KT-333 ammonium 

KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium 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 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium 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)^[1].

KT-333 ammonium (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 ammonium 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.

KT-333 ammonium (5, 10, 15 and 45 mg/kg, iv.; once a week for two weeks) exhibits dose-dependent antitumor activity. Female NOD SCID mice with xenograft tumors of SU-DHL-1 administered with 5 mg/kg achieved 79.9% tumor growth inhibition (TGI), while those administered 10, 15, or 45 mg/kg experienced complete tumor regression, with these effects sustained until the end of the study^[1].
KT-333 ammonium (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.

1274.81

C₆₀H₇₇ClN₁₁O₁₄PS

2839758-34-6

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ding X, et al. Antitumor effect of the novel sphingosine kinase 2 inhibitor ABC294640 is enhanced by inhibition of autophagy and by sorafenib in human cholangiocarcinoma cells. Oncotarget. 2016 Apr 12;7(15):20080-92.  [Content Brief]