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KT-333 ammonium (Compound A) acts as a molecular glue that targets and promotes the degradation of the STAT3 protein through the ubiquitin-proteasome system. This compound achieves selective degradation by binding simultaneously to the STAT3 protein and the E3 ubiquitin ligase von Hippel-Lindau protein (VHL). It exhibits strong selectivity and efficacy in degrading STAT3, possessing notable antitumor properties. KT-333 ammonium is particularly useful for research on hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) [1].
Pack Size | Price | Availability | Quantity |
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10 mg | Inquiry | Inquiry | |
50 mg | Inquiry | Inquiry |
Description | KT-333 ammonium (Compound A) acts as a molecular glue that targets and promotes the degradation of the STAT3 protein through the ubiquitin-proteasome system. This compound achieves selective degradation by binding simultaneously to the STAT3 protein and the E3 ubiquitin ligase von Hippel-Lindau protein (VHL). It exhibits strong selectivity and efficacy in degrading STAT3, possessing notable antitumor properties. KT-333 ammonium is particularly useful for research on hematologic malignancies, including large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) [1]. |
In vitro | KT-333 ammonium, at a concentration of (11.8±2.3 nM over 48 hours), causes irreversible growth inhibition and induces the activity of caspase 3/7, a marker of apoptosis, in the SU-DHL-1 cell line following STAT3 degradation [1]. Additionally, KT-333 ammonium demonstrates STAT3 protein degradation with GI50 values ranging from 8.1 to 57.4 nM across various ALCL cell lines in cell phenotype analysis [1]. |
In vivo | KT-333 ammonium exhibited dose-dependent antitumor activity when administered intravenously at doses of 5, 10, 15, and 45 mg/kg once weekly for two weeks. Mice receiving 5 mg/kg showed 79.9% tumor growth inhibition (TGI), while doses of 10, 15, or 45 mg/kg led to complete tumor regression, sustained until the study's conclusion [1]. Similarly, doses of 10, 20, and 30 mg/kg resulted in dose-dependent antitumor effects, with mice given 10 mg/kg achieving 83.8% TGI, and those receiving 20 or 30 mg/kg experiencing complete tumor regression, also persisting through to the end of the study [1]. |
Molecular Weight | 1274.81 |
Formula | C60H77ClN11O14PS |
Cas No. | 2839758-34-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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