2. Immunology/Inflammation
  3. STING
  4. UM-259 hydrochloride

UM-259 hydrochloride is a STING inhibitor with activity against both murine and human STING (including the STINGR232 mutant). UM-259 hydrochloride inhibits STING-dependent signaling pathways, blocks STING oligomerization, and acts on human primary CD14+ monocytes. UM-259 hydrochloride can be used for research on amyotrophic lateral sclerosis, lupus erythematosus, Aicardi-Goutières syndrome, and infant-onset STING-associated vasculopathy.

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UM-259 hydrochloride

UM-259 hydrochloride Chemical Structure

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UM-259 hydrochloride Related Antibodies

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Description

UM-259 hydrochloride is a STING inhibitor with activity against both murine and human STING (including the STINGR232 mutant). UM-259 hydrochloride inhibits STING-dependent signaling pathways, blocks STING oligomerization, and acts on human primary CD14+ monocytes. UM-259 hydrochloride can be used for research on amyotrophic lateral sclerosis, lupus erythematosus, Aicardi-Goutières syndrome, and infant-onset STING-associated vasculopathy[1].

In Vitro

UM-259 hydrochloride (0.08-40 μM; 1 h + 24 h; diABZI) inhibits STING-dependent signaling pathways in THP1-Dual KI-hSTING-R232 cells, with an EC50 of 1.50 μM[1].
UM-259 hydrochloride (0.2-5 μM; 1 h + 2 h; diABZI) dose-dependently inhibits diABZI-induced IFNβ and IL6 gene expression in iBMDM, and exhibits superior potency to LB244 (HY-156117) at a concentration of 5 μM[1].
UM-259 hydrochloride (0.2-5 μM; 1 h +24 h; diABZI) dose-dependently inhibits diABZI-induced IFNβ secretion in iBMDMs, and its efficacy at 5 μM is superior to that of LB244[1].
UM-259 hydrochloride (2.5 μM; 1 h + 16 h; diABZI) inhibits diABZI-induced IFNβ secretion in primary human CD14+ monocytes[1].
UM-259 hydrochloride (5 μM; 1 h+0-120 min; diABZI) inhibits diABZI-induced phosphorylation of TBK1 and IRF3 in wild-type bone marrow-derived macrophages (BMDMs)[1].
UM-259 hydrochloride (5 μM; 1 h+30 min; diABZI) blocks diABZI-induced STING oligomerization in wild-type bone marrow-derived macrophages (BMDMs)[1].
UM-259 hydrochloride (0.2-5 μM; 24 h) exhibits only limited cytotoxicity against iBMDMs[1].

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

UM-259 hydrochloride Related Antibodies

ELISA Assay[1]

Cell Line: primary human CD14+ monocytes
Concentration: 2.5 μM
Incubation Time: 1 h pre-incubation, followed by 16 h incubation with diABZI
Result: Blocked diABZI-induced IFNβ secretion, reducing levels to near baseline (DMSO without diABZI) levels.

Western Blot Analysis[1]

Cell Line: wild-type bone marrow-derived macrophages (BMDMs)
Concentration: 5 μM
Incubation Time: 1 h pre-incubation, followed by 0-120 min incubation with diABZI
Result: Inhibited diABZI-induced phosphorylation of TBK1 and IRF3, reducing phosphorylated protein levels compared to vehicle-treated cells at all time points tested.
Blocked diABZI-induced STING oligomer formation, with only STING monomers detected in native fractions (similar to unstimulated cells), while vehicle-treated cells showed robust STING oligomer formation.
Molecular Weight

597.96

Formula

C27H22ClF2N7O5
Appearance

Solid

SMILES

O=C(C1=NOC(C2=CC=C(F)C=C2F)=C1)NC3(C4=NC5=CC=CC=C5N4)CCN(C(C6=CC=C([N+]([O-])=O)O6)=N)CC3.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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UM-259 hydrochloride Related Classifications

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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.

Keywords:

UM-259UM259UM 259STINGStimulator of Interferon GenesTMEM173MITAERISMPYSTHP1-Dual KI-hSTING-R232 cellsSTING-associated vasculopathy with onset in infancyR232 variantamyotrophic lateral sclerosisiBMDMslupusAicardi-Goutières syndromeprimary human CD14+ monocytesTBK1Inhibitorinhibitorinhibit

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UM-259 hydrochloride
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HY-178049A
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