TBB is a potent protein kinase CK2 inhibitor, which induces apoptosis and caspase-dependent degradation of haematopoietic lineage cell-specific protein 1 (HS1) in Jurkat cells.
CAS Number: 17374-26-4
Molecular Weight: 434.71
Chemical Name: 4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
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 3L 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.
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).
- Gyenis L, Kuś A, Bretner M, Litchfield DW. Functional proteomics strategy for validation of protein kinase inhibitors reveals new targets for a TBB-derived inhibitor of protein kinase CK2. J Proteomics. 2013 Apr 9;81:70-9. doi: 10.1016/j.jprot.2012.09.017. Epub 2012 Sep 25. PubMed PMID: 23017496.
- Orzechowska E, Kozłowska E, Staroń K, Trzcińska-Danielewicz J. Time schedule-dependent effect of the CK2 inhibitor TBB on PC-3 human prostate cancer cell viability. Oncol Rep. 2012 Jan;27(1):281-5. doi: 10.3892/or.2011.1500. Epub 2011 Oct 12. PubMed PMID: 21993828.
- Isaeva AR, Mitev VI. The protein kinase CK2 inhibitor TBB mediates up-regulation of MEK3/6 and p38δ activities, down-regulation of ERK1/2 activity and induction of G1/S arrest in normal human epidermal autocrine proliferating keratinocytes. J Dermatol Sci. 2011 Aug;63(2):124-6. doi: 10.1016/j.jdermsci.2011.04.005. Epub 2011 Apr 27. PubMed PMID: 21620683.
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