INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia.

ZW4864 is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a Ki value of 0.76 μM and an IC50 value of 0.87 μM.

PRGL493 is a potent and selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor. PRGL493 blocks cell proliferation and tumor growth in both breast and prostate cellular and animal models. PRGL493 is used for cancer research.

N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.

PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice.

LY288513, a selective non-peptide CCK-B receptor antagonist with an IC50 value of 16 nM. LY288513 possesses both anxiolytic and antipsychotic potential.

I-BET151 dihydrochloride (GSK1210151A dihydrochloride) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively.

F1324 is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.

α-Conotoxin Vc1.1 TFA is a disulfide-bonded peptide isolated from Conus victoriae and is a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM, respectively, and has less inhibitory effect on other nAChR subtypes. α-Conotoxin Vc1.1 TFA has the potential for neuropathic pain reserach.

Urocortin, rat TFA (Urocortin (Rattus norvegicus) TFA) is a neuropeptide and a potent endogenous CRFR agonist with Kis of 13 nM, 1.5 nM, and 0.97 nM for human CRF1, rat CRF2α and mouse CRF2β, respectively.

c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively.

PI3K-IN-19 hydrochloride is a phosphotidylinositol-3-kinase (PI3K) inhibitor extracted from patent WO2017153220, step 5.

Mycalolide-B is a specific inhibitor of actomyosin ATPase isolated from marine sponge. Mycalolide-B inhibits ATP-induced contraction and Mg2+-ATPase activity in the absence of Ca2+.

β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total Aβ and IC50=2.5 μM for Aβ1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.

SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM.

LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders.

Lyciumin A, a cyclic octapeptide, exhibits inhibitory activity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a quinolone alkaloid, is a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, with IC50s of 20.1 μM and 34.1 μM, respectively. 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone shows potent anti-Helicobacter pylori activity with the MIC of 10 μg/mL.

Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone9 is an antagonist of angiotensin II receptor (IC50=48.2 μM). Methyl-2-[(6Z,9Z)-6,9-pentadecadienyl]-4(1H)-quinolone9 is a quinolone alkaloid from Evodia rutaecarpa.

MS31 is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 potently inhibits the interactions between SPIN1 and H3K4me3 (IC50=77 nM, AlphaLISA; 243 nM, FP). MS31 selectively binds Tudor domain II of SPIN1 (Kd=91 nM). MS31 potently inhibits binding of trimethyllysine-containing peptides to SPIN1. MS31 is not toxic to nontumorigenic cells.

USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 µΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.

MRL-494, an antibacterial agent, is a inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias.

IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM).

VGSC blocker-1 is a potent and small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5). VGSC blocker-1 blocks INa peak currents 34.9% at 1 μM and inhibits cell invasion 0.3% at 1 μM in human breast cancer cell line MDA-MB-231, without affecting the cell viability.

Carnostatine (SAN9812) is a potent and selective carnosinase 1 (CN1) inhibitor with a Ki of 11 nM for human recombinant CN1. Carnostatine (SAN9812) can be used for the treatment of diabetic nephropathy (DN).

Lesogaberan (hydrochloride) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively.

ICA-105665 (PF-04895162) is a potent and orally active neuronal Kv7.2/7.3 and Kv7.3/7.5 potassium channels opener. ICA-105665 inhibits liver mitochondrial function and bile salt export protein (BSEP) transport (IC50 of 311 μM). ICA-105665 can penetrate the blood-brain barrier and has antiseizure effects.

TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

EEDi-5285 is an exceptionally potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 value of 0.2 nM for binds to the EED protein. EEDi-5285 has anti-cancer activity.