cultures

Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).

Vidarabine (Adenine Arabinoside) is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.

3-(Methylthio)propionic acid (4-Thiapentanoic acid) is one of the metabolites of methionine (especially of D-methionine). Cultures of Streptomyces lincolnensis accumulated 3-methylthioacrylic acid in amounts directly related to the concentration of methionine in the medium. The first intermediate in the pathway may be the keto acid, which is then oxidatively decarboxylated to 3-methylthiopropionic acid.

Tylosin (Tylosine) is a macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.

L-Cystine dihydrochloride is an Nrf2 inducer with whitening and anti-dark spot effects.L-Cystine dihydrochloride has cytoprotective effects in cells, and is often added to various fungal cultures as a carbon source.

CS-722 Free base is a synthetic central muscle relaxant exhibiting muscle relaxant effects and inhibition of spinal reflexes. In hippocampal cultures, CS-722 Free base may suppress spontaneous inhibitory and excitatory post-synaptic currents by inhibiting sodium and calcium currents.

3-MATIDA is an effective mGluR-1 antagonist (IC50: 6.3 μM, rat mGluR-1a). Displays ≥ 40-fold selectivity over other receptors: mGluR-5, mGluR-2, mGluR-4 (mGluR-4a) (IC50 > 300 μM), NMDA and GluR (AMPA) (IC50 = 250 μM). 3-MATIDA act as a neuroprotectant in cultured murine cortical cells and rat hippocampal slice cultures in vitro.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.

Auten-99 HBr (Auten-99) is a myotubularin phosphatase Jumpy inhibitor exerting potent neuroprotective effects. AUTEN-99 activates autophagy in cell cultures and animal models. AUTEN-99 appears to effectively penetrate through the blood-brain barrier, and impedes the progression of neurodegenerative symptoms in Drosophila models of Parkinson’s and Huntington’s diseases. Furthermore, the molecule increases the survival of isolated neurons under normal and oxidative stress-induced conditions. Thus, AUTEN-99 serves as a potent neuroprotective drug candidate for preventing and treating diverse neurodegenerative pathologies, and may promote healthy aging.

Indolelactic acid is a metabolite of tryptophan in Azotobacter vinelandii cultures.

9-Methoxycanthin-6-one has anti-tumour activity, exhibits cytotoxic activity towards KB, LU-1, LNCaP, HL-60 cancer cells and other human cancer cell lines with IC50 values around 1-4 μg/mL.

Lochnericine is a alkaloid isolated from elicited cell cultures of Catharanthus roseus.

Tat-βsyn-degron, an α-synuclein knockdown peptide, integrates three domains: the HIV-1 Tat plasma membrane transduction domain, an α-synuclein binding domain (βsyn) representing amino acids 36-45 of β-synuclein, and a proteasomal targeting domain (degron). It effectively binds to recombinant α-synuclein, demonstrating a significant reduction in α-synuclein levels in primary rat cortical neuron cultures.

Tylosin-d3 is a deuterated compound of Tylosin. Tylosin has a CAS number of 1401-69-0. Tylosin is a macrolide antibiotic obtained from cultures of Streptomyces fradiae. The drug is effective against many microorganisms in animals but not in humans.

DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants. In vivo, DPC-AJ1951 normalizes serum calcium levels in thyroidparathyroidectomized rats.

UNC10112785 is a novel potent inhibitor of CDK8, CDK19, and CDK9 with IC50 at 1.05, 2.67, and 19.9 nM, respectively, causing MYC loss through both transcriptional and posttranslational mechanisms, and suppressing PDAC anchorage-dependent and anchorage-independent growth, inducing the substantial loss of MYC protein in both two-dimensional (2D) and 3D cell cultures.

Camostat, also known as FOY 305, is a serine protease inhibitor. Camostat is used in the treatment of some forms of cancer and is also effective against some viral infections, as well as inhibiting fibrosis in liver or kidney disease or pancreatitis. It is an inhibitor of the enzyme transmembrane protease, serine 2 (TMPRSS2). Inhibition of TMPRSS2 partially blocked infection by SARS-CoV and Human coronavirus NL63 in HeLa cell cultures. In vitro study showed that camostat significantly reduces the infection of Calu-3 lung cells by SARS-CoV-2, the virus responsible for COVID-19.

