1001908-89-9
1001908-89-9
Chemical Structure
SRT 2183
- CAS. Nr.: 1001908-89-9
- Formula:C27H24N4O2S
- Molecular Weight:468.57
IUPAC Name: (R)-N-(2-(3-((3-hydroxypyrrolidin-1-yl)methyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-naphthamide
InChIKey: MUFSINOSQBMSLE-JOCHJYFZSA-N
SMILES: O=C(NC1=C(C2=CN3C(SC=C3CN4CC[C@@H](O)C4)=N2)C=CC=C1)C(C=C5)=CC6=C5C=CC=C6
Biological Activity: SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM[1]. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels[2].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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SRT 2183 | 98.06% | 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. | ||||||||||||||||||||
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SRT 1720 (Standard) | 99.17% | SRT 1720 (Standard) is the analytical standard of SRT 1720. This product is intended for research and analytical applications. SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively. | ||||||||||||||||||||
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SRT 1460 | 98.16% | 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. | ||||||||||||||||||||
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MLKL-IN-2 | 99.45% | MLKL-IN-2 is a MLKL inhibitor extracted from patent WO2021224505A1, compound (i). | ||||||||||||||||||||
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SRT 1720 monohydrochloride | 99.37% | SRT 1720 monohydrochloride is a selective and orally active activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3. | ||||||||||||||||||||
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SRT 1720 dihydrochloride | 99.60% | SRT 1720 dihydrochloride is a selective and orally active activator of SIRT1 with an EC50 of 0.10 μM, and shows less potent activities on SIRT2 and SIRT3. | ||||||||||||||||||||
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BET-IN-13 | BET-IN-13 is a potent BET inhibitor with an IC50 value of 1.6 nM. BET-IN-13 reduces LPS-induced TNF-α, IL-1β, IL-6, and NOS2 mRNA expression levels. BET-IN-13 shows anti-inflammatory activity. BET-IN-13 has the potential for the research of acute liver injury. | |||||||||||||||||||||
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SRT 2104 | 99.27% | SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD+ dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease. | ||||||||||||||||||||
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E235 | 99.86% | E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research. | ||||||||||||||||||||
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Sirtuin modulator 8 | 96.24% | Sirtuin modulator 8 is a sirtuin modulator that can activate Sirtuin activity. Sirtuin modulator 8 significantly downregulates the expression of monocyte chemoattractant protein-1 (MCP-1) and upregulates the expression of fibroblast growth factor 21 (FGF21). Sirtuin modulator 8 regulates the expression of inflammation- and metabolism-related genes, showing potential for studying metabolic diseases (such as diabetes, obesity) and inflammatory diseases. | ||||||||||||||||||||
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Conivaptan hydrochloride | 99.95% | Conivaptan hydrochloride (YM 087) is an orally active dual vasopressin V1a/V2 receptor antagonist with Ki values of 0.48 nM and 3.04 nM for vasopressin V1a receptor and V2 receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure. | ||||||||||||||||||||
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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. [Content Brief]
- [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. [Content Brief]
