Flupenthixol dihydrochloride is a typical antipsychotic of the thioxanthene class that acts as an antagonist at dopamine D2 receptors (Ki = 0.38 nM) and an inverse agonist at serotonin 5-HT2A receptors (Ki = 7 nM).1 It has also been identified as an inhib

Selective RIP3 kinase inhibitor

(E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.

Selnoflast (example 6) is a NLRP3 inhibitor (extracted from patent WO2019008025).

QcrB inhibitor TB47 (TB47) is a novel antimycobacterial agent that fuctions as a putative respiratory complex III (QcrB) inhibitor with MIC of 0.016-0.5 ug/mL against a panel of 56 M. tuberculosis clinical isolates.

BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.

KSQ-4279 is a USP1 and PARP inhibitor. KSQ-4279 showed anti-proliferative effects in a subset of cell lines, often characterized by the presence of homologous recombination deficiencies (HRD), including mutations in BRCA1/2. The combination of KSQ-4279 with olaparib was able to induce strong and durable regressions across a number of ovarian and TNBC PDX models.

Nedisertib (M3814, MSC2490484A) is a highly potent, selective, orally bioavailable inhibitor of DNA-PK.

HRX215 is a first-in-class MKK4 inhibitor with IC50 of 0.02 μM and shows above 100-fold selectivity against JNK1, BRAF, and MKK7. HRX215 increases liver regeneration after hepatectomy in murine and porcine models.

MRTX 1133 is a potent and selective KRAS G12D inhibitor. MRTX1133 targets the KRAS G12D protein in both active and inactive states. In preclinical studies, MRTX1133 exhibited a long half-life, an ability to bind the KRAS G12D protein in both active and inactive states, and selective inhibition of KRAS G12D mutant cancer cells.

TACH101 (QC8222, TACH 101) is a reversible, α-ketoglutarate competitive, selective and potent inhibitor of KDM4 isoforms A-D with IC50 values of <0.1 uM against all four isoforms.TACH101 demonstrated potent increase of H3K36me3 levels (EC50 <0.001 uM, HTRF) in KYSE-150 cell line engineered to overexpress KDM4C and showed potent anti-proliferative activity in multiple cell lines in OncoPanel.Sub-micromolar levels of TACH101 induced apoptosis in human colorectal (HT-29), esophageal (KYSE-150), and triple negative breast cancer (MDA-MB-231) cell lines with EC50s of 0.033-0.092 uM.TACH101 triggered effective tumor growth control in xenograft models including colorectal, esophageal, gastric, breast, and lymphoma with tumor growth inhibition of up to 100%.

Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.

SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukemia (AML).

Dihydroresveratrol is an SIRT1 activator. It is a primary metabolite of resveratrol.

10-Hydroxycanthin-6-one is an antileukemic canthin-6-one alkaloid from Brucea antidysenterica. Antitumor agent.

9-Hydroxycanthin-6-one is an alkaloid compound. 9,10-Dimethoxycanthin-6-one exhibits NF-κB inhibitory effects with an IC50 of 3.8 μM.

9-Methoxycanthin-6-one, a canthin-6-one alkaloid, is present in intact plant parts and in callus tissues of different explants. 9-Methoxycanthin-6-one shows anti-tumor activity.

Canthin-6-one displays a wide range of biological activities, such as antimycobacterial activity.

LOXO-305 is an investigational, novel, selective non-covalent Bruton’s tyrosine kinase (BTK) inhibitor. LOXO-305 was designed to reversibly bind BTK, preserve activity in the presence of the acquired resistance, and avoid off-target kinases that have complicated the development of both covalent and investigational non-covalent BTK inhibitors.LOXO-305 is a highly selective, non-covalent BTKi that inhibits both wild type (WT) and C481-mutated BTK with equal low nM potency was developed.

AZD5462 is a selective oral allosteric relaxin family peptide receptor 1 (RXFP1) agonist with pEC50 of 7.8. AZD5462 has better kinetic solubility and shows much improved metabolic stability compared to AZ7976 in vitro.

Pulchinenoside B4 is a triterpenoid glycoside that inhibits cisplatin-induced apoptosis, increases in reactive oxygen species (ROS) production, and decreases in superoxide dismutase (SOD) and catalase activities. Pulchinenoside B4 also prevents increases in plasma blood urea nitrogen (BUN) and creatinine levels -- markers of kidney injury.

A novel specific glycomimetic E-Selectin antagonist with Kd of 0.46 uM, IC50 of 1.75 uM.

Lipase Substrate is a substrate of lipase to detect activity.

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections.

PC-766B is a macrolide antibiotic. PC-766B is active against Gram-positive bacteria, and some fungi and yeasts, but inactive against Gram-negative bacteria. PC-766B shows antitumor activity against murine tumor cells. PC-766B has weak inhibitory activity against Na+, K+-ATPase.