(-) BI97D6 (BI112D1) is a potent, pan-active inhibitor of Bcl-2 family proteins with IC50 of 76, 31, 25, and 122 nM for Bcl-xL, Bcl-2, Mcl-1, and Bfl-1, respectively.

INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rats, and human 11β-HSD1, respectively.

ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

GPR65 agonist (BTB09089) is a novel GPR65 agonist.

NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2.

IM-250 is a potent HSV-1 helicase primase inhibitor, inhibits HSV-1 replication with IC50 of 20 nM (clinical isolate of HSV-1).IM-250 dispalys similar IC50 values (20-30 nM) against ACV-resistant HSV-1 clinical isolates 2 and 3 and ACV-resistant HSV-2 clinical isolates 7 and 8.IM-250 exhibits a broad therapeutic window against HSV-1 in vitro with pronounced higher SI values as obtained for acyclovir (ACV).IM-250 shows in vivo efficacy and attenuates viral burden in HSV-1 infection mouse model.

SLLK, Control Peptide for TSP1 Inhibitor (TFA) is a control peptide for LSKL, which is a Thrombospondin (TSP-1) inhibitor.

Dinoprost (Prostaglandin F2α, PGF2α) is a naturally occurring prostaglandin used to induce labor and as an abortifacient, causes contraction of vascular, bronchial, intestinal, and myometrial smooth muscle, and also exhibits potent luteolytic activity..

CFI-402257(luvixasertib) is a potent and selective Mps1/TTK kinase inhibitor with Ki of 0.1 nM and cellular Mps1 EC50 of 6.5 nM.

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.TH9619 demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9619 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with IC50 of 47 and 16 nM, respectively.TH9619 displays high potency and cancer selectivity in AML models. induce thymine-less DNA damage and apoptosis, causes uracil misincorporation into DNA, sensitize cancer cells to ATR-signaling blockade.TH9619 impairs cancer progression in vivo.TH9619 displays high selectivity toward binding and stabilizing MTHFD2 over other common folate metabolism targets such as DHFR, thymidylate synthase (TYMS), serine hydroxymethyltransferase (SHMT) 1 and SHMT2.

Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis.

VRK-IN-1 is a potent and selective inhibitor of vaccinia-related kinases 1 (VRK1), with an IC50 of 150 nM. VRK1 is human Ser/Thr protein kinases associated with increased cell division and neurological disorders.

YC-001 is a novel pharmacological chaperone of rod photoreceptor opsin, rescues the transport of multiple rod opsin mutants in mammalian cells.

T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).

GAT1508 (GAT-1508) is a potent, specific activator for brain-expressed GIRK1/2 channels (EC50=75 nM), specifically activates the brain GIRK1/2 over the cardiac GIRK1/4; GAT1508 is an allosteric modulator of channel–phosphatidylinositol 4,5-bisphosphate interactions. GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder.

Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of 87.8 uM.Foldamer 33 disrupts HSP110-STAT3 interaction with IC50 of 35.9 uM in competitive BLI assays.Foldamer 33 inhibits SW480 colorectal cancer cell proliferation, and (5 mg/kg) Foldamer 33 displays an anti-tumor effect (TGI of 40% and 60%) in mice bearing a colorectal cancer.

Rv1625c agonist V-59 (V-59) is a specific small molecule agonist of the Mtb adenylyl cyclase Rv1625c, inhibits Mtb growth in macrophages (EC50=0.3 uM) in an Rv1625c-dependent mechanism.V-59 inhibits Mtb growth in cholesterol media (EC50 0.70 uM), but not in media containing the two-carbon fatty acid acetate, or in standard rich growth media.V-59 stimulates Rv1625c to produce cAMP, which is necessary for V-59 to inhibit Mtb growth.Chemically activating Rv1625c via V-59 preferentially inhibits cholesterol utilization in WT Mtb, rather than equally inhibiting all lipid utilization by the bacterium.

AEP07 (AEP 07) is a selective small molecule inhibitor of PARP4 (vPARP) inhibitor with IC50 of 0.8 uM, >12-fold selective over other PARP family members.

A coumarin-based HIV-1 viral protein R (Vpr) inhibitor, inhibits Vpr-dependent viral infection of human macrophages..

AMXT-1501 (AMXT 1501, AMXT1501) is a novel potent polyamine transport inhibitor, synergistically reduces cell viability in NB cells in combination of with DFMO.

BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 blocked nucleotide exchange to prevent the activation of wild-type KRAS and a broad range of KRAS mutants, including G12A/C/D/F/V/S, G13C/D, V14I, L19F, Q22K, D33E, Q61H, K117N and A146V/T. Inhibition of downstream signalling and proliferation was restricted to cancer cells harbouring mutant KRAS, and drug treatment suppressed KRAS mutant tumour growth in mice, without having a detrimental effect on animal weight.

AP20187 (AP-20187, AP 20187) is a cell-permeable, semisynthetic bivalent ligand (dimerizer) of FK506-binding protein (FKBP F36V).

JSH-150 (JSH150) is a potent, highly selective inhibitor of CDK9 kinase with IC50 of 1 nM in the biochemical assays, displays 300-10000-fold selectivity over other CDK kinase family members (CDK7 IC50=1.72 uM).

dBRD9 is a PROTAC that bridge the BRD9 bromodomain and the cereblon E3 ubiquitin ligase complex.

2-MPPA (GPI-5693) is an orally active and selective glutamate carboxypeptidase II (GCP II; PSMA) inhibitor with an IC50 of 90 nM.

SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.

Fenretinide Glucuronide Monosodium Salt, is the metabolite of Fenretinide (F250000), which is a synthetic retinoid deriverative, substances related to vitamin A. They are also shown to be used for the treatment of cancer, as well as in the treatment of cystic fibrosis, rheumatoid arthritis, acne, and psoriasis.

BFL-1 inhibitor 4E14 (4E14) is a potent, selective, covalent BFL-1 inhibitor that disrupt BH3-binding activity with IC50 of 1.3 uM, targets a unique C55 residue in the BFL-1 groove.4E14 blocks BFL-1 suppression of BAX-mediated mitochondrial apoptosis.

SCB-4380 (SCB 4380, SCB4380) is the first potent, selective inhibitor for PTPRZ (protein tyrosine phosphatase receptor-type Z) with IC50 of 0.4 uM against human Z-ICR-catalyzed hydrolysis. SCB-4380 also strongly inhibits PTPRG (IC50=0.4 uM), and shows little inhibition on PTPRA, PTPRM, PTPRS, PTPRB, PTPN1 and PTPN6. SCB-4380 inhibites PTPRZ activity in C6 glioblastoma cells, and suppresse cell migration and proliferation in vitro and tumor growth in a rat allograft model.