-EA thus represents a potential endogenous anti-inflammatory compound functioning as a natural antagonist of BLTR1.

G* Peptide, also denoted as LVGRQLEEFL (mouse), represents the amino acid sequence 113 to 122 ([113,122] apoJ) found in apolipoprotein J. This compound displays both anti-inflammatory and anti-atherogenic characteristics. When incorporated into an apoJ mimetic, it results in the formation of the HM-10/10 peptide, which functions as a novel chimeric high-density lipoprotein. The HM-10/10 peptide has been shown to confer protection to the retinal pigment epithelium (RPE) and photoreceptors against oxidant-induced cell death [1] [2].

Compound 13, a topoisomerase I inhibitor 10, selectively inhibits leishmanial topoisomerase IB and exhibits antileishmanial activity. Specifically, it demonstrates efficacy against L. donovani promastigotes with an IC50 value of 27.91 μM [1].