RU320521
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555738

CAS#: 2262452-06-0

Description: RU320521, also known as RU.521, is a potent and selective inhibitor of cGAS, inhibiting cGAS-mediated signaling, being active in murine bone marrow-derived macrophage.

Chemical Structure

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RU320521
CAS# 2262452-06-0
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555738
Name: RU320521
CAS#: 2262452-06-0
Chemical Formula: C19H12Cl2N4O3
Exact Mass: 414.03
Molecular Weight: 415.230
Elemental Analysis: C, 54.96; H, 2.91; Cl, 17.07; N, 13.49; O, 11.56

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to ship
10mg USD 250 Ready to ship
25mg USD 450 Ready to ship
50mg USD 750 Ready to ship
100mg USD 1350 Ready to ship
200mg USD 2350 Ready to ship
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Synonym: RU320521; RU-320521; RU 320521; RU521; RU-521; RU 521; RU.521;

IUPAC/Chemical Name: 3-[1-(6,7-Dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-pyrazol-4-yl]-3H-isobenzofuran-1-one

InChi Key: VIQXILLOJLATEF-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H12Cl2N4O3/c1-8-13(16-9-4-2-3-5-10(9)18(27)28-16)17(26)25(24-8)19-22-12-7-6-11(20)14(21)15(12)23-19/h2-7,16,26H,1H3,(H,22,23)

SMILES Code: O=C1OC(C2=C(O)N(C3=NC4=CC=C(Cl)C(Cl)=C4N3)N=C2C)C5=C1C=CC=C5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO and ethanol

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: RU320521 inhibits the cGAS-mediated signaling with IC50 of 700 nM. RU.521 binds to the cGAS/dsDNA complex with Kd of 36.2 nM.
In vitro activity: RU320521 is capable of potently and selectively inhibiting mouse and human cGAS in cell lines and human primary cells. When RU320521 is applied to cells, the production of dsDNA-induced intracellular cGAMP is suppressed in a dose-dependent manner. This work validates the use of RU320521 for probing DNA-induced innate immune responses and underscores its potential as an ideal scaffold towards pre-clinical development, given its potency against human and mouse cGAS. Reference: Sci Rep. 2020 May 5;10(1):7604. https://pubmed.ncbi.nlm.nih.gov/32371942/
In vivo activity: RU320521 was investigated in a study focused on trauma-induced delayed bone healing. In C57BL/6 J mice, RU320521 reduced IFNβ levels in bronchioalveolar fluid at 24 hours. RU320521 administration immediately after injury led to improved bone healing. These data reveal that the cGAS-STING signaling pathway influences trauma-induced delayed bone healing. Reference: J Exp Orthop. 2023 Sep 1;10(1):90. https://pubmed.ncbi.nlm.nih.gov/37656236/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 83.0 199.89
Ethanol 2.0 4.82

Preparing Stock Solutions

The following data is based on the product molecular weight 415.23 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Wiser C, Kim B, Vincent J, Ascano M. Small molecule inhibition of human cGAS reduces total cGAMP output and cytokine expression in cells. Sci Rep. 2020 May 5;10(1):7604. doi: 10.1038/s41598-020-64348-y. PMID: 32371942; PMCID: PMC7200739. 2. Muire PJ, Lofgren AL, Shiels SM, Wenke JC. Fracture healing in a polytrauma rat model is influenced by mtDNA:cGAS complex mediated pro-inflammation. J Exp Orthop. 2023 Sep 1;10(1):90. doi: 10.1186/s40634-023-00637-5. PMID: 37656236. 3. Jiang Z, Jiang Y, Fan J, Zhang J, Xu G, Fan Y, Zhang L, Qin X, Jiang X, Mao L, Liu G, Chen C, Zou Z. Inhibition of cGAS ameliorates acute lung injury triggered by zinc oxide nanoparticles. Toxicol Lett. 2023 Jan 15;373:62-75. doi: 10.1016/j.toxlet.2022.11.002. Epub 2022 Nov 8. PMID: 36368621.
In vitro protocol: 1. Wiser C, Kim B, Vincent J, Ascano M. Small molecule inhibition of human cGAS reduces total cGAMP output and cytokine expression in cells. Sci Rep. 2020 May 5;10(1):7604. doi: 10.1038/s41598-020-64348-y. PMID: 32371942; PMCID: PMC7200739.
In vivo protocol: 1. Muire PJ, Lofgren AL, Shiels SM, Wenke JC. Fracture healing in a polytrauma rat model is influenced by mtDNA:cGAS complex mediated pro-inflammation. J Exp Orthop. 2023 Sep 1;10(1):90. doi: 10.1186/s40634-023-00637-5. PMID: 37656236. 2. Jiang Z, Jiang Y, Fan J, Zhang J, Xu G, Fan Y, Zhang L, Qin X, Jiang X, Mao L, Liu G, Chen C, Zou Z. Inhibition of cGAS ameliorates acute lung injury triggered by zinc oxide nanoparticles. Toxicol Lett. 2023 Jan 15;373:62-75. doi: 10.1016/j.toxlet.2022.11.002. Epub 2022 Nov 8. PMID: 36368621.

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1: Inoue K, Ishizawa M, Kubota T. Monoclonal anti-dsDNA antibody 2C10 escorts DNA to intracellular DNA sensors in normal mononuclear cells and stimulates secretion of multiple cytokines implicated in lupus pathogenesis. Clin Exp Immunol. 2020 Feb;199(2):150-162. doi: 10.1111/cei.13382. Epub 2019 Oct 29. PMID: 31604370; PMCID: PMC6954677.

2: Xie W, Lama L, Adura C, Tomita D, Glickman JF, Tuschl T, Patel DJ. Human cGAS catalytic domain has an additional DNA-binding interface that enhances enzymatic activity and liquid-phase condensation. Proc Natl Acad Sci U S A. 2019 Jun 11;116(24):11946-11955. doi: 10.1073/pnas.1905013116. Epub 2019 May 29. PMID: 31142647; PMCID: PMC6575157.

3: Zhou W, Whiteley AT, de Oliveira Mann CC, Morehouse BR, Nowak RP, Fischer ES, Gray NS, Mekalanos JJ, Kranzusch PJ. Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance. Cell. 2018 Jul 12;174(2):300-311.e11. doi: 10.1016/j.cell.2018.06.026. PMID: 30007416; PMCID: PMC6084792.

4: Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Publisher Correction: Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Nov 23;8(1):1827. doi: 10.1038/s41467-017-01770-3. Erratum for: Nat Commun. 2017 Sep 29;8(1):750. PMID: 29170402; PMCID: PMC5700994.

5: Vincent J, Adura C, Gao P, Luz A, Lama L, Asano Y, Okamoto R, Imaeda T, Aida J, Rothamel K, Gogakos T, Steinberg J, Reasoner S, Aso K, Tuschl T, Patel DJ, Glickman JF, Ascano M. Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice. Nat Commun. 2017 Sep 29;8(1):750. doi: 10.1038/s41467-017-00833-9. Erratum in: Nat Commun. 2017 Nov 23;8(1):1827. PMID: 28963528; PMCID: PMC5622107.