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AB141506

EX-527, SIRT1 Inhibitor

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(14 Publications)

MW 248.71 Da, Purity >97%. Selective, cell-permeable SIRT1 Inhibitor. (IC50= 98 nM, 19.6, 48.7 and > 100 μM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Shows no effect at other HDACs or SIRTs. Enhances p53 acetylation in response to DNA damaging agents.

View Alternative Names

75SirT1, FLJ35621, FLJ37491, HST2, HST2, S. cerevisiae, homolog of, Mitochondrial nicotinamide adenine dinucleotide dependent deacetylase, NAD dependent deacetylase sirtuin 3 mitochondrial, NAD dependent protein deacetylase sirtuin 1, NAD-dependent deacetylase sirtuin-1, NAD-dependent deacetylase sirtuin-2, NAD-dependent protein deacetylase sirtuin-2, NAD-dependent protein deacetylase sirtuin-3, mitochondrial, OTTHUMP00000198111, OTTHUMP00000198112, Regulatory protein SIR2 homolog 1, Regulatory protein SIR2 homolog 2, Regulatory protein SIR2 homolog 3, SIR1_HUMAN, SIR2 L3, SIR2 like 1, SIR2, S. cerevisiae, homolog-loke 2, SIR2, S.cerevisiae, homolog-like 1, SIR2-like protein 1, SIR2-like protein 2, SIR2-like protein 3, SIR2ALPHA, SIR2L, SIR2L1, SIR2L2, SIR3_HUMAN, SIRT 2, SIRT2_HUMAN, Silencing information regulator 2 like, Silent information regulator 2, Silent mating type information regulation 2 S.cerevisiae homolog 3, Sir 2 like 3, Sir2 related protein type 2, SirtT1 75 kDa fragment, Sirtuin (silent mating type information regulation 2 homolog) 1 (S. cerevisiae), Sirtuin (silent mating type information regulation 2 homolog) 2 (S.cerevisiae), Sirtuin 1, Sirtuin 2, Sirtuin 3, Sirtuin silent mating type information regulation 2 homolog 3 (S. cerevisiae), Sirtuin type 1, Sirtuin type 2, Sirtuin type 3, hSIR2, hSIRT 3, hSIRT1

2 Images
Functional Studies - EX-527, SIRT1 Inhibitor (AB141506)
  • FuncS

Unknown

Functional Studies - EX-527, SIRT1 Inhibitor (AB141506)

Time course of SIRT1-substrate deacetylation by recombinant SIRT1 in the presence of EX-527.

Chemical Structure - EX-527, SIRT1 Inhibitor (AB141506)
  • Chemical Structure

Lab

Chemical Structure - EX-527, SIRT1 Inhibitor (AB141506)

2D chemical structure image of ab141506, EX-527, SIRT1 Inhibitor

Key facts

CAS number

49843-98-3

Purity

>97%

Form

Solid

form

Molecular weight

248.71 Da

Molecular formula

C<sub>1</sub><sub>3</sub>H<sub>1</sub><sub>3</sub>ClN<sub>2</sub>O

PubChem

5113032

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 100 mM

Biochemical name

6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

Biological description

Selective, cell-permeable SIRT1 Inhibitor. (IC50= 98 nM, 19.6, 48.7 and > 100 μM for SIRT1, SIRT2, SIRT3, HDAC and NADase respectively). Shows no effect at other HDACs or SIRTs. Enhances p53 acetylation in response to DNA damaging agents.

Canonical smiles

C1CC(C2=C(C1)C3=C(N2)C=CC(=C3)Cl)C(=O)N

InChi

InChI=1S/C13H13ClN2O/c14-7-4-5-11-10(6-7)8-2-1-3-9(13(15)17)12(8)16-11/h4-6,9,16H,1-3H2,(H2,15,17)

InChiKey

FUZYTVDVLBBXDL-UHFFFAOYSA-N

IUPAC Name

6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
It is important to note that this product is reported to be light sensitive|Store in the dark|Store under desiccating conditions

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

SIRT1 SIRT2 and SIRT3 are members of the sirtuin family of proteins also known as Sir2-like proteins which participate in cellular regulation processes. These proteins function as NAD+-dependent deacetylases meaning they remove acetyl groups from protein substrates using NAD+ as a cofactor. SIRT1 is a well-studied protein with a molecular mass of approximately 120 kDa and is expressed in various tissues including the brain liver muscle and heart. SIRT2 and SIRT3 also play roles in cellular processes and are found in different cellular compartments such as the cytoplasm and mitochondria respectively.
Biological function summary

These sirtuins are significant in regulating diverse cellular functions like metabolism aging stress response and inflammation. SIRT1 is involved in deacetylating histones and is part of larger chromatin remodeling complexes. SIRT2 mostly resides in the cytoplasm and influences the cell cycle while SIRT3 acts in the mitochondria to regulate reactive oxygen species production and energy metabolism. These functions establish them as important players in maintaining cellular homeostasis and adaptative responses to changing cellular environments.

Pathways

SIRT1 SIRT2 and SIRT3 play critical roles in vital pathways related to insulin signaling and oxidative stress response. SIRT1 interacts with the PGC-1α pathway which is key in regulating mitochondrial biogenesis and fatty acid oxidation. SIRT3 is actively involved in the antioxidant defense system aiding in the deacetylation of forkhead box proteins particularly FOXO3a. SIRT2's scope extends to influence the regulation of the AMP-activated protein kinase (AMPK) signaling pathway intersecting with cellular energy balance and stress responses.

