1. Immunology/Inflammation
  2. STING
  3. STING antagonist-3

STING antagonist-3 is a potent STING antagonist with an IC50 of 2.3 nM against human wild-type STING. STING antagonist-3 inhibits human wild-type STING and the gain-of-function STING mutants N154S and V155M. STING antagonist-3 suppresses IFN‑α2a production in stimulated human whole blood. STING antagonist-3 inhibits IP-10 production in activated human dermal microvascular endothelial cells (HMVEC-d). STING antagonist-3 can be used for the research of autoimmune diseases, autoinflammatory diseases, interferonopathies, and fibrotic disorders.

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STING antagonist-3

STING antagonist-3 Chemical Structure

CAS No. : 3106554-00-8

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Description

STING antagonist-3 is a potent STING antagonist with an IC50 of 2.3 nM against human wild-type STING. STING antagonist-3 inhibits human wild-type STING and the gain-of-function STING mutants N154S and V155M. STING antagonist-3 suppresses IFN‑α2a production in stimulated human whole blood. STING antagonist-3 inhibits IP-10 production in activated human dermal microvascular endothelial cells (HMVEC-d). STING antagonist-3 can be used for the research of autoimmune diseases, autoinflammatory diseases, interferonopathies, and fibrotic disorders[1].

In Vitro

STING antagonist-3 (Example 21) inhibits human wild-type STINGR232 with an IC50 of 2.3 nM in the competitive HTRF binding assay[1].
STING antagonist-3 (100 μM; temperature ramp from 15°C to 95°C over 160 cycles) stabilizes human wild-type STING protein against thermal denaturation with a ΔTm of 29 K in the DSF assay[1].
STING antagonist-3 (10 μM; 60 min (pre-incubation); 22 h (post-stimulation)) inhibits cGAMP-stimulated IFNα2α production in human whole blood with an IC50 of 0.029 μM[1].
STING antagonist-3 (1 h (pre-incubation); 6 h (stimulation)) inhibits dsDNA-stimulated IP-10 production in human HMVEC cells with an IC50 of 6.8 nM[1].

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

Molecular Weight

577.72

Formula

C35H39N5O3

CAS No.
SMILES

CC(N=C([C@@H]1CC[C@H](CC1)C(O)=O)C=C2)=C2N3C(C)=C(C(C)C)C(C4=CC=CC5=NN(C[C@H](O)C6=CC=CC=C6)C=C54)=N3

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Product Name:
STING antagonist-3
Cat. No.:
HY-185379
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