RGB-286638

RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.

Product Specifications

CAS Number

[784210-87-3]

UNSPSC

12352005

Target

CDK; GSK-3; JAK; MEK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/RGB-286638.html

Purity

99.70

Solubility

DMSO : ≥ 150 mg/mL|H2O : 25 mg/mL (ultrasonic)

Smiles

O=C(NN1CCOCC1)NC2=CC=CC(C3=C4C(C5=CC=C(CN6CCN(CCOC)CC6)C=C5)=NN3)=C2C4=O.[H]Cl.[H]Cl

Molecular Formula

C29H37Cl2N7O4

Molecular Weight

618.55

References & Citations

[1]Cirstea D, et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27 (12) :2366-75.