AHR-10037 is a non-steroidal anti-inflammatory agent with low gastric toxicity. AHR-10037 is a prodrug converted in vivo to a cyclooxygenase inhibitor.

TP-1287, a prodrug of Alvocidib, is an orally active CDK9 inhibitor.

Ethyl methanesulfonate is a DNA ethylating agent, mutagenic to plants and animals and carcinogenic in mammals. It has been used as a model alkylating agent in studies of DNA repair processes. It induces base substitutions of guanine-cytosine (G/C) to adenine-thymine (A/T). EMS also generates point mutations and single nucleotide polymorphisms in genomes.

GBT1118 is a potent and orally active allosteric modifier of hemoglobin oxygen affinity. GBT1118 increases tolerance to severe hypoxia.

MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with pKi of 10.3.

B746 is a clofazimine analog with anti-Mycobacterium avium complex (MAC) activity and is less effective when used with clofazimine or streptomycin.

A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).

BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype.

Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets.

Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

Pateamine A (Pateamine) is a potent small molecule inhibitor of eukaryotic translation that stimulates eIF4AI/II and eIF4AIII activity, but not eIF4E, eIF2α, and elF4B.

Tubulysin B is a cytotoxic agent, used as the cytotoxic component in antibody-drug conjugates.

Phorbol 12-myristate 13-acetate (PMA) is a PKC-activating phorbol ester, increases the intracellular Ca2+ concentration ([Ca2+]i) in a dose-dependent manner, with an EC50 of 11.7 nM.

Tipranavir is a nonpeptidic protease inhibitor. Tipranavir has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and it recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations. Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. Like lopinavir and atazanavir, it is very potent and is effective in salvage therapy for patients with some drug resistance.

Atrovastatin-PEG3-FITC (compound S31) is a KRAS-PDEδ interaction inhibitor. Atrovastatin-PEG3-FITC acts as a ligand in fluorescence anisotropy assay.

BE1218 is a liver X receptor (LXR) inverse agonist with IC50 values of 9 nM and 7 nM against LXRα and LXRβ, respectively.

TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes.

A highly potent agonist of σ1 receptor with Ki of 0.8 nM.

HS94 (DAPK3 inhibitor HS94) is a selective DAPK3 inhibitor with Ki of 126 nM, >20-fold selectivity over Pim kinases..

Novel Potent Allosteric Activator for Ferroptosis Regulator Glutathione Peroxidase 4 (GPX4)

DAUDA (11-(dansylamino) undecanoic acid) is an environment-sensitive fluorescent fatty acid analogue. DAUDA alters its intensities and fluorescent emission spectra on entry into binding proteins. DAUDA is used to determine the relative affinity of natural fatty acids for polymorphs of the Schistosoma mansoni Sm14 fatty acid-binding protein.

Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases.

Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.

Melagatran is a synthetic, small-peptide direct thrombin inhibitor with anticoagulant activity.

JNJ-40411813 is a novel potent positive allosteric modulator of mGlu2 with EC50 of 147 nM. JNJ-40411813 displays >30-fold selectivity over mGlu1 and mGlu3-8, 10-fold over 5-HT2A. JNJ-40411813 displays an optimal interplay between potency, selectivity, favorable ADMET/PK and cardiovascular safety profile, and central EEG activity; has been investigated in the clinic for schizophrenia and anxious depression disorders.

Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.

ML213 is a novel potent, selective KCNQ2 (Kv7.2) and KCNQ4 (Kv7.4) activator with EC50 of 230 and 510 nM, respectively. ML213 displays >80-fold selectivity over other related potassium channels (KCNQ1/3/5). ML213 causes significant hyperpolarization in mesenteric artery smooth muscle cells, shows potent vasorelaxant effects in different blood vessels.

Hi 76-0079 (NNC0076-0079) is a specfic, small molecule inhibitor of hormone-sensitive lipase (HSL) with IC50 of 0.11 uM. Hi 76-0079 does not affect ATGL or other lipases (IC50>50 uM). Hi 76-0079 inhibits lipolysis in vivo.

Enpatoran (M5049) hydrochloride is a potent, orally active, and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM, respectively, in HEK293 cells.

1-Thioglycerol(Mercaptopropanedioltech) is an inhibitor of glycerol kinase activity. It stimulates the synthesis of porphyrin in aerobically growing Escherichia coli.