NH4-6
NH4-6 is a SIRT2 inhibitor with an IC50 of 0.032 μM against SIRT2 and an IC50 of 3 μM against SIRT1. NH4-6 inhibits the deacetylase activity of SIRT1. As a cytotoxic agent, NH4-6 reduces cancer cell viability, suppresses anchorage-independent growth of cancer cells, induces acetylation of α-tubulin, and promotes acetylation of p53. NH4-6 can be used in the research of breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 2375182-58-2
- Formula: C33H59IN4O3S
- Molecular Weight:718.82
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
SIRT2 0.032 μM (IC50) |
SIRT1 3 μM (IC50) |
NH4-6 potently and selectively inhibits purified SIRT2 deacetylase activity with an IC50 of 0.032 μM, shows weaker activity against SIRT1 and SIRT6, and does not inhibit SIRT3 at 83 μM[1].
NH4-6 (25-50 μM; 6 h for permeability) exhibits weaker cytotoxicity than TM at 25 μM but stronger cytotoxicity at 50 μM in MCF7 and MDA-MB-231 breast cancer cells, correlating with its concentration-dependent cellular uptake enabled by superior aqueous solubility[1].
NH4-6 (12 μM; 10 days) shows stronger inhibition of anchorage-independent growth than TM at 12 μM in MCF7 breast cancer cells[1].
NH4-6 (25-100 μM; 6 h) increases α-tubulin acetylation (a marker of SIRT2 inhibition) in MCF7 breast cancer cells at 50 μM and 100 μM, but not at 25 μM, consistent with its concentration-dependent cellular uptake[1].
NH4-6 (10-100 μM) inhibits SIRT1 activity (measured via p53 acetylation) in MCF7 breast cancer cells only at a concentration of 100 μM, likely due to its improved solubility enabling sufficient cellular accumulation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF7, MDA-MB-231 breast cancer cells
-
Concentration:25 μM, 50 μM
-
Incubation Time:6 h
-
Result:Showed slightly weaker cytotoxicity than TM in both MCF7 and MDA-MB-231 cells at lower concentrations.
Showed stronger cytotoxicity than TM in both cell lines at 50 μM.
Reached intracellular levels of 0.19 μg/million cells after 25 μM treatment and 0.86 μg/million cells after 50 μM treatment, compared to saturated levels of TM (~0.29-0.30 μg/million cells) at both concentrations.
-
Cell Line:MCF7 breast cancer cells
-
Concentration:25 μM; 50 μM; 100 μM
-
Incubation Time:6 h
-
Result:Did not increase α-tubulin acetylation levels at 25 μM.
Increased α-tubulin acetylation levels to levels comparable to TM-treated samples at 50 μM and 100 μM.
Chemical Information
-
CAS No. 2375182-58-2
-
Molecular Weight 718.82
-
Formula C33H59IN4O3S
-
SMILES
O=C(OCC1=CC=CC=C1)N[C@@H](CCCCNC(CCCCCCCCCCCCC)=S)C(NCC[N+](C)(C)C)=O.[I-]
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)