SML3802
ARN-3236
≥98% (HPLC)
别名:
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
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
[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
相关类别
生化/生理作用
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Yue Liu et al.
Frontiers in pharmacology, 11, 624429-624429 (2021-02-02)
Depression is a widespread chronic medical illness affecting thoughts, mood, and physical health. However, the limited and delayed therapeutic efficacy of monoaminergic drugs has led to intensive research efforts to develop novel antidepressants. ARN-3236 is the first potent and selective
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)
Liangneng Zou et al.
BMC pulmonary medicine, 22(1), 140-140 (2022-04-13)
Pulmonary fibrosis is a fatal lung disease with complex pathogenesis and limited effective therapies. Salt-inducible kinase 2 (SIK2) is a kinase that phosphorylates CRTCs and regulates many physiological processes. However, the role of SIK2 on pulmonary fibrosis remains unclear, and
Kimberly E Maxfield et al.
Molecular and cellular biology, 36(24), 3048-3057 (2016-10-05)
Triple-negative breast cancer (TNBC) is a highly heterogeneous disease with multiple, distinct molecular subtypes that exhibit unique transcriptional programs and clinical progression trajectories. Despite knowledge of the molecular heterogeneity of the disease, most patients are limited to generic, indiscriminate treatment
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