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tBID 

Cat. No.: HY-100464 Purity: >98.0%
Handling Instructions

tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM.

For research use only. We do not sell to patients.

tBID Chemical Structure

tBID Chemical Structure

CAS No. : 1639895-85-4

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 489 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
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100 mg USD 2520 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of  0.33 µM.

IC50 & Target

IC50: 0.33 µM (HIPK2)[1]

In Vitro

Homeodomain-interacting protein kinase 2 (HIPK2) is a Ser/Thr kinase controlling cell proliferation and survival. TBID, displays toward HIPK2 unprecedented efficacy (IC50=0.33 µM) and selectivity (Gini coefficient 0.592 out of a panel of 76 kinases). The two other members of the HIPK family, HIPK1 and HIPK3, are also inhibited by TBID albeit less efficiently than HIPK2. The mode of action of TBID is competitive with respect to ATP, consistent with modelling. TBID interacts with the hinge region through hydrophobic interactions between Val 213, Val 261, Phe 277, Leu 280, Met 331, Ile 345, and the tetrabromine moiety, while the symmetric nitrogen atom at position 3 interacts with the catalytic Lys 228, thus playing a crucial role in the binding architecture[1].

Molecular Weight

528.78

Formula

C₁₁H₃Br₄N₃O₂

CAS No.

1639895-85-4

SMILES

O=C1N(C2=NC=CN2)C(C3=C(Br)C(Br)=C(Br)C(Br)=C31)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 26 mg/mL (49.17 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8911 mL 9.4557 mL 18.9115 mL
5 mM 0.3782 mL 1.8911 mL 3.7823 mL
10 mM 0.1891 mL 0.9456 mL 1.8911 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

HepG2 cells (human hepatocellular carcinoma) are cultured in Dulbecco's modified Eagle's medium supplemented with 10% fetal calf serum, 2 mM L-glutamine, 100 unit/mL penicillin and 100 µg/mL streptomycin. Treatments with TBID are performed in the same medium but with 1% fetal calf serum; control cells are treated with the solvent (DMSO). Cell viability is evaluated by means of MTT[1]

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

References
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Keywords:

tBIDDYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseInhibitorinhibitorinhibit

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