Cat. No.: HY-13067

Celastrol

(Synonyms: Tripterine; Tripterin)

61 Cited Publications

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Based on 61 publication(s) in Google Scholar

Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC₅₀ of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.

For research use only. We do not sell to patients.

Purity: 99.64%
CAS No.: 34157-83-0
Formula: C₂₉H₃₈O₄
Molecular Weight:450.61

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Celastrol Chemical Structure

CAS No.: 34157-83-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (61)
Solvent & Solubility
- In Vitro
- In Vivo
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Bioz

Biological Activity

Description

IC₅₀ & Target

Human Endogenous Metabolite

Nur77/NR4A1

IKKβ

All Endogenous Metabolite Isoforms :

All Antibiotic Isoforms :

All Nuclear Hormone Receptor 4A/NR4A Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
1A9	ED₅₀	0.091 μg/mL Compound: 6	Cytotoxicity against human 1A9 cells after 3 days by SRB assay Cytotoxicity against human 1A9 cells after 3 days by SRB assay	[PMID: 14640511]
1A9	ED₅₀	0.11 μg/mL Compound: 6	Cytotoxicity against human 1A9 cells after 6 days by SRB assay Cytotoxicity against human 1A9 cells after 6 days by SRB assay	[PMID: 14640511]
1A9/ptx-10	ED₅₀	0.1 μg/mL Compound: 6	Cytotoxicity against human 1A9/PTX10 cells after 3 days by SRB assay Cytotoxicity against human 1A9/PTX10 cells after 3 days by SRB assay	[PMID: 14640511]
1A9/ptx-10	ED₅₀	0.11 μg/mL Compound: 6	Cytotoxicity against human 1A9/PTX10 cells after 6 days by SRB assay Cytotoxicity against human 1A9/PTX10 cells after 6 days by SRB assay	[PMID: 14640511]
3T3-L1	EC₅₀	0.099 μM Compound: Celastrol	Anti-adipogenic activity in mouse 3T3-L1 cells assessed as lipid-lowering activity measured after 9 days by Oil Red O staining based microplate reader analysis Anti-adipogenic activity in mouse 3T3-L1 cells assessed as lipid-lowering activity measured after 9 days by Oil Red O staining based microplate reader analysis	[PMID: 37607439]
3T3-L1	EC₅₀	0.11 μM Compound: Celastrol	Lipid-lowering activity in differentiated mouse 3T3-L1 cells assessed as reduction in lipid droplet accumulation incubated in differentiation medium for 9 days by Oil Red O staining based analysis Lipid-lowering activity in differentiated mouse 3T3-L1 cells assessed as reduction in lipid droplet accumulation incubated in differentiation medium for 9 days by Oil Red O staining based analysis	[PMID: 39163779]
3T3-L1	IC₅₀	0.72 μM Compound: Celastrol	Cytotoxicity against undifferentiated mouse 3T3-L1 cells assessed as reduction in cell viability incubated for 24 hrs by SRB assay Cytotoxicity against undifferentiated mouse 3T3-L1 cells assessed as reduction in cell viability incubated for 24 hrs by SRB assay	[PMID: 39163779]
3T3-L1	IC₅₀	0.73 μM Compound: Celastrol	Cytotoxicity against mouse 3T3-L1 cells assessed as reduction in cell viability incubated for 24 hrs by Sulforhodamine B assay Cytotoxicity against mouse 3T3-L1 cells assessed as reduction in cell viability incubated for 24 hrs by Sulforhodamine B assay	[PMID: 37607439]
A 172	IC₅₀	2.31 μM Compound: CEL	Antiproliferative activity against human A-172 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Antiproliferative activity against human A-172 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 34968902]
A2780	IC₅₀	1.574 μM Compound: Celastrol	Cytotoxicity against human A2780 cells assessed as cell viability measured after 48 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as cell viability measured after 48 hrs by MTT assay	[PMID: 38964974]
A2780	IC₅₀	1.84 μM Compound: Celastrol	Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human A2780 cells incubated for 48 hrs by MTT assay	[PMID: 31279299]
A2780	IC₅₀	2.11 μM Compound: 1	Antiproliferative activity against human A2780 cells assessed as cell growth inhibition Antiproliferative activity against human A2780 cells assessed as cell growth inhibition	[PMID: 31991334]
A-431	ED₅₀	2.4 μg/mL Compound: 3	Cytotoxicity against human A431 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human A431 cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]
A549	ED₅₀	0.25 μg/mL Compound: 6	Cytotoxicity against human A549 cells after 3 days by SRB assay Cytotoxicity against human A549 cells after 3 days by SRB assay	[PMID: 14640511]
A549	IC₅₀	>100 μM Compound: CEL	Antiproliferative activity against human A549 cells expressing Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells expressing Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
A549	IC₅₀	>100 μM Compound: CEL	Antiproliferative activity against human A549 cells expressing Hsp90 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells expressing Hsp90 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
A549	IC₅₀	>100 μM Compound: CEL	Antiproliferative activity against human A549 cells expressing Hsp90-Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells expressing Hsp90-Cdc37 protein assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
A549	IC₅₀	0.98 μM Compound: CEL	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35290844]
A549	IC₅₀	1.1 μM Compound: CEL	Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay	[PMID: 35255689]
A549	IC₅₀	1.28 μM Compound: CE	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
A549	IC₅₀	1.43 μM Compound: 1; CEL	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 30316059]
A549	IC₅₀	1.48 μM Compound: CEL	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
A549	IC₅₀	1.56 μM Compound: 1	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 28688281]
A549	IC₅₀	1.56 μM Compound: 1	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 28865279]
A549	IC₅₀	1.68 μM Compound: CEL	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
A549	IC₅₀	1.8 μM Compound: Celastrol	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
A549	IC₅₀	1.99 μM Compound: 1	Antiproliferative activity against human A549 cells assessed as cell growth inhibition Antiproliferative activity against human A549 cells assessed as cell growth inhibition	[PMID: 31991334]
A549	IC₅₀	2.01 μM Compound: Celastrol	Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
A549	IC₅₀	2.02 μM Compound: Celastrol	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
A549	IC₅₀	2.12 μM Compound: Celastrol	Cytotoxic activity against human A549 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human A549 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
A549	IC₅₀	2.83 μM Compound: 1	Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34256125]
A549	IC₅₀	4.99 μM Compound: Celastrol	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
A549	IC₅₀	6.42 μM Compound: Cel	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay	[PMID: 37499289]
A549	IC₅₀	6.59 μM Compound: Celastrol	Antiproliferative activity against human A549 cells after 48 hrs by MTT assay Antiproliferative activity against human A549 cells after 48 hrs by MTT assay	[PMID: 29486954]
A549	IC₅₀	690 nM Compound: 2	Growth inhibition of human A549 cells measured every 2 hrs over 6 days by live cell imaging based method Growth inhibition of human A549 cells measured every 2 hrs over 6 days by live cell imaging based method	[PMID: 28621943]
A549	IC₅₀	9.28 μM Compound: Cel	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37499289]
AGS	IC₅₀	0.25 μM Compound: 1	Antiproliferative activity against human AGS cells assessed as cell growth inhibition Antiproliferative activity against human AGS cells assessed as cell growth inhibition	[PMID: 31991334]
BC1 cell line	ED₅₀	0.3 μg/mL Compound: 3	Cytotoxicity against human BC1 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human BC1 cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]
BEAS-2B	IC₅₀	0.454 μM Compound: 1	Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human BEAS-2B cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34256125]
