CDK Inhibitor

CDK2-IN-25 (compound 7e) is a CDK2 inhibitor with an IC₅₀ of 0.149 μM.

CDK9-IN-39 (1-7a-B1) is an orally active cyclin-dependent kinase 9 (CDK9) inhibitor with an IC₅₀ of 6.51 nM. CDK9-IN-39 induces cell apoptosis by inhibiting the phosphorylation of RNA polymerase II at Ser2 and can be used for study of colorectal cancer .

CDK9-IN-35 (compound 10j) is an inhibitor of CDK9/Cyclin T1 with an IC₅₀ value of 10.2 nM and against the HCT-116 cell line with an IC₅₀ value of 20 nM.

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

SGK1-IN-3 (Compound 3a) is an ATP-competitive SGK1 inhibitor with an IC₅₀ of <1 nM against hSGK1. SGK1-IN-3 blocks the activity of CDK family members. SGK1-IN-3 is a P-glycoprotein substrate. SGK1-IN-3 can be used for research on osteoarthritis.

KWZL-7f15 is a dual CDK6/BRD4 inhibitor with an IC₅₀ of 31.81 nM against human CDK6. KWZL-7f15 inhibits the CDK6-RB axis and BRD4-Myc axis, and also acts as a pan-BET inhibitor. KWZL-7f15 exhibits antiproliferative activity against triple-negative breast cancer cells. KWZL-7f15 shows antitumor activity in xenograft mouse models. KWZL-7f15 can be used in studies related to triple-negative breast cancer.

CDK7-IN-13 is a potent inhibitor of CDK7. CDK7-IN-13 is a pyrimidinyl derivative compound. CDK7-IN-13 has the potential for the research of various cancers, especially the cancer with transcriptional dysregulation (extracted from patent CN114249712A, compound 1).

PROTAC BRD4 Degrader-16 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-16 induces sustained degradation of both long and short isoforms of BRD4 in cancer cells, causes cell cycle arrest, and exhibits only extremely low apoptosis effects. PROTAC BRD4 Degrader-16 can be used in studies related to acute myeloid leukemia.

KuWal151 is a CLK1, CLK2 and CLK4 inhibitor with a high selectivity margin towards DYRK kinases. KuWal151 has potent antiproliferative activity in an array of cultured cancer cell lines.

XC219 (compound 43) is a cyclin-dependent kinase CDK) inhibitor, that covalently binds to CDK active site Lys. XC219 can be used in antifungal research.

CDC20/HSP90-IN-1 (Compound 2b) is a Cdc20/Hsp90 inhibitor with a K_d of 16.2 μM for Cdc20 and a K_d of 0.241 μM for Hsp90α. CDC20/HSP90-IN-1 exerts potent antitumor activity through reducing p53-mediated Cdc20, upregulating Bim, downregulating Cyclin B1 expression, and disturbing B-Raf and AKT pathways via destroying Hsp90 chaperone function. CDC20/HSP90-IN-1 overcomes Vemurafenib (HY-12057)-induced resistant melanoma.

(Rac)-Roscovitine ((Rac)-Seliciclib) is a selective cyclin-dependent kinases (CDKs) inhibitor. (Rac)-Roscovitine binds to the active sites of CDKs competitively with ATP, inhibiting the phosphorylation activity of CDKs. (Rac)-Roscovitine induces apoptosis in cancer cells. (Rac)-Roscovitine is promising for research of cancers or other diseases associated with CDK dysregulation, such as neurodegenerative diseases, cardiac disorders, viral and protozoan infections, glomerulonephritis, and chronic inflammation.

CDK2-IN-60 is an orally active, ATP-competitive selective CDK2 inhibitor with a K_i of 77 pM. CDK2-IN-60 has high selectivity for both CDK4 and CDK1. CDK2-IN-60 blocks G1/S cell cycle progression to suppress proliferation of CCNE1-amplified tumor cells. CDK2-IN-60 serves as a lead chemical probe for investigating CCNE1-amplified cancers and CDK4/6 inhibitor-resistant HR-positive breast cancer.

CDK9-IN-47 is an orally active and selective CDK9 inhibitor with an IC₅₀ of 1.4 nM. CDK9-IN-47 inhibits tumor cell proliferation, migration and invasion, and induces apoptosis. CDK9-IN-47 can be used for the research of triple-negative breast cancer.

CDK9-IN-48 is a CDK9 inhibitor with an IC₅₀ of 1.37 nM. CDK9-IN-48 inhibits the proliferation of various cancer cells. CDK9-IN-48 can be used in the research of cancers such as acute myeloid leukemia and prostate cancer.

CDK13 Human Pre-designed siRNA Set A contains three designed siRNAs for CDK13 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Cdk14 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk14 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

BLINK11 is a BBB-penetrant CDK5 inhibitor. BLINK11 lowers CDK5 activity for both complexes CDK5/p35 (IC₅₀ = 17.09 nM) and CDK5/p25 (IC₅₀ = 14.69 nM). BLINK11 offers anti-diabetic and neuroprotective benefits. BLINK11 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.

NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC₅₀ value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC₅₀ values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth.

GSPT1 degrader-1 is a highly selective degrader targeting GSPT1. GSPT1 degrader-1 induces degradation via the ubiquitin-proteasome system. GSPT1 degrader-1 induces G₀/G₁ phase arrest, apoptosis (apoptosis) and inhibits proliferation in leukemia cells. GSPT1 degrader-1 reduces the levels of CDK6 and Cyclin B1, while increases the levels of activated caspase-3 and caspase-9 in leukemia cells. GSPT1 degrader-1 can be used in leukemia research.