XL-3158

• Description:

  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].

• 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