Free shipping on all orders over $ 500

Triptolide

Cat. No. M3985

All AbMole products are for research use only, cannot be used for human consumption.

Triptolide Structure
Synonym:

PG490

Size Price Availability Quantity
10mM*1mL in DMSO USD 87  USD87 In stock
1mg USD 35  USD35 In stock
2mg USD 65  USD65 In stock
5mg USD 105  USD105 In stock
10mg USD 165  USD165 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Triptolide covalently binds to human XPB and inhibits its DNA-dependent ATPase activity, which leads to the inhibition of RNA polymerase II-mediated transcription and likely nucleotide excision repair.PG490 inhibits interleukin(IL)-2 expression by normal human peripheral blood lymphocytes stimulated with phorbol 12-myristate 13-acetate (PMA) and antibody to CD3 (IC50 of 10 ng/ml), and with PMA and ionomycin (Iono, IC50 of 40 ng/ml).PG490 inhibits the induction of DNA binding activity at the purine-box/antigen receptor response element (ARRE)/nuclear factor of activated T-cells (NF-AT) target sequence but not at the NF-kappaB site.PG490 also inhibits PMA-stimulated activation of a chimeric transcription factor in which the C-terminal TA1 transactivation domain of NF-kappaB p65 is fused to the DNA binding domain of GAL4. In 16HBE human bronchial epithelial cells, IL-8 expression is regulated predominantly by NF-kappaB, and PG490 but not cyclosporin A can completely inhibit expression of IL-8.PG490 potently inhibited TNF-alpha-induced activation of NF-kappaB. PG490 also blocked TNF-alpha-mediated induction of c-IAP2 (hiap-1) and c-IAP1 (hiap-2), members of the inhibitor of apoptosis (IAP) family. Interestingly, PG490 did not block DNA binding of NF-kappaB, but it blocked transactivation of NF-kappaB.

Product Citations
Customer Product Validations & Biological Datas
Source Transl Lung Cancer Res (2021). Figure 5. Triptolide (Abmole Bioscience, Houston, TX, USA)
Method Tumor model in vivo
Cell Lines Male Bagg Albino (BALB)/c nude 6-week-old mice
Concentrations 0.4 mg/kg; 0.8 mg/kg
Incubation Time 24 d
Results The mean volumes of subcutaneous tumors in low-dose (0.4 mg/kg) and high-dose (0.8 mg/kg) triptolide groups were smaller than those in the vehicle group
Source Transl Lung Cancer Res (2021). Figure 2. Triptolide (Abmole Bioscience, Houston, TX, USA)
Method cell viability assay
Cell Lines The A549/TaxR cells
Concentrations 0, 20, 40, and 60 nM
Incubation Time 24 h
Results Additionally, as shown in Figure 3B, cell viability increased to 92% after triptolide treatment (20 nM, 24 hours). A549/TaxR cells remained viable after triptolide treatment (20 nM), apoptosis was induced (Figure 2E), and migration and invasion was inhibited.
Protocol (for reference only)
Cell Experiment
Cell lines N2a and SKNSH cells
Preparation method Cell viability determination
Cells were seeded in serum-containing media onto 96-well plates at densities of 3 × 103 cells per well for N2a and 5 × 103 cells per well for SKNSH. Following overnight incubation, cells were treated with varying concentrations of triptolide in serum-free media and re-incubated for varying time courses at 37 °C. Controls were treated with serum-free media.Cell viability was determined using an MTT assay. Reagent was prepared by dissolving thiazolyl blue tetrazolium bromide in phosphate-buffered saline at a concentration of 2 mg/mL and filtering. After cells were incubated in 96-well plates and subsequently exposed to triptolide at varying doses and time durations, 20 μL MTT reagent were added to each well. Cells were re-incubated at 37°C for 4 hours, after which all liquid was aspirated from each well and absorbances were measured at 550 and 650 nm. These experiments were performed in triplicate and repeated 4 times.
Concentrations 31.25 to 500 nM
Incubation time 24 and 48 h
Animal Experiment
Animal models Female A/J mice bearing Orthotopic neuroblastoma model
Formulation DMSO
Dosages 0.4 mg/kg
Administration intraperitoneal injections
Chemical Information
Molecular Weight 360.40
Formula C20H24O6
CAS Number 38748-32-2
Solubility (25°C) DMSO 25 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Titov DV, et al. Nat Chem Biol. XPB, a subunit of TFIIH, is a target of the natural product triptolide.

[2] Antonoff MB, et al. Surgery. Triptolide therapy for neuroblastoma decreases cell viability in vitro and inhibits tumor growth in vivo.

[3] Lee KY, et al. J Biol Chem. PG490 (triptolide) cooperates with tumor necrosis factor-alpha to induce apoptosis in tumor cells.

[4] Qiu D, et al. J Biol Chem. Immunosuppressant PG490 (triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T-cells and NF-kappaB transcriptional activation.

Related NF-κB Products
QNZ

QNZ is an inhibitor of NF-κB activation with IC50 of 11 nM.

Caffeic Acid Phenethyl Ester

Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities.

Cepharanthine

Cepharanthine is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production.

JSH-23

Jsh-23 is a NF-κB inhibitor, inhibited NF-κB transcriptional activity in lipopolysaccharid-stimulated macrophages RAW 264.7 with IC50 of 7.1 μM. Jsh-23 inhibited the nuclear translocation of NF-κB P65 without affecting the degradation of IκBα.

Methylthiouracil

Methylthiouracil is an anti-thyroid agent. Methylthiouracil inhibits TNF-α and IL-6 production and NF-κB and ERK1/2 activation.

  Catalog
Abmole Inhibitor Catalog




Keywords: Triptolide, PG490 supplier, NF-κB, inhibitors, activators

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.