CDK Inhibitor

CDK4-IN-4 (example 30) is a selective CDK4 inhibitor (IC₅₀＜10 nM) that can be used in cancer research.

CDK7-IN-5 is a CDK7 inhibitor with an IC₅₀ value <100 nM. CDK7-IN-5 has anticancer effects. (WO2015154022A1 (Compound 104)).

EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC₅₀s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC₅₀ of 2.74 μM.

CDK6/9-IN-2 is a highly active dual inhibitor of CDK6 (IC₅₀ = 15 nM) and CDK9 (IC₅₀ = 22 nM). CDK6/9-IN-2 is selective for CDK2, CDK8, and CDK11. CDK6/9-IN-2 inhibits the proliferation of HaCaT cells induced by IFN-γ/TNF-α and suppresses the STAT3 pathway and the expression of inflammatory factors. CDK6/9-IN-2 can alleviate psoriatic dermatitis and is useful in psoriasis research.

DL-Aspartic acid (Standard) is the analytical standard of DL-Aspartic acid. This product is intended for research and analytical applications. DL-Aspartic acid (DL-Asp-OH) is a kind of biological materials or organic compounds that are widely used in life science research.

CDK8-IN-11 hydrochloride is a potent and selective CDK8 inhibitor with an IC₅₀ value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of colon cancer.

LS-Q2 is a highly selective CDK4/9 inhibitor with IC₅₀ values of 1.4 nM and 6.2 nM. LS-Q2 inhibits cancer cells proliferation, induces G2/M phase arrest, apoptosis and reduces pSer2 RNA polymerase II expression. LS-Q2 interacts synergistically with BET and Bcl-2 inhibitors to drive antitumor activity. LS-Q2 can be used for the research of cancer, such as malignant solid tumors.

Apoptosis inducer 50 (Compound 5e) is an apoptosis inducer as well as an autophagy inducer agent. Apoptosis inducer 50 exhibits potent and selective anti-cancer activity against triple-negative breast cancer cells and metastatic colon cancer cells. Apoptosis inducer 50 upregulates the expression of pro-apoptotic proteins (Bax, Bim, cleaved Caspase-9) and downregulates the expression of the anti-apoptotic protein (BCL-XL). Apoptosis inducer 50 upregulates key autophagy markers such as Beclin-1 and ATG5, and enhances the conversion of LC3-I to LC3-II., Apoptosis inducer 50 arrests cancer cells in the G1/S phase by upregulating the expression of p21 and p27 while downregulating Cyclin D1. Apoptosis inducer 50 increases the level of ROS.

EGFR-IN-169 is an epidermal growth factor (EGFR) (IC₅₀ = 5.19 μM) inhibitor form panaxadiol. EGFR-IN-169 interferes with the migration and growth of colorectal cancer cells by inhibiting EGFR-mediated RalA/EMT pathway. EGFR-IN-169 shows an IC₅₀ value of 4.46 μM and SI of 16.92 for HCT-116 cells. EGFR-IN-169 inhibits CDKs activity, induces G0/G1 cycle arrest and inhibits migration and invasion. EGFR-IN-169 reduces mitochondrial membrane potential and induces apoptosis and ROS production. EGFR-IN-169 can be used for the research of cancer, such as colorectal cancer.

Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a CDK2 inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner.

CDK2-IN-45 (Compound 8f) is a CDK2 inhibitor (IC₅₀: 0.64 μM). CDK2-IN-45 inhibits the proliferation of DU-145 and PC-3 cell lines with IC₅₀ of 2.20 μM and 4.17 μM, respectively. CDK2-IN-45 induces G0/G1 cell cycle arrest and apoptosis. CDK2-IN-45 can be used in prostate cancer research.

CDK1-IN-7 (compound M7) is a potent CDK1 inhibitor. CDK1-IN-7 inhibits the proliferation and migration of HCT116 and Lovo cells. CDK1-IN-7 can be used in the study of colorectal cancer.

Haspin-IN-1 (compound 2a) is a haspin inhibitor with an IC₅₀ of 119 nM. Haspin-IN-1 also inbibits CLK1 and DYRK1A with IC₅₀s of 221 nM and 916.3 nM, respectively.

CDK8/BRD4-IN-1 is a dual CDK8/BRD4 inhibitor, with an IC₅₀ of 5.44 μM against CDK8 and an IC₅₀ of 4.03 μM against BRD4. CDK8/BRD4-IN-1 exhibits anticancer activity against colorectal cancer. CDK8/BRD4-IN-1 can be used for the research of colorectal cancer.

BMK-Y101 is a potent CDK kinase inhibitor. BMK-Y101 induces tumor cell apoptosis by inhibiting CDK kinases. BMK-Y101 can be used for research on hepatocellular carcinoma.

CDK2-IN-52 (Compound Cpb No 39) is a selective cyclin-dependent kinase 2 (CDK2) inhibitor with a DC₅₀ value of 1-10 nM. CDK2-IN-52 induces cell cycle arrest and suppresses tumor cell proliferation. CDK2-IN-52 is promising for research of CDK2-overexpressing malignancies such as breast and ovarian cancers.

CDK2-IN-14 (compound 4f) is a highly selective CDK2 inhibitor. CDK2-IN-14 can be used in research of cancer.

Briciclib (ON 014185) sodium is a eukaryotic translation initiation factor 4E (eIF4E) inhibitor. Briciclib sodium exhibits broad-spectrum anti-cancer activity, including in mantle cell leukemia, breast cancer, gastric cancer, and esophageal cancer cells. Briciclib sodium reduces the expression of cyclin D1 and c-Myc, and enhances the expression of P53 and Cleaved Caspase 3 pro-apoptotic proteins. Briciclib sodium can be used for the study of hematological system tumors and solid tumors.

LQ23 is a selective inhibitor for CDC2-like kinase 2 (CLK2) with an IC₅₀ of 1.4 nM. LQ23 exhibits anti-inflammatory activity.

CDK4/6-IN-10 is a potent, selective and orally active CDK4 and CDK6 inhibitor with IC₅₀s of 22 nM and 10 nM, respectively. CDK4/6-IN-10 shows antitumor activity. CDK4/6-IN-10 has the potential for the research of Multiple myeloma (MM).