Bel-7402	IC₅₀	0.44 μM Compound: Celastrol	Cytotoxic activity against human Bel7402 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human Bel7402 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
Bel-7402	IC₅₀	1.55 μM Compound: Celastrol	Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 38107170]
Bel-7402	IC₅₀	1.81 μM Compound: CEL	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35290844]
BGC-823	IC₅₀	1.1 μM Compound: CEL	Antiproliferative activity against human BGC-823 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human BGC-823 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 35536757]
BJ	IC₅₀	2.74 μM Compound: 1	Cytotoxicity against human BJ cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human BJ cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 28688281]
BJ	IC₅₀	2.74 μM Compound: 1	Antiproliferative activity against human BJ cells after 72 hrs by MTT assay Antiproliferative activity against human BJ cells after 72 hrs by MTT assay	[PMID: 28865279]
C3A	IC₅₀	3.6 μM Compound: 1	Antiproliferative activity against human C3A cells assessed as cell growth inhibition Antiproliferative activity against human C3A cells assessed as cell growth inhibition	[PMID: 31991334]
Col2	ED₅₀	0.4 μg/mL Compound: 3	Cytotoxicity against human Col2 cells after 96 hrs by sulforhodamine B assay Cytotoxicity against human Col2 cells after 96 hrs by sulforhodamine B assay	[PMID: 8158155]
Daudi	IC₅₀	<1 μM Compound: CE11	Cytotoxicity in human Daudi cells assessed as reduction in cell viability Cytotoxicity in human Daudi cells assessed as reduction in cell viability	[PMID: 28754470]
DU-145	IC₅₀	1.48 μM Compound: 1	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition	[PMID: 31991334]
H4	IC₅₀	2.09 μM Compound: Celastrol	Antiproliferative activity against human H4 cells assessed as cell growth inhibition Antiproliferative activity against human H4 cells assessed as cell growth inhibition	[PMID: 38107170]
HCC827	IC₅₀	1.3 μM Compound: 1	Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition	[PMID: 31991334]
HCT-116	IC₅₀	0.29 μM Compound: 23	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth	[PMID: 38142509]
HCT-116	IC₅₀	1.4 μM Compound: 1	Inhibition of cell viability in human HCT-116 cells incubated for 72 hrs by Cell Titer Glo assay Inhibition of cell viability in human HCT-116 cells incubated for 72 hrs by Cell Titer Glo assay	[PMID: 38679872]
HCT-116	IC₅₀	1.81 μM Compound: CEL	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
HCT-116	IC₅₀	1.9 μM Compound: CEL	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 35536757]
HCT-116	IC₅₀	5.26 μM Compound: Celastrol	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 29486954]
HCT-8	ED₅₀	0.23 μg/mL Compound: 6	Cytotoxicity against human HCT8 cells after 3 days by SRB assay Cytotoxicity against human HCT8 cells after 3 days by SRB assay	[PMID: 14640511]
HEK-293T	IC₅₀	0.67 μM Compound: 22	Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay	[PMID: 21393004]
HeLa	CC₅₀	3 μM Compound: Celastrol	Cytotoxicity against human HeLa cells after 72 hrs by MTS assay Cytotoxicity against human HeLa cells after 72 hrs by MTS assay	[PMID: 19502057]
HeLa	EC₅₀	1.1 μM Compound: Celastrol	Amplification of HSF1 transcriptional activity in human heat shock-induced HeLa cells assessed as granule formation treated 1 hr before heat shock challenge measured after 2 hrs without recovery time by immunocytochemical staining Amplification of HSF1 transcriptional activity in human heat shock-induced HeLa cells assessed as granule formation treated 1 hr before heat shock challenge measured after 2 hrs without recovery time by immunocytochemical staining	[PMID: 19502057]
HeLa	EC₅₀	2.6 μM Compound: Celastrol	Amplification of HSF1 transcriptional activity in human HeLa cells assessed as granule formation pretreated for 3 hrs by immunocytochemical staining Amplification of HSF1 transcriptional activity in human HeLa cells assessed as granule formation pretreated for 3 hrs by immunocytochemical staining	[PMID: 19502057]
HeLa	IC₅₀	0.15 μM Compound: Celastrol	Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells by SEAP reporter gene assay Inhibition of TNF-alpha-induced NF-kappaB activation in human HeLa cells by SEAP reporter gene assay	[PMID: 18841906]
HeLa	IC₅₀	0.15 μM Compound: celastrol	Inhibition of NF-kappaB activity in human HeLa cells by SEAP reporter assay Inhibition of NF-kappaB activity in human HeLa cells by SEAP reporter assay	[PMID: 20469887]
HeLa	IC₅₀	0.72 μg/mL Compound: Celastrol	Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) expressed in HeLa cells cotreated with compound and 10 ng/ml TNF-alpha for 24 hr by reporter gene assay Inhibition of TNFalpha-induced NF-kappaB activity (unknown origin) expressed in HeLa cells cotreated with compound and 10 ng/ml TNF-alpha for 24 hr by reporter gene assay	10.1007/s00044-010-9409-z
HeLa	IC₅₀	0.84 μM Compound: Celastrol	Cytotoxic activity against human HeLa cells incubated for 48 hrs by MTT assay Cytotoxic activity against human HeLa cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
HeLa	IC₅₀	1.21 μM Compound: Celastrol	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
HeLa	IC₅₀	1.7 μM Compound: CEL	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 35536757]
HeLa	IC₅₀	1.9 μM Compound: 1	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition Antiproliferative activity against human HeLa cells assessed as cell growth inhibition	[PMID: 31991334]
Hep 3B2	IC₅₀	0.76 μM Compound: Celastrol	Cytotoxicity against human Hep3B cells assessed as reduction in cell viability incubated for 24 hrs under normaxic condition by MTT assay Cytotoxicity against human Hep3B cells assessed as reduction in cell viability incubated for 24 hrs under normaxic condition by MTT assay	[PMID: 33930802]
HepG2	IC₅₀	0.58 μM Compound: Celastrol	Cytotoxic activity against human HepG2 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human HepG2 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
HepG2	IC₅₀	0.94 μM Compound: 1	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34256125]
HepG2	IC₅₀	1.3 μM Compound: PC1	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
HepG2	IC₅₀	1.33 μM Compound: CE	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
HepG2	IC₅₀	1.5 μM Compound: CEL	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 35536757]
HepG2	IC₅₀	1.62 μM Compound: 1; CEL	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 30316059]
HepG2	IC₅₀	2.4 μM Compound: 1	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition	[PMID: 31991334]
HepG2	IC₅₀	3.18 μM Compound: CEL	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
HepG2	IC₅₀	3.73 μM Compound: Celastrol	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
HepG2	IC₅₀	4.01 μM Compound: 1	Anticancer activity against human HepG2 cells assessed as cell survival after 48 hrs by MTT assay Anticancer activity against human HepG2 cells assessed as cell survival after 48 hrs by MTT assay	[PMID: 25812966]
HepG2	IC₅₀	6.17 μM Compound: Celastrol	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 29486954]
HL-60	IC₅₀	<1 μM Compound: CE11	Cytotoxicity in human HL60 cells assessed as reduction in cell viability Cytotoxicity in human HL60 cells assessed as reduction in cell viability	[PMID: 28754470]
HOS	IC₅₀	0.93 μM Compound: 1; CEL	Antiproliferative activity against human HOS cells after 48 hrs by MTT assay Antiproliferative activity against human HOS cells after 48 hrs by MTT assay	[PMID: 30316059]
HOS	IC₅₀	1.46 μM Compound: CEL	Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human HOS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
HOS	IC₅₀	2.55 μM Compound: 1	Antiproliferative activity against human HOS cells assessed as cell growth inhibition Antiproliferative activity against human HOS cells assessed as cell growth inhibition	[PMID: 31991334]
HT-1080	ED₅₀	0.5 μg/mL Compound: 3	Cytotoxicity against human HT1080 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against human HT1080 cells after 48 hrs by sulforhodamine B assay	[PMID: 8158155]
