1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
  2. Casein Kinase

TBB (Synonyms: NSC 231634; TBB (enzyme inhibitor))

Cat. No.: HY-14394 Purity: 98.14%
Data Sheet SDS Handling Instructions

TBB is a selective inhibitor for the protein kinase CK2 with IC50 of 1.6 μM.

For research use only. We do not sell to patients.
TBB Chemical Structure

TBB Chemical Structure

CAS No. : 17374-26-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 75 In-stock
10 mg USD 68 In-stock
50 mg USD 234 In-stock
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    TBB purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Dec 6;148:41-51.

    Knockdown of CK2α expression with siRNA inhibits the expressions of fibronectin (FN) and intercellular adhesion molecule-1 (ICAM-1) in glomerular mesangial cells (GMCs)s induced by TBB (1 μM).

    TBB purchased from MCE. Usage Cited in: Biochem Pharmacol. 2017 Dec 6;148:41-51.

    Inhibition of CK2α activity by TBB shows a similar effect, restrains the expression of myocardin-related transcription factor A (MRTF-A) in kidneys of diabetic mice.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    TBB is a selective inhibitor for the protein kinase CK2 with IC50 of 1.6 μM.

    IC50 & Target

    IC50: 1.6 μM (CK2), 11.2 μM (GSK3β), 15.6 μM (CDK2)[1]

    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[1]. 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[2]. 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[3].

    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)[4].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.3004 mL 11.5019 mL 23.0038 mL
    5 mM 0.4601 mL 2.3004 mL 4.6008 mL
    10 mM 0.2300 mL 1.1502 mL 2.3004 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [4]

    TBB is dissolved in PBS (pH 7.2) with 20% polyethylene glycol 400 (PEG 400) and 2% Tween-80 (Mice)[4].

    Mice[4]
    The heterozygous C57BL/6J mice are used. Emodin and TBB are injected intraperitoneally in volumes of 50 μL or less per mouse at doses of 15 to 30 mg/kg body weight, twice daily, starting from day 11. Control mice are injected with PEG-Tween vehicle alone. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 98.14%

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    Product Name:
    TBB
    Cat. No.:
    HY-14394
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