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SIRT1/2 Inhibitor IV (CAS 14513-15-6) LS-H97

SIRT1 inhibitor, SIRT2 inhibitor
LS-H97-1 / 1 mg / $175
LS-H97-5 / 5 mg / $225
LS-H97-10 / 10 mg / $285
LS-H97-25 / 25 mg / $425
USA Shipment Only
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Description: SIRT1/2 inhibitor IV is a cell-permeable inhibitor of SIRT1 (IC50 = 56 µM) and SIRT2 (IC50 = 59 µM), blocking NAD+-dependent deacetylase activity in a substrate competitive manner. It less effectively inhibits SIRT5 (IC50 >300 µM) and has no effect on class I and II histone deacetylases. By inhibiting SIRT1, SIRT1/2 inhibitor IV sensitizes H460 lung cancer cells to etoposide and paclitaxel and enhances etoposide-induced G2 arrest. It also blocks a SIRT1-dependent hypoxic response in vivo, suppressing HIF-1 alpha protein accumulation as well as EPO and VEGF expression in HepG2 tumors in mice. H97_ChemicalStructureImage.png
2,3-dihydro-5-[(2-hydroxy-1-naphthalenyl)methyl]-6-phenyl-2-thioxo-4(1H)-pyrimidinone
Cambinol
NSC112546
SIRT1InhibitorII
SIRT2InhibitorVI
biochemical, chemical, inhibitor
LS-H97
14513-15-6
C21H16N2O2S
≥98%
A crystalline solid
 
S=C1NC(C(CC2=C(C=CC=C3)C3=CC=C2O)=C(C4=CC=CC=C4)N1)=O
InChI=1S/C21H16N2O2S/c24-18-11-10-13-6-4-5-9-15(13)16(18)12-17-19(14-7-2-1-3-8-14)22-21(26)23-20(17)25/h1-11,24H,12H2,(H2,22,23,25,26)
RVNSQVIUFZVNAU-UHFFFAOYSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: SIRT1 / Sirtuin 1 SIRT2 / Sirtuin 2 related products

Usage Information

SIRT1/2 inhibitor IV is supplied as a crystalline solid. A stock solution may be made by dissolving the SIRT1/2 inhibitor IV in the solvent of choice. SIRT1/2 inhibitor IV is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide, which should be purged with an inert gas. The solubility of SIRT1/2 inhibitor IV in these solvents is approximately 0.33, 20, and 16 mg/ml, respectively. SIRT1/2 inhibitor IV is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, SIRT1/2 inhibitor IV should first be dissolved in DMSO and then diluted with the aqueous buffer of choice. SIRT1/2 inhibitor IV has a solubility of approximately 0.14 mg/ml in a 1:6 solution of DMSO:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Heltweg, B., Gatbonton, T., Schuler, A.D., et al. Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes. Cancer Res. 66, 4368-4377 (2006).
  2. Laemmle, A., Lechleiter, A., Roh, V., et al. Inhibition of SIRT1 impairs the accumulation and transcriptional activity of HIF-1a protein under hypoxic conditions. PLoS One 7(3), (2012).

 


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