CDK Inhibitor

CGP-79807 is a purine-based CDK inhibitor. CGP-79807 can block the cell cycle by inhibiting CDK activity to suppress the proliferation of tumor cells. CGP-79807 can be used in the study of cancer.

G721-0282 is an orally active CHI3L1 inhibitor. G721-0282 can reduce the expression of inflammatory proteins and cytokines. G721-0282 inhibits the activation of the NF-κB signaling pathway. G721-0282 inhibits neuroinflammation and reduces anxious behavior. G721-0282 significantly inhibits the proliferation of osteosarcoma (OS) cells by suppressing the STAT3 signaling pathway. G721-0282 induces OS cell apoptosis by upregulating pro-apoptotic protein levels and downregulating anti-apoptotic protein levels. G721-0282 can be used for researches on neuroinflammatory conditions and cancer.

SM253 is an Hsp90 inhibitor that inhibits Hsp90-dependent protein folding. SM253 blocks chaperone function by binding to the N-middle linker region and the C-terminal M domain, reducing co-chaperone and client protein binding and activation. SM253 induces cancer cell apoptosis, activates caspase 3/7, causes cell cycle arrest and reduces cell proliferation, while decreasing Hsp90 client proteins such as AR, FKBP51, PSA, Cdk4, AKT, ERK, and p23, and reducing Hsp27/Hsp70 expression without inducing heat shock proteins. SM253 causes dose-dependent fibronectin loss in cells expressing LRP1. SM253 can be used for research on colon cancer, pancreatic cancer, and prostate cancer.

Multi-target kinase-IN-7 (Compound 1e) is an orally active multi-target kinase inhibitor (IC₅₀ values: CDK2=0.314 μM, EGFR=0.183 μM, HER-2=0.197 μM, VEGFR-2=0.235 μM). Multi-target kinase-IN-7 is promising for research of solid tumors (e.g., lung, breast, prostate cancer).

VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma.

SKLB70326 is a small molecule inhibitor of cell cycle progression that induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cells. SKLB70326 is involved in downregulating cyclin-dependent kinase (CDK) 2, CDK4, and CDK6, while also activating PARP, caspase-3, caspase-9, and Bax, and downregulating Bcl-2.

Cdk7 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk7 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC₅₀ values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research. CDK2/4/6-IN-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

PARP1/CDK12-IN-1 (107) is a dual inhibitor of CDK12 and PARP1, with IC₅₀ values of 285 nM and 34 nM for CDK12 and PARP1, respectively.

CDK2-IN-24 (compound 3f) is an inhibitor of cyclin-dependent kinase 2 with an elevated binding energy value .

PI3Kα/CDK7-IN-1 is a dual-target hybrid inhibitor of PI3Kα and CDK7, with IC₅₀ values of 87.9 nM and 638 nM, respectively. PI3Kα/CDK7-IN-1 acts as a cytotoxic agent and cell death inducer that triggers apoptotic death in cancer cells. PI3Kα/CDK7-IN-1 can be used in cancer research such as colorectal cancer.

CDK7-IN-22 (compound 101) is an CDK7 inhibitor with antitumor activity. CDK7-IN-22 shows selectivity on CDK7.

LBM22 is a CDC2-like kinase 2 (CLK2) inhibitor with the IC₅₀ of 3.9 nM. LBM22 has antiproliferative activity and inhibits serine/arginine-rich (SR) protein phosphorylation. LBM22 down-regulates the expression of Wnt-related proteins and anti-apoptotic proteins and can be used for study of non-small cell lung cancer.

CDK7-IN-14 is a potent inhibitor of CDK7. CDK7-IN-14 is a pyrimidinyl derivative compound. CDK7-IN-14 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 3).

Cdk12 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk12 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK5-IN-4 (compound 4) is a potent multikinase type-II inhibitor targeting CDK5, with an IC₅₀ of 9.8 μM. CDK5-IN-4 also inhibits GSK-3α, GSK-3β, CDK9, and CDK2, with IC₅₀ values of 0.98, 4.00, 1.76, and 6.24 μM, respectively. CDK5-IN-4 can be used for glioblastoma research.

CDKI-IN-1 (Compound SNX12) is a cyclin-dependent kinase inhibitor (CDKI) inhibitor that can be used for research into degenerative diseases of the central nervous system.

Calactin is a glycoside that can be isolated from Asclepias curassavica L.. Calactin activates caspase-3, caspase-8, caspase-9, and phosphorylates ERK. Calactin induces DNA damage, apoptosis, PARP cleavage, G2/M phase cell cycle arrest, shifts Bax/Bcl-2 expression, and shows anti-proliferation effects in leukemia cells. Calactin can be used for the research of leukemia.

Crozbaciclib fumarate is a CDK4/6 inhibitor with IC₅₀s of 3 and 1 nM, respectively.

CDK9 ligand 1 is a CDK9-targeting ligand. CDK9 ligand 1 can be used for PROTAC synthesis, and serves as the target protein ligand for PROTAC CDK9 Degrader-1 (HY-103628).