SIRT1-IN-2 (compound 3h) is a potent and selective SIRT1 (silent information regulator 1) inhibitor, with an IC50 of 1.6 μM[1].
IC50 & Target
SIRT1
1.6 μM (IC50)
SIRT2
39 μM (IC50)
体外研究 (In Vitro)
SIRT1-IN-2 (compound 3h) (0-100 μM, 48 h) inhibits the proliferation of Human cancer cell lines including K562, HCT-116, HepG2, A549, and MCF-7, and shows significantly less cytotoxic on 293T cells and HUVEC[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay
Cell Line:
Human cancer cell lines (K562, HCT-116, H460, HepG2, A549, HT-29, MCF-7) and normal cell lines (293T, HUVEC). [1]
Concentration:
0, 0.01，0.1，1，10，100 μM
Incubation Time:
48 h
Result:
Inhibited the proliferation of Human cancer cell lines including K562, HCT-116, HepG2, A549, and MCF-7, with IC50 values of 51, 37, 40, 48, and 48 μM, respectively. And showed significantly less cytotoxic on 293T cells and HUVEC, with IC50 values of > 100 and 45 μM, respectively.
分子量
250.72
Formula
C13H15ClN2O
CAS 号
2470969-89-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Laaroussi H, Ding Y, Teng Y, et al. Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents. Eur J Med Chem. 2020;202:112561.
SIRT1-IN-3 (compound 3j) is a potent and selective SIRT1 inhibitor, with an IC50 of 4.2 μM[1].
IC50 & Target
SIRT1
4.2 μM (IC50)
SIRT2
38 μM (IC50)
体外研究 (In Vitro)
SIRT1-IN-3 (compound 3j) (0-100 μM, 48 h) inhibits the proliferation of human cancer cell lines including K562, HCT-116, H460, HepG2, A549, and MCF-7, and shows low cytotoxic on 293T and HUVEC[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cytotoxicity Assay
Cell Line:
Human cancer cell lines (K562, HCT-116, H460, HepG2, A549, HT-29, MCF-7) and normal cell lines (293T, HUVEC)[1]
Concentration:
0, 0.01, 0.1, 1, 10, 100 μM
Incubation Time:
48 h
Result:
Inhibited the proliferation of Human cancer cell lines including K562, HCT-116, H460, HepG2, A549, and MCF-7, with IC50 values of 47, 41, 66, 93, 52, and 64 μM, respectively. And showed low cytotoxic on 293T and HUVEC, with an IC50 values of 49 and 45 μM, respectively.
分子量
295.18
Formula
C13H15BrN2O
CAS 号
2470969-91-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Laaroussi H, Ding Y, Teng Y, et al. Synthesis of indole inhibitors of silent information regulator 1 (SIRT1), and their evaluation as cytotoxic agents. Eur J Med Chem. 2020;202:112561.
SIRT-IN-1 is a potent inhibitor of SIRT1/2/3, with IC50s of 15, 10, 33 μM, respectively.
IC50 & Target
SIRT1
15 nM (IC50)
SIRT2
10 nM (IC50)
SIRT3
33 nM (IC50)
体外研究 (In Vitro)
SIRT-IN-1 (compound 28) is one of the most potent truncated pan SIRT1/ 2/3 inhibitor, the IC50 values are 0.015, 0.010, 0.033 μM, respectively. SIRT-IN-1 (SIRT1/2/3 pan inhibitor) binds identically in the catalytic active site (RMS=0.29 Å), occupying the nicotinamide C-pocket and acetyl lysine substrate channel[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
389.52
Formula
C19H27N5O2S
CAS 号
1431411-60-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Disch JS, et al. Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3. J Med Chem. 2013 May 9;56(9):3666-79.
SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2[1].
IC50 & Target
IC50: 2.4 μM (Sirt2)[1].
分子量
424.54
Formula
C21H20N4O2S2
CAS 号
1862237-99-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491.
SIRT-IN-3 is a potent SIRT inhibitor, with an IC50 of 17 μM for SIRT1. SIRT-IN-3 shows about 4-fold and 14-fold selectivity for SIRT1 over SIRT2 and SIRT3, respectively (IC50 of 74 μM and 235 μM for SIRT2 and SIRT3, respectively)[1].
体外研究 (In Vitro)
SIRT-IN-3 (Compound 7) (30-300 μM; 8 hours) causes p53 acetylation in in HCT116 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
212.25
Formula
C13H12N2O
CAS 号
1211-19-4
运输条件
Room temperature in continental US; may vary elsewhere.
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[1][2][3].
