SRT 2183

SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.

Product information

CAS Number: 1001908-89-9

Molecular Weight: 468.57

Formula: C27H24N4O2S

Chemical Name: N-[2-(3-{[(3R)-3-hydroxypyrrolidin-1-yl]methyl}imidazo[2, 1-b][1, 3]thiazol-6-yl)phenyl]naphthalene-2-carboxamide

Smiles: O[C@H]1CN(CC2=CSC3=NC(=CN23)C2=CC=CC=C2NC(=O)C2=CC3=CC=CC=C3C=C2)CC1

InChiKey: MUFSINOSQBMSLE-JOCHJYFZSA-N

InChi: InChI=1S/C27H24N4O2S/c32-22-11-12-30(15-22)14-21-17-34-27-29-25(16-31(21)27)23-7-3-4-8-24(23)28-26(33)20-10-9-18-5-1-2-6-19(18)13-20/h1-10,13,16-17,22,32H,11-12,14-15H2,(H,28,33)/t22-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (533.54 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

SRT 2183 (1-10 μM; 24-72 hours) inhibits the growth of Reh and Nalm-6 cells in a time- and dose-dependent manner. SRT 2183 (5-10 μM in Reh cells; 10 μM in Ly3 cells; 24 hours) induces expression of DNA-damage response genes associated with accumulation of phospho-H2A.X levels. SRT2183 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival.

References:

1. Milne JC, et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature. 2007 Nov 29; 450(7170): 712–716.
2. Scuto A, et al. SIRT1 activation enhances HDAC inhibition-mediated upregulation of GADD45G by repressing the binding of NF-κB/STAT3 complex to its promoter in malignant lymphoid cells. Cell Death Dis. 2013 May; 4(5): e635.
3. Gurt I, et al. The Sirt1 Activators SRT2183 and SRT3025 Inhibit RANKL-Induced Osteoclastogenesis in Bone Marrow-Derived Macrophages and Down-Regulate Sirt3 in Sirt1 Null Cells. PLoS One. 2015 Jul 30;10(7):e0134391.

Products are for research use only. Not for human use.