CDK Inhibitor

PKMYT1-IN-15 is an orally active PKMYT1 inhibitor with an IC₅₀ of 6.02 nM. PKMYT1-IN-15 inhibits the phosphorylation of CDK1 at Thr14. As an antiproliferative agent, DNA damage inducer and antitumor agent, PKMYT1-IN-15 triggers replication-associated DNA damage and cell death in CCNE1-amplified cancer cells, and suppresses tumor growth in the OVCAR3 xenograft model. PKMYT1-IN-15 can be used for the research of CCNE1-amplified cancers (e.g., ovarian cancer, breast cancer).

CGP-74514 hydrochloride is a highly selective cyclin-dependent kinase 1 (CDK1) inhibitor (IC₅₀: 25 nM). CGP-74514 hydrochloride inhibits CDK1/cyclin B complex activity, arrests the cell cycle at G₂/M phase and induces tumor cell apoptosis. CGP-74514 hydrochloride is promising for research of bladder cancer.

SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC₅₀ values ​​of 4 nM and 44 nM, respectively, and a K_i of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease.

JD128 (Compound 22) is a CDK4/6 inhibitor.

Anticancer agent 299 (compound P12) is a cell-cycle inhibitor, senescence inducer, apoptosis inducer, and antiproliferative agent. Anticancer agent 299 exhibits selective activity against cancer cells with minimal effects on non-tumoral chondrocyte cells at relevant concentrations. Anticancer agent 299 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma.

Cdc7-IN-8 is a potent inhibitor of Cdc7. Cdc7 is a serine/threonine kinase which activates MCM promotion by phosphorylating the microchromosome maintenance protein (MCM protein), an important element of the DNA replication initiator. Cdc7-IN-8 has the potential for the research of cancer diseases (extracted from patent WO2021032170A1, compound 1-1/1-2).

GW780056X is a CDK12 inhibitor. GW780056X decreases nuclear foci count in DM1 cells. GW780056X can be used for the research of myotonic dystrophy type 1.

CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3) and PDGFRA, with IC₅₀s of 1.672, 0.554, and 0.629 μM, respectively. CDK2/FLT4/PDGFRA-IN-1 exhibits potent antiproliferative effects against cancer cells (lung EBC-1, pancreatic ductal adenocarcinoma AsPC-1, colorectal HT-29 cells). CDK2/FLT4/PDGFRA-IN-1 can also induce apoptosis in cancer cells.

Cdk6 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk6 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK8-IN-18 (compound BRD-2299) is a potent inhibitor of CDK8, with the IC₅₀ of 43 μM. CDK8-IN-18 plays an important role in cancer research.

CDK-IN-20 is a selective CDK2 inhibitor with an IC₅₀ value of <10 nM. CDK-IN-20 can be used for cancer research.

Anticancer agent 29 (Compd E/Z-6f) is an anticancer agent, with IC₅₀ values of 0.054 μM, 0.127 μM, 0.129 μM, 0.396 μM for CDK2, CDK1, CDK4 and CDK6, respectively.

GIT1-IN-1 is an inhibitor of ARF GTPase-activating protein 1 (GIT1) with a K_D of 6.2 μM. GIT1-IN-1 induces apoptosis (apoptosis) in liver and colon cancer cells, arrests the cell cycle at the G2/M phase, and inhibits cell proliferation, colony formation and migration. GIT1-IN-1 inhibits the activities of MEK and ERK, reduces the expression level of cyclin D1, and stabilizes cyclin B1 protein in liver and colon cancer cells. GIT1-IN-1 can be used in the research of liver cancer and colon cancer.

CDK7/9-IN-1 is a cyclin-dependent kinases 7/9 (CDK7/9) inhibitor. CDK7/9-IN-1 selectively inhibits CDK7 over CDK9. CDK7/9-IN-1 inhibits CDK7 with IC₅₀s of 0.0656 μM and 0.00574 μM without pre-incubation and after 3 hours pre-incubation, respectively. CDK7/9-IN-1 inhibits CDK9 with an IC₅₀ of 2.14 μM after 3 hours pre-incubation. CDK7/9-IN-1 can be used for the research of cancer.

CDK12-IN-7 (Compound 2) is a CDK12 and CDK2 inhibitor with IC₅₀ values ​​of 42 and 196 nM, respectively. CDK12-IN-7 has anti-cell proliferation activity and can be used in cancer research.

BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-958 shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-958 exhibits good metabolic stability. BAY-958 effectively inhibits tumor growth in mouse xenograft models without significant toxicity.

CDK7-IN-26 (compound 36) is an orally active CDK7 inhibitor (IC₅₀: 7.4 nM). CDK7-IN-26 potently inhibits the growth of triple-negative breast cancer (TNBC) cell line-derived xenograft (CDX) tumors in vivo and inhibits MDA-MB-453 cells in vitro with an IC₅₀ of 0.15 μM.

CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC₅₀ of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC₅₀>20 μM) and CDK9/Cyclin T1 (IC₅₀>20 μM) at high ATP (2 mM) (WO2021116178A1).

Anticancer agent 264 (Compound 5w) is an anticancer agent that exhibits significant antiproliferative activity across tumor cell lines, with an IC₅₀ range of 7.5-33.67 μM. Anticancer agent 264 significantly induces G2/M phase arrest in MDA-MB-231, MIA PaCa-2, and DU-145 cell lines. Anticancer agent 264 reduces the expression of key cell cycle proteins, including CDK1, CDK2, and Cyclin B1, in a dose-dependent manner, and shows strong binding affinity with inhibitor of differentiation (ID) proteins and DNA-binding proteins. Anticancer agent 264 can be used for research in the field of cancer-related diseases.

CDK9-IN-25 (compound 4a) is an imidazopyrazine CDK9 inhibitor (IC₅₀: 0.24 μM). CDK9-IN-25 has good affinity to the main protease of COVID-19 and has antiviral activity against human coronavirus 229E (IC₅₀: 63.28 μM).