IC50 & Target
SIRT1
体内研究 (In Vivo)
SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) increases SIRT1 protein without altering Sirt1 mRNA in diabetic mice[2]. SRT 2104 (100 mg/kg/day, supplemented in diet for 24 weeks) decreases testicular oxidative stress, activation of apoptotic signaling, and ER stress in diabetic mice[2]. SRT 2104 (0.5%; for 18 weeks) improves motor function and increases survival in N171-82Q HD mice[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male C57BL/6 mice (8-week-old)[2]
Dosage:
100 mg/kg/day
Administration:
Supplemented in diet for 24 weeks
Result:
Enhanced SIRT1 protein without evelating Sirt1 mRNA level. Attenuated diabetes mellitus (DM)-induced oxidative stress, apoptotic signaling, and ER stress.
Animal Model:
WT and N171-82Q HD mice (6 weeks old)[3]
Dosage:
0.5%
Administration:
0.5% SRT 2104 containing diet for 6, 12, 18 weeks
Result:
Ameliorated motor deficits and increased survival in N171-82Q HD mice.
Clinical Trial
分子量
516.64
Formula
C26H24N6O2S2
CAS 号
1093403-33-8
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Hoffmann E, et al. Pharmacokinetics and tolerability of SRT2104, a first-in-class small molecule activator of SIRT1, after single and repeated oral administration in man.
[2]. Jiao D, et al. MicroRNA-34a targets sirtuin 1 and leads to diabetes-induced testicular apoptotic cell death. J Mol Med (Berl). 2018 Sep;96(9):939-949.
[3]. Jiang M, et al. Sirtuin 1 activator SRT2104 protects Huntington’s disease mice. Ann Clin Transl Neurol. 2014 Dec;1(12):1047-52.
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker, and a bona fide Cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s>100 μM)[1].
IC50 & Target[1]
SIRT2
0.25 μM (IC50)
体外研究 (In Vitro)
PROTAC Sirt2 Degrader-1 (Compound 12; 10 µM, 1-6 hours) induces Sirt2 degradation in HeLa cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis[1]
Cell Line:
HeLa cells
Concentration:
10 µM
Incubation Time:
1-6 hours
Result:
Caused Sirt2 degradation, but showed no effect on Sirt1 levels.
分子量
852.94
Formula
C40H40N10O8S2
CAS 号
2098487-75-1
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491.
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway.[1].
IC50 & Target[1]
SIRT7
325 nM (IC50)
体外研究 (In Vitro)
SIRT7 inhibitor 97491 (1-10 μM) reduces cell growth in MES-SA cells, without causing cytotoxicity in HEK293 cells[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Proliferation Assay[1]
Cell Line:
Human uterine sarcoma MES-SA cells
Concentration:
1, 5, 10 μM
Incubation Time:
72 hours
Result:
Led to more than 50% decrease in cell proliferation at concentrations of 5 and 10 μM.
Cell Cytotoxicity Assay[1]
Cell Line:
Human embryonic kidney cell line HEK293 cells
Concentration:
1, 5, 10 μM
Incubation Time:
24 hours
Result:
HEK293 cells were almost unaffected.
体内研究 (In Vivo)
SIRT7 inhibitor 97491 (2 mg/kg; intraperitoneally injected; for 3 weeks, except on weekends) inhibits tumor growth in xenograft mice[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
SIRT-IN-2 is a potent inhibitor of SIRT1/2/3, with IC50s of 4, 4, 7 μM, respectively.
IC50 & Target
SIRT1
4 μM (IC50)
SIRT2
1 μM (IC50)
SIRT3
7 μM (IC50)
体外研究 (In Vitro)
SIRT-IN-2 (compound 31) is one of the most potent truncated pan SIRT1/ 2/3 inhibitor, the IC50 values are 4, 4, 7 μM, respectively. SIRT-IN-2 (SIRT1/2/3 pan inhibitor) binds identically in the catalytic active site (RMS=0.29 Å), occupying the nicotinamide C-pocket and acetyl lysine substrate channel[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
383.49
Formula
C15H21N5O3S2
CAS 号
1431411-66-3
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
[1]. Disch JS, et al. Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3. J Med Chem. 2013 May 9;56(9):3666-79.
Sirt1/2-IN-1 (Compound 7) is a SIRT1 and SIRT2 inhibitor with IC50 values of 1.81, 2.10 and 20.5 µg/mL against SIRT1, SIRT2 and SIRT3, respectively. Sirt1/2-IN-1 displays activity in hyperacetylation of α-tubulin protein with an IC50 of 32.05 µg/mL. Sirt1/2-IN-1 shows prominent anticancer activity[1].
