- ARN-3236
-
- $55.00
-
2026-07-27
- CAS:1613710-01-2
- Purity: 99.57%
- Supply Ability: 10g
|
| | ARN-3236 Basic information |
| Product Name: | ARN-3236 | | Synonyms: | ARN-3236;3-(2,4-DIMETHOXYPHENYL)-4-(THIOPHEN-3-YL)-1H-PYRROLO[2,3-B]PYRIDINE;ARN-3236; ARN 3236; ARN3236;1H-Pyrrolo[2,3-b]pyridine, 3-(2,4-dimethoxyphenyl)-4-(3-thienyl)-;3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine;inhibit,ARN3236,Salt-inducible Kinase (SIK),ARN-3236,ARN 3236,Inhibitor;ARN-3236, 10 mM in DMSO;ARN-3236 (ARN3236) | | CAS: | 1613710-01-2 | | MF: | C19H16N2O2S | | MW: | 336.41 | | EINECS: | | | Product Categories: | | | Mol File: | 1613710-01-2.mol |  |
| | ARN-3236 Chemical Properties |
| density | 1.278±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:65.67(Max Conc. mg/mL);195.21(Max Conc. mM)
Ethanol:2.0(Max Conc. mg/mL);5.95(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);89.18(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:4):0.2(Max Conc. mg/mL);0.59(Max Conc. mM) | | form | A crystalline solid | | pka | 13.33±0.40(Predicted) | | color | White to off-white | | InChI | 1S/C19H16N2O2S/c1-22-13-3-4-15(17(9-13)23-2)16-10-21-19-18(16)14(5-7-20-19)12-6-8-24-11-12/h3-11H,1-2H3,(H,20,21) | | InChIKey | WEHOIIGXTMKVRG-UHFFFAOYSA-N | | SMILES | [s]1cc(cc1)c2c3c([nH]cc3c4c(cc(cc4)OC)OC)ncc2 |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | ARN-3236 Usage And Synthesis |
| Uses | ARN-3236 is an oral active and selective inhibitor of salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has anti-cancer activity[1][2]. | | Biological Activity | ARN-3236 is an orally active, ATP-competitive, SIK2-selective salt-inducible kinase inhibitor (IC50 = 21.63 nM/SIK1, <1 nM/SIK2, 6.63 nM/SIK3) th at suppresses cellular SIK2 activity (by 58% at 1 μM; SKOv3-SIK2 cells, 48 h) with high selectivity over >456 kinases. ARN-3236 effectively suppresses SIK2-dependent growth of ovarian cancer cultures (IC50 = 0.8-2.6 μM in 10 lines, 72 h) and in murine xenograft models in vivo (30, 60, 100 mg/kg/day p.o.). In addition, ARN-3236 sensitizes ovarian cancer cells to paclitaxel in vitro and in vivo. ARN-3236 completes the SIK1-selective HG-9-91-01 (SIK1/2/3 IC50 = 0.6/6.6/9.6 nM) in probing SIKs-mediated cellular signaling events. | | in vivo | ARN-3236 (60 mg/kg, orally) sensitizes ovarian cancer to NSC 125973 in vivo[2]. | Animal Model: | SKOv3ip-bearing mice and OVCAR8-bearing mice[2]. | | Dosage: | 60 mg/kg. | | Administration: | Orally once daily for 3 weeks (SKOv3ip-bearing mice) and 4 weeks (OVCAR8-bearing mice). | | Result: | Sensitized ovarian cancer to NSC 125973. |
| | IC 50 | SIK2: <1 nM (IC50); SIK1: 21.63 nM (IC50); SIK3: 6.63 nM (IC50) | | storage | Store at -20°C | | References | [1] Lombardi MS, et al. SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J Leukoc Biol. 2016 May;99(5):711-21. DOI:10.1189/jlb.2A0715-307R
[2] Zhou J, et al. A Novel Compound ARN-3236 Inhibits Salt-Inducible Kinase 2 and Sensitizes Ovarian Cancer Cell Lines and Xenografts. Clin Cancer Res. 2017 Apr 15;23(8):1945-1954. DOI:10.1158/1078-0432.CCR-16-1562 |
| | ARN-3236 Preparation Products And Raw materials |
|