tBID
Based on 6 publication(s) in Google Scholar
tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC50 of 0.33 μM.
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- 純度: 98.24%
- CAS 番号: 1639895-85-4
- 分子式: C11H3Br4N3O2
- 分子量:528.78
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
生物活性
IC50: 0.33 μM (HIPK2)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1639895-85-4
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性状 Solid
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分子量 528.78
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分子式 C11H3Br4N3O2
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Color Light yellow to yellow
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SMILES
O=C1N(C2=NC=CN2)C(C3=C(Br)C(Br)=C(Br)C(Br)=C31)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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EBioMedicine
2022 Nov:85:104274. PMID: 36182775 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
Biol Direct
Phosphorylation-stabilized CRTC1 cooperates with CBP and androgen receptor to transactivate AMH expression and drive polycystic ovary syndrome. [Abstract]2025 Jun 19;20(1):71. PMID: 40537816 -
Exp Neurol
Neuronal HIPK2-HDAC3 axis regulates mitochondrial fragmentation to participate in stroke injury and post-stroke anxiety like behavior. [Abstract]2024 Jul 28:380:114906. PMID: 39079624 -
Exp Ther Med
HIPK2 sustains inflammatory cytokine production by promoting endoplasmic reticulum stress in macrophages. [Abstract]2020 Dec;20(6):171. PMID: 33101464 -
溶剤 & 溶解度
DMSO : 20 mg/mL (37.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8911 mL | 9.4557 mL | 18.9115 mL | 47.2786 mL |
| 5 mM | 0.3782 mL | 1.8911 mL | 3.7823 mL | 9.4557 mL | |
| 10 mM | 0.1891 mL | 0.9456 mL | 1.8911 mL | 4.7279 mL | |
| 15 mM | 0.1261 mL | 0.6304 mL | 1.2608 mL | 3.1519 mL | |
| 20 mM | 0.0946 mL | 0.4728 mL | 0.9456 mL | 2.3639 mL | |
| 25 mM | 0.0756 mL | 0.3782 mL | 0.7565 mL | 1.8911 mL | |
| 30 mM | 0.0630 mL | 0.3152 mL | 0.6304 mL | 1.5760 mL |