HT-29	IC₅₀	0.6 μM Compound: CEL	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35290844]
HT-29	IC₅₀	1.28 μM Compound: 1	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28865279]
HT-29	IC₅₀	1300 ng/mL Compound: 5	Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay	[PMID: 9644053]
Huh-7	IC₅₀	4.45 μM Compound: Celastrol	Antiproliferative activity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human Huh-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
Huh-7	IC₅₀	4.7 μM Compound: 1	Antiproliferative activity against human Huh-7 cells assessed as cell growth inhibition Antiproliferative activity against human Huh-7 cells assessed as cell growth inhibition	[PMID: 31991334]
K562	IC₅₀	0.4 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as cell growth inhibition Antiproliferative activity against human K562 cells assessed as cell growth inhibition	[PMID: 31991334]
Kasumi 1	IC₅₀	2.2 μM Compound: 1	Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition Antiproliferative activity against human Kasumi 1 cells assessed as cell growth inhibition	[PMID: 31991334]
KATO III stomach cancer cell line	IC₅₀	0.54 μM Compound: 1	Antiproliferative activity against human KATO III stomach cancer cell line assessed as cell growth inhibition Antiproliferative activity against human KATO III stomach cancer cell line assessed as cell growth inhibition	[PMID: 31991334]
KB	ED₅₀	0.2 μg/mL Compound: 6	Cytotoxicity against human KB cells after 3 days by SRB assay Cytotoxicity against human KB cells after 3 days by SRB assay	[PMID: 14640511]
KB	ED₅₀	2.3 μg/mL Compound: 3	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]
KB	IC₅₀	1.7 μM Compound: Celastrol	Antiproliferative activity against human KB cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human KB cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
KBM5	IC₅₀	0.5 μM Compound: 1	Antiproliferative activity against human KBM5 cells assessed as cell growth inhibition Antiproliferative activity against human KBM5 cells assessed as cell growth inhibition	[PMID: 31991334]
KBM5	IC₅₀	0.52 μM Compound: 1	Antiproliferative activity against human KBM5 cells expressing Bcr-Abl harboring T315I mutant assessed as cell growth inhibition Antiproliferative activity against human KBM5 cells expressing Bcr-Abl harboring T315I mutant assessed as cell growth inhibition	[PMID: 31991334]
KB-V1	ED₅₀	1.2 μg/mL Compound: 3	Cytotoxicity against human KBV1 cells after 72 hrs by sulforhodamine B assay in presence of vinblastine Cytotoxicity against human KBV1 cells after 72 hrs by sulforhodamine B assay in presence of vinblastine	[PMID: 8158155]
KB-V1	ED₅₀	1.7 μg/mL Compound: 3	Cytotoxicity against human KBV1 cells after 72 hrs by sulforhodamine B assay in absence of vinblastine Cytotoxicity against human KBV1 cells after 72 hrs by sulforhodamine B assay in absence of vinblastine	[PMID: 8158155]
L02	IC₅₀	0.64 μM Compound: CEL	Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35290844]
L02	IC₅₀	0.78 μM Compound: 1	Cytotoxicity against human L02 cells assessed as cell viability measured after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as cell viability measured after 72 hrs by MTT assay	[PMID: 34256125]
L02	IC₅₀	0.83 μM Compound: CEL	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 34968902]
L02	IC₅₀	1.12 μM Compound: Celastrol	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
L02	IC₅₀	1.94 μM Compound: PC1	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
LN-229	IC₅₀	3.13 μM Compound: CEL	Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Antiproliferative activity against human LN-229 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 34968902]
LNCaP	ED₅₀	0.6 μg/mL Compound: 3	Cytotoxicity against human LNCAP cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human LNCAP cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]
LNCaP	IC₅₀	1.76 μM Compound: 1	Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition	[PMID: 31991334]
LNCaP	IC₅₀	2.5 μM Compound: celastrol	Antitumor activity against human LNCAP cells Antitumor activity against human LNCAP cells	[PMID: 20627556]
LP-1	IC₅₀	0.88 μM Compound: 1	Antiproliferative activity against human LP-1 cells assessed as cell growth inhibition Antiproliferative activity against human LP-1 cells assessed as cell growth inhibition	[PMID: 31991334]
Lu1	ED₅₀	1.3 μg/mL Compound: 3	Cytotoxicity against human Lu1 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human Lu1 cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]
MCF-10A	IC₅₀	5.45 μM Compound: Celastrol	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
MCF7	ED₅₀	0.21 μg/mL Compound: 6	Cytotoxicity against human MCF7 cells after 3 days by SRB assay Cytotoxicity against human MCF7 cells after 3 days by SRB assay	[PMID: 14640511]
MCF7	IC₅₀	0.153 μM Compound: 2	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTS/PMS assay	[PMID: 25756299]
MCF7	IC₅₀	1.06 μM Compound: CE	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31051401]
MCF7	IC₅₀	1.2 μM Compound: Celastrol	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
MCF7	IC₅₀	1.35 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28865279]
MCF7	IC₅₀	1.56 μM Compound: 1; CEL	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 30316059]
MCF7	IC₅₀	1.58 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition	[PMID: 31991334]
MCF7	IC₅₀	1.7 μM Compound: CEL	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 35536757]
MCF7	IC₅₀	2.04 μM Compound: CEL	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 31725288]
MCF7	IC₅₀	2.13 μM Compound: Celastrol	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
MCF7	IC₅₀	2.23 μM Compound: CEL	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35290844]
MCF7	IC₅₀	6.84 μM Compound: Celastrol	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 29486954]
MDA-MB-231	IC₅₀	0.67 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition	[PMID: 31991334]
MDA-MB-231	IC₅₀	0.9 μM Compound: Celastrol	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 34170694]
MDA-MB-231	IC₅₀	1.08 μM Compound: Celastrol	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
MDA-MB-231	IC₅₀	1.08 μM Compound: Celastrol	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
MDA-MB-231	IC₅₀	1.32 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 28688281]
MDA-MB-231	IC₅₀	1.32 μM Compound: 1	Antiproliferative activity against human MDA-MB-231cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231cells after 72 hrs by MTT assay	[PMID: 28865279]
MDA-MB-231	IC₅₀	1.98 μM Compound: CEL	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
MDA-MB-231	IC₅₀	4.86 μM Compound: Cel	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay	[PMID: 37499289]
MDA-MB-231	IC₅₀	4.88 μM Compound: Cel	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37499289]
Mesenchymal stem cells	IC₅₀	0.7 μM Compound: Celastrol	Cytotoxicity against human mesenchymal bone marrow stem cells measured after 48 hrs by MTT assay Cytotoxicity against human mesenchymal bone marrow stem cells measured after 48 hrs by MTT assay	[PMID: 34170694]
MG-63	IC₅₀	1.97 μM Compound: 1	Antiproliferative activity against human MG-63 cells assessed as cell growth inhibition Antiproliferative activity against human MG-63 cells assessed as cell growth inhibition	[PMID: 31991334]
MGC-803	IC₅₀	0.78 μM Compound: 1	Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA Inhibition of telomerase in human MGC803 cell extracts after 24 hrs by TRAP-PCR-ELISA	[PMID: 25812966]
MGC-803	IC₅₀	1.55 μM Compound: 1	Anticancer activity against human MGC803 cells assessed as cell survival after 48 hrs by MTT assay Anticancer activity against human MGC803 cells assessed as cell survival after 48 hrs by MTT assay	[PMID: 25812966]
MIA PaCa-2	IC₅₀	0.46 μM Compound: 1	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay	[PMID: 28688281]
