RU.521
- CAS No.
- 2262452-06-0
- Chemical Name:
- RU.521
- Synonyms
- RU32052;RU320521;RU.521 RU320521;RU320521 RU-320521;RU.521;RU521;RU-320521;1(3H)-Isobenzofuranone, 3-[1-(6,7-dichloro-1H-benzimidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl]-;3-(1-(6,7-dichloro-1H-benzo[d]imidazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol-4-yl)isobenzofuran-1(3H)-one;inflammatory,oxidative stress,RU 320521,cGAS,RU-320521,Inhibitor,inhibit,RU.521,Cyclic GMP-AMP Synthase,signaling pathway
- CBNumber:
- CB44869399
- Molecular Formula:
- C19H12Cl2N4O3
- Molecular Weight:
- 415.23
- MDL Number:
- MOL File:
- 2262452-06-0.mol
| Boiling point | 658.2±65.0 °C(Predicted) |
|---|---|
| Density | 1.73±0.1 g/cm3(Predicted) |
| storage temp. | Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
| solubility | Soluble in DMSO (>25 mg/ml) |
| form | solid |
| pka | 6.17±0.30(Predicted) |
| color | Off-white to pale pink |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| InChI | 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) |
| InChIKey | VIQXILLOJLATEF-UHFFFAOYSA-N |
| SMILES | C1(=O)C2=C(C=CC=C2)C(C2=C(O)N(C3NC4=C(Cl)C(Cl)=CC=C4N=3)N=C2C)O1 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
RU.521 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0078769 | RU.521 98.24% | 2262452-06-0 | 5mg | $120 | 2021-12-16 | Buy |
| ChemScene | CS-0078769 | RU.521 98.24% | 2262452-06-0 | 10mg | $210 | 2021-12-16 | Buy |
| ChemScene | CS-0078769 | RU.521 98.24% | 2262452-06-0 | 50mg | $820 | 2021-12-16 | Buy |
| ChemScene | CS-0078769 | RU.521 98.24% | 2262452-06-0 | 100mg | $1450 | 2021-12-16 | Buy |
| DC Chemicals | DC22305 | RU-521 >98% | 2262452-06-0 | 1g | $2200 | 2021-12-16 | Buy |
RU.521 Chemical Properties,Uses,Production
Description
RU.521 (2262452-06-0) is an inhibitor of cyclic GMP-AMP synthase (cGAS), an important innate immune system sensor of foreign cytoplasmic double-stranded DNA.1,2 IC50 = 0.70 μM in dsDNA-stimulated RAW macrophages1 and ~0.80 μM in wild type human THP-1 cells2. It is selective for cGAS with no targeting of IFNB1 protein, interferon receptors, or downstream signaling components of the JAK/STAT pathway. RU.521 was able to significantly increase cardiac output in a mouse model of sepsis.3 Active in both mouse and human cell lines.
Biochem/physiol Actions
The potency and selectivity of a chemically improved inhibitor, RU.521, in cellular assays show that while it inhibits cGAS-mediated interferon upregulation, it has reduced to no effect on inflammatory pathways independent of cGAS. Furthermore, RU.521 suppresses the chronically elevated levels of type I interferon observed in primary macrophages from Trex1 null mice, a model of AGS. Crystal structures show that RU.521 occupies the catalytic pocket of murine cGAS, thus interfering with the entry of its ATP and GTP substrates. RU.521 inhibits cytoplasmic DNA-dependent upregulation of IRF3-dependent transcriptional targets only in the presence of an intact cGAS-STING pathway[1-2].
storage
Store at -20°C
References
Vincent et al. (2017), Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice; Nat. Commun. 8 750
Wiser et al. (2020), Small molecule inhibition of human cGAS reduces total cGAMP output and cytokine expression in cells; Sci. Rep. 10 7604
Xu et al. (2020), Small molecule inhibition of cyclic GMP-AMP synthase ameliorates sepsis-induced cardiac dysfunction in mice; Life Sci. 260 118315
[1] Jessica Vincent. “Small molecule inhibition of cGAS reduces interferon expression in primary macrophages from autoimmune mice.” Nature Communications (2017): 750.
[2] Caroline Wiser. “Small molecule inhibition of human cGAS reduces total cGAMP output and cytokine expression in cells.” Scientific Reports (2020): 7604.
RU.521 Preparation Products And Raw materials
Raw materials
Preparation Products
RU.521 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Wuhan Topule Biopharmaceutical Co., Ltd | +8618327326525 | masar@topule.com | China | 8474 | 58 |
| LEAPCHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 43348 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |