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XL-3158

XL-3158 is a selective and cross-species Cyclic GMP-AMP synthase (cGAS) inhibitor (IC50: 11.1 μM for human cGAS, 2.19 μM for mouse cGAS) . XL-3158 simultaneously occupy allosteric and orthosteric sites, stabilizing the activation loop in a closed, inactive conformation and thereby attenuating the cGAS-DNA interactions. XL-3158 inhibits cGAS by targeting phase separation. XL-3158 efficiently penetrates cells by inhibiting aggregate formation, effectively reducing the local concentration of cGAS within cells. XL-3158 can be used for the study of cGAS-dependent inflammatory diseases[1].

Product Specifications

UNSPSC

12352100

Target

Cyclic GMP-AMP Synthase; IFNAR; IKK

Related Pathways

Immunology/Inflammation; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology; Neurological Disease

Purity

99.55

Solubility

DMSO : 50 mg/mL (ultrasonic)

Smiles

CC1=NN(C(O)=C1C(C2=C(N(N=C2C)C3=NC4=C(S3)C=C(C=C4F)F)O)C5=CC=C(C(F)(F)F)C=C5)C6=NC7=C(S6)C=C(C=C7F)F

Molecular Formula

C30H17F7N6O2S2

Molecular Weight

690.61

References & Citations

[1]Wenfeng Zhao, et al. De novo design of protein condensation inhibitors by targeting an allosteric site of cGAS. Nat Commun. 2025 Jun 3 16 (1) :5140.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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