Art. -Nr.: HY-174802

XL-3158

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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.

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Reinheit: 99.55%
CAS. Nr.: 3117797-77-7
Formel: C₃₀H₁₇F₇N₆O₂S₂
Molecular Weight:690.61

Speicherung:

4°C, protect from light

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

XL-3158 Chemical Structure

CAS. Nr.: 3117797-77-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle IKK Isoform-spezifische Produkte anzeigen :

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.

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.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-t
Mice^[1]	10 mg/kg	i.p.	4415 ng/mL	27044 ng·h/mL
Mice^[1]	5 mg/kg	i.v.	14696 ng/mL	56875 ng·h/mL
Mice^[1]	50 mg/kg	p.o.	90565 ng/mL	365133 ng·h/mL

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.

Chemical Information

CAS. Nr. 3117797-77-7
Appearance Solid
Molecular Weight 690.61
Formel C₃₀H₁₇F₇N₆O₂S₂
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4480 mL

7.2400 mL

14.4800 mL

5 mM

0.2896 mL

1.4480 mL

2.8960 mL

10 mM

0.1448 mL

0.7240 mL

1.4480 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Pyroptosis Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Lactylation Compound Library

Alle IKK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XL-3158

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Pyroptosis Compound Library

Anti-Liver Cancer Compound Library

Anti-Prostate Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Autoimmune Disease Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Pattern Recognition Receptors Library

Lactylation Compound Library

Alle IKK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

XL-3158 Related Classifications

HY-174802 Related Classifications