2. Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. Sirtuin HDAC Akt mTOR Ribosomal S6 Kinase (RSK) ERK
  4. SIRT6-IN-3

SIRT6-IN-3 (compound 8a) 是 SIRT6 的选择性抑制剂 (IC50 为 7.49 μM)。SIRT6-IN-3 抑制胰腺导管腺癌 (PDAC) 细胞增殖并诱导细胞凋亡 (apoptosis)。SIRT6-IN-3 通过阻止 DNA 损伤修复来增加吉西他滨 (HY-17026) 对癌细胞的敏感性。SIRT6-IN-3 用于胰腺癌研究。

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SIRT6-IN-3 Chemical Structure

SIRT6-IN-3 Chemical Structure

CAS No. : 3023471-40-8

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SIRT6-IN-3 相关抗体

Top Publications Citing Use of Products

查看 Sirtuin 亚型特异性产品:

查看所有亚型
Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

查看 Akt 亚型特异性产品:

查看所有亚型
Akt Akt1 Akt2 Akt3

查看 mTOR 亚型特异性产品:

查看所有亚型
mTOR mTORC1 mTORC2

查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

查看所有亚型
p70S6K RSK1 RSK2 RSK3 RSK4

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SIRT6-IN-3 (compound 8a) is a selective inhibitor of SIRT6 (IC50=7.49 μM). SIRT6-IN-3 inhibits pancreatic ductal adenocarcinoma (PDAC) cells proliferation and induces apoptosis. SIRT6-IN-3 increases the sensitivity of cancer cells to gemcitabine (HY-17026) via blocking the DNA damage repair pathway. SIRT6-IN-3 is used in pancreatic cancer research[1].

IC50 & Target

SIRT1

80.52 μM (IC50)

SIRT2

92.21 μM (IC50)

SIRT6

7.46 μM (IC50)

HDAC3

111.9 μM (IC50)

HDAC6

96.77 μM (IC50)

HDAC8

102 μM (IC50)

体外研究
(In Vitro)

SIRT6-IN-3 (25 μM，48 小时) 诱导 PDAC 细胞周期阻滞和细胞凋亡[1]。
SIRT6-IN-3 (25 μM，72 小时) 通过抑制细胞信号通路来抑制胰腺癌细胞的增殖[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SIRT6-IN-3 相关抗体:

Apoptosis Analysis[1]

Cell Line: PDAC cells
Concentration: 0, 6.25, 12.5, 25 μM
Incubation Time: 48 h
Result: Increased the percentages of the G0-G1 phase and decreased cyclin D1 expression in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: PDAC cells
Concentration: 0, 6.25, 12.5, 25 μM
Incubation Time: Overnight
Result: Significantly down-regulated p-mTOR, p-P70S6K, p-AKT, and p-ERK.
Inhibited the activity of both mTORC1 and mTORC2.
Significantly up-regulated the expression of cleaved-PARP, cleaved-Caspase3, and cleaved-Caspase9.
体内研究
(In Vivo)

SIRT6-IN-3 (HY-156027；20 mg/kg，腹腔注射；两天一次，连用四周) 在肿瘤小鼠模型中有抗肿瘤作用[1]。
SIRT6-IN-3 (HY-156027；20 mg/kg，腹腔注射；两天一次，连用四周) 在与吉西他滨 (比例 2 : 1 ) 联用时增强了吉西他滨的抗肿瘤作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tumor mouse model[1]
Dosage: 20 mg/kg (in combination with 10 mg/kg gemcitabine)
Administration: Intraperitoneal injection (i.p.); Once every 2 days for 4 weeks
Result: Inhibited the tumor mass 71.3% in mice with combinations of gemcitabine.
Greatly increased the expression of apoptosis maker.
分子量

673.73

Formula

C21H30Br3ClN6S
CAS 号
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.
纯度 & 产品资料
参考文献

SIRT6-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SIRT6-IN-33023471-40-8SirtuinHDACAktmTORRibosomal S6 Kinase (RSK)ERKHistone deacetylasesPKBProtein kinase BMammalian target of RapamycinS6KExtracellular signal regulated kinasesPancreatic cancerPancreatic ductal adenocarcinomaPDACInhibitorinhibitorinhibit

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