BH3I-1
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- CAS號:
- 300817-68-9
- 英文名:
- BH3I-1
- 英文別名:
- BHI1;BHI1;BH 3I1;BH3I 1 ;BH3I1;5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid;5-(p-Bromobenzylidene)-a-isopropyl-4-oxo-2-thioxo-3-thiazolidine acetic acid;2-(5-(4-Bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic acid;3-Thiazolidineacetic acid, 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-;MDM-2/p53,BH3I 1,Inhibitor,Ubiquitin ligase,BH3I-1,E3 ligating enzyme,Ubiquitin conjugating enzyme,BH3I1,E2 conjugating enzyme,Bcl-2 Family,BHI 1,E1 activating enzyme,inhibit,BHI-1,BH 3I1,E1/E2/E3 Enzyme,Ubiquitin activating enzyme,BH-3I-1
- 中文名:
- BH3I-1
- 中文別名:
- 化合物BH3I1;BH3I-1游離態(tài);2-(5-(4-溴苯基亞甲基)-4-氧代-2-硫代噻唑-3-基)-3-甲基丁酸
- CBNumber:
- CB6497943
- 分子式:
- C15H14BrNO3S2
- 分子量:
- 400.31
- MOL File:
- 300817-68-9.mol
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BH3I-1化學(xué)性質(zhì)
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沸點(diǎn):
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535.2±60.0 °C(Predicted)
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密度:
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1?+-.0.1 g/cm3(Predicted)
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儲存條件:
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Sealed in dry,2-8°C
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溶解度:
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DMSO: >10 mg/mL, soluble
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形態(tài):
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powder, yellow
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酸度系數(shù)(pKa):
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3.39±0.10(Predicted)
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顏色:
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Light yellow to yellow
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BH3I-1性質(zhì)、用途與生產(chǎn)工藝
BH3I-1 是一種 Bcl-2家族 拮抗劑，抑制 Bak BH3 肽與 Bcl-xL 結(jié)合，Ki 為 2.4±0.2 μM。BH3I-1 作用于 p53/mDM2，Kd 為 5.3 μM。
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Bcl-2
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Bcl-xL
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Bim
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Bak
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p53/mDM2
5.3 μM (Kd)
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BH3I-1, while inhibiting its reported target Bcl-2/Bim and Bcl-xL/Bim, shows significant inhibition of both the p53/hDM2 and p300/Hif-1α interactions. This surprising promiscuity, displays by a well studied compound leads to further interrogate the p53/hDM2 interaction utilizing a standard fluorescence polarization (FP) assay with purified protein. The results from the FP assay validates the split-luciferase screen and demonstrates that BH3I-1 has a K
d
=5.3 μM against the p53/mDM2 pair, which is comparable to its low micromolar potency reported for the BH3 family of receptors. BH3I-1 inhibits interaction between the BH3 domain and Bcl-xL. NMR analyses reveal that BH3I-1 targets the BH3-binding pocket of Bcl-xL with a K
i
of 7.8±0.9 μM.
BH3I-1
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
300817-68-9, BH3I-1 相關(guān)搜索:
- API
- 藥靶配體
- 抑制劑
- 標(biāo)準(zhǔn)品
- C15H14BrNS2O3
- 2-(5-(4-溴苯基亞甲基)-4-氧代-2-硫代噻唑-3-基)-3-甲基丁酸
- 化合物BH3I1
- BH3I-1游離態(tài)
- 300817-68-9
- MDM-2/p53,BH3I 1,Inhibitor,Ubiquitin ligase,BH3I-1,E3 ligating enzyme,Ubiquitin conjugating enzyme,BH3I1,E2 conjugating enzyme,Bcl-2 Family,BHI 1,E1 activating enzyme,inhibit,BHI-1,BH 3I1,E1/E2/E3 Enzyme,Ubiquitin activating enzyme,BH-3I-1
- 2-(5-(4-Bromobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)-3-methylbutanoic acid
- 5-(p-Bromobenzylidene)-a-isopropyl-4-oxo-2-thioxo-3-thiazolidine acetic acid
- 3-Thiazolidineacetic acid, 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-
- BHI1;BH 3I1
- BHI1
- BH3I 1 ;BH3I1
- 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid