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.
Transl Lung Cancer Res. 2021 Feb;10(2):1007-1019.
Triptolide inhibits epithelial-mesenchymal transition phenotype through the p70S6k/GSK3/β-catenin signaling pathway in taxol-resistant human lung adenocarcinoma
Triptolide purchased from AbMole
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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 |
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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. |
| 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 |
| 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 |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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