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) 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.

For research use only. We do not sell to patients.

SIRT6-IN-3 Chemical Structure

SIRT6-IN-3 Chemical Structure

CAS No. : 3023471-40-8

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Based on 1 publication(s) in Google Scholar

SIRT6-IN-3 Related Antibodies

Top Publications Citing Use of Products

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Sirtuin SIRT1 SIRT2 SIRT3 SIRT6 SIRT5 SIRT7

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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p70S6K RSK1 RSK2 RSK3 RSK4

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ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

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Description

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)

In Vitro

SIRT6-IN-3 (25 μM, 48 h) induces PDAC cell-cycle arrest and apoptosis[1].
SIRT6-IN-3 (25 μM, 72 h) inhibits the proliferation of pancreatic cancer cells by inhibiting signaling pathways[1].

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

SIRT6-IN-3 Related Antibodies

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.
In Vivo

SIRT6-IN-3 (HY-156027; 20 mg/kg for i.p; once every 2 days for 4 weeks) has antitumor effects on tumor mouse model[1].
SIRT6-IN-3 (HY-156027; 20 mg/kg for i.p; once every 2 days for 4 weeks) enhances the antitumor effects of gemcitabine in vivo when in combination with gemcitabine (ratio 2 : 1)[1].

MedChemExpress (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.
Molecular Weight

673.73

Formula

C21H30Br3ClN6S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

BrC1=C(Br)NC(C2=NC=CC3=C2N=CN3CCCCCCS/C(N(C)C)=[N+](C)\C)=C1.Cl.[Br-]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 120 mg/mL (178.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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SIRT6-IN-3 Related Classifications

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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