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49843-98-3 - EX 527 - 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide - J64753 - Alfa Aesar

J64753 EX 527

Codice CAS
49843-98-3
Sinonimi
6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

Dimensioni Prezzo ($) Quantità Disponibilità
10mg 119,00
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EX 527

MDL
MFCD03009471

Proprietà chimiche

Formula
C13H13ClN2O
Peso formula
248.71
Modulo
Powder
Solubilità
Soluble in dimethyl sulfoxide, ethanol and dimethyl formamide.

Applicazioni

EX-527 is a potent and selective sirtuin 1 (SIRT1) inhibitor (IC50 38 nM) identified from a high throughput screen. EX-527 is more selective (200-500-fold) for SIRT1 than for SIRT2 or SIRT3 and has been shown to be a potent SIRT6 inhibitor using H3K56 deacetylation site based substrate. EX-527 does not inhibit class I/II HDAC activity at concentrations up to 100uM. Enhances p53 acetylation in response to DNA damaging agents. EX-527 is racemic; the active isomer (EX-243) gives similar results and potency whereas the other isomer (designated EX-242) is inactive.

Note

Keep container tightly closed. Store in cool, dry conditions in well sealed containers.

Letteratura

Marcus Freitag.; Jorg Schemies.; Tim Larsen.; Khattab El Gaghlab.; Felix Schulz.; Tobias Rumpf.; Manfred Jung.; Andreas Link. Synthesis and biological activity of splitomicin analogs targeted at human NAD+-dependent histone deacetylases (sirtuins). Cell Calcium. 2011 19, (12), 3669-3677.

Mohosin Layek.; Y. Syam Kumar.; Aminul Islam.; Ravikumar Karavarapu.; Amrita Sengupta.; Devyani Halder.; K. Mukkanti.; Manojit Pal. Alkynylation of N-(3-iodopyridin-2-yl)sulfonamide under Pd/C-Cu catalysis: a direct one pot synthesis of 7-azaindoles and their pharmacological evaluation as potential inhibitors of sirtuins. 2011, 2, 478-485.

Rischio GHS e dichiarazioni precauzionali

Dichiarazioni di rischio (UE): H302-H319

Harmful if swallowed. Causes serious eye irritation.

Dichiarazioni precauzionali: P280i-P264-P305+P351+P338-P301+P312a-P337+P313-P501a

Wear eye/face protection. Wash thoroughly after handling. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF SWALLOWED: If eye irritation persists: Get medical advice/attention. Dispose of contents/container in accordance with local/regional/national/international regulations.

Altri riferimenti

Codice tariffe armonizzato
2933.99
TSCA
No

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