Celastrol, IL-17A (IL-17A Inhibitor)

Celastrol, IL-17A Inhibitor Inhibitor [NBP2-29362]

Celastrol, IL-17A Inhibitor Inhibitor [NBP2-29362] - Celastrol, IL-17A Inhibitor Inhibitor Evaluation of inhibitory activity on induction of IL-17A. IL-17A Prom/ LUCPorterTM HEK 293 cells were plated in 96-well white plates at 5 x 10^4 cells/well for 16 h. Cells were treated with different concentrations of IL-17A inhibitor between 0 and 100 uM as noted [A] for 6 h. The luciferase reporter assay reagent was then directly added to the cell plates (50 ul/well). After 10 min, the plates were analyzed by reading in a plate luminometer. The values from [A] were used to determine the IC50 of the IL-17A inhibitor [B]. Data Summary: Celastrol inhibited the IL-17A promoter induction in a dose-response manner, of which IC50 was measured as 0.7 uM.

Celastrol, IL-17A Inhibitor Inhibitor [NBP2-29362] - The inhibitor suppresses IL-17A production in human PBMC stimulated with anti-CD3/CD28. Perpheral blood mononuclear cells (PBMC) were stimulated with anti-CD3 and anti-CD28 in the presence or absence of celastrol (0.5, 5 and 50 uM) for 3 days. IL-17A was then measured from the cell culture media using the Human IL-17A ActivELISA. Data Summary: PBMCs that were stimulated with anti-CD3/CD28 produced IL-17A, of which induction was inhibited by the IL-17A inhibitor. Vehicle: DMSO, Nil: no anti-CD3/CD28 stimulated PBMCs.

Celastrol, IL-17A (IL-17A Inhibitor) Summary

• Immunogen: CAS Number 34157-83-0
  Empirical Formula (Hill Notation) C29H38O4
  Molecular Weight 450.61
• Preparation Method: 1. To make a 50 mM stock solution, dissolve 1 mg celastrol in 44.5 ul anhydrous dimethyl sulfoxide (DMSO) by gentle vortex.
  2. Divide into useable aliquots and store them at -20oC.
  3. The stock solution may be diluted further to make working solutions in DMSO. The final DMSO concentration in the cells to be analyzed should not exceed 1%.

Applications/Dilutions

• Application Notes: Celastrol is used in assays to inhibit IL-17A induction. We recommend an initial titration of the inhibitor from 0-50 uM for in vitro assays along with vehicle. The IL-17A Prom/LUCPorter cell line (NBP2-26283), which is a semi-constitutively active cell line, is a useful positive control model system for studying inhibition of IL-17A induction by celastrol (Figure 2). The anti-CD3/CD28-stimulated peripheral blood mononuclear cells (PBMC) are another model system for studying inhibition of IL-17A production (Figure 3).

Packaging, Storage & Formulations

• Storage: Store at -20C in powder form. Store at -80C once reconstituted.
• Buffer: Solubility:DMSO: >10 mg/mL
  assay:>or equal to 98% (HPLC)

Alternate Names for Celastrol, IL-17A (IL-17A Inhibitor)

• Celastrol (IL-17A Inhibitor)
• Celastrol IL17A Inhibitor
• Celastrol IL-17A Inhibitor

Background

Celastrol is a potent antioxidant, and anti-inflammatory agent. It is a novel HSP90 inhibitor (disrupts Hsp90/Cdc37 complex), that exhibits anticancer (anti-angiogenic - suppresses VEGFR expression); antioxidant (inhibits lipid peroxidation) and anti-inflammatory activity (suppresses iNOS and inflammatory cytokine production).
Celastrol is a pentacyclic-triterpene extracted from Tripterygium wilfordii (Thunder of God Vine). This IL-17A inhibitor is known for its role in the prevention of inflammatory diseases and cancer. Molecular targets include inhibition of IKKa/b kinases, inactivation of Cdc37 and p23 proteins that are co-chaperones of HSP90, inhibition of proteasome function, and activation of heat-shock transcription factor 1 (HSF1). A recent study showed that this inhibitor suppressed rheumatoid arthritis through modulation of the key proinflammatory cytokines such as IL-17, IL-6 and IFNg; the authors indeed observed that those cytokine responses were significantly inhibited in arthritic rats when treated with the inhibitor. Our data also show that it directly suppresses IL-17A induction, in which constitutive activation of the IL-17A promoter in the IL-17A Prom/LUCPorter™ HEK 293 cell line has been highly inhibited by celastrol with the IC50 of 0.1545 uM (Figure 2). Furthermore, the inhibitor suppresses IL-17A production in peripheral blood mononuclear cells stimulated with anti-CD3/CD28 (Figure 3).

Limitations

This product is for research use only and is not approved for use in humans or in clinical diagnosis. Inhibitors are guaranteed for 1 year from date of receipt.