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

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
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 120 mg/mL (178.11 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4843 mL 7.4214 mL 14.8427 mL
5 mM 0.2969 mL 1.4843 mL 2.9685 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4843 mL 7.4214 mL 14.8427 mL 37.1069 mL
5 mM 0.2969 mL 1.4843 mL 2.9685 mL 7.4214 mL
10 mM 0.1484 mL 0.7421 mL 1.4843 mL 3.7107 mL
15 mM 0.0990 mL 0.4948 mL 0.9895 mL 2.4738 mL
20 mM 0.0742 mL 0.3711 mL 0.7421 mL 1.8553 mL
25 mM 0.0594 mL 0.2969 mL 0.5937 mL 1.4843 mL
30 mM 0.0495 mL 0.2474 mL 0.4948 mL 1.2369 mL
40 mM 0.0371 mL 0.1855 mL 0.3711 mL 0.9277 mL
50 mM 0.0297 mL 0.1484 mL 0.2969 mL 0.7421 mL
60 mM 0.0247 mL 0.1237 mL 0.2474 mL 0.6184 mL
80 mM 0.0186 mL 0.0928 mL 0.1855 mL 0.4638 mL
100 mM 0.0148 mL 0.0742 mL 0.1484 mL 0.3711 mL
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.

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产品名称:
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目录号:
HY-156027
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