4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt
TBB
CAS: 17374-26-4
Molecular Formula: C6HBr4N3
4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt - Names and Identifiers
4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt - Physico-chemical Properties
| Molecular Formula | C6HBr4N3 |
| Molar Mass | 434.71 |
| Density | 2.840±0.06 g/cm3(Predicted) |
| Melting Point | 262-266°C |
| Boling Point | 552.5±45.0 °C(Predicted) |
| Solubility | Soluble in DMSO (100 mM), ethanol (20 mM), DMF (~20 mg/ml), and 1:1 solution of DMF:P |
| Appearance | grayish white solid |
| Color | white |
| Maximum wavelength(λmax) | ['300nm(MeOH)(lit.)'] |
| pKa | 3.87±0.40(Predicted) |
| Storage Condition | 2-8°C |
| MDL | MFCD06411399 |
| Use | A highly selective CK2α, Dyrk1A, and NS3 viral helicase inhibitor. |
| In vitro study | Investigation of the inhibitory power of TBB with a panel of 33 protein kinases shows highest potency for CK2 (casein kinase 2) (human CK2: IC 50 =1.6 μM at 100 μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC 50 =15.6 μM), phosphorylase kinase (IC 50 =8.7 μM) and glycogen synthase kinase 3β (GSK3β) (IC 50 =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 3L and cyclin-dependent kinase 2/cyclin A) underwent moderate inhibition, with IC 50 values one-two orders of magnitude higher than CK2 (IC 50 =0.9 μM). TBB also inhibits endogenous CK2 in cultured Jurkat cells. |
| In vivo study | 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). |
4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt - Risk and Safety
| WGK Germany | 3 |
| HS Code | 29349990 |
4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt - Introduction
TBB(NSC 231634) is a ATP/GTP competitive CK2 inhibitor with IC50 of 0.9 and 1.6 μM for rat liver and human recombinant CK2, respectively.
Last Update：2022-10-16 17:41:29
4,5,6,7-Tetrabromo-2-azabenzimidazole, 4,5,6,7-Tetrabromobenzotriazole, NSC 231634, TBBt - Reference Information
| biological activity | TBB is a permeable cell, ATP competitive CK2 inhibitor, and the IC50 value of inhibiting rat liver CK2 is 0.15 μM. |
Last Update：2024-04-09 02:00:08
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Product Name: TBB Visit Supplier Webpage Request for quotationCAS: 17374-26-4
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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