SIRT1 SIRT2 and SIRT3 have associations with several metabolic and neurodegenerative diseases including type 2 diabetes and Alzheimer's disease. SIRT1 is linked with protective roles in diabetes by enhancing insulin sensitivity through interaction with FOXO proteins and influencing glucose metabolism. SIRT2 has connections to neurodegenerative conditions like Alzheimer's through its involvement in amyloid-beta peptide processing. SIRT3 offers protective effects in age-related disorders by regulating mitochondrial function and managing oxidative stress displaying interactions with key mitochondrial enzymes. These insights into their roles suggest potential for therapeutic targets possibly through selective inhibition or activation of these sirtuins.

Product protocols

Publications (14)

Recent publications for all applications. Explore the full list and refine your search

Redox biology 79:103472 PubMed39752998

2025

Molecular hydrogen reduces dermatitis-induced itch, diabetic itch and cholestatic itch by inhibiting spinal oxidative stress and synaptic plasticity via SIRT1-β-catenin pathway in mice.

Applications

Unspecified application

Species

Unspecified reactive species

Linlin Zhang,Fangshi Zhao,Yize Li,Zhenhua Song,Lingyue Hu,Yuanjie Li,Rui Zhang,Yonghao Yu,Guolin Wang,Chunyan Wang

Brain and behavior 14:e70095 PubMed39682063

2024

Baihui-Penetrating-Qubin Acupuncture Attenuates Neurological Deficits Through SIRT1/FOXO1 Reducing Oxidative Stress and Neuronal Apoptosis in Intracerebral Hemorrhage Rats.

Applications

Unspecified application

Species

Unspecified reactive species

Shan-Shan Dong,Ming-Yue Li,Xue-Ping Yu,Yu-Na Kan,Xiao-Hong Dai,Lei Zheng,Hong-Tao Cao,Wen-Hui Duan,En-Li Luo,Wei Zou

Drug design, development and therapy 18:3903-3919 PubMed39224902

2024

ED-71 Ameliorates Bone Loss in Type 2 Diabetes Mellitus by Enhancing Osteogenesis Through Upregulation of the Circadian Rhythm Coregulator BMAL1.

Applications

Unspecified application

Species

Unspecified reactive species

Ting Liu,Luxu Wang,Tuo Shi,Hongrui Liu,Bo Liu,Jie Guo,Minqi Li

Cellular and molecular life sciences : CMLS 81:324 PubMed39080028

2024

Decreased AMPK/SIRT1/PDK4 induced by androgen excess inhibits human endometrial stromal cell decidualization in PCOS.

Applications

Unspecified application

Species

Unspecified reactive species

Ling Hong,Shan Xiao,Lianghui Diao,Ruochun Lian,Cong Chen,Yong Zeng,Su Liu

Diabetes, metabolic syndrome and obesity : targets and therapy 17:247-257 PubMed38269338

2024

Empagliflozin Induces Vascular Relaxation in Rat Coronary Artery Due to Activation of BK Channels.

Applications

Unspecified application

Species

Unspecified reactive species

Qi Kong,Ling-Ling Qian,Lei Zhang,Huan-Huan Liu,Fan Yang,Xiao-Lu Zhang,Chao Wang,Xiao-Xi Zhao,Ku-Lin Li,Ru-Xing Wang

Journal of food biochemistry 46:e14463 PubMed36314441

2022

Resveratrol inhibits hepatic stellate cell activation by regulating autophagy and apoptosis through the SIRT1 and JNK signaling pathways.

Applications

Unspecified application

Species

Unspecified reactive species

Jing Zhang,Jian Ping,Na Jiang,Lieming Xu

The FEBS journal 290:1596-1624 PubMed36239430

2022

Early loss of endogenous NAD following rotenone treatment leads to mitochondrial dysfunction and Sarm1 induction that is ameliorated by PARP inhibition.

Applications

Unspecified application

Species

Unspecified reactive species

Ankita Sarkar,Sourav Dutta,Malinki Sur,Semanti Chakraborty,Puja Dey,Piyali Mukherjee

Oxidative medicine and cellular longevity 2022:7444430 PubMed35126819

2022

Fucoxanthin Attenuates Oxidative Damage by Activating the Sirt1/Nrf2/HO-1 Signaling Pathway to Protect the Kidney from Ischemia-Reperfusion Injury.

Applications

Unspecified application

Species

Unspecified reactive species

Hu Mao,Lei Wang,Yufeng Xiong,Guanjun Jiang,Xiuheng Liu

Oxidative medicine and cellular longevity 2021:8889195 PubMed34646427

2021

Downregulation of miR-128 Ameliorates Ang II-Induced Cardiac Remodeling via SIRT1/PIK3R1 Multiple Targets.

Applications

Unspecified application

Species

Unspecified reactive species

Heqin Zhan,Feng Huang,Qian Niu,Mingli Jiao,Xumeng Han,Kaina Zhang,WenZhuo Ma,Shan Mi,Shiyu Guo,Zhenghang Zhao

Brain and behavior 11:e2335 PubMed34473417

2021

Neuroprotective effects of metformin on cerebral ischemia-reperfusion injury by regulating PI3K/Akt pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Cailian Ruan,Hongtao Guo,Jiaqi Gao,Yiwei Wang,Zhiyong Liu,Jinyi Yan,Xiaoji Li,Haixia Lv
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