Hypogeic acid is isolable from cultures of autotrophic bacteria linked to sulfate accumulation in biofilters [1].

PD-L1-IN-1, a powerful PD-L1 inhibitor, demonstrated an IC50 of 115 nM. By forming a robust bond with the PD-L1 protein, PD-L1-IN-1 effectively suppressed tumor growth by enhancing the antitumor immune activity of peripheral blood mononuclear cells in co-cultures with PD-L1 expressing cancer cells (PC9 and HCC827 cells). It significantly elevated the release of interferon γ and induced apoptosis in cancer cells, while exhibiting minimal cytotoxicity in healthy cells [1].

GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood

1-Hydroxy-2,3,5-trimethoxyxanthone (HM-1) exhibits vasodilator action through an endothelium-dependent mechanism involving NO and an endothelium-independent mechanism by inhibiting Ca(2+) influx via L-type voltage-operated Ca(2+) channels. A minor contribution to HM-1's effects may stem from inhibiting protein kinase C-mediated release of intracellular Ca(2+) stores. At 1 µg mL, HM-1 effectively inhibits osteoclast differentiation in co-cultures with mouse osteoblastic calvarial and bone marrow cells and protects mice from acute lung injury induced by lipopolysaccharide (LPS), likely by increasing IκB-α protein expression and suppressing inducible nitric oxide synthase and cyclooxygenase-Ⅱ protein expression.

Esperamicin A1, an exceedingly potent antitumor antibiotic, is derived from Actinomadura verrucosospora cultures. This compound plays a crucial role in antitumor research.

WNK-IN-B is an inhibitor of Wnk signalling. WNK-IN-B is a cell-permeable diaminoacridine derivative that targets the CCT domain of SPAK and OSR1 via reversible binding. WNK-IN-B selectively suppress hypotonic shock-induced WNK signaling pathway activation

Kanzonol D, a flavonoid derived from the hairy root cultures of Glycyrrhiza glabra [1], exhibits anti-inflammatory and anticancer properties by inhibiting nitric oxide production and suppressing NF-κB activation. It also shows potential in osteoblast differentiation, suggesting its utility in bone diseases.

High affinity α7 nAChR partial agonist (Ki = 1.1 nM in rat; Emax < 10% of the response to ACh in rat and human). Inhibits ACh (IC50 = 2.7 nM) at α7 nAChR. Reduces LPS-induced TNF-α release from microglia enriched cultures. Anti-inflammatory. Briggs et al (2009) Role of channel activation in cognitive enhancement mediated by α7 nicotinic acetylcholine receptors. Br.J.Pharmacol. 158 1486 PMID:19845675 |Thomsen et al (2012) The α7 nicotinic acetylcholine receptor ligands methyllycaconitine, NS6740 and GTS-21 reduce lipopolysaccharide-induced TNF-α release from microglia. J.Neuroimmunol. 251 65 PMID:22884467 |Papke et al (2015) The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor. Neuropharmacology 91 34 PMID:25497451

20-carboxy Arachidonic acid (20-COOH-AA) is the major metabolite of 20-HETE that is produced in renal tubular epithelial, endothelial, and microvascular smooth muscle cell cultures. This ω-oxidation conversion can take place using purified alcohol dehydrogenases three and four or by microsomes containing recombinant human CYP4F3B. Like 20-HETE, 20-COOH-AA inhibits ion transport in the kidneys. It also produces vasorelaxation of porcine coronary microvessels constricted with endothelin. 20-COOH-AA binds to isolated ligand binding domains of peroxisome proliferator-activated receptor α (PPARα) (Kd = 0.87 ± 0.12 μM) and PPARγ (Kd = 1.7 ± 0.5 μM), and is a dual activator of PPARα and PPARγ in a transiently transfected COS-7 cell reporter system.

Sphynolactone-7 (SPL7) acts as an agonist for the Striga hyposensitive to light receptor 7 (ShHTL7) found in the parasitic plant Striga hermonthica. SPL7 selectively targets ShHTL7 with an IC50 of 0.31 µM, demonstrating higher specificity compared to ShHTL2-6, ShHTL9-10, and the strigolactone receptor AtD14 at a concentration of 10 µM, though it still inhibits ShHTL8 and ShHTL11 with IC50s of 1.2 and 7.8 µM, respectively. This compound triggers fatal germination of Striga hermonthica seeds in the absence of a host by inducing suicidal germination at a minimum effective concentration of 10 fM. Additionally, SPL7 can reduce the emergence of this obligate parasite from the soil and alleviate Striga hermonthica-induced senescence in maize when applied at a 10 nM concentration to the soil of maize and Striga hermonthica seed co-cultures.

