8α-Tigloyloxyhirsutinolide 13-O-acetate (Synonyms: 8αTGH)

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8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo.

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

8α-Tigloyloxyhirsutinolide 13-O-acetate Chemical Structure

CAS No. : 83182-58-5

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STAT3 STAT5 STAT6 STAT1

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

STAT3

Bcl-2

Bcl-xL

Mcl-1

In Vitro

8α-Tigloyloxyhirsutinolide 13-O-acetate (R001) (0-30 μM, 72 h) dose-dependently suppresses the viable cell numbers of the human cancer lines^[1].
8α-Tigloyloxyhirsutinolide 13-O-acetate (0-10 μM, 0-24 h) leads to early pyroptosis and late DNA damage, cell cycle arrest, and apoptosis only in the TNBC cells^[1].
8α-Tigloyloxyhirsutinolide 13-O-acetate (0-20 μM, 0-48 h) promotes ROS induction in triple-negative breast cancer cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	Multiple human cancer lines, normal human breast epithelial cells and normal human brain microvascular endothelial cells (HBMEC)
Concentration:	0, 1, 2.5, 5, 10, 20, 30 μM
Incubation Time:	72 h
Result:	Dose-dependently suppressed the viable cell numbers of the human cancer lines, MDA-MB-468, MDA-MB-231, Panc-1, A549, DU145, HCC1937, and MDA-MB-436 cells with IC₅₀ values of 2.3, 4.4, 4.3, 5.2, 5.8, 6.3, and 7.1 µM, respectively, compared to much weaker effects on the normal human breast epithelial cells, MCF-10A or HBMEC, with IC₅₀ of 23.9 or 14.2 µM, respectively.

Western Blot Analysis^[1]

Cell Line:	NIH3T3/v-Src fibroblasts, MDA-MB-231, MDA-MB-468, or MCF-10A cells
Concentration:	0, 2, 5, 10, 20 μM
Incubation Time:	30 min, 3 h, 24 h
Result:	Suppressed STAT3:STAT3 DNA-binding activity, with IC₅₀ of 5 µM. Showed the inhibition of STAT3 Tyr phosphorylation in time- and dose-dependent manner, while phospho-Ser-STAT3 (pS727-STAT3), pY1068EGFR, and pY-Jak2 were largely unaffected. Attenuated the expression of STAT3 downstream target genes, including c-Myc, Mcl-1, Bcl-2, Bcl-xL, and vascular endothelial growth factor (VEGF) in MDA-MB-468 and MDA-MB-231 cells.

Apoptosis Analysis^[1]

Cell Line:	Triple-negative breast cancer (TNBC), MDA-MB-231 and MDA-MB-468 cells, or normal human breast epithelial cells, MCF-10A
Concentration:	0, 2.5, 5 or 10 µM
Incubation Time:	6 or 24 h
Result:	Showed no significant induction of early apoptosis at 6 h, while the evidence of extensive cell death of 56.2% occurred at later time (24 h), with cleavage of poly (ADP-ribose) polymerase (PARP) and caspase 3 at 24-48 h.

In Vivo

8α-Tigloyloxyhirsutinolide 13-O-acetate (5 mg/kg, Oral gavage, 5 times per week for 75 days) suppresses tumor growth in mice^[1].

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

Animal Model:	Five-week-old female athymic nude mice (injected subcutaneously in the right flank area with MDA-MB-468 cells in 100 μL PBS)
Dosage:	5 mg/kg
Administration:	Oral gavage, every day, 5 times per week for 75 days
Result:	Inhibited MDA-MB-468 xenografts growth in mice, with reduced pY705-STAT3, G6PD, TrxR1, and GSH levels.

Molecular Weight

420.45

Formula

C₂₂H₂₈O₈

CAS No.

83182-58-5

SMILES

O=C(/C(C)=C/C)O[C@@H](C[C@H]1C)C(/C(OC2=O)=C\[C@](O[C@]13O)(CC3)C)=C2COC(C)=O

Structure Classification

Initial Source

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

Handling Instructions (2659 KB)

References

[1]. Zhu Y, et al. Natural product preferentially targets redox and metabolic adaptations and aberrantly active STAT3 to inhibit breast tumor growth in vivo. Cell Death Dis. 2022 Dec 6;13(12):1022. [Content Brief]

[2]. A Bardón, et al. Glaucolides and related sesquiterpene lactones fromVernonia nudiflora and Chrysolaena propinqua. Phytochemistry, 1992, 31(2):609-613.

8α-Tigloyloxyhirsutinolide 13-O-acetate Related Classifications

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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.

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