BTM-3566

Chemical Information
OMA1 Activator BTM-3566 is an orally bioavailable activator of the mitochondrial protease OMA1, with potential antineoplastic activity. Upon oral administration, OMA1 activator BTM-3566 activates OMA1. This leads to OMA1-dependent cleavage of DAP3-binding cell death enhancer 1 (DELE1) and mitochondrial dynamin-like GTPase OPA1, mitochondrial fragmentation, and activation of the eIF2alpha-kinase heme-regulated inhibitor (HRI), and induces cyclic AMP-dependent transcription factor ATF-4-mediated integrated stress response (ISR) and hyperactivates mitochondrial ISR, which result in apoptosis. OMA1 plays a key role in the activation of the ISR pathway in response to hypoxia, amino acid deprivation, and accumulation of misfolded proteins. While ISR promotes the adaptation of tumor cells to hypoxic stress, prolonged activation of ISR induces apoptosis.
| CAS Number | 2228857-70-1 |
| PubChem CID | 134564305 |
| IUPAC Name | 4-(3-fluorophenyl)-3-methyl-1-[5-propan-2-ylsulfanyl-4-[4-(trifluoromethyl)cyclohexen-1-yl]-1,3-thiazol-2-yl]pyrazole-5-carboxylic acid |
| Molecular Formula | C24H23F4N3O2S2 |
| Molecular Weight | 525.6 |
| XLogP | 7.3 |
| Topological Polar Surface Area | 122 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 6 |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 799 |
| Property | Value |
|---|---|
| Molecular Weight | 525.6 |
| XLogP3 | 7.3 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 6 |
| Exact Mass | 525.11678198 |
| Monoisotopic Mass | 525.11678198 |
| Topological Polar Surface Area | 122 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 799 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 1 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
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