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) 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

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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.

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

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • 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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Product Name:
SIRT6-IN-3
Cat. No.:
HY-156027
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