Celastrol
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MedKoo CAT#: 200694

CAS#: 34157-83-0 (castrol)

Description: Celastrol, also known as tripterine, is a remedial ingredient isolated from the root extracts of Tripterygium Wilfordi (Thunder of God vine) and Celastrus Regelii. In in vitro and in vivo animal experiments, celastrol exhibits antioxidant, anti-inflammatory, anticancer, and insecticidal activities. Celastrol has attracted great interest recently, especially for its potential anti-inflammatory and anti-cancer activities. The anti-inflammatory effects of this triterpene have been demonstrated in animal models of different inflammatory diseases, including arthritis, Alzheimer's disease, asthma, and systemic lupus erythematosus.


Chemical Structure

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Celastrol
CAS# 34157-83-0 (castrol)

Theoretical Analysis

MedKoo Cat#: 200694
Name: Celastrol
CAS#: 34157-83-0 (castrol)
Chemical Formula: C29H38O4
Exact Mass: 450.27701
Molecular Weight: 450.61
Elemental Analysis: C, 77.30; H, 8.50; O, 14.20

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50.0mg USD 120.0 Same day
100.0mg USD 190.0 Same day
200.0mg USD 350.0 Same day
500.0mg USD 750.0 Same day
1.0g USD 1250.0 Same day
2.0g USD 2150.0 Same day
5.0g USD 4250.0 2 Weeks
10.0g USD 6750.0 2 Weeks
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Related CAS #: 34157-83-0 (castrol)   193957-88-9 (dihydrocelastrol)    

Synonym: Tripterine; Celastrol; Tripterin.

IUPAC/Chemical Name: 3-Hydroxy-9β,13α-dimethyl-2-oxo-24,25,26-trinoroleana-1(10),3,5,7-tetraen-29-oic acid

InChi Key: KQJSQWZMSAGSHN-JJWQIEBTSA-N

InChi Code: InChI=1S/C29H38O4/c1-17-18-7-8-21-27(4,19(18)15-20(30)23(17)31)12-14-29(6)22-16-26(3,24(32)33)10-9-25(22,2)11-13-28(21,29)5/h7-8,15,22,31H,9-14,16H2,1-6H3,(H,32,33)/t22-,25-,26-,27+,28-,29+/m1/s1

SMILES Code: O=C([C@@](CC[C@]1(C)CC[C@]2(C)C3=CC=C4C(C)=C5O)(C)C[C@@]1([H])[C@]2(C)CC[C@@]3(C)C4=CC5=O)O

Appearance: Red solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO (45 mg/ml) or Ethanol (30 mg/ml), not soluble in water.

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Biological target: Tripterin (Celastrol) is a proteasome inhibitor which inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
In vitro activity: The OS detection assay showed decreased ROS and RNS levels in celastrol-treated cells compared to control cultures after 24 and 48 h, suggesting an antioxidant role of celastrol under experimental conditions. Interestingly, the effect of celastrol on the expression of reporter genes suggests that celastrol may play an independent antioxidant regulatory role in hGL cells. In experimental conditions, in celastrol-treated hGL cells, the expression levels of ALDH3A2, FSHR, PAPP, and CYP19A1 genes significantly decreased compared to control, an effect that seems to be independent of the antioxidant effect of celastrol. To this study’s knowledge, this is the first evidence for a role of celastrol in the regulation of OS and gene expression in hGL cells. Reference: Int J Mol Sci. 2021 Apr; 22(7): 3596. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8037896/
In vivo activity: The tumor xenograft model fed with HFD (high fat diet) showed that the cancer was poorly differentiated and invaded into the mucous membrane, accompanied by degeneration and necrosis of crypt cells and an amount of infiltrative inflammation (Figure 2B). Celastrol significantly relieved these symptoms, only showing moderate edema in lamina propria interstitial or mild inflammatory cell infiltration (Figure 2B), and similar results were observed in atorvastatin group (Figure 2B). The lipid accumulation was increased in the high-fat diet-fed animal model and celastrol significantly reduced lipid deposition in tumor tissues (Figures 2C,D). Biochemical analysis showed that celastrol increased HDL level, while reduced plasma levels of TC, TG, LDL and VLDL in nude mice fed HFD (Figures 2E–I). In addition, the tumor resected from the HFD group expressed higher levels of CAV-1, LOX-1, CD133, Bmi-1, SOX-2, p-GSK-3β (S9)/GSK-3β and β-catenin than the tumor from the control group, while celastrol down-regulated the levels of these proteins (Figure 2J). The protein levels of these molecules were also confirmed by IHC (Supplementary Figures S1B–I). These results indicated that celastrol inhibited tumor growth of ccRCC in mice fed with high-fat diet through reducing lipid deposition and stemness proteins expression. Reference: Front Pharmacol. 2021; 12: 658092. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8085775/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 33.45 74.23
DMF 20.0 44.38
DMF:PBS (pH 7.2) (1:10) 1.0 2.22
Ethanol 21.9 48.6