MIA PaCa-2	IC₅₀	0.46 μM Compound: 1	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay	[PMID: 28865279]
MKN-28	IC₅₀	2.3 μM Compound: 1	Antiproliferative activity against human MKN-28 cells assessed as cell growth inhibition Antiproliferative activity against human MKN-28 cells assessed as cell growth inhibition	[PMID: 31991334]
MKN-45	IC₅₀	3.4 μM Compound: 1	Antiproliferative activity against human MKN-45 cells assessed as cell growth inhibition Antiproliferative activity against human MKN-45 cells assessed as cell growth inhibition	[PMID: 31991334]
MM1.S	IC₅₀	0.63 μM Compound: 1	Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition	[PMID: 31991334]
MRC5	IC₅₀	4.4 μM Compound: CEL	Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay Cytotoxicity against human MRC5 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay	[PMID: 35255689]
NCI-H1299	IC₅₀	<1 μM Compound: CE11	Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability Cytotoxicity in human NCI-H1299 cells assessed as reduction in cell viability	[PMID: 28754470]
NCI-H1299	IC₅₀	1.49 μM Compound: 1	Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H1299 cells assessed as cell growth inhibition	[PMID: 31991334]
NCI-H1650	IC₅₀	0.79 μM Compound: 1	Antiproliferative activity against human NCI-H1650 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H1650 cells assessed as cell growth inhibition	[PMID: 31991334]
NCI-H1975	IC₅₀	0.6 μM Compound: 1	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as cell growth inhibition Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as cell growth inhibition	[PMID: 31991334]
NCI-H1975	IC₅₀	1.66 μM Compound: 1	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition	[PMID: 31991334]
NCI-H1975	IC₅₀	5.61 μM Compound: Cel	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay	[PMID: 37499289]
NCI-H1975	IC₅₀	6.05 μM Compound: Cel	Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37499289]
NCI-H2228	IC₅₀	1.95 μM Compound: 1	Antiproliferative activity against human NCI-H2228 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H2228 cells assessed as cell growth inhibition	[PMID: 31991334]
NCI-H460	IC₅₀	12.3 μM Compound: Celastrol	Cytotoxicity against human NCI-H460 cells after overnight incubation by MTT assay Cytotoxicity against human NCI-H460 cells after overnight incubation by MTT assay	[PMID: 21942765]
NCI-H460	IC₅₀	2.2 μM Compound: 1	Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition	[PMID: 31991334]
NCI-H929	IC₅₀	0.31 μM Compound: 1	Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition Antiproliferative activity against human NCI-H929 cells assessed as cell growth inhibition	[PMID: 31991334]
NSCLC	IC₅₀	1.48 μM Compound: 1	Antiproliferative activity against human NSCLC cells assessed as cell growth inhibition Antiproliferative activity against human NSCLC cells assessed as cell growth inhibition	[PMID: 31991334]
OVCAR-3	IC₅₀	1.93 μM Compound: Celastrol	Antiproliferative activity against human OVCAR3 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human OVCAR3 cells incubated for 48 hrs by MTT assay	[PMID: 31279299]
P388	ED₅₀	3.5 μg/mL Compound: 3	Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay Cytotoxicity against mouse P388 cells after 48 hrs by sulforhodamine B assay	[PMID: 8158155]
PANC-1	IC₅₀	2.48 μM Compound: Celastrol	Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 27647369]
PANC-1	IC₅₀	3 μM Compound: 44	Antiproliferative activity against human PANC1 cells after 24 hrs by MTS assay Antiproliferative activity against human PANC1 cells after 24 hrs by MTS assay	[PMID: 31663736]
PC-12	IC₅₀	3.15 μM Compound: celastrol	Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability Cytoprotective activity against t-BPH-induced cell damage in rat PC12 cells assessed as cell viability	[PMID: 20627556]
PC-3	ED₅₀	0.27 μg/mL Compound: 6	Cytotoxicity against human PC3 cells after 3 days by SRB assay Cytotoxicity against human PC3 cells after 3 days by SRB assay	[PMID: 14640511]
PC-3	IC₅₀	1.52 μM Compound: 1	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition	[PMID: 31991334]
PC-3	IC₅₀	1.68 μM Compound: CEL	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 96 hrs by MTT assay	[PMID: 35290844]
QGY-7703	IC₅₀	2.43 μM Compound: PC1	Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human QGY-7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
RAW264.7	IC₅₀	>50 μM Compound: 5	Cytotoxicity against mouse RAW264.7 cells after 18 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells after 18 hrs by MTT assay	[PMID: 22705020]
RAW264.7	IC₅₀	0.2 μM Compound: 5	Inhibition of LPS-stimulated NFkappaB activation transfected in mouse RAW264.7 cells after 18 hrs by luciferase reporter gene assay Inhibition of LPS-stimulated NFkappaB activation transfected in mouse RAW264.7 cells after 18 hrs by luciferase reporter gene assay	[PMID: 22705020]
RAW264.7	IC₅₀	0.23 μM Compound: 7	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production treated 3 hrs before LPS challenge assessed after 24 hrs by Griess reagent assay Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production treated 3 hrs before LPS challenge assessed after 24 hrs by Griess reagent assay	[PMID: 11809076]
RAW264.7	IC₅₀	0.27 μM Compound: 7	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NF-kappaB activation treated 3 hrs before LPS challenge assessed after 24 hrs by SEAP reporter gene assay Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NF-kappaB activation treated 3 hrs before LPS challenge assessed after 24 hrs by SEAP reporter gene assay	[PMID: 11809076]
RAW264.7	IC₅₀	0.3 μM Compound: Celastrol	Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells by SEAP reporter gene assay Inhibition of LPS-induced NF-kappaB activation in mouse RAW264.7 cells by SEAP reporter gene assay	[PMID: 18841906]
RAW264.7	IC₅₀	0.8 μM Compound: Celastrol	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 24 hrs by ELISA	[PMID: 23234407]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess reagent method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess reagent method	[PMID: 21978676]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by griess assay	[PMID: 22024033]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method	[PMID: 23127886]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide generation incubated for 24 hrs	[PMID: 23234407]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by Griess reaction based method Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by Griess reaction based method	[PMID: 25637363]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method	[PMID: 29730029]
RAW264.7	IC₅₀	1 μM Compound: Celastrol	Antiinflammatory activity in mouse RAW264.7 cells assessed as suppression of LPS-induced iNOS expression preincubated with compound for 1 hrs followed by LPS-stimulation and measured after 24 hrs by Western blot analysis Antiinflammatory activity in mouse RAW264.7 cells assessed as suppression of LPS-induced iNOS expression preincubated with compound for 1 hrs followed by LPS-stimulation and measured after 24 hrs by Western blot analysis	[PMID: 37683361]
RCC4	IC₅₀	1.88 μM Compound: 1	Antiproliferative activity against human RCC4 cells assessed as cell growth inhibition Antiproliferative activity against human RCC4 cells assessed as cell growth inhibition	[PMID: 31991334]
RPMI-8226	IC₅₀	0.52 μM Compound: 1	Antiproliferative activity against doxorubicin resistant human RPMI-8226 cells assessed as cell growth inhibition Antiproliferative activity against doxorubicin resistant human RPMI-8226 cells assessed as cell growth inhibition	[PMID: 31991334]
RPMI-8226	IC₅₀	0.52 μM Compound: 1	Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition Antiproliferative activity against human RPMI-8226 cells assessed as cell growth inhibition	[PMID: 31991334]
