- BH3I-1
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- $1.00 / 1g
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2019-12-24
- CAS:300817-68-9
- Min. Order: 1g
- Purity: 99%
- Supply Ability: 20kg
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| Product Name: | BH3I-1 | | Synonyms: | 5-(p-Bromobenzylidine)-α-isopropyl-4-oxo-2-thioxo-3-thiozolidineacetic acid;BH3I 1 ;BH3I1;BHI1;BHI1;BH 3I1;3-Thiazolidineacetic acid, 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-;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;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 | | CAS: | 300817-68-9 | | MF: | C15H14BrNO3S2 | | MW: | 400.31 | | EINECS: | | | Product Categories: | API | | Mol File: | 300817-68-9.mol |  |
| | BH3I-1 Chemical Properties |
| Boiling point | 535.2±60.0 °C(Predicted) | | density | 1?+-.0.1 g/cm3(Predicted) | | storage temp. | Sealed in dry,2-8°C | | solubility | DMSO: >10 mg/mL, soluble | | form | powder, yellow | | pka | 3.39±0.10(Predicted) | | color | Light yellow to yellow |
| Hazard Codes | Xn | | Risk Statements | 20/21/22 | | Safety Statements | 36 | | WGK Germany | 3 |
| | BH3I-1 Usage And Synthesis |
| Description | The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains. BH3I-1 is a cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis. It inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 μM, respectively. BH3I-1 enhances radiation sensitivity in non-small cell lung cancer cells. | | Uses | BH3I-1 is a BH3 mimetic that binds to Bcl-xL. | | in vitro | the bcl-2 inhibitors bh3i-1 and it analog bh3i-2 had been applied as lead compounds to find possible bcl-2 or bcl-x(l) inhibitors by using computer-assisted screening of in-house database. the identified compounds were further studied regarding their possible application as a drug. it was found that the induction of apoptosis, which was shown as number of hypodiploid cells, was increased by adding bh3i-1 and it analog bh3i-2 to bjab bcl-xl and bjab neo/mock cells. in addition, the effects of the pro-apoptotic proteins bax and bak on the induction of apoptosis via bh3i-1 and it analog bh3i-2 were investigated with a variety of knockout cell lines, and resulted showed that the presence or absence of bak or bax has no significant influence on the amount of apoptotic events induced by bh3i-1 and it analog bh3i-2 [1]. | | IC 50 | 293.95 μm | | references | [1] füllbeck m,gebhardt n,hossbach j,daniel pt,preissner r. computer-assisted identification of small-molecule bcl-2 modulators. comput biol chem.2009 dec;33(6):451-6. |
| | BH3I-1 Preparation Products And Raw materials |
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