2. Immunology/Inflammation NF-κB
  3. Cyclic GMP-AMP Synthase IKK IFNAR
  4. 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 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases.

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XL-3158

XL-3158 Chemical Structure

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Based on 1 publication(s) in Google Scholar

XL-3158 Related Antibodies

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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 has no obvious cytotoxicity within the effective concentration range and is suitable for subsequent cell function experiments. XL-3158 overcomes species selectivity barriers and serves as a drug candidate for cGAS-dependent inflammatory diseases[1].

In Vitro

XL-3158 (Compound XL-3158) (20 μM, 4 h) blocks cGAS intracellular condensation with DNA by inhibiting cGAS phase separation in L929 cells[1].

XL-3158 (10-40 μM, 4 h) specifically inhibits downstream signaling activation of the cGAS-STING pathway in THP-1 Dual cells[1].

XL-3158 (10 μM, 4 h) selectively inhibits the DNA-triggered cGAS-dependent interferon pathway in THP-1 Dual cells[1].

XL-3158 (0-20 μM, 24 h) has CC50 values of 77.55 μM against THP-1 cells and 56.79 μM against RAW-ISG cells[1].

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

XL-3158 Related Antibodies

Western Blot Analysis[1]

Cell Line: THP-1 Dual cells
Concentration: 10 μM, 20 μM, 40μM
Incubation Time: 4 h
Result: Inhibited HT-DNA-induced TBK-1 and IRF3 phosphorylation in a dose-dependent manner.
Had no inhibitory effect on pathways activated by Poly (I:C) or cGAMP.

RT-PCR[1]

Cell Line: THP-1 Dual cells
Concentration: 10 μM, 20 μM, 40μM
Incubation Time: 4 h
Result: Significantly reduced HT-DNA-induced IFN-β1 mRNA expression.

Immunofluorescence[1]

Cell Line: L929 cells
Concentration: 20 μM
Incubation Time: 4 h
Result: Significantly reduced the number of co-localized condensates of cGAS and Cy5-DNA.
Confirmed that the condensates had liquid-like properties (LLPS) and inhibited their formation.
In Vivo

XL-3158 (Compound XL-3158) (25 mg/kg, i.g. twice administration) attenuates Cerulein (HY-A0190)-induced acute pancreatitis[1].

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

Animal Model: Cerulean (HY-A0190) (50 µg/kg, i.p, injections once every hour for 7 times) induced acute pancreatitis model in C57BL/6J nude female mice (6-8 weeks)[1].
Dosage: 25mg/kg
Administration: Intragastric gavage (i.g.), administration at 0 hour and 6 h after the first Cerulein injection.
Result: Significantly reduced pancreatic pathological damage and the pancreas/body weight ratio, indicating that pancreatic edema was relieved.
Significantly reduced serum amylase and serum lipase activities.
Significantly reduced serum inflammatory factor levels.
Molecular Weight

690.61

Formula

C30H17F7N6O2S2
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (72.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4480 mL 7.2400 mL 14.4800 mL
5 mM 0.2896 mL 1.4480 mL 2.8960 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4480 mL 7.2400 mL 14.4800 mL 36.1999 mL
5 mM 0.2896 mL 1.4480 mL 2.8960 mL 7.2400 mL
10 mM 0.1448 mL 0.7240 mL 1.4480 mL 3.6200 mL
15 mM 0.0965 mL 0.4827 mL 0.9653 mL 2.4133 mL
20 mM 0.0724 mL 0.3620 mL 0.7240 mL 1.8100 mL
25 mM 0.0579 mL 0.2896 mL 0.5792 mL 1.4480 mL
30 mM 0.0483 mL 0.2413 mL 0.4827 mL 1.2067 mL
40 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9050 mL
50 mM 0.0290 mL 0.1448 mL 0.2896 mL 0.7240 mL
60 mM 0.0241 mL 0.1207 mL 0.2413 mL 0.6033 mL
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XL-3158 Related Classifications

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:

XL-3158XL3158XL 3158Cyclic GMP-AMP SynthaseIKKIFNARcGASIκB kinaseI kappa B kinase Interferon-α/β receptorInterferon-alpha/beta receptorAcute Pancreatitis modelC57BL/6J miceICR miceAllosteric inhibitorOral bioavailabilityTHP-1 Dual cellsInhibitorinhibitorinhibit

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