RPMI-8226	IC₅₀	0.73 μM Compound: 1	Antiproliferative activity against bortezomib resistant human RPMI-8226 cells assessed as cell growth inhibition Antiproliferative activity against bortezomib resistant human RPMI-8226 cells assessed as cell growth inhibition	[PMID: 31991334]
RPMI-8226	IC₅₀	3 μM Compound: 4	Growth inhibition of human RPMI8226 cells Growth inhibition of human RPMI8226 cells	[PMID: 18164197]
SAOS-2	IC₅₀	1.05 μM Compound: 1	Antiproliferative activity against human SAOS-2 cells assessed as cell growth inhibition Antiproliferative activity against human SAOS-2 cells assessed as cell growth inhibition	[PMID: 31991334]
SCC-38	IC₅₀	1.7 μM Compound: 1	Antiproliferative activity against human SCC-38 cells assessed as cell growth inhibition Antiproliferative activity against human SCC-38 cells assessed as cell growth inhibition	[PMID: 31991334]
SCC-4	IC₅₀	2.8 μM Compound: 1	Antiproliferative activity against human SCC-4 cells assessed as cell growth inhibition Antiproliferative activity against human SCC-4 cells assessed as cell growth inhibition	[PMID: 31991334]
SGC-7901	IC₅₀	0.15 μM Compound: 1	Anticancer activity against human SGC7901 cells assessed as cell survival after 48 hrs by MTT assay Anticancer activity against human SGC7901 cells assessed as cell survival after 48 hrs by MTT assay	[PMID: 25812966]
SGC-7901	IC₅₀	0.87 μM Compound: Celastrol	Cytotoxic activity against human SGC7901 cells incubated for 48 hrs by MTT assay Cytotoxic activity against human SGC7901 cells incubated for 48 hrs by MTT assay	[PMID: 28587825]
SH-SY5Y	EC₅₀	37.64 nM Compound: Celastrol	Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release Neuroprotection against beta-amyloid peptide 1-42-induced toxicity in human SH-SY5Y cells assessed as lactate dehydrogenase release	[PMID: 19138859]
SK-BR-3	IC₅₀	0.72 μM Compound: 1	Antiproliferative activity against human SKBR3 cells after 72 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 72 hrs by MTT assay	[PMID: 28688281]
SK-HEP1	IC₅₀	10 μM Compound: Cel	Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 37499289]
SK-HEP1	IC₅₀	9.67 μM Compound: Cel	Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay Antiproliferative activity against human SK-HEP1 cells assessed as inhibition of cell growth incubated for 48 hrs in presence of ligustrazine by MTT assay	[PMID: 37499289]
SK-MEL-2	ED₅₀	0.6 μg/mL Compound: 3	Cytotoxicity against human SK-MEL-2 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human SK-MEL-2 cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]
SK-MEL-28	IC₅₀	1.72 μM Compound: 1	Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition Antiproliferative activity against human SK-MEL-28 cells assessed as cell growth inhibition	[PMID: 31991334]
SK-N-SH	CC₅₀	1.6 μM Compound: Celastrol	Cytotoxicity against human SK-N-SH cells after 72 hrs by MTS assay Cytotoxicity against human SK-N-SH cells after 72 hrs by MTS assay	[PMID: 19502057]
SK-OV-3	IC₅₀	1.16 μM Compound: 1	Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 28688281]
SK-OV-3	IC₅₀	1.16 μM Compound: 1	Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay Antiproliferative activity against human SKOV3 cells after 72 hrs by MTT assay	[PMID: 28865279]
SK-OV-3	IC₅₀	1.68 μM Compound: Celastrol	Antiproliferative activity against human SKOV3 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human SKOV3 cells incubated for 48 hrs by MTT assay	[PMID: 31279299]
SK-OV-3	IC₅₀	2.29 μM Compound: 1	Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition Antiproliferative activity against human SK-OV-3 cells assessed as cell growth inhibition	[PMID: 31991334]
SMMC-7721	IC₅₀	0.58 μM Compound: 1	Anticancer activity against human SMMC7721 cells assessed as cell survival after 48 hrs by MTT assay Anticancer activity against human SMMC7721 cells assessed as cell survival after 48 hrs by MTT assay	[PMID: 25812966]
SMMC-7721	IC₅₀	1.07 μM Compound: PC1	Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 32717483]
SMMC-7721	IC₅₀	6.04 μM Compound: Celastrol	Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 36274272]
SW13	IC₅₀	0.1 μM Compound: 1	Antiproliferative activity against human SW13 cells assessed as cell growth inhibition Antiproliferative activity against human SW13 cells assessed as cell growth inhibition	[PMID: 31991334]
SW-620	IC₅₀	0.29 μM Compound: 23	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth	[PMID: 38142509]
SW-620	IC₅₀	0.67 μM Compound: 1	Inhibition of cell viability in human SW620 cells incubated for 72 hrs by Cell Titer Glo assay Inhibition of cell viability in human SW620 cells incubated for 72 hrs by Cell Titer Glo assay	[PMID: 38679872]
T cell line	CC₅₀	0.1 μM Compound: Celastrol	Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32822186]
T cell line	IC₅₀	83 nM Compound: Celastrol	Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay	[PMID: 32822186]
T47D	IC₅₀	>20 μM Compound: Celastrol	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
T-ALL	IC₅₀	<1 μM Compound: CE11	Cytotoxicity in human T-ALL cells assessed as reduction in cell viability Cytotoxicity in human T-ALL cells assessed as reduction in cell viability	[PMID: 28754470]
THP-1	EC₅₀	15 μM Compound: Celastrol	Induction of apoptosis in TRAIL-resistant human THP1 cells after 24 hrs by annexin-V staining Induction of apoptosis in TRAIL-resistant human THP1 cells after 24 hrs by annexin-V staining	[PMID: 20864342]
U-251	IC₅₀	0.69 μM Compound: 1	Antiproliferative activity against human U-251MG cells assessed as cell growth inhibition Antiproliferative activity against human U-251MG cells assessed as cell growth inhibition	[PMID: 31991334]
U-251	IC₅₀	4.43 μM Compound: CEL	Antiproliferative activity against human U-251 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Antiproliferative activity against human U-251 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 34968902]
U-266	IC₅₀	0.47 μM Compound: 1	Antiproliferative activity against human U-266 cells assessed as cell growth inhibition Antiproliferative activity against human U-266 cells assessed as cell growth inhibition	[PMID: 31991334]
U2OS	IC₅₀	1.86 μM Compound: CEL	Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human U2OS cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35238566]
U2OS	IC₅₀	2.11 μM Compound: 1	Antiproliferative activity against human U2OS cells assessed as cell growth inhibition Antiproliferative activity against human U2OS cells assessed as cell growth inhibition	[PMID: 31991334]
U-373MG ATCC	ED₅₀	0.4 μg/mL Compound: 3	Cytotoxicity against human U373 cells after 96 hrs by sulforhodamine B assay Cytotoxicity against human U373 cells after 96 hrs by sulforhodamine B assay	[PMID: 8158155]
U-373MG ATCC	IC₅₀	2 μM Compound: 1	Antiproliferative activity against human U373 MG cells assessed as cell growth inhibition Antiproliferative activity against human U373 MG cells assessed as cell growth inhibition	[PMID: 31991334]
U-87MG ATCC	ED₅₀	0.22 μg/mL Compound: 6	Cytotoxicity against human U87MG cells after 3 days by SRB assay Cytotoxicity against human U87MG cells after 3 days by SRB assay	[PMID: 14640511]
U-87MG ATCC	IC₅₀	2.23 μM Compound: CEL	Antiproliferative activity against human U87 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay Antiproliferative activity against human U87 cells assessed as reduction in cell viability incubated for 96 hrs by MTT assay	[PMID: 34968902]
U-937	IC₅₀	2 μM Compound: 1	Antiproliferative activity against human U-937 cells assessed as cell growth inhibition Antiproliferative activity against human U-937 cells assessed as cell growth inhibition	[PMID: 31991334]
UMSCC1	IC₅₀	0.76 μM Compound: 1	Antiproliferative activity against human UMSCC1 cells assessed as cell growth inhibition Antiproliferative activity against human UMSCC1 cells assessed as cell growth inhibition	[PMID: 31991334]
ZR-75-1	ED₅₀	0.3 μg/mL Compound: 3	Cytotoxicity against human ZR-75-1 cells after 72 hrs by sulforhodamine B assay Cytotoxicity against human ZR-75-1 cells after 72 hrs by sulforhodamine B assay	[PMID: 8158155]

