Celastrol

Catalog No.S1290 Synonyms: Tripterine

Celastrol Chemical Structure

Molecular Weight(MW): 450.61

Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.

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Cited by 2 Publications

2 Customer Reviews

  • SK-BR-3, A549, HCT-116 and BT-474 cells were incubated with or without X66 for 1 h before exposed to GM, celastrol or MG132 for 8 h. Cell lysates were analyzed by Western blot with indicated antibodies.

    Oncotarget, 2016, 7(20):29648-63.. Celastrol purchased from Selleck.

    Effects of compound 10 and celastrol on client proteins degradation. Both compound 10 and celastrol induces decreases of Hsp90 client proteins (Akt and Cdk4) through a concentration -dependent manner by Western blot. Meanwhile, compound 10 and celastrol have no effect on the expression level of Hsp90.

    Eur J Med Chem, 2017, 136:63-73. Celastrol purchased from Selleck.

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Biological Activity

Description Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
Features A potent antioxidant and anti-inflammatory drug.
Targets
20S proteasome [1]
(Cell-free assay)
2.5 μM
In vitro

Celastrol at 5 μM inhibits the chymotrypsin-like, PGPH-like, and trypsin-like activities of the purified 20S proteasome by 80%, 5%, and <1%, respectively, whereas at 10 μM, it inhibits these three proteasomal activities by ∼90%, 15%, and <1%, respectively. Celastrol significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner. Celastrol at 2.5 μM to 5 μM induces caspase-3 activity by 4.7-fold to 5.5-fold in PC-3 cells. Celastrol (5 μM) treated cells, the levels of the proteasome target proteins, IκB-α and Bax, are increased after 1 hour and further increased to its peak for 4 hours to 12 hours. Celastrol (2.5 μM) treatment induces proteasome inhibition by 40%, as shown by the decreased levels of chymotrypsin-like activity and increased accumulation of ubiquitinated proteins in LNCaP cells. Celastrol (2.5 μM) induces apoptosis in the Celastrol-treated LNCaP cells, as shown by increased levels of caspase-3 activity (up to 3.5-fold), PARP cleavage, and apoptotic morphology. [1] Celastrol (300 nM) is found to suppress LPS-induced production of TNF-alpha and IL-1beta by human monocytes and macrophages. Celastrol (100 nM) also decreases LPS-induced expression of class II MHC molecules by microglia. Celastrol strongly inhibits LPS and IFN-y-induced NO production with IC50 of 200 nM in macrophage lineage cells. Celastrol strongly inhibits TNF-α and IFN-γ-induced NO production with IC50 of 200 nM in endothelial cells. [2] Celastrol (2.5 μM) potentiates the apoptosis induced by TNF and chemotherapeutic agents and inhibits invasion, both regulated by NF-kappaB activation, in KBM-5 cells. Celastrol (2.5 μM) suppresses the expression of TNF induced the expression of gene products