General description
A cell-permeable dibromocarbazole-piperazinyl derivative that displays anti-apoptotic properties. Reported to effectively block Bid-induced cytochrome c release from HeLa cell mitochondria (~80% inhibition at 5 µM) by inhibiting Bax channel activity.
A cell-permeable dibromocarbazolo-piperazinyl derivative that displays anti-apoptotic properties. Effectively blocks Bid-induced cyctochrome c release from HeLa cell mitochondria (~80% inhibition at 5 µM) by inhibiting Bax channel-forming activity (IC50 = 520 nM in a liposome channel assay).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Bax-channel forming activity
Product does not compete with ATP.
Reversible: no
Target IC50: 520 nM blocks Bid-induced cyctochrome c release from HeLa cell mitochondria by inhibiting Bax channel-forming activity in a liposome channel assay
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Peixoto, P., et al. 2009. Biochem J.423, 381.
Bombrun, A., et al. 2003. J. Med. Chem.46, 4365.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,desiccated (hygroscopic),protect from light |
| color | off-white |
| solubility | DMSO: 10 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | FC(F)(F)C(=O)O.FC(F)(F)C(=O)O.Brc1cc2c([n](c4c2cc(cc4)Br)CC(O)CN3CCNCC3)cc1 |
| InChI | 1S/C19H21Br2N3O.2C2HF3O2/c20-13-1-3-18-16(9-13)17-10-14(21)2-4-19(17)24(18)12-15(25)11-23-7-5-22-6-8-23;2*3-2(4,5)1(6)7/h1-4,9-10,15,22,25H,5-8,11-12H2;2*(H,6,7) |
| InChI key | LPXZQYWZSBDVIG-UHFFFAOYSA-N |
