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.
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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 |
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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 |
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ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
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K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
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LDN-193189 dihydrochloride |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
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LDN-214117 |
++
ALK2, IC50: 24 nM |
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DMH-1 |
+
ALK2, IC50: 107.9 nM |
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SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
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Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
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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 |
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GW788388 |
+++
ALK5, IC50: 18 nM |
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LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
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SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
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SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
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LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
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Galunisertib |
++
TβRI, IC50: 56 nM |
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SB 431542 |
+
ALK5, IC50: 94 nM |
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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。 |
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]. |
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 |
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 |