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925432-73-1

925432-73-1 structure
925432-73-1 structure
  • Name: SRT 1460
  • Chemical Name: 3,4,5-trimethoxy-N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]benzamide
  • CAS Number: 925432-73-1
  • Molecular Formula: C26H29N5O4S
  • Molecular Weight: 507.60
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Sirtuin
  • Create Date: 2018-12-25 19:22:28
  • Modify Date: 2024-01-02 12:27:02
  • SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM), and is more potent than Resveratrol and the closest sirtuin homologues[1].

Name 3,4,5-trimethoxy-N-[2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]benzamide
Synonyms 3,4,5-Trimethoxy-N-{2-[3-(1-piperazinylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl}benzamide
Benzamide, 3,4,5-trimethoxy-N-[2-[3-(1-piperazinylmethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-
3,4,5-trimethoxy-N-{2-[3-(piperazin-1-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl}benzamide
3,4,5-trimethoxy-N-(2-(3-(piperazin-1-ylmethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)benzamide
SRT-1460
Description SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5 > 300 μM), and is more potent than Resveratrol and the closest sirtuin homologues[1].
Related Catalog
Target

SIRT1:2.9 μM (EC1.5)

In Vitro SRT 1460 (2-6 μM; 72 hours) inhibits cell viability in a dose-dependent manner, with all pancreatic cancer cells being more sensitive than the control HPDE cell. The IC50s of those cells are: Patu8988t, 1.62±0.13 μM; SU86.86, 2.31±0.23 μM; Panc-1, 0.66 ±0.02 μM; HPDE, 2.39±0.29 μM[2]. SRT 1460 (5 μM; 16 hours) increases expression of the autophagy marker LC3-II[2]. Cell Viability Assay[2] Cell Line: Patu8988t (pancreatic cancer cells), Panc-1 (pancreatic cancer cells), SU86.86 (pancreatic cancer cells), HPDE cells Concentration: 2 μM, 4 μM, 6 μM Incubation Time: 72 hours Result: Inhibited cell viability in a dose-dependent manner, with all pancreatic cancer cells being more sensitive than the control HPDE cell. The IC50s of those cells were: Patu8988t, 1.62±0.13 μM; SU86.86, 2.31±0.23 μM; Panc-1, 0.66 ±0.02 μM; HPDE, 2.39±0.29 μM. Western Blot Analysis[2] Cell Line: Patu8988t cells Concentration: 5 μM Incubation Time: 16 hours Result: SRT1460 increased expression of the autophagy marker LC3-II.
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]. Chini CC, et al. SIRT1-Activating Compounds (STAC) Negatively Regulate Pancreatic Cancer Cell Growth and Viability Through a SIRT1 Lysosomal-Dependent Pathway. Clin Cancer Res. 2016 May 15;22(10):2496-507.

Density 1.4±0.1 g/cm3
Molecular Formula C26H29N5O4S
Molecular Weight 507.60
Exact Mass 507.194031
PSA 117.60000
LogP 3.88
Index of Refraction 1.669
Hazard Codes Xi
HS Code 2934100090
HS Code 2934100090
Summary 2934100090 other compounds containing an unfused thiazole ring (whether or not hydrogenated) in the structure VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:20.0%