involved in antiapoptosis (IAP1, IAP2, Bcl-2, Bcl-XL, c-FLIP, and survivin), proliferation (cyclin D1 and COX-2), invasion (MMP-9), and angiogenesis (VEGF) in KBM-5 cells. Celastrol (5 μM) is found to inhibit the TNF-induced activation of IkappaBalpha kinase, IkappaBalpha phosphorylation, IkappaBalpha degradation, p65 nuclear translocation and phosphorylation, and NF-kappaB-mediated reporter gene expression. [3] Celastrol inhibits proliferating of RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells with IC50 of 0.52 μM, 0.54 μM, 0.76 μM, 0.69 μM and 0.67 μM, respectively. Celastrol (1 μM) inhibits growth of RPMI 8226 with a decrease in the levels of cyclin D1 and cyclin E, but concomitant increase in the levels of p21 and p27. Celastrol induces apoptosis in RPMI-8226 cells indicated by the activation of caspase-8, bid cleavage, caspase-9 activation, caspase-3 activation, PARP cleavage and through the down regulation of anti-apoptototic proteins. Celastrol (1 μM) suppresses Akt pathway and activates JNK kinase in RPMI-8226 cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SH-SY5Y cells MmHISpVv[3Srb36gZZN{[Xl? NEHHdXNP\XW{b4Dyc5Rm[3Srb36gZYdicW6|dDDi[ZRiNWGveXzvbYQheGWydHnk[UAyNTR{LXnu[JVk\WRidH;4bYNqfHliaX6gbJVu[W5iU1itV3k2YSClZXzsd{Bie3Onc4Pl[EBieyCuYXP0ZZRmKGSnaInkdo9o\W6jc3WgdoVt\WG|ZTygSWM2OD1yLkCzO|Y1KM7:TR?= NIHsZnAyQTF|OEi1PS=>
human SGC7901 cells M1;pXGZ2dmO2aX;uJIF{e2G7 MmXSOFghcA>? MUXBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1fDO|kxOSClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJN2en[rdnHsJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6xOUDPxE1? NUn4dZZjOjV6MUK5OlY>
HeLa cells NXO3VXdQTnWwY4Tpc44h[XO|YYm= MkDlTY5pcWKrdHnvckBw\iCQRj3rZZBx[UJiYXP0bZZqfHliaX6gbJVu[W5iSHXMZUBk\WyuczDifUBUTUGSIILldI9zfGW{IHHzd4F6NCCLQ{WwQVAvOTVizszN NEf0O5ozODR4OUi4Oy=>
human MCF7 cells M4XzN2N6fG:2b4jpZ:Kh[XO|YYm= MX23NkBp M1TSdGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KE2WUz;QUXMh[XO|YYmsJGlEPTB;MD6xOVMh|ryP NHPmbokzPTd3NkK5PS=>
human 293T cells MmeySpVv[3Srb36gZZN{[Xl? NVTTOGdDOzBibXnudy=> MknsTY5pcWKrdHnvckBw\iCOUGOtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBqdiCqdX3hckAzQTOWIHPlcIx{KGmwY4XiZZRm\CCob4KgN|AhdWmwczDmc4xtd3enZDDifUB1emWjdHXkJJdqfGhiTGDTJIZweiB4IHjyd{BjgSCmdXHsMYx2[2moZYLhd4UhemWyb4L0[ZIh[XO|YYmsJGlEPTB;MD6xO{DPxE1? M{jLdFIyOzl|MEC0
mouse RAW264.7 cells NH24OZlHfW6ldHnvckBie3OjeR?= NF;PR5IyQCCq MXLJcohq[mm2aX;uJI9nKEySUz3zeIlufWyjdHXkJG5Hc2GycHHCJIFkfGm4YYTpc44hfHKjboPm[YN1\WRiaX6gcY92e2ViUlHXNlY1NjdiY3XscJMh[W[2ZYKgNVghcHK|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiSVO1NF0xNjJizszN NVzlWpN5OjJ5MEWwNlA>
human SMMC7721 cells NIfM[HJHfW6ldHnvckBie3OjeR?= MkSyOFghcA>? MW\BcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU13NR|c4OjFiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB{fXK4aY\hcEBi\nSncjC0PEBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuOVgh|ryP NGfoSoszPThzMkm2Oi=>
