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Tripterin (Celastrol) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol down-regulated the basal and DNA damaging agents-induced monoubiquitination of FANCD2, followed by proteolytic degradation. Celastrol treatment abrogated the G2 checkpoint induced by IR,and enhanced the ICL agents-induced DNA damage and inhibitory effects on lung cancer cells through depletion of FANCD2.Celastrol presented striking growth inhibition and apoptosis induction potency on DU145 cells in vitro in a time- and dose-dependent manner.Celastrol exhibits its antiprostate cancer effects partially through the downregulation of the expression level of hERG channel in DU145 cells,suggesting that celastrol may be a potential agent against prostate cancer with a mechanism of blocking the hERG channel.Celastrol ameliorates experimental colitis in IL-10 deficient mice via the up-regulation of autophagy by suppressing the PI3K/Akt/mTOR signaling pathway.Celastrol has the potential to inhibit cytochrome P450 activities and may cause the herb-drug interactions.Celastrol induces apoptosis in TNBC cells and indicated that apoptosis might be mediated through mitochondrial dysfunction and PI3K/Akt signaling pathway.
ACS Appl Mater Interfaces. 2024 Sep 11;16(36):47270-47283.
Engineered Carrier-Free Nanosystem-Induced In Situ Therapeutic Vaccines for Potent Cancer Immunotherapy
Celastrol purchased from AbMole
Front Microbiol. 2023 Mar 2;14:1120048.
Specific TLR-mediated HSP70 activation plays a potential role in host defense against the intestinal parasite Giardia duodenalis
Celastrol purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | RPMI 8226, KATOIII, UM-SCC1, U251MG and MDA-MB-231 cells |
| Preparation method | Determining the anti-proliferative effect of celastrol on various human tumor cell lines by the MTT uptake method. Briefly, incubating 5×103 cells with Celastrol in triplicate in a 96-well plate at 37 ℃. Then adding MTT solution to each well. After a 2 hours incubation at 37 ℃, adding extraction buffer (20% SDS, 50% dimethylformamide) , incubating cells overnight at 37 ℃, and then measuring the optical density at 570 nm using a Tecan plate reader. |
| Concentrations | ~5 μM |
| Incubation time | 2 hours |
| Animal Experiment | |
|---|---|
| Animal models | nude mice bearing C4-2B tumors |
| Formulation | 10% DMSO, 70% Cremophor/ethanol (3:1), and 20% PBS |
| Dosages | 3 mg/kg |
| Administration | Intraperitoneal injection |
| Molecular Weight | 450.61 |
| Formula | C29H38O4 |
| CAS Number | 34157-83-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Proteasome Products |
|---|
| Proteasome inhibitor IX
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. |
| NIC-0102
NIC-0102 is an orally potent proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammasome activation.NIC-0102 showed potent anti-inflammatory effects in vivo in a DSS-induced ulcerative colitis model. In addition, NIC-0102 inhibited the production of pro-IL-1β. |
| Ac-WLA-AMC
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate. |
| Ac-Nle-Pro-Nle-Asp-AMC
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome. |
| PR-39
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. |
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