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Triptolide

Cat. No. M3985
Triptolide Structure
Synonym:

PG490

Size Price Availability Quantity
2mg USD 75 In stock
5mg USD 120 In stock
10mg USD 188 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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.

Protocol
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 (Sigma-Aldrich) in phosphate-buffered saline (Invitrogen) 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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 360.40
Formula C20H24O6
CAS Number 38748-32-2
Purity >99%
Solubility DMSO 25mg/ml
Storage at -20°C
References

XPB, a subunit of TFIIH, is a target of the natural product triptolide.
Titov DV, et al. Nat Chem Biol. 2011 Mar;7(3):182-8. PMID: 21278739.

Triptolide therapy for neuroblastoma decreases cell viability in vitro and inhibits tumor growth in vivo.
Antonoff MB, et al. Surgery. 2009 Aug;146(2):282-90. PMID: 19628086.

PG490 (triptolide) cooperates with tumor necrosis factor-alpha to induce apoptosis in tumor cells.
Lee KY, et al. J Biol Chem. 1999 May 7;274(19):13451-5. PMID: 10224110.

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.
Qiu D, et al. J Biol Chem. 1999 May 7;274(19):13443-50. PMID: 10224109.

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Abmole Inhibitor Catalog 2017




Keywords: Triptolide, PG490 supplier, 5-HT Receptor, inhibitors

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