SML3802
ARN-3236
≥98% (HPLC)
Synonym(s):
3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine, 3-(2,4-Dimethoxyphenyl)-4-(thiophen-3-yl)-1H-pyrrolo[2,3-b]pyridin, ARN 3236, ARN3236
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About This Item
Empirical Formula (Hill Notation):
C19H16N2O2S
CAS Number:
Molecular Weight:
336.41
UNSPSC Code:
12352200
NACRES:
NA.21
MDL number:
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
SMILES string
[s]1cc(cc1)c2c3c([nH]cc3c4c(cc(cc4)OC)OC)ncc2
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)
InChI key
WEHOIIGXTMKVRG-UHFFFAOYSA-N
Biochem/physiol Actions
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) that 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.
Orally active, ATP-competitive, highly potent and selective SIK2 inhibitor with anti-ovarian cancer efficacy in vitro and in vivo.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Jinhua Zhou et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 23(8), 1945-1954 (2016-09-30)
Purpose: Salt-inducible kinase 2 (SIK2) is a centrosome kinase required for mitotic spindle formation and a potential target for ovarian cancer therapy. Here, we examine the effects of a novel small-molecule SIK2 inhibitor, ARN-3236, on sensitivity to paclitaxel in ovarian
Venipuncture: simple and aafe.
C E Murphy
Dental survey, 47(1), 31-33 (1971-01-01)
Tissue viability. Measuring the pressure.
M Clark
Nursing times, 84(25), 72-75 (1988-06-22)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3802-5MG | 04065270217721 |
| SML3802-25MG | 04065270217714 |