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Celastrol

Cat. No. M3884
Celastrol Structure
Synonym:

Tripterin

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 40  USD40 In stock
10mg USD 60  USD60 In stock
50mg USD 140  USD140 In stock
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Quality Control
Biological Activity

Celastrol down-regulated the basal and DNA damaging agents-induced monoubiquitination of FANCD2,followed by proteolytic degradation. Celastrol treatment abrogated the G2 checkpoint induced by IR,and enhanced the ICL agents-induced DNA damage and inhibitory effects on lung cancer cells through depletion of FANCD2.Celastrol presented striking growth inhibition and apoptosis induction potency on DU145 cells in vitro in a time- and dose-dependent manner.Celastrol exhibits its antiprostate cancer effects partially through the downregulation of the expression level of hERG channel in DU145 cells,suggesting that celastrol may be a potential agent against prostate cancer with a mechanism of blocking the hERG channel.Celastrol ameliorates experimental colitis in IL-10 deficient mice via the up-regulation of autophagy by suppressing the PI3K/Akt/mTOR signaling pathway.Celastrol has the potential to inhibit cytochrome P450 activities and may cause the herb-drug interactions.Celastrol induces apoptosis in TNBC cells and indicated that apoptosis might be mediated through mitochondrial dysfunction and PI3K/Akt signaling pathway.

Protocol
Cell Experiment
Cell lines RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells
Preparation method Determining the anti-proliferative effect of celastrol on various human tumor cell lines by the MTT uptake method. Briefly, incubating 5×103 cells with Celastrol in triplicate in a 96-well plate at 37 ℃. Then adding MTT solution to each well. After a 2 hours incubation at 37 ℃, adding extraction buffer (20% SDS, 50% dimethylformamide) , incubating cells overnight at 37 ℃, and then measuring the optical density at 570 nm using a Tecan plate reader.
Concentrations ~5 μM
Incubation time 2 hours
Animal Experiment
Animal models nude mice bearing C4-2B tumors
Formulation 10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS
Dosages 3 mg/kg
Administration Intraperitoneal injection
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 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.

Chemical Information
Molecular Weight 450.61
Formula C29H38O4
CAS Number 34157-83-0
Purity 100.0%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
References

[1] Gwag T, et al. J Physiol Pharmacol. Celastrol overcomes HSP72 gene silencing-mediated muscle atrophy and induces myofiber preservation.

[2] Wang GZ, et al. Cancer Sci. Celastrol induces proteasomal degradation of FANCD2 to sensitize lung cancer cells to DNA crosslinking agents.

[3] Ji N, et al. Biomed Res Int. Effect of Celastrol on Growth Inhibition of Prostate Cancer Cells through the Regulation of hERG Channel In Vitro.

[4] Zhao J, et al. Int Immunopharmacol. Celastrol ameliorates experimental colitis in IL-10 deficient mice via the up-regulation of autophagy.

[5] Shrivastava S, et al. Exp Mol Pathol. Anticancer effect of celastrol on human triple negative breast cancer: Possible involvement of oxidative stress, mitochondrial dysfunction, apoptosis and PI3K/Akt pathways.

[6] Jin C, et al. Xenobiotica. Inhibitory mechanisms of celastrol on human liver cytochrome P450 1A2, 2C19, 2D6, 2E1 and 3A4.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Celastrol, Tripterin supplier, HSP, inhibitors

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