TBB NEW
Price | $38 | $54 | $68 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: TBB | CAS No.: 17374-26-4 |
Purity: 99.45% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | TBB |
Description | TBB (NSC-231634)(NSC-231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2). |
Cell Research | TBB is dissolved in DMSO and stored, and then diluted with appropriate media before use[2]. 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[2]. |
Kinase Assay | Kinase assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid. |
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[1]. 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[2]. 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[3]. |
In vivo | In a mouse OIR model, treatment with TBB (60 mg/kg per day for 6 days), the most specific CK2 inhibitor known[4], reduces retinal neovascularization by approximately 60%. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 43.5 mg/mL (100 mM) Ethanol : 100 mM |
Keywords | inhibit | Casein Kinase | NSC-231634 | Inhibitor | NSC231634 | TBB |
Inhibitors Related | Ribociclib | Cromolyn sodium | CHIR-99021 | Emodin | 4-Chloro-2'-bromoacetophenone | Palbociclib monohydrochloride | CASIN | Palbociclib | Sodium Oxamate | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |
Related Compound Libraries | Highly Selective Inhibitor Library | Anti-Lung Cancer Compound Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Kinase Inhibitor Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Oxidation-Reduction Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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