CDK Inhibitor

TrkA Inhibitor (Compound 18) is a CDK2 inhibitor with an IC₅₀ of 0.69  μM over CDK1. TrkA Inhibitor can be used for chemotherapy-induced alopecia research.

Cdk4 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Cdk4 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK11-IN-1 hydrochloride is an orally active cyclin-dependent kinase 11 (CDK11) inhibitor with an IC₅₀ of 4 nM, and it exhibits high selectivity against other kinases including CDK7 and CDK9. CDK11-IN-1 hydrochloride inhibits tumor growth in lung cancer xenograft models. CDK11-IN-1 hydrochloride can be used for lung cancer research.

Maleimide-Val-Ala-PAB-SNS032 is a conjugate of ADC toxin and linker. SNS032 is an inhibitor for CDK, inhibiting the cell cycle at G1/S phase and cell viability of cancer cells. Maleimide-Val-Ala-PAB is a cleavable ADC linker. Maleimide-Val-Ala-PAB-SNS032 can be utilized for the synthesis of ADC molecules.

CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC₅₀ value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML).

CLK1-IN-5 is a potent and selective CLK1 inhibitor with an IC₅₀ of 23 nM. CLK1-IN-5 can be used in the research of cancer and Alzheimer's disease.

CDK9-IN-22 is a potent CDK9 inhibitor with IC₅₀s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity.

Chikusetsusaponin IVa methyl ester (CME) is a natural triterpenoid saponin compound. Chikusetsusaponin IVa methyl ester induces G0/G1 cell cycle arrest and apoptosis in colon cancer cells by inhibiting the Wnt/β-catenin signaling pathway. By inhibiting the NF-κB and AP-1 signaling pathways, Chikusetsusaponin IVa methyl ester significantly reduces the production of NO, PGE₂ and pro-inflammatory cytokines (TNF-α, IL-6, IL-1β), and downregulates the levels of iNOS and COX-2. Chikusetsusaponin IVa methyl ester can be used in researches on colorectal cancer and inflammation.

P18IN005 hydrochloride is a novel inhibitor of p18, exhibiting potent activity in negatively regulating haematopoietic stem cell (HSC) self-renewal. P18IN005 hydrochloride has been shown to be more effective than p27 in inhibiting HSC self-renewal in mouse models. P18IN005 hydrochloride promotes the expansion of functional HSCs in short-term cultures. P18IN005 hydrochloride serves as a valuable tool for dissecting the signaling pathways involved in stem cell self-renewal.

NUAK1-IN-1 (Compound 9) is a NUAK1 (IC₅₀ of 5.012 nM) and CDK4 inhibitor. NUAK1-IN-1 can be used in cancer, neurodevelopmental disorders and Alzheimer's disease research.

Cdc7-IN-17 is a potent CDC7 inhibitor with an IC₅₀ of <10 μM, extracted from patent WO2018217439A1. Cdc7-IN-17 can be used for cancer research.

Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM.

CDK2-IN-20 (compound 3b) is an inhibitor of CDK2. CDK2-IN-20 has cytotoxicity on tumor cells presenting an IC₅₀ range of 5.52-17.09 µM. CDK2-IN-20 arrests the MCF-7 cell cycle at the S phase and induces apoptosis.

GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC₅₀ values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo.

USP10-IN-4 is a potent ubiquitin-specific protease 10 (USP10) inhibitor with an IC₅₀ of 10.87 μM and a K_d of 365 nM. USP10-IN-4 effectively inhibits USP10-mediated proteasomal degradation of downstream proteins YAP and p53, leading to the subsequent downregulation of CDK4 in the p53 signaling pathway. USP10-IN-4 promotes apoptosis in HCC cells and inhibits the onset and progression of liver cancer. USP10-IN-4 can used for the study of hepatocellular carcinoma (HCC).

CDK4/6-IN-14 is a potent and highly selective CDK4 and CDK6 (CDK) inhibitor with IC₅₀s of 10 nM and 16 nM, respectively. CDK4/6-IN-14 exhibits more than 60-fold selectivity over CDKs 1, 2, 7, and 9, and shows high selectivity among other 205 kinases.

Metralindole hydrochloride is an inhibitor of human cyclin-dependent kinase CDK2 and human protein kinase CK2 holoenzyme. Metralindole hydrochloride shows good potential as a non-small cell lung cancer inhibitor.

CDK9-IN-15 (compound 50) is a potent CDK9 inhibitor.

CDK4/6/BRD4-IN-1 (B15) is an inhibitor of CDK4, CDK6 and BRD4, with IC₅₀ values of 220 nM, 146 nM, 106 nM and 85 nM for BRD4-BD2, BRD4-BD1, CDK6 and CDK4, respectively. CDK4/6/BRD4-IN-1 (B15) can be used in the study of NSCLC (Non-Small Cell Lung Cancer). CDK4/6/BRD4-IN-1 (B15) induces cell cycle arrest and apoptosis.

FOXM1-IN-3 is a potent FOXM1 inhibitor. FOXM1-IN-3 downregulates FOXM1 expression at protein and mRNA levels, suppressing downstream effectors CCNB1 and CDC25. FOXM1-IN-3 induces G2/M cell cycle arrest and apoptosis in colorectal cancer cells. FOXM1-IN-3 inhibits colony formation and cell migration in colorectal cancer cells. FOXM1-IN-3 targets the cancer stem cell phenotype in colorectal cancer cells, reducing cancer stem cell marker expression. FOXM1-IN-3 reduces tumor growth in a zebrafish xenograft model. FOXM1-IN-3 can be used for the research of colorectal cancer.