MM-3122 is a selective inhibitor of host cell serine protease TMPRSS2 (transmembrane protease serine 2) with IC50 of 0.34 nM against recombinant full-length TMPRSS2 protein.

MYF-03-176 is an orally active and potent anticancer agent. MYF-03-176 shows strong antitumor efficacy in MPM mouse xenograft model via oral administration[1].

YX-2-107 is a CRBN-recruiting and specific CDK6-degrading PROTAC with IC50 of 0.69 and 4.4 nM for CDK4 and CDK6 in vitro, selectively degardes CDK6 in Ph+ BV173 ALL cells with a degradation constant of 4 nM.YX-2-107 does not affect expression of IKZF1 and IKZF3, and does not degarde CDK4 protein.YX-2-107 inhibits S-phase entry, cell proliferation, RB phosphorylation, and FOXM1 expression and induces the selective degradation of CDK6 in Ph+ BV173 and SUP-B15 cells.|PROTAC YX-2-107 is bioavailable in mice and pharmacologically active in suppressing Ph+ ALL proliferation in a mouse xenograft of Ph+ ALL, comparable or superior to that of the CDK4/6 enzymatic inhibitor palbociclib.

MS9715 (MS-9715) is a NSD3-targeting PROTAC designed by linking BI-9321, a NSD3 antagonist, which binds NSD3's PWWP1 domain, with an E3 ligase VHL ligand.MS9715 achieves effective and specific targeting of NSD3 and associated cMyc node in tumor cells.MS9715 effectively suppresses growth of NSD3-dependent hematological cancer cells.MS 9715 effectively suppresses NSD3-and cMyc-associated gene expression programs, resembling effects of the CRISPR-Cas9-mediated knockout of NSD3.

TD165(TD 165) is a PROTAC-based cereblon (CRBN) degrader that degrads Cav1.2α with the DC50 of 20.4 nM, comprising a cereblon (CRBN) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group.

Siponimod, also known as BAF-312, is a a potent and orally selective S1P Receptor Modulator with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively. Development of sphingosine-1-phosphate receptor 1 (S1P1) modulators to dampen inflammation and its sequelae is becoming increasingly promising for treating medical conditions characterized by significant immunopathology.

4-CPPC is the first reversible and selective inhibitor of pro-inflammatory protein macrophage migration inhibitory factor-2 (MIF-2) with Ki of 33 uM, 13-fold selectivity for human MIF-2 versus human MIF-1.

6-Thioguanosine (6-Mercaptoguanosine), an active nucleoside, is an Azathioprine metabolite. 6-Thioguanosine has immunosuppressive effects.

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.

Alpha-Lipoic Acid Choline Ester, also known as alpha-LACE, EV-06 or UNR844, is a drug candidate potentially for the treatment of presbyopia. Alpha-LACE was designed to permeate biological membranes with the incorporation of the cationic choline head grou

Apostatin-1 (Apt-1) is a novel TRADD inhibitor.Apostatin-1 inhibits RIPK1-dependent apoptosis (RDA) with IC50 of 1.28 μM and shows no significant off-target activity on 97 kinases in KINOME scan profiling.Inhibition of TRADD by Apostatin-1 blocks apoptosi

BAY-1816032 (BAY1816032) is a highly potent, selective, orally active BUB1 mitotic checkpoint serine/threonine kinase with IC50 of 7 nM, displays excellent selectivity on a panel of 395 kinases.

BMS-1166 Hcl salt is a potent PD-1/PD-L1 interaction inhibitor with IC50 of 1.4 nM in a homogenous time-resolved fluorescence binding assay.

Danicamtiv (MYK-491), an inotropic agent, is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.

Ensitrelvir (S-217622) fumarate is the first orally active non-covalent, non-peptidic, SARS-CoV-2 3CL protease inhibitor (IC50=13 nM).

KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2.

LDN193189 HCl is a selective BMP signaling inhibitor, inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM, respectively, exhibits 200-fold selectivity for BMP versus TGF-β.

LEI110 (LEI－110) is a potent Phospholipase A2 group XVI (PLA2G16) inhibitor with Ki of 20 nM, also has activity on HRASLS2, RARRES3 and iNAT (pIC50=6.8-7.6).

Maytansinoid DM4, a chemical derivative of maytansine, is a potent and selective cytotoxic agent with promising anticancer properties. Anticancer properties of maytansinoids have been attributed to their ability to disrupt microtubule function. Maytansin

Methacholine chloride is used to constrict airway smooth muscle and to assess bronchial reactivity. Methacholine chloride is a cholinergic agonist and parasympathomimetic bronchoconstrictor. A metabolically stable analog of acetylcholine, it is a muscarin

ORY-1001 dihydrochloride (RG-6016, Ladademstat) is a highly potent, selective inhibitor of lysine-specific demethylase KDM1A (LSD1) with IC50 of 18 nM, displays high selectivity for KDM1A over other FAD-containing monoamine oxidases.

P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1[1].

Parsaclisib (INCB050465) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib can be used for the research of relapsed or refractory B-cell malignancies.

PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research ofcancer[1][2]. PF-9363 (0~1 μM; 1 day; ZR75-1, T47D and MCF7 cells) down-regulates the expression of H3K23Ac biomarker[1]. PF-9363

Potent Allosteric Agonist-Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptors

preQ1 is a precursor in the biosynthesis of queuosine, a bacterial nucleoside incorporated into tRNA by tRNA transglycosylase. preQ1 binds to an aptamer domain on tRNA that acts as a riboswitch to repress gene expression.

Sacubitril, also known as AHU377, is angiotensin receptor neprilysin inhibitor being studied for use in combination with valsartan for heart failure. Sacubitril is a prodrug that is activated to LBQ657 by de-ethylation via esterases. LBQ657 inhibits the e

Zabedosertib (BAY 1834845) is a IRAK4 inhibitor with immunomodulatory potential. IRAK4 is a protein kinase involved in signaling innate immune responses from Toll-like receptors.

GO289 (GO-289, GO 289) is a potent and selective inhibitor of casein kinase 2 (CK2) with IC50 of 7 nM in in vitro kinase assays, shows minor effects on CKIδ and CKIα activity in vitro.

Cyclo(Gly-Gln) is a cyclic dipeptide.