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A 83-01 sodium {[allProObj[0].p_purity_real_show]}

货号:A1159477 Ambeed 开学季,买赠积分,赢豪礼

A 83-01 Sodium Salt is a selective inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50 values of 12, 45 and 7.5 nM, respectively.

A 83-01 sodium 化学结构 CAS号:2828431-89-4
A 83-01 sodium 化学结构
CAS号:2828431-89-4
A 83-01 sodium 3D分子结构
CAS号:2828431-89-4
A 83-01 sodium 化学结构 CAS号:2828431-89-4
A 83-01 sodium 3D分子结构 CAS号:2828431-89-4
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A 83-01 sodium 纯度/质量文件 产品仅供科研

货号:A1159477 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 ALK1 ALK2 ALK3 ALK4 ALK6 Smad3 TGF-β TGFβRI/ALK5 TGFβRII 其他靶点 纯度
LDN193189 ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

{[allProObj[0].p_purity_real_show]}
LDN-212854 ++++

ALK1, IC50: 2.4 nM

++++

ALK2, IC50: 1.3 nM

+

ALK3, IC50: 85.8 nM

+

ALK4, IC50: 2133 nM

+

ALK5, IC50: 9276 nM

{[allProObj[0].p_purity_real_show]}
ML347 ++

ALK1, IC50: 46 nM

++

ALK2, IC50: 32 nM

{[allProObj[0].p_purity_real_show]}
K02288 ++++

ALK1, IC50: 1.8 nM

++++

ALK2, IC50: 1.1 nM

++

ALK3, IC50: 34.4 nM

+++

ALK6, IC50: 6.4 nM

{[allProObj[0].p_purity_real_show]}
LDN-193189 dihydrochloride ++++

ALK1, IC50: 0.8 nM

++++

ALK2, IC50: 0.8 nM

+++

ALK3, IC50: 5.3 nM

+++

ALK6, IC50: 16.7 nM

{[allProObj[0].p_purity_real_show]}
LDN-214117 ++

ALK2, IC50: 24 nM

{[allProObj[0].p_purity_real_show]}
DMH-1 +

ALK2, IC50: 107.9 nM

{[allProObj[0].p_purity_real_show]}
SB-505124 +

ALK4, IC50: 129 nM

++

ALK5, IC50: 47 nM

{[allProObj[0].p_purity_real_show]}
Vactosertib +++

ALK4, IC50: 13 nM

+++

ALK5, IC50: 11 nM

{[allProObj[0].p_purity_real_show]}
Alantolactone {[allProObj[0].p_purity_real_show]}
SIS3 {[allProObj[0].p_purity_real_show]}
Pirfenidone {[allProObj[0].p_purity_real_show]}
Hesperetin {[allProObj[0].p_purity_real_show]}
RepSox ++++

TGFβR1(ALK5), IC50: 4 nM

{[allProObj[0].p_purity_real_show]}
GW788388 +++

ALK5, IC50: 18 nM

{[allProObj[0].p_purity_real_show]}
LY364947 ++

TGFβRI, IC50: 59 nM

+

TGFβRII, IC50: 0.4 μM

{[allProObj[0].p_purity_real_show]}
SD-208 ++

TGF-βRI (ALK5), IC50: 48 nM

{[allProObj[0].p_purity_real_show]}
SB-525334 +++

TGFβR1(ALK5), IC50: 14.3 nM

{[allProObj[0].p_purity_real_show]}
LY2109761 ++

TβRI, Ki: 38 nM

+

TβRII, Ki: 300 nM

{[allProObj[0].p_purity_real_show]}
Galunisertib ++

TβRI, IC50: 56 nM

{[allProObj[0].p_purity_real_show]}
SB 431542 +

ALK5, IC50: 94 nM

{[allProObj[0].p_purity_real_show]}
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。

A 83-01 sodium 生物活性

描述 Transforming growth factor (TGF)-beta signaling facilitates tumor growth and metastasis in advanced cancer. Use of inhibitors of TGF-beta signaling may thus be a novel strategy for the treatment of patients with such cancer[1]. A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively[1]. A 83-01 sodium salt (0.03-10 µM) potently prevents the growth-inhibitory effects of TGF-β, and completely inhibits the effect at 3 µM. A 83-01 (1-10 µM) inhibits TGF-β-induced Smad activation in HaCaT cells[1]. A 83-01 sodium salt (1 µM) decreases cell motility, adhesion and invasion increased by TGF-β1 in HM-1 cells, but does not change cell proliferation[2]. A 83-01 sodium salt (50, 150 and 500 μg/mouse, i.p.) significantly improves survival of the mice without body weight or neurobehavioral appearances[2]. A 83-01 sodium salt (0.5 mg/kg, i.p.) shows a significantly strong antitumor effect in mice bearing M109 cells[3].

A 83-01 sodium 参考文献

[1]Tojo M, Hamashima Y, Hanyu A, Kajimoto T, Saitoh M, Miyazono K, Node M, Imamura T. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800. doi: 10.1111/j.1349-7006.2005.00103.x. PMID: 16271073.

[2]Yamamura S, Matsumura N, Mandai M, Huang Z, Oura T, Baba T, Hamanishi J, Yamaguchi K, Kang HS, Okamoto T, Abiko K, Mori S, Murphy SK, Konishi I. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8. doi: 10.1002/ijc.25961. Epub 2011 Apr 18. PMID: 21503873.

[3]Taniguchi Y, Kawano K, Minowa T, Sugino T, Shimojo Y, Maitani Y. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13. doi: 10.1111/j.1349-7006.2010.01646.x. Epub 2010 Jul 1. PMID: 20608940.

A 83-01 sodium 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.23mL

11.27mL

2.25mL

1.13mL

22.55mL

4.51mL

2.25mL

A 83-01 sodium 技术信息

CAS号2828431-89-4
分子式C25H18N5NaS
分子量 443.499
别名
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(236.75 mM),配合低频超声助溶,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

动物实验配方
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