Cancer Targeted Therapy

Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a K_i of 0.13 nM.

CQ211 is a potent and selective RIOK2 inhibitor with a K_d of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines.

Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

CPI-455 hydrochloride is a specific, pan-KDM5 inhibitor with an IC₅₀ of 10 nM for KDM5A. CPI-455 hydrochloride mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.

Zandelisib (ME-401) is a selective, orally active, non-covalent inhibitor of PI3Kδ. Zandelisib can sustainably inhibit AKT phosphorylation and downstream signaling pathways. Zandelisib can be used in the study of malignancies such as relapsed/refractory B-cell lymphoma.

Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC₅₀s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively.

K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity.

Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with K_is of 5.2 nM and 2.9 nM in cell-free assays, respectively.

ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC₅₀ value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.

SS-208 is a selective HDAC6 inhibitor, with an IC₅₀ of 12 nM. SS-208 possesses anti-tumor activity in melanoma.

CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC₅₀=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6.

Allopurinol sodium is a potent and orally active xanthine oxidase inhibitor with an IC₅₀ value of 0.2-50 μM. Allopurinol sodium can be used in the research of hyperuricemia and gout. Allopurinol sodium decreases the expression of HIF-1α and HIF-2α protein. Allopurinol sodium shows anti-depressant and anti-nociception activity. Anti-leishmanial effect.

Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with K_is of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC₅₀s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with K_d values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC₅₀ of 24 nM for ITK.

CP5V is a Cdc20 PROTAC degrader with a DC₅₀ of 1.6 μM and a K_d value of 12.4 μM. CP5V couples Cdc20 with the VHL/VBC complex, triggering its ubiquitination and proteasomal degradation, thereby reducing the protein levels of Cdc20 and securin. CP5V induces mitotic arrest, inhibits cell proliferation, resensitizes Paclitaxel-resistant breast cancer cells, and suppresses breast tumor progression in xenograft models. CP5V inhibits excessive proliferation and induces apoptosis in pulmonary arterial hypertension smooth muscle cells and fibroblasts. CP5V can be used in studies related to breast cancer and pulmonary arterial hypertension.

Zilurgisertib (INCB-000928; NBU-928) is a selective ALK2 inhibitor with an IC₅₀ value of 15 nM. Zilurgisertib inhibits SMAD1/5 phosphorylation with an IC₅₀ value of 63 nM. Zilurgisertib inhibits hepcidin production and improve anemia. Zilurgisertib can be used in melanoma research.

USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC₅₀s of 0.42 μM and 1.0 μM, respectively.

Bisindolylmaleimide X hydrochloride(Ro 31-8425 hydrochloride, BIM-X hydrochloride) is a cell-penetrating PKC inhibitor. Bisindolylmaleimide X hydrochloride is a potent cyclin-dependent kinase 2 (CDK2) antagonist with an IC₅₀ of 200 nM. Bisindolylmaleimide X hydrochloride inhibits the proliferation of CD4 T cells in vitro. Bisindolylmaleimide X hydrochloride inhibits eNOS-Ser1177 phosphorylation in human embryonic vein endothelial cells. Bisindolylmaleimide X hydrochloride can be used for research on the immune system and cardiovascular diseases.

NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC₅₀ values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT.