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Formula | C22H26N4O3 |
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Molecular Weight | 394.47 | CAS No. | 1401223-22-0 | |
Solubility (25°C)* | In vitro | DMSO | 78 mg/mL (197.73 mM) | |
Ethanol | 33 mg/mL (83.65 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). | ||
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Targets |
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In vitro | PI-1840 potently inhibits proteasomal CT-L activity with IC50 of 0.37 μM in intact human MDA-MB-468 cancer cells, and inhibits proliferation/survival of human MDA-MB-468 cells. [1] In intact cancer cells, PI-1840 inhibits CT-L activity, induces the accumulation of proteasome substrates p27, Bax, and IκB-α, inhibits survival pathways and viability, and induces apoptosis. [2] | ||
In vivo | PI-1840 (150 mg/kg i.p.) inhibits the tumor growth in mice of MDA-MB-231 breast tumors. [2] |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[2] |
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Gasdermin E mediates resistance of pancreatic adenocarcinoma to enzymatic digestion through a YBX1-mucin pathway [ Nat Cell Biol, 2022, 24(3):364-372] | PubMed: 35292781 |
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] | PubMed: 33067904 |
Non‑covalent proteasome inhibitor PI‑1840 induces apoptosis and autophagy in osteosarcoma cells [Yuxi Chen, et al. Oncol Rep, 2019, 10.3892/or.2019.7040] | |
Non‑covalent proteasome inhibitor PI‑1840 induces apoptosis and autophagy in osteosarcoma cells. [ Oncol Rep, 2019, 41(5):2803-2817] | PubMed: 30864717 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.