1. Immunology/Inflammation
  2. STING IFNAR Interleukin Related
  3. UM-242

UM-242 is a STING inhibitor, with an EC50 of 1.70 μM in THP1-Dual cells expressing wild-type STING. UM-242 blocks STING oligomerization and inhibits diABZI-induced phosphorylation of TBK1 and IRF3, thereby suppressing the transcription of IFNβ and IL6 and reducing IFNβ secretion. UM-242 can be used for the study of STING-dependent inflammatory and neurological diseases.

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UM-242

UM-242 Chemical Structure

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Description

UM-242 is a STING inhibitor, with an EC50 of 1.70 μM in THP1-Dual cells expressing wild-type STING. UM-242 blocks STING oligomerization and inhibits diABZI-induced phosphorylation of TBK1 and IRF3, thereby suppressing the transcription of IFNβ and IL6 and reducing IFNβ secretion. UM-242 can be used for the study of STING-dependent inflammatory and neurological diseases[1].

In Vitro

UM-242 (0.2-5 μM, pretreated for 1 h) exerts potent inhibitory activity on diABZI-induced IFNβ and IL6 gene transcription in iBMDMs[1].
UM-242 (2.5 μM, pretreated for 1 h) displays potent activity in blocking STING-dependent IFNβ secretion in primary human CD14+ monocytes[1].
UM-242 (5 μM, pretreated for 1 h) shows potent inhibitory activity on diABZI-induced phosphorylation of TBK1 and IRF3and exhibits potent activity in inhibiting STING oligomerization in WT BMDMs, effectively blocking STING downstream signal transduction[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: WT BMDMs
Concentration: 5 μM
Incubation Time: Pretreated for 1 h
Result: Showed potent inhibitory activity on diABZI-induced phosphorylation of TBK1 and IRF3.
Exhibited potent activity in inhibiting STING oligomerization in WT BMDMs.
Molecular Weight

536.45

Formula

C24H18F2N8O5

SMILES

O=C(C1=NOC(C2=CC(F)=CC=C2F)=N1)N[C@H](C3=NC4=CC=CC=C4N3)CCNC(C5=CC=C([N+]([O-])=O)O5)=N

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
UM-242
Cat. No.:
HY-178047
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