Preparing Stock Solutions

The following data is based on the product molecular weight 450.61 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Martín-Ramírez R, González-Fernández R, Rotoli D, Hernández J, Martín-Vasallo P, Palumbo A, Ávila J. Celastrol Prevents Oxidative Stress Effects on FSHR, PAPP, and CYP19A1 Gene Expression in Cultured Human Granulosa-Lutein Cells. Int J Mol Sci. 2021 Mar 30;22(7):3596. doi: 10.3390/ijms22073596. PMID: 33808393; PMCID: PMC8037896. 2. Si H, Wang H, Xiao H, Fang Y, Wu Z. Anti-Tumor Effect of Celastrol on Hepatocellular Carcinoma by the circ_SLIT3/miR-223-3p/CXCR4 Axis. Cancer Manag Res. 2021 Feb 5;13:1099-1111. doi: 10.2147/CMAR.S278023. PMID: 33574707; PMCID: PMC7872924. 3. Zhang CJ, Zhu N, Wang YX, Liu LP, Zhao TJ, Wu HT, Liao DF, Qin L. Celastrol Attenuates Lipid Accumulation and Stemness of Clear Cell Renal Cell Carcinoma via CAV-1/LOX-1 Pathway. Front Pharmacol. 2021 Apr 16;12:658092. doi: 10.3389/fphar.2021.658092. PMID: 33935779; PMCID: PMC8085775. 4. Su Z, Zong P, Chen J, Yang S, Shen Y, Lu Y, Yang C, Kong X, Sheng Y, Sun W. Celastrol attenuates arterial and valvular calcification via inhibiting BMP2/Smad1/5 signalling. J Cell Mol Med. 2020 Nov;24(21):12476-12490. doi: 10.1111/jcmm.15779. Epub 2020 Sep 20. PMID: 32954678; PMCID: PMC7686965.
In vitro protocol: 1. Martín-Ramírez R, González-Fernández R, Rotoli D, Hernández J, Martín-Vasallo P, Palumbo A, Ávila J. Celastrol Prevents Oxidative Stress Effects on FSHR, PAPP, and CYP19A1 Gene Expression in Cultured Human Granulosa-Lutein Cells. Int J Mol Sci. 2021 Mar 30;22(7):3596. doi: 10.3390/ijms22073596. PMID: 33808393; PMCID: PMC8037896. 2. Si H, Wang H, Xiao H, Fang Y, Wu Z. Anti-Tumor Effect of Celastrol on Hepatocellular Carcinoma by the circ_SLIT3/miR-223-3p/CXCR4 Axis. Cancer Manag Res. 2021 Feb 5;13:1099-1111. doi: 10.2147/CMAR.S278023. PMID: 33574707; PMCID: PMC7872924.
In vivo protocol: 1. Zhang CJ, Zhu N, Wang YX, Liu LP, Zhao TJ, Wu HT, Liao DF, Qin L. Celastrol Attenuates Lipid Accumulation and Stemness of Clear Cell Renal Cell Carcinoma via CAV-1/LOX-1 Pathway. Front Pharmacol. 2021 Apr 16;12:658092. doi: 10.3389/fphar.2021.658092. PMID: 33935779; PMCID: PMC8085775. 2. Su Z, Zong P, Chen J, Yang S, Shen Y, Lu Y, Yang C, Kong X, Sheng Y, Sun W. Celastrol attenuates arterial and valvular calcification via inhibiting BMP2/Smad1/5 signalling. J Cell Mol Med. 2020 Nov;24(21):12476-12490. doi: 10.1111/jcmm.15779. Epub 2020 Sep 20. PMID: 32954678; PMCID: PMC7686965.