In Vitro

Celastrol (Tripterine;Tripterin) significantly inhibits the proteasomal chymotrypsin activity in PC-3 cells in a concentration-dependent manner; at 2.5 μM it reaches ~55% inhibition, comparable to its potency to a purified 20S proteasome (IC₅₀=2.5 μM). Furthermore, increased levels of IκB-α, Bax, and p27 are observed, three well known target proteins of the proteasome in PC-3 cells treated with Celastrol^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Treatment of PC-3 tumor-bearing nude mice with Celastrol (1-3 mg/kg/d, i.p., 1-31 days) results in significant inhibition (65-93%) of the tumor growth^[1]. Following treatment with 3 and 6 mg/kg Celastrol, the levels of malondialdehyde (MDA) are significantly decreased by 35.2 and 36.7% (P<0.05), respectively. Treatment with 3 and 6 mg/kg Celastrol markedly restores the GSH level (P<0.05) to almost normal levels^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 34157-83-0
Appearance Solid
Molecular Weight 450.61
Formula C₂₉H₃₈O₄
Color Orange to red
SMILES

OC1=C(C2=CC=C3[C@](C)([C@]4(CC[C@]3(C2=CC1=O)C)C)CC[C@@]5(C)CC[C@@](C(O)=O)(C[C@]54[H])C)C
Synonyms

Tripterine; Tripterin
Structure Classification
- Terpenoids
- Triterpenes
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (61)

All WB

Sort by:

Journal Impact Factor

Signal Transduct Target Ther

Selective depletion of tumor-associated SAMHD1 enhances chemotherapeutic efficacy and antitumor immune responses. [Abstract]

2025 Dec 15;10(1):406. PMID: 41392286
J Adv Res

In silico transcriptome-based drug screening identifies celastrol as a multi-species therapeutic agent against aging-related sarcopenia and mitochondrial dysfunction. [Abstract]

2026 Feb 3:S2090-1232(26)00107-4. PMID: 41644092
J Nanobiotechnology

Injectable celastrol-loading emulsion hydrogel for immunotherapy of low-immunogenic cancer. [Abstract]

2025 Mar 6;23(1):183. PMID: 40050985
J Nanobiotechnology

Peptide-anchored neutrophil membrane-coated biomimetic nanodrug for targeted treatment of rheumatoid arthritis. [Abstract]

2023 Jan 13;21(1):13. PMID: 36639772
Hum Reprod Open

Hypoxia exposure impairs male fertility via inhibiting Septin2-mediated spermatogonial proliferation. [Abstract]

2025 May 14;2025(3):hoaf027. PMID: 40487848
Cell Death Dis

Celastrol alleviates renal fibrosis by upregulating cannabinoid receptor 2 expression. [Abstract]

2018 May 22;9(6):601. PMID: 29789558

Celastrol purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):601. [Abstract]

Serum-starved HK-2 cells are pretreated with or without indicated concentrations of Celastrol (CEL) for 1 h and then stimulated with TGF-β1 (10 ng/mL) for 24 h. Representative western blots and quantification data of CB2R expression in HK-2 cells are presented.
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Phytomedicine

Celastrol induces DNA damage and cell death in BCR-ABL T315I-mutant CML by targeting YY1 and HMCES. [Abstract]

2024 Nov:134:155937. PMID: 39255723
Phytomedicine

Celastrol upregulated ATG7 triggers autophagy via targeting Nur77 in colorectal cancer. [Abstract]

2022 Sep:104:154280. PMID: 35752079
NPJ Sci Food

Bone-targeted celastrol nanocarrier suppresses osteoclastogenesis in postmenopausal osteoporosis. [Abstract]

2025 Oct 31;9(1):215. PMID: 41173888
Br J Pharmacol

SGK3 promotes estrogen receptor-positive breast cancer proliferation by activating STAT3/ZMIZ2 pathway to stabilise β-catenin. [Abstract]

2025 Apr;182(8):1856-1875. PMID: 39876548
NPJ Breast Cancer

SIMD: Synergistic integration mutualistic platform based on single-cell and proteotranscriptomics for drug repositioning. [Abstract]

2025 Dec 24;12(1):4. PMID: 41444222
Biomed Pharmacother

Targeting ER stress in adrenocortical carcinoma: Celastrol as a novel therapeutic candidate. [Abstract]

2026 Feb 25:197:119156. PMID: 41747473
Biomed Pharmacother

Celastrol inhibits LL37-induced rosacea by inhibiting Ca2+/CaMKII-mTOR-NF-κB activation. [Abstract]

2022 Sep:153:113292. PMID: 35717785
Mol Med

Celastrol improves endothelial function in diet-induced obesity mice via attenuating endoplasmic reticulum stress through the activation of AMPK pathway. [Abstract]

2025 Jun 11;31(1):233. PMID: 40500724
Phytother Res

Celastrol Ameliorates Hypoxia-Induced Pulmonary Hypertension by Regulation of the PDE5-cGMP-PKG Signaling Pathway. [Abstract]

2025 Mar;39(3):1549-1564. PMID: 39887769
Cell Mol Life Sci

NR4A1 deficiency promotes carotid plaque vulnerability by activating integrated stress response via targeting Bcat1. [Abstract]

2025 Feb 22;82(1):91. PMID: 39985585
J Agric Food Chem

Chemoproteomic Profiling of Cobalamin-Independent Methionine Synthases in Plants with a Covalent Probe. [Abstract]