EGIS-8332 is a potent and selective non-competitive AMPA receptor antagonist. EGIS-8332 inhibits AMPA/kainate ion channels and cell death. EGIS-8332 inhibited AMPA currents in rat cerebellar Purkinje cells and inhibited the AMPA- and quisqualate-induced excitotoxicity in primary cultures of telencephalon neurons (IC(50)=5.1-9.0 microM), in vitro. EGIS-8332 seems suitable for further development for the treatment of epilepsy, ischaemia and stroke based on its efficacy in a variety of experimental disease models, and on its low side effect potential.

Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells.

MAO-B-IN-18 is a potent, selective inhibitor of MAO B with IC50 values of 52 nM for hMAO B and 14 μM for hMAO A. It exhibits cytoprotective effects against hydrogen peroxide-induced damage in neuroblastoma and astrocyte cultures [1].

SB02024 is a VPS34 inhibitor. SB02024 activates cGAS-STING signaling and sensitizes tumors to STING agonist. SB02024 blocked autophagy in vitro and reduced xenograft growth of two breast cancer cell lines, MDA-MB-231 and MCF-7, in vivo. Vps34 inhibitor significantly potentiated cytotoxicity of Sunitinib and Erlotinib in MCF-7 and MDA-MB-231 in vitro in monolayer cultures and when grown as multicellular spheroids. Our data suggests that inhibition of autophagy significantly improves sensitivity to Sunitinib and Erlotinib and that Vps34 is a promising therapeutic target for combination strategies in breast cancer.

DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.Target: TNF-αin vitro: DCVC inhibits pathogen stimulated cytokine release from tissue punch cultures. DCVC (5-50 μM) significantly inhibits LTA-, LPS-, and GBS-stimulated cytokine release from tissue cultures as early as 4 h (P ≤ 0.05). In contrast, TCA (up to 500 μM) does not inhibit LTA-stimulated cytokine release from tissue punches. DCVC effects on LTA-stimulated and LPS-stimulated TNF-α release from tissue punch cultures of extraplacental membranes. DCVC effects on GBS-stimulated release of pro-inflammatory cytokines from extraplacental membranes in transwell cultures. [1]. Boldenow E, et al. The trichloroethylene metabolite S-(1,2-dichlorovinyl)-l-cysteine but not trichloroacetate inhibits pathogen-stimulated TNF-α in human extraplacental membranes in vitro. Reprod Toxicol. 2015 Apr;52:1-6. [2]. Lash LH, et al. Multigenerational study of chemically induced cytotoxicity and proliferation in cultures of human proximal tubular cells. Int J Mol Sci. 2014 Nov 18;15(11):21348-65. [3]. Yoo HS, et al. Comparative analysis of the relationship between trichloroethylene metabolism and tissue-specific toxicity among inbred mouse strains: kidney effects. J Toxicol Environ Health A. 2015;78(1):32-49.

5-Bromouridine is a brominated analog of the nucleoside uridine .1It can be incorporated into RNA and subsequently detected by antibodies against bromodeoxyuridine .25-Bromouridine decreases the viability of HL-60 and MOLT-4 cells (LC50s = 10 and 20 μM, respectively). It induces apoptosis and halts the cell cycle at the S phase in HL-60 cells. It is photoreactive, and UV irradiation has been used to cross-link RNA containing 5-bromouridine to proteins in the study of of RNA-protein interactions.1,35-Bromouridine can also be incorporated into RNA using 5-bromouridine 5'-triphosphate . 1.Tanner, N.K., Hanna, M.M., and Abelson, J.Binding interactions between yeast tRNA ligase and a precursor transfer ribonucleic acid containing two photoreactive uridine analoguesBiochemistry27(24)8852-8861(1988) 2.Li, X., Patel, R., Melamed, M.R., et al.The cell cycle effects and induction of apoptosis by 5-bromouridine in cultures of human leukaemic MOLT-4 and HL-60 cell lines and mitogen-stimulated normal lymphocytesCell Prolif.27(6)307-319(1994) 3.Gott, J.M., Willis, M.C., Koch, T.H., et al.A specific, UV-induced RNA-protein cross-link using 5-bromouridine-substituted RNABiochemistry30(25)6290-6295(1991)

