TBB

SKU: orb1305153

Description

TBB (NSC-231634) is a potent and selective ATP-competitive inhibitor of casein kinase 2 (CK2). It is widely used in biochemical and cellular research to study CK2's role in signaling pathways, cell proliferation, and apoptosis, with applications in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 17374-26-4
• MW: 434.71
• Purity: 99.45% (May vary between batches)
• Formula: C₆HBr₄N₃
• SMILES: BrC1=C2C(=C(Br)C(Br)=C1Br)N=NN2
• Target: Casein Kinase,CDK,GSK-3
• Solubility: DMSO:43.5 mg/mL (100.07 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.6 mM);Ethanol:100 mM

Bioactivity

• Target IC50:
  DYRK2:0.99 μM|PIM3:0.86 μM|HIPK2:5.3 μM|DYRK1A:4.36 μM|HIPK3:4.9 μM|DYRK3:5.3 μM|CDK2:14 μM|PIM2:4.3 μM|PKD1:5.9 μM|CK2:0.4 μM(Ki)|PIM1:1.04 μM|CK1:47 μM(Ki)
• In Vivo:
  In a mouse OIR model, treatment with TBB (60 mg/kg per day for 6 days), the most specific CK2 inhibitor known, reduces retinal neovascularization by approximately 60%.
• In Vitro:
  Investigation of the inhibitory power of TBB against a panel of 33 protein kinases reveals the highest potency for CK2 (casein kinase 2) (human CK2: IC50=1.6 μM at 100 μM ATP). TBB also shows moderate inhibition for CDK2 (IC50=15.6 μM), phosphorylase kinase (IC50=8.7 μM), and glycogen synthase kinase 3β (GSK3β) (IC50=11.2 μM), while IC50 values for all other kinases are 50-fold greater than for CK2. TBB (60 μM) may reduce the viability of androgen-insensitive PC-3 cells either alone or in combination with anticancer agents CPT or TRAIL, when administered with a specific schedule, although this time-dependent activity is not due to its effect on apoptosis in PC-3 cells. TBB is an ATP/GTP competitive inhibitor of CK2 and has been tested against 33 protein kinases, both Ser/Thr- and Tyr-specific. At 10 μM TBB (and 100 μM ATP), CK2 is drastically inhibited (>85%), with moderate inhibition observed for phosphorylase kinase, glycogen synthase kinase 3L, and cyclin-dependent kinase 2/cyclin A, with IC50 values one to two orders of magnitude higher than for CK2 (IC50=0.9 μM). Additionally, TBB inhibits endogenous CK2 in cultured Jurkat cells.
• Cell Research:
  TBB is dissolved in DMSO and stored, and then diluted with appropriate media before use. PC-3 or HeLa cells are cultured routinely in RPMI-1640 and DMEM media, respectively, which are supplemented with 10% FBS, Penicillin (100 U/mL) and Streptomycin (100 μg/mL) at 37°C in a humidified atmosphere of 5% CO2. Cells are seeded at 5×104 cells/well (PC-3) or 2×104 (HeLa) in 24-wells plates and cultured for 72 h. TBB (final concentration 60 μM), CPT (final concentration 5.8 nM), 2-deoxyglucose (2-DG; final concentration 0.5 mM) or TRAIL (final concentration 13.3 ng/mL) are added to the medium individually or in a combination and the cells are cultured for additional time, indicated on each figure. After treatment, the medium with the agent is removed and 500 μL of MTT mixture (0.5 mg/mL for PC-3 and 5.0 mg/mL for HeLa cells in medium without phenol red) is added to each well and incubated for an additional 1 h at 37°C. The formazan crystals are diluted in 250 μL of DMSO. The absorbance is measured at 570 nm.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TBB, CK2, CDK2, Casein Kinase II Inhibitor I, CaseinKinase, Casein Kinase, 4,5,6,7-tetrabromobenzotriazole, Inhibitor, GSK-3β, GSK3, NSC 231634, NSC-231634, NSC231634, inhibit

Compound Identifiers

PubChem CID

1694