2020 Jul 29;68(30):8050-8056. PMID: 32618189
Cancer Cell Int

Celastrol attenuates the invasion and migration and augments the anticancer effects of olaparib in prostate cancer. [Abstract]

2024 Oct 26;24(1):352. PMID: 39462410
Cell Biol Toxicol

Celastrol modulates IRS1 expression to alleviate ovarian aging and to enhance follicular development. [Abstract]

2025 Sep 2;41(1):129. PMID: 40897829
Front Immunol

Candidate Drugs Screening for Behcet's Disease Based on Bioinformatics Analysis and Mouse Experiments. [Abstract]

2022 Jun 21;13:895869. PMID: 35799784
Am J Chin Med

Celastrol Alleviates Intestinal Epithelial Permeability by Inhibiting Ferroptosis through PI3K/Akt/FOXO1/HO-1 Signaling Pathway. [Abstract]

2025;53(4):1207-1224. PMID: 40582719
J Am Heart Assoc

Nuclear Receptor Nur77 Protects Against Abdominal Aortic Aneurysm by Ameliorating Inflammation Via Suppressing LOX-1. [Abstract]

2021 Aug 3;10(15):e021707. PMID: 34325521
Life Sci

Celastrol attenuates incision-induced inflammation and pain associated with inhibition of the NF-κB signalling pathway via SARM. [Abstract]

2018 Jul 15:205:136-144. PMID: 29750991

Celastrol purchased from MedChemExpress. Usage Cited in: Life Sci. 2018 Jul 15:205:136-144. [Abstract]

Effects of Celastrol (CEL) on the expression of F4/80 in plantar skin. CEL treatment suppresses macrophage expression in plantar skin. Western blot assay shows significantly downregulated F4/80 levels in 10 and 20 μg/paw CEL groups.
J Drug Deliv Sci Technol

2025 Jun 7.
Front Pharmacol

Celastrol Alleviates Autoimmune Hepatitis Through the PI3K/AKT Signaling Pathway Based on Network Pharmacology and Experiments. [Abstract]

2022 Mar 10;13:816350. PMID: 35359864
ACS Appl Bio Mater

Celastrol-Loaded Zwitterionic Nanogels Trigger Pyroptosis for Potent Antitumor Effects. [Abstract]

2025 Dec 29. PMID: 41460983
Bioorg Chem

Revealing a new target: Celastrol alleviates pulmonary fibrosis by inhibiting PCAF. [Abstract]

2025 Aug:163:108722. PMID: 40616946
Int Immunopharmacol

Breaking CHIPS-Mediated immune evasion with tripterin to promote neutrophil chemotaxis against MRSA infection. [Abstract]

2024 Mar 10:129:111597. PMID: 38295543
J Mol Cell Cardiol

Nuclear receptor Nur77 protects against oxidative stress by maintaining mitochondrial homeostasis via regulating mitochondrial fission and mitophagy in smooth muscle cell. [Abstract]

2022 Sep:170:22-33. PMID: 35661620
RSC Adv

2016,6, 42537-42544.

Celastrol purchased from MedChemExpress. Usage Cited in: RSC Adv. 2016,6, 42537-42544.

Celastrol is able to increase HSP70 protein expression by more than 1.8-fold in PC-3 cells after 24 h of incubation.
Cancers (Basel)

PKCθ Regulates Pituitary Adenoma Bone Invasion by Activating Osteoclast in NF-κB/IL-1β-Dependent Manner. [Abstract]

2023 Mar 6;15(5):1624. PMID: 36900414
Exp Neurol

Neuroprotection of celastrol against postoperative cognitive dysfunction through dampening cGAS-STING signaling. [Abstract]

2024 Dec:382:114987. PMID: 39369806
J Mol Med (Berl)

Celastrol-loaded biomimetic nanodrug ameliorates APAP-induced liver injury through modulating macrophage polarization. [Abstract]

2023 Jun;101(6):699-716. PMID: 37129620
BMC Microbiol

Celastrol mitigates staphyloxanthin biosynthesis and biofilm formation in Staphylococcus aureus via targeting key regulators of virulence; in vitro and in vivo approach. [Abstract]

2022 Apr 15;22(1):106. PMID: 35421933
J Inflamm Res

Celastrol Mitigates Acute Pancreatitis Associated Inflammation by Modulating the IL-34/CSF-1R Axis and Suppressing NF-κB/ERK Signaling. [Abstract]

2026 Mar 12:19:572609. PMID: 41847424
Sci Rep

Celastrol inhibits ezrin-mediated migration of hepatocellular carcinoma cells. [Abstract]

2020 Jul 9;10(1):11273. PMID: 32647287
AMB Express

Celastrol boosts fluconazole efficacy against vaginal candidiasis: in vitro and in vivo evidence. [Abstract]

2025 Jan 29;15(1):18. PMID: 39881021
Metab Brain Dis

Celastrol assuages oxygen-glucose deprivation and reoxygenation-induced damage in human brain microvascular endothelial cells through the circDLGAP4/miR-6085/GDF11 pathway. [Abstract]

2023 Jan;38(1):255-267. PMID: 36445630
Med Oncol

Celastrol inhibits the migration and invasion and enhances the anti-cancer effects of docetaxel in human triple-negative breast cancer cells. [Abstract]

2022 Sep 7;39(12):189. PMID: 36071249
BMC Cancer

Impact of celastrol on mitochondrial dynamics and proliferation in glioblastoma. [Abstract]

2025 Mar 6;25(1):412. PMID: 40050778
BMC Complement Med Ther

Celastrol slows the progression of early diabetic nephropathy in rats via the PI3K/AKT pathway. [Abstract]

2020 Oct 23;20(1):321. PMID: 33097050
Curr Top Med Chem

An Exosome-Liposome Hybrid Platform for Celastrol Delivery Enhances Anti-Tumor Efficacy in Hepatocellular Carcinoma. [Abstract]

2026 Mar 5. PMID: 41820787
Discov Oncol

Celastrol inhibits mouse B16-F10 melanoma cell survival by regulating the PI3K/AKT/mTOR signaling pathway and repressing HIF-1α expression. [Abstract]

2024 May 21;15(1):178. PMID: 38771435
Discov Oncol

Celastrol suppresses human pancreatic cancer via m6A-YTHDF3-mediated downregulation of Claspin and Bcl-2. [Abstract]

2023 Dec 18;14(1):233. PMID: 38110764
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
Vet Microbiol

Identification and evaluation of Nordihydroguaiaretic acid (NDGA) as an active traditional Chinese medicine compound inhibiting the 3C-like protease of feline infectious peritonitis virus. [Abstract]

2025 Sep 15:310:110730. PMID: 40976146
Fitoterapia

Natural bioactive compounds and FOXO3a in cancer therapeutics: An update. [Abstract]

2024 Mar:173:105807. PMID: 38168566
J Nat Med

Celastrol attenuates chronic constrictive injury-induced neuropathic pain and inhibits the TLR4/NF-κB signaling pathway in the spinal cord. [Abstract]

2022 Jan;76(1):268-275. PMID: 34510370
Biochem Biophys Res Commun

mTORC2/Akt axis promotes proteotoxic stress and mitochondrial Ca2+ overload during celastrol-induced paraptosis. [Abstract]

2025 Aug 11:781:152474. PMID: 40834605
Biochem Biophys Res Commun

Celastrol inhibits platelet function and thrombus formation. [Abstract]

