research use only
Cat.No.S8865
| Related Targets | Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas |
|---|---|
| Other Bcl-2 Inhibitors | Navitoclax (ABT-263) S63845 ABT-737 Obatoclax Mesylate (GX15-070) A-1331852 A-1210477 TW-37 A-1155463 Dihydrochloride AZD5991 UMI-77 |
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In vitro |
DMSO
: 18 mg/mL
(38.52 mM)
Ethanol : 3 mg/mL Water : Insoluble |
|
In vivo |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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| Molecular Weight | 467.20 | Formula | C19H21Br2N3O |
Storage (From the date of receipt) | 3 years -20°C powder |
|---|---|---|---|---|---|
| CAS No. | 335165-68-9 | -- | Storage of Stock Solutions |
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| Synonyms | N/A | Smiles | C1CN(CCN1)CC(CN2C3=C(C=C(C=C3)Br)C4=C2C=CC(=C4)Br)O.Cl.Cl | ||
| Targets/IC50/Ki |
Bax
(Cell-free assay) 15.0 μM(Kd)
|
|---|---|
| In vitro |
BAX activation inhibitor 1 (BAI1) demonstrates inhibition of tBID-induced BAX-mediated membrane permeabilization in a dose dependent manner with an IC50 of 3.3 μM. This compound binds to monomeric BAX at a novel allosteric site. It is a potent inhibitor of BAX conformational activation and oligomerization in solution, not by direct competition with the activator, but rather through an allosteric mechanism that favors the inactive BAX. Moreover, this chemical inhibited BAX membrane association and translocation induced either by tBID (IC50 = 5 ± 1 μΜ) or BIM SAHB (IC50 = 2 ± 1 μΜ) in a dose dependent manner and with a similar IC50 to BAX-mediated liposomal release. It selectively inhibits BAX-dependent cell death. |
References |
(data from https://clinicaltrials.gov, updated on 2024-05-22)
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05477862 | Enrolling by invitation | Alzheimer Disease |
Northwestern University |
October 15 2023 | Not Applicable |
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