JHK-02-108-2

JHK-02-108-2 (1 μM; 5 h) selectively degrades CDK6 in MOLT-4 cells, as measured by global proteomics^[1].
JHK-02-108-2 (0.01-50 μM; 6 h, 24 h) induces dose-dependent, selective, and sustained degradation of CDK6 (with no hook effect) in MOLT-4 cells^[1].
JHK-02-108-2 (0.001-100 μM) induces dose-dependent degradation of CDK6 in K562-Cas9 reporter cells, which is blocked by palbociclib (a CDK6 ATP-competitive inhibitor) but not by regorafenib^[1].
JHK-02-108-2 (0.0001-100 μM) does not inhibit CDK6/cyclin D1 kinase activity at concentrations up to 100 μM in an in vitro kinase assay^[1].
JHK-02-108-2 (0.0001-100 μM) binds purified CDK6 protein with a K_d of 1900 nM in an in vitro binding assay^[1].
JHK-02-108-2 (200 nM; 7-60 sec) induces CRBN-dependent ubiquitination of purified CDK6 protein in an in vitro ubiquitination assay, with detectable activity within 7 sec of incubation^[1].
JHK-02-108-2 (0.001-100 μM) induces ternary complex formation between purified CRBN-DDB1 and CDK6 proteins with an EC₅₀ of 0.22 μM in a TR-FRET assay, with a hook effect at concentrations above 1 μM^[1].
JHK-02-108-2 (0.01-10 μM; 72 h, 1 μM; 24 h) inhibits growth (IC₅₀ = 0.64 μM), induces G1 cell cycle arrest, and degrades CDK6 (DC₅₀ = 11 nM) in BT145 GBM cells, with near-complete CDK6 loss after 24 h treatment with 1 μM^[1].
JHK-02-108-2 (0.001-10 μM; 72 h) reduces cell viability and induces G1 arrest in FLT3^WT and FLT3^ITD AML cell lines, with greater selectivity over its negative control in FLT3^WT lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.