CDK Inhibitor

CA224 (Standard) is the analytical standard of CA224 (HY-111207). This product is intended for research and analytical applications. CA224 (Compound 1) is a selective and orally active Cdk4–cyclin D1 inhibitor with an IC₅₀ of 6.2 µM. CA224 induces cell apoptosis and shows antitumor activity.

PHA-793887 hydrochloride is a CDK inhibitor (with IC₅₀ values of 8 nM for Cdk2, 60 nM for Cdk1, 62 nM for Cdk4, 138 nM for Cdk9). PHA-793887 hydrochloride inhibits purified GSK3β (IC₅₀ 79 nM). PHA-793887 hydrochloride reduces the phosphorylation level of nucleophosmin/cdc6, induces G1/G2/M phase arrest, and triggers Apoptosis by activating Caspase-3. PHA-793887 hydrochloride exhibits anticancer activity against leukemia. PHA-793887 hydrochloride can be used in research related to acute leukemia, chronic myeloid leukemia, and advanced/metastatic solid tumors.

Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer.

CDK2-IN-27 (compound 1) is a potent CDK2 inhibitor with IC₅₀ values of <10, >10-20 nM for CDK2/cyclin E1, CDK2/cyclin B1, respectively.

CDK9-IN-1 (Standard) is the analytical standard of CDK9-IN-1. This product is intended for research and analytical applications. 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.

BDE30671203 is a highly selective PLK1 inhibitor (IC₅₀ = 2.163 nM). BDE30671203 induces G2/M phase arrest and Apoptosis. BDE30671203 downregulates key cell cycle regulators (CDC20, CDK1) and the anti-apoptotic gene Bcl-2. BDE30671203 exhibits anticancer activity against non-small cell lung cancer, large cell lung cancer, and liver cancer.

Purvalanol A (Standard) is the analytical standard of Purvalanol A. This product is intended for research and analytical applications. Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.

CGC-11144 hydrochloride is a polyamine analog. CGC-11144 hydrochloride reduces the kinase activities of CDK4, CDK2 and CDK6, induces activation of the p53 pathway and p53-dependent p21 expression, and mediates cell cycle regulation, growth inhibition and apoptosis. CGC-11144 hydrochloride induces G1 phase cell cycle arrest, downregulates cyclin D1 and cyclin B1, upregulates cyclin E, induces dephosphorylation of pRb, and inhibits ERα-mediated transcriptional activity by disrupting the DNA binding of Sp1/Sp3 to the ERα promoter, while also stimulating activation of the JNK/AP-1 pathway. CGC-11144 hydrochloride can be used in research related to breast cancer, choroidal neovascularization and cancer.

PF 477736 (PF 00477736) (Standard) is the analytical standard of PF 477736 (HY-10032). This product is intended for research and analytical applications. PF 477736 (PF 00477736) is a potent, selective and ATP-competitive inhibitor of Chk1, with a K_i of 0.49 nM, it is also a Chk2 inhibitor, with a K_i of 47 nM. PF 477736 shows <100-fold selectivity for Chk1 over VEGFR2, Fms, Yes, Aurora-A, FGFR3, Flt3, and Ret (IC₅₀=8 (K_i), 10, 14, 23, 23, 25, and 39 nM, respectively). PF 477736 can enhance Gemcitabine antitumor activity in vitro and in vivo.

(R)-DRF053 is a CDK inhibitor. (R)-DRF053 inhibits Cdk5 and promotes the formation of ductal precursor β cells. (R)-DRF053 inhibits Dil-ox-LDL uptake and CD36 gene expression induced by advanced glycation end products (AGEs) in U937 cells.

NG 52 (Standard) is the analytical standard of NG 52. This product is intended for research and analytical applications. NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p.

Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

O6-Benzylguanine sodium is an orally active, blood-brain barrier-penetrant inhibitor of O⁶-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine sodium modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine sodium is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction.

(2S,3R)-Fadraciclib is the 2S,3R isomer of Fadraciclib (HY-101212). Fadraciclib is an orally potent ATP-competitive CDK2/CDK9 kinase inhibitor with IC₅₀ values of 5 and 26 nM, respectively.

MK256 is an orally active, selective CDK8 inhibitor and CDK19/cyclin C inhibitor with IC₅₀ values of 2.5 nM and 3.3 nM, respectively. MK256 downregulates phosphorylated STAT1 ^(S727), STAT5 ^(S726), MCL-1 mRNA and CCL2 mRNA. MK256 exhibits anti-tumor activity in acute myeloid leukemia. MK256 can be used for the research of acute myeloid leukemia.

2-Cyanoethylalsterpaullone (compound 7) is an Alsterpaullone (HY-108359) derivative, which exhibits potent and selective inhibitory activities against CDK1/Cyclin B and GSK-3β (GSK-3β: IC₅₀=0.8 nM; CDK1/Cyclin B: IC₅₀=0.23 nM).

NSC 625987 (Standard) is the analytical standard of NSC 625987 (HY-103380). This product is intended for research and analytical applications. NSC 625987 is a specific and high-affinity CDK4 inhibitor with an IC₅₀ of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2.

O6-Benzylguanine Standard is the analytical standard of O6-Benzylguanine (HY-W002585). This product is intended for research and analytical applications. O6-Benzylguanine is an orally active, blood-brain barrier-penetrant inhibitor of O⁶-methylguanine-DNA methyltransferase (MGMT/AGT). O6-Benzylguanine modulates p53 and its downstream p21 and cyclins to induce cell cycle arrest and apoptosis, and on the other hand activates mTORC1/MAPK and other signaling pathways to induce cellular senescence by inhibiting intracellular MGMT. O6-Benzylguanine is used in research related to various tumors, cellular senescence, and vascular smooth muscle dysfunction.

Flavopiridol (Standard) is the analytical standard of Flavopiridol (HY-10005). This product is intended for research and analytical applications. Flavopiridol (Alvocidib) is a broad spectrum and competitive inhibitor of CDKs, inhibiting CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.

Icariside I (Standard) is the analytical standard of Icariside I (HY-N1939). This product is intended for research and analytical applications. Icariside I (GH01) is an orally active metabolite of icalin. Icariside I improves estrogen deficiency-induced osteoporosis by simultaneously regulating osteoblast and osteoclast differentiation. Icariside I promotes ATP (HY-B2176) or Nigericin (HY-127019)-induced mtROS production and NLRP3 inflammasome activation and causes idiosyncratic hepatotoxicity. Icariside I does not alter the activation of NLRC4 and AIM2 inflammasomes. Icariside I inhibits breast cancer proliferation, apoptosis, invasion, and metastasis by targeting the IL-6/STAT3 pathway. Icariside I is a kynurenine-AhR pathway inhibitor that alleviates cancer by blocking tumor immune escape.