2. JAK/STAT Signaling Stem Cell/Wnt Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease
  3. STAT Pyroptosis Apoptosis Reactive Oxygen Species c-Myc Bcl-2 Family TrxR
  4. 8α-Tigloyloxyhirsutinolide 13-O-acetate

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

目录号: HY-138071
产品使用指南

摩尔计算器

8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) 是一种口服有效的 STAT3 抑制剂。8α-Tigloyloxyhirsutinolide 13-O-acetate 在 TNBC 细胞中诱导早期氧化应激和细胞焦亡 (pyroptosis)，以及晚期 DNA 损伤、细胞周期停滞、细胞凋亡 (apoptosis)。 8α-Tigloyloxyhirsutinolide 13-O-acetate 在体外和体内可抑制肿瘤细胞生长。

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8α-Tigloyloxyhirsutinolide 13-O-acetate Chemical Structure

8α-Tigloyloxyhirsutinolide 13-O-acetate Chemical Structure

CAS No. : 83182-58-5

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8α-Tigloyloxyhirsutinolide 13-O-acetate 相关抗体

Top Publications Citing Use of Products

查看 STAT 亚型特异性产品:

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STAT3 STAT5 STAT6 STAT1

查看 Bcl-2 Family 亚型特异性产品:

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2].

IC50 & Target

STAT3

 

Bcl-2

 

Bcl-xL

 

Mcl-1

 

细胞效力
(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]
体外研究
(In Vitro)

8α-Tigloyloxyhirsutinolide 13-O-acetate (R001) (0-30 μM, 72 h) 剂量依赖性地抑制人类癌细胞系的活细胞数量[1]。
8α-Tigloyloxyhirsutinolide 13-O-acetate (0-10 μM, 0-24 h) 仅在 TNBC 细胞中诱导早期细胞焦亡和晚期 DNA 损伤、细胞周期停滞和细胞凋亡[1]。
8α-Tigloyloxyhirsutinolide 13-O-acetate (0-20 μM, 0-48 h) 促进三阴性乳腺癌细胞中 ROS 的诱导[1]。

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

8α-Tigloyloxyhirsutinolide 13-O-acetate 相关抗体:

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.
体内研究
(In Vivo)

8α-Tigloyloxyhirsutinolide 13-O-acetate (5 mg/kg，口服灌胃，每周 5 次，持续 75 天) 抑制小鼠肿瘤生长[1]。

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.
分子量

420.45

Formula

C22H28O8
CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

8α-Tigloyloxyhirsutinolide 13-O-acetate 相关分类

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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.

Keywords:

8α-Tigloyloxyhirsutinolide 13-O-acetate83182-58-58αTGHSTATPyroptosisApoptosisReactive Oxygen Speciesc-MycBcl-2 FamilyTrxRMycThioredoxin ReductaseTNBC cellsVernonia nudifloraTriple-negative breast cancerMDA-MB-231MDA-MB-468 cellsnormal human breast epithelial cellsMCF-10AHBMECorally activeInhibitorinhibitorinhibit

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