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ID-8 {[allProObj[0].p_purity_real_show]}

货号:A512614

ID-8 is an inhibitor of DYRK inhibitor that can sustain embryonic stem cell self-renewal and survival without differentiation.

ID-8 化学结构 CAS号:147591-46-6
ID-8 化学结构
CAS号:147591-46-6
ID-8 3D分子结构
CAS号:147591-46-6
ID-8 化学结构 CAS号:147591-46-6
ID-8 3D分子结构 CAS号:147591-46-6
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ID-8 纯度/质量文件 产品仅供科研

货号:A512614 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 DYRK DYRK1 DYRK2 其他靶点 纯度
ID-8 99%+
AZ191 ++++

DYRK1A, IC50: 88 nM

DYRK1B, IC50: 17 nM

99%
Harmine +++

DYRK1A, IC50: 33 nM

DYRK1B, IC50: 166 nM

++

DYRK2, IC50: 1.9 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ID-8 生物活性

靶点
  • DYRK

描述 The dual-specificity tyrosine-phosphorylation-regulated (DYRK) kinases belong to a family collectively referred to as CMGC kinases that includes cyclin dependent kinases, mitogen associated protein kinases, glycogen synthase kinases, and cyclin dependent-like kinases. ID-8, a DYRK inhibitor, shows high specificity for DYRK1A and DYRK1B with IC50s of 78 and 54 nM, respectively[3]. ID-8 increased hESC (human embryonic stem cells) survival (∼1.1% at 0.5 μM). The combination of Wnt3a and ID-8 further increased survival (∼1.7%) and completely prevented Wnt-induced differentiation morphologically without disrupting proliferation. Wnt-induced differentiation marker gene expression was dramatically reduced by ID-8 at a dose that maintained the undifferentiated state[4]. Treatment with ID-8 (10 µM) promoted significant increases in cell number after 24 hours of damage in at least two different damage models[5].

ID-8 细胞实验

Cell Line
Concentration Treated Time Description References
ID-8 cells 0, 1.2, 2.4, 4.8, 9.6 μg/mL 24 hours To evaluate the effect of Tanshinone IIA on VEGF and COX2 mRNA expression in ID-8 cells, results showed that Tanshinone IIA significantly inhibited VEGF and COX2 mRNA expression. Ann Transl Med. 2020 Oct;8(20):1295
ID-8 cells 0, 1.2, 2.4, 4.8, 9.6 μg/mL 24 hours To evaluate the effect of Tanshinone IIA on the migration of ID-8 cells, results showed that Tanshinone IIA significantly inhibited cell migration. Ann Transl Med. 2020 Oct;8(20):1295
ID-8 cells 0, 1.2, 2.4, 4.8, 9.6 μg/mL 24 hours To evaluate the effect of Tanshinone IIA on the apoptosis of ID-8 cells, results showed that Tanshinone IIA significantly upregulated Bax mRNA expression and downregulated Bcl-2 mRNA expression, promoting apoptosis. Ann Transl Med. 2020 Oct;8(20):1295
ID-8 cells 0, 1.2, 2.4, 4.8, 9.6 μg/mL 24 hours To evaluate the effect of Tanshinone IIA on the proliferation of ID-8 cells, results showed that Tanshinone IIA significantly inhibited the proliferation of ID-8 cells in a dose-dependent manner. Ann Transl Med. 2020 Oct;8(20):1295
ID-8 cells 1000 nM 6 hours (migration) and 16 hours (invasion) To evaluate the effect of DEX on cell migration and invasion abilities, results showed that DEX significantly reduced the migration and invasion abilities of ID-8 cells, and this inhibition could be abrogated by depletion of endogenous miR-708 PLoS One. 2017 Jun 7;12(6):e0178937
ID-8 cells 100-1000 nM 48 hours To evaluate the effect of DEX on Rap1B expression, results showed that DEX reduced Rap1B expression PLoS One. 2017 Jun 7;12(6):e0178937
ID-8 cells 100-1000 nM 72 hours To evaluate the effect of DEX on miR-708 expression, results showed that DEX significantly induced miR-708 expression PLoS One. 2017 Jun 7;12(6):e0178937

ID-8 参考文献

[1]Hasegawa K, Yasuda SY, et al. Wnt signaling orchestration with a small molecule DYRK inhibitor provides long-term xeno-free human pluripotent cell expansion. Stem Cells Transl Med. 2012 Jan;1(1):18-28.

[2]Miyabayashi T, Yamamoto M, et al. Indole derivatives sustain embryonic stem cell self-renewal in long-term culture. Biosci Biotechnol Biochem. 2008 May;72(5):1242-8.

[3]Bellmaine SF, Ovchinnikov DA, Manallack DT, et al. Inhibition of DYRK1A disrupts neural lineage specificationin human pluripotent stem cells. Elife. 2017;6:e24502

[4]Hasegawa K, Yasuda SY, Teo JL, et al. Wnt signaling orchestration with a small molecule DYRK inhibitor provides long-term xeno-free human pluripotent cell expansion. Stem Cells Transl Med. 2012;1(1):18-28

[5]Monteiro MB, Ramm S, Chandrasekaran V, et al. A High-Throughput Screen Identifies DYRK1A Inhibitor ID-8 that Stimulates Human Kidney Tubular Epithelial Cell Proliferation. J Am Soc Nephrol. 2018;29(12):2820-2833

ID-8 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.34mL

16.76mL

3.35mL

1.68mL

33.52mL

6.70mL

3.35mL

ID-8 技术信息

CAS号147591-46-6
分子式C16H14N2O4
分子量 298.29
SMILES Code OC1=CC2=C(C=C1)C([N+]([O-])=O)=C(C)N2C3=CC=C(OC)C=C3
MDL No. MFCD00593367
别名
运输蓝冰
InChI Key VVZNWYXIOADGSW-UHFFFAOYSA-N
Pubchem ID 791637
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 45 mg/mL(150.86 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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