2024 Jan 22:693:149366. PMID: 38091842
Thyroid Res

Celastrol promotes apoptotic cell death in thyroid cancer cells through a caspases-dependent pathway. [Abstract]

2025 Feb 26;18(1):9. PMID: 40001245
Neuroreport

Celastrol exerts a neuroprotective effect by inhibiting necroptosis and inflammation in intracerebral hemorrhage-induced brain injury. [Abstract]

2026 Feb 4;37(2):45-52. PMID: 41460030
Curr Med Sci

Celastrol Induces Apoptosis and Autophagy via the AKT/mTOR Signaling Pathway in the Pituitary ACTH-secreting Adenoma Cells. [Abstract]

2022 Apr;42(2):387-396. PMID: 35419676
bioRxiv

2024 October 27.
bioRxiv

2024 Jul 25.
J Tradit Chinese Medical Sci

2024 Jun 5.
The Hong Kong Polytechnic University

2023 Aug.
Ann Transl Med

Regulating mitochondrial homeostasis and inhibiting inflammatory responses through Celastrol. [Abstract]

2022 Apr;10(7):400. PMID: 35530963
SSRN

27 Jan 2022.
Mol Biosyst

Competitive profiling of celastrol targets in human cervical cancer HeLa cells via quantitative chemical proteomics. [Abstract]

2016 Dec 20;13(1):83-91. PMID: 27819370

Celastrol purchased from MedChemExpress. Usage Cited in: Mol Biosyst. 2016 Dec 20;13(1):83-91. [Abstract]

Validation of selected targets of Celastrol identified by competitive proteomics. Western blotting (by using anti-GSTO1 and anti-PDI antibodies) of the pull-down samples upon labeling with IA-yne.

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (73.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2192 mL

11.0961 mL

22.1921 mL

5 mM

0.4438 mL

2.2192 mL

4.4384 mL

10 mM

0.2219 mL

1.1096 mL

2.2192 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Kinase Assay^[1]

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 or Oridonin at different concentrations or in the solvent DMSO for 2 hours at 37°C, followed by measurement of inhibition of each proteasomal activity^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

Prostate cancer cells (5,000-8,000) are plated in each well of a 96-well plate and then treated with either DMSO, Celastrol, or Oridonin at different concentrations for 12 to 16 hours, followed by an additional 2-hour incubation with Z-Gly-Gly-Leu-AMC (at 40 μM). After that, the proteasome activity is measured using the whole plate^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]^[2]

Mice^[1]
Male nude immunodeficient mice NCRNU-M, aged 5 weeks, are used. On day 0, human prostate cancer PC-3 or C4-2B cells (5-10×10⁶) suspended in 0.1 mL of serum-free RPMI 1640 are inoculated s.c. in the right flank of each mouse (four mice per group). For the first experiment using PC-3 cells, on day 14 after inoculation, the animals started daily i.p. injection with either 50 to 100 μL of a vehicle [10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS], and 1.0 or 3.0 mg/kg of Celastrol. Tumor sizes are measured daily using calipers and their volumes are calculated using a standard formula: width²×length/2. Body weight is measured weekly. To study whether the proteasome is inhibited in an early phase of the experiment, after 3 days of treatment, one control and one 3.0 mg/kg Celastrol -treated mouse is sacrificed. The rest are sacrificed after 16 days of treatment when control tumors reach 1,400 mm³. For the second PC-3 tumor experiment, 12 days after inoculation, mice are randomly divided into three groups and treated with either control, Celastrol, or Oridonin at 1.5 mg/kg daily for the duration of the study (31 days). In another experiment, to study the effects of Celastrol on AR expression, nude mice bearing C4-2B tumors receive daily i.p. injection of the vehicle or 3.0 mg/kg Celastrol.
Rats^[2]
Male Sprague-Dawley (SD) rats (n=90, 6 weeks old), weighing 161±9 g, are randomly divided into the control (NC) and the high energy diet (HED) groups. In the control group, the animals receive a standard chow diet, while the rats in the HED group are fed with an additional high energy emulsion. After 8 weeks on their respective diets, Streptozotocin (STZ; 45 mg/kg) dissolved in 0.1 mol/l citrate buffer (pH 4.5) is injected into the caudal vein of the rats in the HED group to establish a model of T2DM, while the rats in the control group are injected with sodium citrate buffer. The rats with blood glucose levels ≥16.7 mM at 7 days after the STZ injection are selected as the model of diabetes. On average, 80% of the rats injected with STZ met these criteria. At 1 week following the injection of STZ, the rats with successfully-induced diabetes are randomly divided into the diabetes model (DM) group, the Celastrol low-dose group (1 mg/kg/day), the Celastrol middle-dose group (3 mg/kg/day) and the Celastrol high-dose group (6 mg/kg/day) (n=15 rats per group). The rats in the treatment groups are administered Celastrol by gavage, whereas the rats in the NC and DM groups are administered an equal amount of distilled water (2 mL). Following 8 weeks of the respective treatments, rats are anesthetized with an intraperitoneal injection of sodium pentobarbital (30 mg/kg body weight) and tissue samples are collected for analysis. The paravertebral muscle is excised from the rat bodies, and is cut perpendicularly along the longitudinal axis and fixed in phosphate-buffered 20% formaldehyde. Histological paraffin-embedded sections (5 μm) are then prepared for H&E staining. The sections of paravertebral muscle are snap-frozen in liquid nitrogen and stored at ?80°C until further analysis.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yang H, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res. 2006 May 1;66(9):4758-65 [Content Brief]

[2]. Guan Y, et al. 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. [Content Brief]

[3]. Yuan Z, et al. Celastrol Combats Methicillin‐Resistant Staphylococcus aureus by Targeting Δ1‐Pyrroline‐5‐Carboxylate Dehydrogenase[J]. Advanced Science, 2023, 10(25): 2302459. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2192 mL	11.0961 mL	22.1921 mL	55.4804 mL
	5 mM	0.4438 mL	2.2192 mL	4.4384 mL	11.0961 mL
	10 mM	0.2219 mL	1.1096 mL	2.2192 mL	5.5480 mL
	15 mM	0.1479 mL	0.7397 mL	1.4795 mL	3.6987 mL
	20 mM	0.1110 mL	0.5548 mL	1.1096 mL	2.7740 mL
	25 mM	0.0888 mL	0.4438 mL	0.8877 mL	2.2192 mL
	30 mM	0.0740 mL	0.3699 mL	0.7397 mL	1.8493 mL
	40 mM	0.0555 mL	0.2774 mL	0.5548 mL	1.3870 mL
	50 mM	0.0444 mL	0.2219 mL	0.4438 mL	1.1096 mL
	60 mM	0.0370 mL	0.1849 mL	0.3699 mL	0.9247 mL

Keywords

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Celastrol

MCE Bioactive Compound Library

Natural Product Library Plus

Publications Citing Use of MedChemExpress (MCE) Celastrol

All Endogenous Metabolite Isoforms

All Antibiotic Isoforms

All Nuclear Hormone Receptor 4A/NR4A Isoforms

Biological Activity

Chemical Information

Publications (61)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Celastrol

MCE Bioactive Compound Library

Natural Product Library Plus

Publications Citing Use of MedChemExpress (MCE) Celastrol

All Endogenous Metabolite Isoforms

All Antibiotic Isoforms

All Nuclear Hormone Receptor 4A/NR4A Isoforms

Biological Activity

Chemical Information

Publications (61)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Celastrol Related Classifications

Cat. No.: HY-13067