LK1/2-IN-3 (compound 3) is a potent and selective CLK1 and CLK2 inhibitor with IC50 values of 1.1, 2.1, 130, 260, 260 nM for CLK1, CLK2, SRPK1, SRPK2, SRPK3, respectively. CLK1/2-IN-3 shows anti-proliferative activity. CLK1/2-IN-3 reduces the levels of endogenous phosphorylated SR proteins and increases the expression of S6K mRNAs[1].
Cdk4/6 Inhibitor IV is a cell-permeable triaminopyrimidine compound acting as a reversible and ATP-competitive inhibitor of Cdk4/6 (IC50 = 1.5 ��M and 5.6 ��M for Cdk4/D1 and Cdk6/D1, respectively)
(2S,3R)-Voruciclib is the (2S,3R)-enantiomer of Voruciclib. (2S,3R)-Voruciclib is an orally active CDK inhibitor[1].
BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].
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[1].
(S)-Cdc7-IN-18 is a potent inhibitor of CDC7. Overexpression of huCdc7 promotes overactivation of MCM2, an important marker of tumor cells, and thus promotes aberrant proliferation of tumor cells. (S)-Cdc7-IN-18 has the potential for the research of cancer diseases (extracted from patent WO2020239107A1, compound 1-1)[1].
CDK2-IN-4 is a potent and selective CDK2 inhibitor with an IC50 of 44 nM for CDK2/cyclin A, shows 2,000-fold selectivity over CDK1/cyclin B (IC50=86 uM)[1].
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division[1][2][3].
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)[1].