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%
Handling Instructions

TBB is a selective inhibitor for the protein kinase CK2 with IC50 of 0.15 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
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Estimated Time of Arrival: December 31
10 mg USD 68 In-stock
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Estimated Time of Arrival: December 31
50 mg USD 234 In-stock
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Estimated Time of Arrival: December 31
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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.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    TBB is a selective inhibitor for the protein kinase CK2 with IC50 of 0.15 μM.

    IC50 & Target[5]

    CK2

    0.15 μM (IC50, Human CK2)

    PIM1

    1.04 μM (IC50)

    PIM2

    4.3 μM (IC50)

    PIM3

    0.86 μM (IC50)

    HIPK2

    5.3 μM (IC50)

    HIPK3

    4.9 μM (IC50)

    DYRK1a

    4.36 μM (IC50)

    DYRK2

    0.99 μM (IC50)

    DYRK3

    5.3 μM (IC50)

    PKD1

    5.9 μM (IC50)

    CDK2

    14 μM (IC50)

    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].

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 430 mg/mL (989.17 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent 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.
    In Vivo:
    • 1.

      TBB is prepared in 0.3% CMC-Na[6].

    References
    Cell Assay
    [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]

    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
    Molecular Weight

    434.71

    Formula

    C₆HBr₄N₃

    CAS No.

    17374-26-4

    SMILES

    BrC1=C2C(NN=N2)=C(Br)C(Br)=C1Br

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 98.14%

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    This equation is commonly abbreviated as: C1V1 = C2V2

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

    Cat. No.: HY-14394