TBB

SKU: orb1225935

Description

TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively).

Key Properties

• CAS Number: 17374-26-4
• MW: 434.71
• Purity: >98% (HPLC)
• Formula: C₆HBr₄N₃
• SMILES: BrC1=C(NN=N2)C2=C(Br)C(Br)=C1Br
• Target: CDK
• Solubility: DMSO, Ethanol: 100 mM

Bioactivity

• In Vivo:
  The extent of retinal neovascularization in a mouse OIR model is reduced by approximately 60% after treatment with TBB (6 days at 60 mg/kg per day).
• In Vitro:
  Investigation of the inhibitory power of TBB with a panel of 33 protein kinases shows highest potency for CK2 (casein kinase 2) (human CK2: IC50 = 1.6 μM at 100 μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC50 = 15.6 μM), phosphorylase kinase (IC50 = 8.7 μM) and glycogen synthase kinase 3β (GSK3β) (IC50 = 11.2 μM). All other kinases tested have IC50 values 50-fold greater than that for CK2. The viability of the androgen insensitive PC-3 cells may be diminished by TBB (60 μM TBB) acting either alone or combined with anticancer agents CPT or TRAIL when a proper time schedule of the administration is applied. The time schedule-dependent activity of TBB does not come from its effect on apoptosis in PC-3 cells. TBB is an ATP/GTP competitive inhibitor of protein kinase casein kinase-2 (CK2), has been examined against a panel of 33 protein kinases, either Ser/Thr- or Tyr-specific. In the presence of 10 μM TBB (and 100 μM ATP) only CK2 is drastically inhibited (> 85%) whereas three kinases (phosphorylase kinase, glycogen synthase kinase 3 L and cyclin-dependent kinase 2/cyclin A) underwent moderate inhibition, with IC50 values one-two orders of magnitude higher than CK2 (IC50 = 0.9 μM). TBB also inhibits endogenous CK2 in cultured Jurkat cells.

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

NSC 231634 | Tetrabromobenzotriazole

Quick Database Links

Gene Symbol

CDK