KT-333 diammonium
KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL).
For research use only. We do not sell to patients.
- CAS No.: 2502186-80-1
- Formula: C60H80ClN12O14PS
- Molecular Weight:1291.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
STAT3 |
In Vitro
KT-333 diammonium (11.8±2.3 nM, 48 h) degrades STAT3 resulted in irreversible growth inhibition of SU-DHL-1 cell line and induces caspase 3/7 activity in the SU-DHL-1 cell line[1].
KT-333 diammonium has a good degradation effect on STAT3 protein, and in cell phenotypic analysis, its GI50 value in multiple ALCL cell lines ranges from 8.1 to 57.4 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
KT-333 diammonium (10, 20 and 30 mg/kg, iv.; once a week for two weeks) exhibits dose-dependent antitumor activity. Female NOD SCID mice with xenograft tumors of SUP-M2 administered with 10 mg/kg achieved 83.8% tumor growth inhibition (TGI), while those administered 20 or 30 mg/kg experienced complete tumor regression, with these effects sustained until the end of the study[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2502186-80-1
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Molecular Weight 1291.84
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Formula C60H80ClN12O14PS
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SMILES
ClC(C(CCCC(N[C@@H](C(C)(C)C)C(N1[C@@H](C[C@H](C1)O)C(N[C@H](C2=CC=C(C3=C(N=CS3)C)C=C2)C)=O)=O)=O)=CC=C4)=C4OC[C@H](CCC(N)=O)NC([C@H]5N6[C@](CCN(C[C@@H](C6=O)NC(C7=CC8=CC(C(P(O)(O)=O)=O)=CC=C8N7)=O)C(C)=O)([H])CC5)=O.N.N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KT-333 diammonium Related Classifications
HY-156730B Related Classifications
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