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

Cat. No.: HY-138071: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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

Size		Stock
MOQ		Minimum order quantity
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All STAT Isoform Specific Products:

View All Isoforms

STAT3 STAT5 STAT6 STAT1

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms

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

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.6 μM Compound: 4	Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay Inhibition of TNFalpha-induced NF-kappaB activity expressed in human HEK 293 cells after 6 hrs by luciferase reporter gene assay	[PMID: 22850207]
MCF7	IC₅₀	10.4 μM Compound: 6	Antiproliferative activity against human MCF7 cells for 72 hrs by cyquant assay Antiproliferative activity against human MCF7 cells for 72 hrs by cyquant assay	[PMID: 26331426]
MDA-MB-231	IC₅₀	1.8 μM Compound: 6	Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by cyquant assay Antiproliferative activity against human MDA-MB-231 cells for 72 hrs by cyquant assay	[PMID: 26331426]
NIH3T3	IC₅₀	2 μM Compound: 6	Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by cyquant cells Cytotoxicity against mouse NIH/3T3 cells after 72 hrs by cyquant cells	[PMID: 26331426]
RAW264.7	IC₅₀	2 μM Compound: 4	Antiinflammatory activity against LPS-induced NO production in mouse RAW264.7 cells assessed as reduction in nitrite level preincubated for 15 mins prior to LPS treatment by Griess method Antiinflammatory activity against LPS-induced NO production in mouse RAW264.7 cells assessed as reduction in nitrite level preincubated for 15 mins prior to LPS treatment by Griess method	[PMID: 22850207]
SF-295	IC₅₀	7.5 μM Compound: 6	Antiproliferative activity against human SF295 cells for 72 hrs by cyquant assay Antiproliferative activity against human SF295 cells for 72 hrs by cyquant assay	[PMID: 26331426]
U-251	IC₅₀	1.7 μM Compound: 6	Antiproliferative activity against human U251MG cells for 72 hrs by cyquant assay Antiproliferative activity against human U251MG cells for 72 hrs by cyquant assay	[PMID: 26331426]
U-251	IC₅₀	2.2 μM Compound: 6	Inhibition of Stat3 dimer DNA binding activity in human U251MG cells nuclear extract after 1.5 hrs by EMSA using radiolabeled probe hSIE Inhibition of Stat3 dimer DNA binding activity in human U251MG cells nuclear extract after 1.5 hrs by EMSA using radiolabeled probe hSIE	[PMID: 26331426]
U-373MG ATCC	IC₅₀	2.3 μM Compound: 6	Inhibition of Stat3 dimer DNA binding activity in human U373MG cells nuclear extract after 1.5 hrs by EMSA using radiolabeled probe hSIE Inhibition of Stat3 dimer DNA binding activity in human U373MG cells nuclear extract after 1.5 hrs by EMSA using radiolabeled probe hSIE	[PMID: 26331426]
U-373MG ATCC	IC₅₀	3.5 μM Compound: 6	Antiproliferative activity against human U373MG cells for 72 hrs by cyquant assay Antiproliferative activity against human U373MG cells for 72 hrs by cyquant assay	[PMID: 26331426]

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

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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.

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks