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ARN 3236

Cat. No. 7511 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent inhibitor of salt-inducible kinases
化学名： 3-(2,4-Dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine
纯度： ≥98% (HPLC)
说明书
引用文献
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生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for ARN 3236

ARN 3236 is a potent of salt-inducible kinase 2 (SIK2) inhibitor (IC50 values are <1 nM, 6.63 nM and 21.63 nM for SIK2, SIK3 and SIK1 respectively). ARN 3236 inhibits centrosome separation by uncoupling the centrosome from the nucleus. It also induces cell-cycle arrest and apoptosis by attenuating the AKT/survivin pathway. ARN 3236 inhibits growth and enhances Taxol (Cat. No. 1097) sensitivity in ovarian cancer cell lines in vitro and in vivo. In human myeloid cells, ARN 3236 blocks TNF and induces IL-10 upon LPS stimulation; it also reduces the production of IL-1β upon activation of TLR4 and TLR2 signaling. In depression models, ARN 3236 exhibits antidepressant-like effects via the hippocampal CRTC1-CREB-BDNF pathway. ARN 3236 penetrates the blood-brain barrier, and it is orally bioavailable.

技术数据 for ARN 3236

分子量 336.41
公式 C19H16N2O2S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1613710-01-2
PubChem ID 74766530
InChI Key WEHOIIGXTMKVRG-UHFFFAOYSA-N
Smiles COC1=CC(OC)=C(C=C1)C2=CNC3=C2C(C4=CSC=C4)=CC=N3

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for ARN 3236

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 6.73 20

制备储备液 for ARN 3236

以下数据基于产品分子量 336.41。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 14.86 mL 74.31 mL 148.63 mL
1 mM 2.97 mL 14.86 mL 29.73 mL
2 mM 1.49 mL 7.43 mL 14.86 mL
10 mM 0.3 mL 1.49 mL 2.97 mL

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参考文献 for ARN 3236

参考文献是支持产品生物活性的出版物。

Zhou et al (2017) A novel compound ARN-3236 inhibits salt-inducible kinase 2 and sensitizes ovarian cancer cell lines and xenografts to Paclitaxel. Clin.Cancer Res. 23 1945 PMID: 27678456

Lombardi et al (2016) SIK inhibition in human myeloid cells modulates TLR and IL-1R signaling and induces an anti-inflammatory phenotype. J.Leukoc.Biol. 99 711 PMID: 26590148

Liu et al (2021) The selective SIK2 inhibitor ARN-3236 Produces strong antidepressant-like efficacy in mice via the hippocampal CRTC1-CREB-BDNF pathway. Front.Pharmacol. 11 624429 PMID: 33519490

If you know of a relevant reference for ARN 3236, please let us know.

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关键词: ARN 3236, ARN 3236 supplier, ARN3236, potent, inhibitors, inhibits, salt-inducible, kinase, 2, SIK2, centrosome, separation, antidepressant, depression, anti-inflammatory, Other, Kinases, 7511, Tocris Bioscience

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