1. JAK/STAT Signaling
    Stem Cell/Wnt
    Apoptosis
  2. STAT
    Apoptosis
  3. UC-514321

UC-514321 

Cat. No.: HY-120395
Handling Instructions

UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity.

For research use only. We do not sell to patients.

UC-514321 Chemical Structure

UC-514321 Chemical Structure

CAS No. : 299420-83-0

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Description

UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity[1].

IC50 & Target

STAT3

 

STAT5

 

In Vitro

UC-514321 increases apoptosis in AML cells not in normal HSPCs[1].
UC-514321 (0-500 nM, 48 h) inhibits AML cells viability TET1-signaling dependently[1].

Cell Viability Assay[1]

Cell Line: MONOMAC-6, THP-1, KOCL-48, KASUMI-1, ML-2, and NB4 cells.
Concentration: 0-500 nM.
Incubation Time: 48 hours.
Result: Most significantly repressed MONOMAC-6 cell viability.
Showed no inhibitory effect on the viability of TET1-low AML.

RT-PCR[1]

Cell Line: MONOMAC-6 cells.
Concentration: 0-500 nM.
Incubation Time: 48 hours.
Result: Functioned as TET1-transcription inhibitors in TET1-high AMLs and their anti-leukemic effects are TET1-dependent.
In Vivo

UC-514321 (2.5 mg/kg, ip, once per day, for 10 days) exhibits more potant anti-tumor activity than NSC370284 in AML mice models[1].

Animal Model: MLL-AF9-AML mice and AE9a-AML model[1].
Dosage: 2.5 mg/kg.
Administration: IP., once per day, for 10 days.
Result: Showed an improved therapeutic effect in AML mouse models in vivo.
Prolonged the median survival over three fold.
Molecular Weight

441.56

Formula

C₂₆H₃₅NO₅

CAS No.

299420-83-0

SMILES

OC1=C(C(C2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2)N3CCOCC3)C=C(OCO4)C4=C1

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

UC-514321UC514321UC 514321STATApoptosisacutemyeloidleukemiaAMLlowtoxicityInhibitorinhibitorinhibit

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