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1: Deane CA, Brown IR. Induction of heat shock proteins in differentiated human neuronal cells following co-application of celastrol and arimoclomol. Cell Stress Chaperones. 2016 Jun 8. [Epub ahead of print] PubMed PMID: 27273088.

2: Aqil F, Kausar H, Agrawal AK, Jeyabalan J, Kyakulaga AH, Munagala R, Gupta R. Exosomal formulation enhances therapeutic response of celastrol against lung cancer. Exp Mol Pathol. 2016 May 24;101(1):12-21. doi: 10.1016/j.yexmp.2016.05.013. [Epub ahead of print] PubMed PMID: 27235383.

3: Shen YF, Zhang X, Wang Y, Cao FF, Uzan G, Peng B, Zhang DH. Celastrol targets IRAKs to block Toll-like receptor 4-mediated nuclear factor-κB activation. J Integr Med. 2016 May;14(3):203-8. doi: 10.1016/S2095-4964(16)60257-1. PubMed PMID: 27181127.

4: Chang W, He W, Li PP, Song SS, Yuan PF, Lu JT, Wei W. Protective effects of Celastrol on diethylnitrosamine-induced hepatocellular carcinoma in rats and its mechanisms. Eur J Pharmacol. 2016 May 12;784:173-180. doi: 10.1016/j.ejphar.2016.04.045. [Epub ahead of print] PubMed PMID: 27181068.

5: Choi JY, Ramasamy T, Kim SY, Kim J, Ku SK, Youn YS, Kim JR, Jeong JH, Choi HG, Yong CS, Kim JO. PEGylated lipid bilayer-supported mesoporous silica nanoparticle composite for synergistic co-delivery of axitinib and celastrol in multi-targeted cancer therapy. Acta Biomater. 2016 Jul 15;39:94-105. doi: 10.1016/j.actbio.2016.05.012. Epub 2016 May 6. PubMed PMID: 27163403.

6: Cheng M, Wu G, Song Y, Wang L, Tu L, Zhang L, Zhang C. Celastrol-Induced Suppression of the MiR-21/ERK Signalling Pathway Attenuates Cardiac Fibrosis and Dysfunction. Cell Physiol Biochem. 2016;38(5):1928-38. doi: 10.1159/000445554. Epub 2016 May 9. PubMed PMID: 27160852.

7: Li H, Li J, Liu L, Zhang Y, Luo Y, Zhang X, Yang P, Zhang M, Yu W, Qu S. Elucidation of the Intestinal Absorption Mechanism of Celastrol Using the Caco-2 Cell Transwell Model. Planta Med. 2016 May 9. [Epub ahead of print] PubMed PMID: 27159672.

8: Yu X, Ruan X, Zhang J, Zhao Q. Celastrol Induces Cell Apoptosis and Inhibits the Expression of the AML1-ETO/C-KIT Oncoprotein in t(8;21) Leukemia. Molecules. 2016 Apr 30;21(5). pii: E574. doi: 10.3390/molecules21050574. PubMed PMID: 27144550.

9: Kapoor S. Tumor Growth Attenuating Effect of Celastrol In Systemic Malignancies. Int J Cancer. 2016 Apr 20. doi: 10.1002/ijc.30151. [Epub ahead of print] PubMed PMID: 27097353.

10: Choi SK, Park S, Jang S, Cho HH, Lee S, You S, Kim SH, Moon HS. Cascade regulation of PPARγ(2) and C/EBPα signaling pathways by celastrol impairs adipocyte differentiation and stimulates lipolysis in 3T3-L1 adipocytes. Metabolism. 2016 May;65(5):646-54. doi: 10.1016/j.metabol.2016.01.009. Epub 2016 Jan 25. PubMed PMID: 27085773.

