Ro-3306

SKU: orb1223785

Description

Ro-3306 is a potent, selective, ATP-competitive CDK1 inhibitor with Ki of 35 nM against CDK1/cyclin B1, 10-fold selectivity relative to CDK2/cyclin E and >50-fold relative to CDK4/cyclin D; also inhibits CDK1/cyclin A complexes with Ki of 110 nM, shows >15-fold selectivity against a diverse panel of 8 human kinases; reversibly arrests human cells at the G(2)/M border of the cell cycle and allows for effective cell synchronization in early mitosis; enhances p53-mediated Bax activation and mitochondrial apoptosis in AML.

Key Properties

• CAS Number: 872573-93-8
• MW: 351.4453
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₃N₃OS₂
• SMILES: O=C1N=C(NCC2=CC=CS2)S/C1=C/C3=CC=C4N=CC=CC4=C3
• Target: CDK
• Solubility: DMSO: ≥ 47 mg/mL

Bioactivity

• In Vitro:
  RO-3306 is an ATP-competitive inhibitor, and inhibits CDK1/cyclin A complexes with Ki of 110 nM. RO-3306 blocks the cell cycle in the G2/M phase of human cancer cells. RO-3306 (4 μM) induces apoptosis in cancer cells. RO-3306 (5 μM) induces G2/M-phase cell cycle arrest and apoptosis of AML cells in a time-dependent manner. RO-3306 treatment significantly increases the percentage of Annexin V-positive cells in G1-phase cells without affecting the cell cycle distribution. RO-3306 enhances p53-mediated apoptosis. RO-3306 cooperates with Nutlin-3 in activating Bax and inducing mitochondrial apoptosis. RO-3306 (5 μM) downregulates antiapoptotic p21, Bcl-2 and survivin protein expression in AML. RO-3306 inhibits p53-induced p21 synthesis. RO-3306 does not inhibit RNA polymerase II CTD phosphorylation. RO-3306 (10 μM) effectively arrests oocyte maturation. RO-3306 reduces the blastocyst formation in oocytes.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ro3306

Quick Database Links

Gene Symbol

CDK