General description
A cell permeable diarylamine derivative that acts as a selective, reversible, substrate-binding site directed inhibitor of aldehyde dehydrogenase ALDH3A1 (Ki = 4.7 µM, IC50 = 16 µM). Does not inhibit the activity of ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, and ALDH2 even at higher concentrations (250 µM). Shown to significantly reduce the activity of ALDH3A1 in A549 and SF767 cell lysates, but does not affect CCD-13Lu cells that lack ALDH3A1 activity. Although it does not affect tumor cell proliferation, it significantly improves the sensitivity of cancer cells to mafosfamide.
A cell permeable diarylamine derivative that acts as a selective, reversible, substrate-binding site directed inhibitor of aldehyde dehydrogenase ALDH3A1 (Ki = 4.7 µM, IC50 = 16 µM). Does not inhibit the activity of ALDH1A1, ALDH1A2, ALDH1A3, ALDH1B1, and ALDH2 even at higher concentrations (250 µM). Shown to significantly reduce the activity of ALDH3A1 in A549 and SF767 cell lysates, but does not affect CCD-13Lu cells that lack ALDH3A1 activity. Although it does not affect tumor cell proliferation, it significantly improves the sensitivity of cancer cells to mafosfamide.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
ALDH3A1
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Parajuli, B. et al. 2014. Chembiochem.15, 701.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 349.36. Empirical Formula: C15H15N3O5S. Assay: ≥. 98% (HPLC). Quality Level: 100. form: powder. potency: 4.7 . μ. M Ki. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 50 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 12352200
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5311700001