IC50 & Target
SIRT1
1.81 μg/mL (IC50)
SIRT2
2.10 μg/mL (IC50)
SIRT3
20.5 μg/mL (IC50)
分子量
420.93
Formula
C22H13ClN2OS2
CAS 号
2402779-21-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Khalil NA, et al. Synthesis of certain benzothieno[3,2-d]pyrimidine derivatives as a selective SIRT2 inhibitors. Eur J Med Chem. 2020 Feb 1;187:111926.
SIRT5 inhibitor 3 (compound 46) is a potent and competitive SIRT5 inhibitor with an IC50 value of 5.9 μM. SIRT5 inhibitor 3 can inhibit SIRT5 desuccinylation. SIRT5 inhibitor 3 can be used for researching cancer and neurodegenerative diseases[1].
IC50 & Target[1]
SIRT5
5.9 μM (IC50)
分子量
401.35
Formula
C22H12FN3O4
CAS 号
2128651-12-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Wang Y, et al. Overview of SIRT5 as a potential therapeutic target: Structure, function and inhibitors. Eur J Med Chem. 2022;236:114363.
SIRT5 inhibitor 2 (compound 49) is a potent SIRT5 inhibitor with an IC50 value of 2.3 μM. SIRT5 inhibitor 2 has inhibitory activity against the SIRT5-dependent desuccinylation. SIRT5 inhibitor 2 can be used for researching cancer and neurodegenerative diseases[1].
IC50 & Target[1]
SIRT5
2.3 μM (IC50)
分子量
407.27
Formula
C18H12Cl2N2O3S
CAS 号
340306-87-8
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Wang Y, et al. Overview of SIRT5 as a potential therapeutic target: Structure, function and inhibitors. Eur J Med Chem. 2022;236:114363.
Sirt2-IN-5 shows 47.95% SIRT2 inhibition at 100 µM[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
528.43
Formula
C26H27Cl2N5O3
CAS 号
902456-47-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sukuroglu, M.K., et al. The potential of 4-aryl-6-morpholino-3(2H)-pyridazinone-2-arylpiperazinylacetamide as a new scaffold for SIRT2 inhibition: in silico approach guided by pharmacophore mapping and molecular docking. Med Chem Res 30, 1915–1924 (2021).
Sirt2-IN-5 shows 47.95% SIRT2 inhibition at 100 µM[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
528.43
Formula
C26H27Cl2N5O3
CAS 号
902456-47-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sukuroglu, M.K., et al. The potential of 4-aryl-6-morpholino-3(2H)-pyridazinone-2-arylpiperazinylacetamide as a new scaffold for SIRT2 inhibition: in silico approach guided by pharmacophore mapping and molecular docking. Med Chem Res 30, 1915–1924 (2021).
Sirt2-IN-5 shows 47.95% SIRT2 inhibition at 100 µM[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
528.43
Formula
C26H27Cl2N5O3
CAS 号
902456-47-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Sukuroglu, M.K., et al. The potential of 4-aryl-6-morpholino-3(2H)-pyridazinone-2-arylpiperazinylacetamide as a new scaffold for SIRT2 inhibition: in silico approach guided by pharmacophore mapping and molecular docking. Med Chem Res 30, 1915–1924 (2021).
Sirt2-IN-6 (compound 24a) potent and selective inhibitor of SIRT2, with an IC50 of 0.815 μM. Sirt2-IN-6 can be used for the research of cancer[1].
IC50 & Target[1]
SIRT2
0.815 μM (IC50)
分子量
502.59
Formula
C26H26N6O3S
CAS 号
2243151-81-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yang LL, et, al. X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells. Eur J Med Chem. 2018 Jul 15;155:806-823.
Sirt2-IN-6 (compound 24a) potent and selective inhibitor of SIRT2, with an IC50 of 0.815 μM. Sirt2-IN-6 can be used for the research of cancer[1].
IC50 & Target[1]
SIRT2
0.815 μM (IC50)
分子量
502.59
Formula
C26H26N6O3S
CAS 号
2243151-81-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yang LL, et, al. X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells. Eur J Med Chem. 2018 Jul 15;155:806-823.
Sirt2-IN-6 (compound 24a) potent and selective inhibitor of SIRT2, with an IC50 of 0.815 μM. Sirt2-IN-6 can be used for the research of cancer[1].
IC50 & Target[1]
SIRT2
0.815 μM (IC50)
分子量
502.59
Formula
C26H26N6O3S
CAS 号
2243151-81-5
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yang LL, et, al. X-ray crystal structure guided discovery of new selective, substrate-mimicking sirtuin 2 inhibitors that exhibit activities against non-small cell lung cancer cells. Eur J Med Chem. 2018 Jul 15;155:806-823.