human 293T cells NWn2OFhES3m2b4TvfIlkyqCjc4PhfS=> NYLXfHZJS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hOjl|VDDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCkeTDkeYFtNWy3Y3nm[ZJie2VicnXwc5J1\XJiYYPzZZktKEmFNUC9NE43PyEQvF2= M2Lrb|IyOzl|MEC0
human MGC803 cells NIfWVGpHfW6ldHnvckBie3OjeR?= NID3UoQ1QCCq NEjhZllCdnSrY3HuZ4VzKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gUWdEQDB|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhe3W{dnn2ZYwh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2xMlU2KM7:TR?= M{PWfFI2QDF{OU[2
human SK-N-SH cells MVHDfZRwfG:6aXRCpIF{e2G7 MXi3NkBp M2nyPWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU5vU1igZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiQ1O1NF0yNjZizszN NVLS[HRsOTl3MEKwOVc>
human LNCAP cells MkH0SpVv[3Srb36gZZN{[Xl? MnzlRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTF7DRXAh[2WubIOsJGlEPTB;Mj61JO69VQ>? NXHKZppGOjB4Mke1OVY>
HeLa cells MmTYSpVv[3Srb36gZZN{[Xl? MUKzJIg> MkK3RY1xdGmoaXPheIlwdiCxZjDIV2YyKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCqdX3hckBJ\UyjIHPlcIx{KGG|c3Xzd4VlKGG|IHfyZY52dGViZn;ycYF1cW:wIIDy[ZRz\WG2ZXSg[o9zKDNiaILzJIJ6KGmvbYXuc4N6fG:laHXtbYNidCC|dHHpcolv\yxiRVO1NF0zNjZizszN Mne1NVk2ODJyNUe=
human RPMI8226 cells M2K2cWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnviS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gVnBOUTh{Mk[gZ4VtdHNuIFnDOVA:OyEQvF2= NGS2PFAyQDF4NEG5Oy=>
human HeLa cells NGHkUWpEgXSxdH;4bYPDqGG|c3H5 M{O5U|czKGh? NWjsTVRHS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWOYTDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwQVMh|ryP NUXwRmtjOTl3MEKwOVc>
rat PC12 cells MXzGeY5kfGmxbjDhd5NigQ>? NVi4cGRpS3m2b4Dyc5Rm[3SrdnWgZYN1cX[rdImgZYdicW6|dDD0MWJRUC2rbnT1Z4VlKGOnbHyg[IFu[WenIHnuJJJifCCSQ{GyJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7LDDJR|UxRTNwMUWg{txO MWWyNFYzPzV3Nh?=
human HepG2 cells NEDUcFRHfW6ldHnvckBie3OjeR?= MYO0PEBp MWjBcpRq[2GwY3XyJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDzeZJ3cX[jbDDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTRwMEGg{txO MofQNlU5OTJ7Nk[=
human NCI-H460 cells MnnKR5l1d3SxeHnjxsBie3OjeR?= NV2y[mF3S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVi0OlAh[2WubIOgZYZ1\XJib4\ldo5q\2i2IHnuZ5Vj[XSrb36gZpkhVVSWIHHzd4F6NCCLQ{WwQVEzNjNizszN MmDNNlE6PDJ5NkW=
human THP1 cells M33Jd2Z2dmO2aX;uJIF{e2G7 M1r4cVI1KGh? MXXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIGTSRWlNNXKnc3nzeIFvfCCqdX3hckBVUFBzIHPlcIx{KGGodHXyJFI1KGi{czDifUBidm6neHnuMXYhe3SjaX7pcoctKEWFNUC9NVUh|ryP MmLtNlA5PjR|NEK=
human MCF7 cells MXfGeY5kfGmxbjDhd5NigQ>? MVKyOEBp NUnmSIZqUW6qaXLpeIlwdiCxZjDIV3A6OCCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJHJi\iCmZXfyZYRifGmxbjDheEA2KHSrbXXzJGlEPTBiYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= MnT5NlU4PTZ{OUm=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
HIF-1α; 

