NCT-501 is a potent and selective inhibitor of Aldehyde dehydrogenase ALDH1A1, a dehydrogenase that has been found to be elevated in certain cancers and in cancer stem cells. NCT-501 had an IC50 value of 40 nM and was found to be 1000-fold selective for ALDH1A1 over other ALDH enzymes and other dehydrogenases. NCT-501 treatment of head and neck squamous-cell carcinoma (HNSCC) explants in combination with cisplatin resulted in a significant decrease in proliferating cells.
| Molecular Weight | 416.52 |
| Formula | C21H32N6O3 |
| CAS Number | 1802088-50-1 |
| Form | Solid |
| Solubility (25°C) | DMSO: 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[3] Rosemary E McDowell, et al. Diabetes Impairs the Aldehyde Detoxifying Capacity of the Retina
| Related ALDH Products |
|---|
| RV01
RV01 is a novel quinolyl-substituted analogue of resveratrol, it inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol. RV01 exhibits hydroxyl radical scavenging activity. |
| IGUANA-1
IGUANA-1 is a potent inhibitor of ALDH1B1, which is a mitochondrial enzyme that promotes colorectal and pancreatic cancer. IGUANA-1 has significant inhibition against cancer cells. |
| IGUANA-1 free base
IGUANA-1 free base (STL5-T-0057) is an selective ALDH1 B1 inhibitor with an IC50 value of 30 nM. IGUANA-1 free base inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC50 values of 2.46 and 0.39 μM, respectively. IGUANA-1 free base can be used for the research of cancer. |
| EN40
EN40 is a potent, selective aldehyde dehydrogenase 3A1 (ALDH3A1) inhibitor as a covalent ligand, exhibits an IC50 value of 2 uM. |
| CM10
CM10 is a potent and selective inhibitor of aldehyde dehydrogenase 1A family (ALDH1A) with IC50 of 1700 nM, 740 nM and 640 nM for ALDH1A1, ALDH1A2 and ALDH1A3, respectively. CM10 exhibits anti-cancer activity. |
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