Dasycarpol(9beta-Hydroxyfraxinellone) shows significant neuroprotective activity against glutamate-induced neurotoxicity in primary cultures of rat cortical cells at a concentration of 0.1 microM. Dasycarpol also shows moderate inhibitory activity on lung

Myelopeptide-2, a peptide isolated from the supernatant of porcine bone marrow cell cultures, can restore the mitogenic reactivity of human T lymphocytes inhibited by HL-60 leukemia cells or measles virus conditions. It also enhances depressed interleukin-2 (IL-2) synthesis and interleukin-2 receptor (IL-2R) expression, playing a role in immunity homeostasis. This compound shows potential for application in antitumor and antivirus research [1] [2].

Survivin (also known as baculoviral IAP repeat-containing protein 5 (BIRC5)) is a member of the inhibitor of apoptosis (IAP) family that interacts with and inhibits the apoptotic function of several proteins. LLP-3 is a cell-permeable ligand of Survivin that blocks its interaction with Ran, resulting in the induction of apoptosis (IAP) in glioma stem cells (IC50 = 31 μM). It abolishes the growth of glioblastoma multiforme cell in spheres and in tumor slice cultures.

(S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid ((S)-3-(4-Hydroxyphenyl)lactic acid) (compound 1) is a metabolite found in the culture medium of Leuconostoc mesenteroides, exhibiting significant DPPH radical-scavenging and antioxidative activities.

4beta-Hydroxywithanolide E(4bHWE) can inhibit the growth of colon cancer monolayer and spheroid cultures, it assert its anti-tumor activity in carcinogenic progression and develop into a dietary chemopreventive agent, it affects alternative splicing by mo

Xylocydine is a novel Cdk inhibitor, which is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Xylocydine also strongly inhibits the activity of Cdk7 and Cdk9, in vitro as well as in cell cultures, that is temporally associated with apoptotic cell death in xylocydine-induced HCC cells. Xylocydine can effectively suppress the growth of HCC xenografts in Balb/C-nude mice by preferentially inducing apoptosis in the xenografts, whereas the drug did not cause any apparent toxic effect on other tissues.Xylocydine is a good candidate for an anti-cancer drug for HCC therapy.

Senecionine n-oxide is a major product of pyrrolizidine nucleic alkaloid biosynthesis in unusual root cultures of Trichoderma lucidum.Senecionine N-oxide (Senecionine oxide) has antitumor activity but induces hepatic sinusoidal obstruction syndrome.Senecionine n-oxide acts as a chelating tracer for N-oxide.

Compound CMC23, an FPR2 agonist, mitigates lactate dehydrogenase release in LPS-stimulated cultures and reduces pro-inflammatory IL-1β and IL-6 levels. It also attenuates phosphor-STAT3 levels through the STAT3/SOCS3 signaling pathway [1].

Sporidesmolide V, a cyclodepsipeptide, has been isolated from Pithornyces chartarum cultures [1].

Semicochliodinol, a compound that can be isolated from rice cultures of the fungus genus Chaetomium, has been identified [1].

12-Oxo phytodienoic acid (12-oxo PDA) is an endogenous signal converter that increases alkaloid biosynthesis in E. californica cell cultures, increases b. dioica tendril curls, And inhibited jasmonic acid-induced programmed cell death in conditioned A. fru mutants.

Gonadorelin, a gonadotropin-releasing hormone receptor (GNRHR; Ki= 13 nM in CHO cells expressing the human receptor) agonist and tropic hormone, effectively stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) from rat anterior pituitary cultures at 0.1 μg doses. Additionally, it triggers LH release from bovine anterior pituitary cultures at a 1 μM concentration. In vivo, gonadorelin induces ovulation in rats pretreated with fluphenazine (ED50= 610.3 ng/kg). Gonadorelin-based formulations are utilized as diagnostic tools to evaluate pituitary gland function.

Albrassitriol is a natural product from the cultures of the fungus Penicillium sp.