CDK Inhibitor

Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC₅₀s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3).

Abemaciclib (Standard) is the analytical standard of Abemaciclib. This product is intended for research and analytical applications. Abemaciclib (LY2835219) is a selective and BBB-permeable CDK4/6 inhibitor with IC₅₀ values of 2 nM and 10 nM for CDK4 and CDK6, respectively.

SGC-CLK-1, a chemical probe, is a potent and selective inhibitor of Cdc2-like kinases CLK1, CLK2, and CLK4. SGC-CLK-1 can inhibit the growth of melanoma and glioblastoma cells.

Aminopurvalanol A is a potent, selective, and cell permeable inhibitor of Cyclins/Cdk complexes. Aminopurvalanol A preferentially targets the G2/M-phase transition inhibiting cancer cell differentiation. Aminopurvalanol A causes the inhibition of sperm fertilizing ability via the inhibition of physiological capacitation-dependent actin polymerization.

CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain.

CDK2-IN-23 (Compound 17) is a kinase selective and highly potent CDK2 inhibitor (IC₅₀ = 0.29 nM). CDK2-IN-23 shows the pharmacodynamic inhibition of CDK2 in CCNE1-amplified mouse models. CDK2-IN-23 can be used for the research of cancer.

CP681301 is a potent CDK5 inhibitor. CP681301 shows antiproliferative activity. CP681301 decreases the expression of CD133, OLIG2, SOX2, KI67, pCDK5 protein level in GSCs (Glioma stem cells). CP681301 reduces self-renewal in mouse glioma xenografts. CP681301 shows anti-tumor activity in Drosophila.

SRI-29329 is a specific CLK inhibitor, with IC₅₀ values of 78 nM, 16 nM and 86 nM for CLK1, CLK2 and CLK4, respectively.

BML-259 is a potent cyclin-dependent kinase 5 (Cdk5) inhibitor, with IC₅₀s of 64 and 98 nM for Cdk5 and Cdk2, respectively.

Licoisoflavone A is an orally active isoflavone. Licoisoflavone A inhibits proliferation, induces apoptosis, and causes G1/S phase arrest in colorectal cancer (CRC) cells. Licoisoflavone A inhibits the CDK2-Cyclin E1 axis. Licoisoflavone A inhibits lipid peroxidation with an IC₅₀ of 7.2 μM. Licoisoflavone A shows a dose-dependent inhibition effect on SARS-CoV-2 infection. Licoisoflavone A exhibits significant anti-tumor efficacy in mice bearing CT26 cell subcutaneous xenografts. Licoisoflavone A can be used for the study of colorectal cancer and SARS-CoV-2 infection.

Ribociclib (Standard) is the analytical standard of Ribociclib. This product is intended for research and analytical applications. Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

Dehydrozingerone is a ginger-derived component and cyclin D1 inhibitor that downregulates cyclin D1 expression and induces cell cycle G₁ phase arrest. Dehydrozingerone reduces the proliferative capacity of castration-resistant prostate cancer cells under in vitro conditions. Dehydrozingerone reduces subcutaneous tumor growth by inhibiting cell proliferation and angiogenesis. Dehydrozingerone exerts antibacterial and antifungal activities via its α,β-unsaturated carbonyl conjugated system. Dehydrozingerone can be used in studies related to castration-resistant prostate cancer, bacterial infections, and food spoilage fungal infections.

CDK4/6-IN-15 hydrochloride is an orally active and selective CDK4/6 inhibitor. CDK4/6-IN-15 hydrochloride potently inhibits cancer cells growth. CDK4/6-IN-15 hydrochloride arrests cell cycle at G1 phase and suppresses retinoblastoma tumour suppressor protein (Rb) phosphorylation at S780 and E2 factor (E2F)-regulated gene expression.

bio-THZ1 is a biotinylated version of THZ1 and binds irreversibly to CDK7. THZ1 is a selective and potent covalent CDK7 inhibitor with an IC₅₀ of 3.2 nM.

Ribociclib-d₆ (LEE011-d₆) hydrochloride is a deuterium labeled Ribociclib. Ribociclib is a highly specific CDK4/6 inhibitor with IC₅₀ values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.

ZNL-05-044 is a CDK11 inhibitor with an IC₅₀s of 0.23 μM and 0.27 μM against CDK11A and CDK11B, respectively (NanoBRET assay). ZNL-05-044 leads to G2/M cell cycle arrest and impairs RNA splicing.

(-)-Syringaresinol is an orally active isomer of syringaresinol (HY-N8307) found in Annona Montana. (-)-Syringaresinol exhibits antioxidant, anti-inflammatory, and anticancer activities. (-)-Syringaresinol can alleviate ulcerative colitis via the PI3K-Akt/MAPK/Wnt signaling pathway. (-)-Syringaresinol inhibits HL-60 cell proliferation by arresting the G1 phase and inducing apoptosis. (-)-Syringaresinol inhibits LPS (HY-D1056)-induced microglial activation by downregulating the NF-κB p65 signaling pathway and its interaction with ERβ, exerting anti-neuroinflammatory effects.

CCT036477 is a Wnt/β-catenin pathway inhibitor. CCT036477 blocks transcription at β-catenin without altering its levels. CCT036477 inhibits proliferation of various cancer cells, development of embryos, and expression of Wnt target genes (PPARδ, Cyclin D1, TCF4, and ID2).

TG693 is an orally active inhibitor of CLK1. TG693 regulates the mutated exon 31 of the dystrophin gene in vivo. TG693 is used in Duchenne muscular dystrophy (DMD) research.

Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.