PubMed: 25383959     


Celastrol enhanced HIF-1α expression in multiple cell lines. MCF-7, HeLa, PC-3 and H1299 cells were treated with the indicated doses of Celastrol for 12 h under 3% hypoxia, and western blotting was used to detect the HIF-1 proteins.

Akt / p-Akt / p-p70S6K ; 

PubMed: 25383959     


Celastrol induced AKT/p70S6K activation under normoxia and hypoxia. HepG2 cells were challenged with the indicated doses of Celastrol for 6 h under normoxia or hypoxia. The protein levels were analyzed by western blotting with the corresponding antibodies. 

PARP / p53 / p21 / cIAP1 / Bcl-xl / Bcl-2 ; 

PubMed: 25383959     


Celastrol transiently activates p53 under normoxia but persistently activates p53 under hypoxia. HepG2 cells were cultured in normoxia or hypoxia with or without 4 µM Celastrol for the indicated times. The proteins were detected by western blotting. 

IκBα / p-IKKα/β ; 

PubMed: 28388439     


Inhibition of TNFα-induced IKKα/β phosphorylation and IκBα degradation by celastrol. Cells treated with celastrol and/or TNFα (20 ng/mL) for 30 min were analyzed by western blotting (WB).

iNOS / COX-2 / Arg-1 ; 

PubMed: 29040966     


Effects of celastrol on the expression of iNOS, COX‐2 and arginase-1 in LPS-stimulated RAW264.7 cells. After 24 h treatment with LPS and/or celastrol, the cellular proteins were analyzed by Western blotting with specific antibodies and GAPDH (as loading control). The blots (n = 3) were quantified by a densitometric method. Representative blots were shown

Chk2 / p-Chk2 / Cyclin B1 / Cdc25c / p-Cdc25c ; 

PubMed: 31053160     


U251, U87-MG and C6 cells were treated with celastrol (0, 0.3, 1, 3 and 10 μM) for 24 h. The levels of cell cycle-associated protein expressions were analyzed by western blotting. β-actin was used as an internal control.

25383959 28388439 29040966 31053160
Immunofluorescence
p21 / Nur77 ; 

PubMed: 28388439     


Colocalization of Nur77 with p62. Representative images illustrate colocalization of transfected endogenous Nur77 (E) or transfected GFP-Nur77 (F) with p62 in HepG2 cells after treatment with 4 μM celastrol and 20 ng/mL TNFα for 1 hr, analyzed by immunostaining. Scale bar, 10 μm.

28388439
Growth inhibition assay
Cell viability; 

PubMed: 29040966     


Cytotoxicity of celastrol. Following 48 h treatment, RAW264.7 cells were determined for the cell viability by a colorimetric MTT assay relative to the untreated controls (n = 3). **, p < 0.01 (Celastrol vs Control).

29040966
In vivo Celastrol (3 mg/kg) results in significant inhibition (up to 70%) of tumor growth in male nude mice bearing PC-3 tumors, associated with increased p27 levels and Bax level. Celastrol (3 mg/kg) results more apoptotic tumor cells with the appearance of various PARP cleavage fragments in tumor of male nude mice bearing PC-3 tumors. Celastrol (3 mg/kg) causes 35% of tumor inhibition, associated with decreased proteasome activity and decreased expression of AR protein in nude mice bearing C4-2B tumors. [1] Celastrol (3 mg/kg) is found to suppress strongly joint swelling and other manifestations of adjuvant arthritis in mice. Celastrol (0.2 mg/kg) significantly improves the performance in memory, learning and psychomotor activity tests in rats. [2]

Protocol

Kinase Assay:[1]
+ Expand

Inhibition of purified 20S proteasome activity:

A purified rabbit 20S proteasome (0.1 μg) is incubated with 40 μM of various fluorogenic peptide substrates in 100 μL assay buffer (20 mM Tris-HCl (pH 7.5)), in the presence of Celastrol at different concentrations or in the solvent DMSO for 2 hours at 37 ℃, followed by measurement of inhibition of each proteasomal activity.
Cell Research:[4]
+ Expand
  • Cell lines: RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells
  • Concentrations: ~5 μM
  • Incubation Time: 2 hours
  • Method: The anti-proliferative effect of celastrol on various human tumor cell lines is determined by the MTT uptake method. Briefly, 5×103 cells are incubated with Celastrol in triplicate in a 96-well plate at 37 ℃. MTT solution is then added to each well. After a 2 hours incubation at 37 ℃, extraction buffer (20% SDS, 50% dimethylformamide) is added, cells are incubated overnight at 37 ℃, and the optical density is then measured at 570 nm using a Tecan plate reader.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.72 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.61
Formula

C29H38O4

CAS No. 34157-83-0
Storage powder
in solvent
Synonyms Tripterine

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID