CDK Inhibitor

YK-2168 is a potent and selective CDK9 inhibitor with an IC50 of 5.9 nM. YK-2168 inhibits phosphorylation of the CDK9 substrate pS2-RNA Pol II C-terminal domain. YK-2168 induces apoptosis in tumor cells, suppresses expression of CDK9-regulated genes including MYC and Mcl1, and inhibits tumor growth in CDX mice models. YK-2168 can be used for the research of cancer, such as leukemia.

Ipivivint (Compound 38) is an orally active and potent CDC-like kinase (CLK) inhibitor with EC₅₀ of 1 nM and 7 nM for CLK2 (human) and CLK3 (human), respectively. Ipivivint also inhibits the Wnt pathway (EC50=13 nM) and tyrosine phosphorylation-regulated kinase 1A (human) (EC₅₀=5 nM).

Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC₅₀ of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC₅₀ of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI₅₀ values between 0.2-0.3 μM. Samuraciclib hydrochloride hydrate has anti-tumor effects.

JH-XVI-178 is a highly efficient and selective CDK8/19 inhibitor, with IC₅₀ values of 1 and 2 nM for CDK8 and CDK19, respectively. JH-XVI-178 has a low clearance rate and moderate oral pharmacokinetic properties.

LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC₅₀ 11 nM) and other transcription kinases CDK8 (IC₅₀ 16 nM), and CDK7 (IC₅₀ 246 nM).

MFH290 is an orally active, selective covalent CDK12/CDK13 inhibitor, with an IC₅₀ of 25 nM against human CDK12 and 49 nM against human CDK13. MFH290 reduces the phosphorylation level of CTD-RNAPII-Ser2, downregulates genes related to DNA damage response (DDR), and inhibits transcription factors regulated by super-enhancers. MFH290 can be used in research related to various cancers including leukemia.

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization.

CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection, with an IC₅₀ of 39 nM for CDK9/CycT1, extracted from reference, compound 87.

Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC₅₀s of  5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.

CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain.

YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC₅₀s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.

BSJ-03-204 triTFA is a PROTAC-based CDK degrader derived from Palbociclib (HY-50767). BSJ-03-204 triTFA targets bovine CDK4/CCND1 and CDK6/CCND1 complexes with IC₅₀ values of 26.9 nM and 10.4 nM, respectively. BSJ-03-204 triTFA also triggers ubiquitination and degradation of RB1, reduces pRb levels, thereby inducing G1 cell cycle arrest and exerting antiproliferative effects, as well as inducing time-dependent KLHL8 accumulation. BSJ-03-204 triTFA can be used in research related to pancreatic ductal adenocarcinoma, breast cancer, lung cancer, mantle cell lymphoma, and cloned bovine placental hyperplasia.

CDK9 inhibitor HH1 is a potent and selectively CDK9 inhibitor. CDK9 inhibitor HH1 inhibits the transcription of CDK. CDK9 inhibitor HH1 can be used in research of cancer.

TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC₅₀ values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs).

AZD5597 is an inhibitor of CDK with IC₅₀ values of both 2 nM for CDK1 and CDK2. AZD5597 can inhibit the proliferation of tumor cells and has anti-tumor activity.

Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC₅₀ of 0.5 µM and suppresses monomethylation of H₄K₂₀. Ryuvidine also inhibits CDK4 with an IC₅₀ of 6.0 μM. Ryuvidine also inhibits KDM5A and blocks DNA synthesis. Ryuvidine has anticancer activity against tumors such as breast cancer. Ryuvidine improves arthritis.

Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity. Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1). Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes.

CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC₅₀ = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer.

CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila.

ECI830 (CDK2-IN-37) is an orally active, ATP-competitive and highly selective CDK2 inhibitor. ECI830 shows high selectivity over other CDK family members. ECI830 can be used for the study of HR+/HER2- breast cancer and CCNE1-amplified tumors (such as ovarian cancer and lung cancer).