11: Pazhang Y, Jaliani HZ, Imani M, Dariushnejad H. Synergism between NF-kappa B inhibitor, celastrol, and XIAP inhibitor, embelin, in an acute myeloid leukemia cell line, HL-60. J Cancer Res Ther. 2016 Jan-Mar;12(1):155-60. doi: 10.4103/0973-1482.150407. PubMed PMID: 27072230.

12: Han LP, Li CJ, Sun B, Xie Y, Guan Y, Ma ZJ, Chen LM. Protective Effects of Celastrol on Diabetic Liver Injury via TLR4/MyD88/NF-κB Signaling Pathway in Type 2 Diabetic Rats. J Diabetes Res. 2016;2016:2641248. doi: 10.1155/2016/2641248. Epub 2016 Jan 19. PubMed PMID: 27057550; PubMed Central PMCID: PMC4745324.

13: Guan Y, Cui ZJ, Sun B, Han LP, Li CJ, Chen LM. Celastrol attenuates oxidative stress in the skeletal muscle of diabetic rats by regulating the AMPK-PGC1α-SIRT3 signaling pathway. Int J Mol Med. 2016 May;37(5):1229-38. doi: 10.3892/ijmm.2016.2549. Epub 2016 Apr 5. PubMed PMID: 27049825; PubMed Central PMCID: PMC4829141.

14: Zou YC, Yang XW, Yuan SG, Zhang P, Li YK. Celastrol inhibits prostaglandin E2-induced proliferation and osteogenic differentiation of fibroblasts isolated from ankylosing spondylitis hip tissues in vitro. Drug Des Devel Ther. 2016 Mar 7;10:933-48. doi: 10.2147/DDDT.S97463. eCollection 2016. PubMed PMID: 27022241; PubMed Central PMCID: PMC4790082.

15: Wang R, Gu X, Dai W, Ye J, Lu F, Chai Y, Fan G, Gonzalez FJ, Duan G, Qi Y. A lipidomics investigation into the intervention of celastrol in experimental colitis. Mol Biosyst. 2016 Apr 26;12(5):1436-44. doi: 10.1039/c5mb00864f. PubMed PMID: 27021137.

16: Liu X, Cai F, Zhang Y, Yang A, Liu L. Celastrol, an NF-κB inhibitor, ameliorates hypercalciuria and articular cartilage lesions in a mouse model of secondary osteoporosis. J Pharmacol Sci. 2016 Apr;130(4):204-11. doi: 10.1016/j.jphs.2016.02.001. Epub 2016 Feb 8. PubMed PMID: 26980429.

17: Bian M, Du X, Cui J, Wang P, Wang W, Zhu W, Zhang T, Chen Y. Celastrol protects mouse retinas from bright light-induced degeneration through inhibition of oxidative stress and inflammation. J Neuroinflammation. 2016 Feb 27;13:50. doi: 10.1186/s12974-016-0516-8. PubMed PMID: 26920853; PubMed Central PMCID: PMC4769581.

18: Lin L, Sun Y, Wang D, Zheng S, Zhang J, Zheng C. Celastrol Ameliorates Ulcerative Colitis-Related Colorectal Cancer in Mice via Suppressing Inflammatory Responses and Epithelial-Mesenchymal Transition. Front Pharmacol. 2016 Jan 13;6:320. doi: 10.3389/fphar.2015.00320. eCollection 2015. PubMed PMID: 26793111; PubMed Central PMCID: PMC4711309.

19: Liu YJ, Zhao YJ, Su P, Zhang M, Tong YR, Hu TY, Huang LQ, Gao W. The MVA pathway genes expressions and accumulation of celastrol in Tripterygium wilfordii suspension cells in response to methyl jasmonate treatment. J Asian Nat Prod Res. 2016 Jul;18(7):619-28. doi: 10.1080/10286020.2015.1134504. Epub 2016 Jan 19. PubMed PMID: 26785825.

20: Divya T, Dineshbabu V, Soumyakrishnan S, Sureshkumar A, Sudhandiran G. Celastrol enhances Nrf2 mediated antioxidant enzymes and exhibits anti-fibrotic effect through regulation of collagen production against bleomycin-induced pulmonary fibrosis. Chem Biol Interact. 2016 Feb 25;246:52-62. doi: 10.1016/j.cbi.2016.01.006. Epub 2016 Jan 6. PubMed PMID: 26768587.



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