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Submit ReviewBax channel blocker is a allosteric inhibitor of Bax channel activation. Binds inactive Bax at allosteric site and inhibits tBID-mediated Bax activation (IC50 = 3.3 μM). Selectively inhibits Bax-dependent apoptosis. Potent inhibitor of Bax-mediated mitochondrial cytochrome c release (IC50 = 0.52 μM).
Bax channel blocker is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 540.12 |
Formula | C19H21Br2N3O.2HCl |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 329349-20-4 |
PubChem ID | 2729026 |
InChI Key | HWFKCAFKXZFOQT-UHFFFAOYSA-N |
Smiles | Cl.Cl.OC(CN1C2=C(C=C(Br)C=C2)C2=C1C=CC(Br)=C2)CN1CCNCC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 2.34 | 5 | |
DMSO | 46.72 | 100 |
The following data is based on the product molecular weight 540.12. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.85 mL | 9.26 mL | 18.51 mL |
5 mM | 0.37 mL | 1.85 mL | 3.7 mL |
10 mM | 0.19 mL | 0.93 mL | 1.85 mL |
50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
References are publications that support the biological activity of the product.
Bombrun et al (2003) 3,6-Dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome c release via Bax channel modulation. J.Med.Chem. 46 21
Garner et al (2019) Small-molecule allosteric inhibitors of BAX. Nat.Chem.Biol. 15 322 PMID: 30718816
If you know of a relevant reference for Bax channel blocker, please let us know.
Keywords: Bax channel blocker, Bax channel blocker supplier, inhibitors, inhibits, Bax-mediated, mitochondrial, cytochrome, c, release, Bcl-2, Family, allosteric, activation, BAI1, 2160, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Bax channel blocker include:
Sano et al (2016) Vacuolin-1 inhibits autophagy by impairing lysosomal maturation via PIKfyve inhibition. FEBS Lett 590 1576 PMID: 27135648
Ono et al (2017) Feedback activation of AMPK-mediated autophagy acceleration is a key resistance mechanism against SCD1 inhibitor-induced cell growth inhibition. PLoS One 12 e0181243 PMID: 28704514
Do you know of a great paper that uses Bax channel blocker from Tocris? Please let us know.
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.