CDK Inhibitor

JHD205 is a CDK4/6 inhibitor that induces apoptosis and DNA damage. JHD205 inhibits DNA repair by upregulating Caspase3 and p-H2AX. JHD205 has superior potency to Abemaciclib (HY-16297A) in a xenograft chick embryo breast cancer model..

A-800141 is an orally active, selective, sulfonamide-based MetAP2 inhibitor (IC₅₀=12 nM) that binds reversibly to MetAP2 and interacts with its manganese ions. A-800141 induces the production of N-terminal methionine-unprocessed GAPDH variants, which in turn triggers G1-phase cell cycle arrest, elevates p21 levels, and reduces the levels of phosphorylated Rb and total cyclin A. A-800141 exhibits anti-angiogenic and tumor growth inhibitory effects, and produces synergistic effects when combined with cytotoxic inhibitors or BCL-2 inhibitors. A-800141 has been widely used in scientific research related to B-cell lymphoma, neuroblastoma, prostate cancer, colon cancer, melanoma and other fields.

Aloisine B (compound 9) is a cyclin-dependent kinase (CDK) inhibitor. Aloisine B inhibits cell proliferation by arresting cells in both G1 and G2 via competing with ATP-binding pocket.

FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC₅₀ of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research.

Multi-kinase-IN-7 is a multikinase inhibitor with IC₅₀s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC₅₀ values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.

PSTAIR is a monoclonal antibody that recognizes the PSTAIR sequence in Cdc28, PSTAIR can be used as loading control.

Garcinone C (Standard) is the analytical standard of Garcinone C. This product is intended for research and analytical applications. Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia that is used as an anti-inflammatory, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, arrests the cell cycle, inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner through inhibition of Hedgehog signaling pathway. Garcinone C is orally active.

Cdk1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

BLINK15 is a BBB-penetrant CDK5 inhibitor. BLINK15 lowers CDK5 activity for both complexes CDK5/p35 (IC₅₀ = 29.34 nM) and CDK5/p25 (IC₅₀ = 12.08 nM). BLINK15 offers anti-diabetic and neuroprotective benefits. BLINK15 lowers blood glucose, enhances cognition, and reduces neurodegeneration in T2D mice.

Cyclin A/B RxL-IN-1 is a inhibitor targeting the Cyclin A/B RxL interaction at the hydrophobic patch (HP). Cyclin A/B RxL-IN-1 inhibits Cyclin A with an IC₅₀ of 0.12 μM. Cyclin A/B RxL-IN-1 demonstrates antitumor efficacy in mouse cell line-derived xenograft (CDX) models. CDK-IN-19 can be used for the study of E2F-driven cancers such as small-cell lung cancer (SCLC).

Contragestazol (DL111-IT) is a non-hormonal antifertility agent. Contragestazol reduces the expression of Cyclin D1 and CDK4, increases the expression of total retinoblastoma protein (pRb), and decreases the level of hyperphosphorylated pRb. Contragestazol induces G₀/G₁ phase cell cycle arrest. Contragestazol inhibits embryonic development by inducing luteal cell apoptosis and reducing intrauterine polyamine levels. Contragestazol exhibits antitumor activity against prostate cancer, S180 tumor and H22 tumor. Contragestazol shows extremely potent activity in terminating early pregnancy in animals.

CDK9-IN-41 is a potent CDK9, EGFR, HER2, and COX-2 kinases inhibitor with IC₅₀s of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM. COX-2-IN-18 exhibits remarkable antitumor activity against leukemia cancer cells, colon cancer cells, melanoma cells, ovarian cells and breast cells.

PKMYT1-IN-12 (Compound 4) is a selective inhibitor of PKMYT1, with an IC₅₀ of 2.6 nM. PKMYT1-IN-12 can effectively inhibit the phosphorylation of CDK1, with an IC₅₀ of 44 nM. PKMYT1-IN-12 is a target protein ligand that can be used for the synthesis of PROTAC D16-M1P2 (HY-180485).

Cdk2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Cdk2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

CDK2-IN-29 (Compound 13q) is an inhibitor for cyclin-dependent kinase (CDK), with IC₅₀ of 96 nM and 360 nM, for CDK 2 and CDK 4, respectively.

IRAK4-IN-35 is an orally active IRAK4 inhibitor with an IRAK4 IC₅₀ of 9.88 nM. IRAK4-IN-35 also inhibits JAK3, EGFR, CDK2 with IC₅₀ values of 6.72 nM, 32.35 nM, and 39.08 nM, respectively. IRAK4-IN-35 inhibits the production of proinflammatory cytokines, blocks inflammatory signaling pathways, and reduces serum TNF-α levels and spleen index in mouse models of acute inflammation. IRAK4-IN-35 decreases the disease activity index, paw swelling degree, and spleen index in a collagen-induced arthritis mouse model. IRAK4-IN-35 can be used for the research of rheumatoid arthritis.

CDK8-IN-19 (Compound 3d) is a CDK8 inhibitor with an IC₅₀ of 25.08 nM. CDK8-IN-19 has a broad-spectrum anticancer activity, such as leukemia, melanoma and breast cancer, without significant cytotoxic effect on the normal Vero cells (mean IC₅₀s of 2.87, 3.65, 3.79 and 45.48 μM, respectively).

Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC₅₀s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells.

3-Methylthienyl-carbonyl-JNJ-7706621 is a potent and selective inhibitor of cyclin-dependent kinase (CDK), with IC₅₀s of 6.4 nM and 2 nM for CDK1/cyclin B and CDK2/cyclin A, respectively. 3-Methylthienyl-carbonyl-JNJ-7706621 also shows potent inhibition of GSK-3 (IC₅₀=0.041 μM) and modest potency against CDK4, VEGF-R2, and FGF-R2 (IC₅₀=0.11, 0.13, 0.22 μM, respectively). 3-Methylthienyl-carbonyl-JNJ-7706621 can be used for the research of cancer.

EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR/HER2/CDK9 with IC₅₀s of 191.08, 132.65, and 113.98 nM, respectively. EGFR/HER2/CDK9-IN-3 exhibits remarkable antitumor activity.