SB-505124
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- CAS號(hào):
- 694433-59-5
- 英文名:
- 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride
- 英文別名:
- SB-505124 hydrochloride hydrate;CS-872;SB505124 ，S2186;SB505124;SB505124;SB-505124, 10 mM in DMSO;SB 505124, ALK5 inhibitor;SB-505124 hydrate hydrochloride;SB-505124 hydrochloride hydrate SB505124;SB-505124, 98%, a selective inhibitor of TGFβR for ALK4, ALK5;2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-iMidazol-4-yl)-6-Methylpyridine
- 中文名:
- SB-505124
- 中文別名:
- 抑制劑SB-505124;化合物SB-505124;抑制劑SB-505124;SB505124 ,S2186;SB 505124,ALK5抑制劑;SB505124,競(jìng)爭(zhēng)性ALK5抑制劑;化合物SB-505124,10 MM DMSO 溶液;SB-505124, 一種選擇性TGFΒ受體ALK4和ALK5抑制劑;2-[4-(1,3-苯并二惡茂-5-基)-2-(叔丁基)-1H-咪唑-5-基]-6-甲基吡啶;2-[4-(1,3-苯并二惡英-5-基)-2-(1,1-二甲基乙基)-1H-咪唑-5-基]-6-甲基吡啶
- CBNumber:
- CB12100798
- 分子式:
- C20H21N3O2
- 分子量:
- 335.4
- MOL File:
- 694433-59-5.mol
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SB-505124化學(xué)性質(zhì)
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熔點(diǎn):
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168 °C
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沸點(diǎn):
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509.7±50.0 °C(Predicted)
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密度:
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1.202
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儲(chǔ)存條件:
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Sealed in dry,2-8°C
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溶解度:
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DMSO: >10mg/mL
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酸度系數(shù)(pKa):
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11.26±0.10(Predicted)
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形態(tài):
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powder
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顏色:
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yellow
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InChI:
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1S/C20H21N3O2.ClH.H2O/c1-12-6-5-7-14(21-12)18-17(22-19(23-18)20(2,3)4)13-8-9-15-16(10-13)25-11-24-15;;/h5-10H,11H2,1-4H3,(H,22,23);1H;1H2
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InChIKey:
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DIDCCMVWCVRTNB-UHFFFAOYSA-N
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SMILES:
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O.Cl.Cc1cccc(n1)-c2[nH]c(nc2-c3ccc4OCOc4c3)C(C)(C)C
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SB-505124性質(zhì)、用途與生產(chǎn)工藝
SB505124是一種選擇性TGFβR抑制劑，作用于ALK4和ALK5，無(wú)細(xì)胞試驗(yàn)中IC50分別為129 nM和47 nM，也抑制ALK7，但不抑制ALK1，2，3或6。
| Target | Value |
ALK5
(Cell-free assay)
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47 nM
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ALK4
(Cell-free assay)
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129 nM
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SB-505124抑制緊密相關(guān)的ALK4,IC50為129 nM，選擇性比作用于 ALK5低2.5倍。SB-505124濃度高達(dá)10 μM時(shí)也不抑制ALK2。SB-505124 作用于COS-1細(xì)胞，也抑制內(nèi)源性Smad2磷酸化。加入SB-505124不影響組成型活性 ALK1, ALK2, ALK3, 和 ALK6 磷酸化的Smad1。ALK4和ALK5 激活Smad1和Smad2，加入SB-505124抑制激活。SB-505124作用于HepG2人類肝癌細(xì)胞，C2C12小鼠成肌細(xì)胞和Mv1Lu水貂肺細(xì)胞，抑制TGF-β誘導(dǎo)的Smad2磷酸化，這種作用存在濃度依賴性。1 μM SB-505124也抑制活化素誘導(dǎo)的Smad2磷酸化。SB-505124有效抑制TGF-β和活化素誘導(dǎo)CAGA12-熒光素酶和ARE-熒光素酶受體結(jié)構(gòu)的活力，這種作用存在濃度依賴性。 SB-505124可清除TGF-β1對(duì)E-鈣粘蛋白啟動(dòng)子, mRNA和蛋白表達(dá)的抑制。 SB-505124 損害Smad2磷酸化和 CTGF與α-SMA的表達(dá)。
SB-505124處理青光眼濾過(guò)手術(shù)中的濾過(guò)泡，持續(xù)10天以上，沒有任何嚴(yán)重的術(shù)后并發(fā)癥，并清楚地觀察到濾泡。第一周眼內(nèi)壓 (IOP)低于10 mmHg，然而 SB-505124處理一周后，眼內(nèi)壓漲到10 mmHg。
用途
SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptor ALK5 and as well as being a selective inhibitor of ALK4 but with less potency. SB-505124 blocks TGF-β鈥搃nduced apop
tosis of FaO cells and NRP 154 cells in a concentration-dependent manner. SB-505124 has been shown to suppress the migration and invasion of breast cancer MCF-7-M5 cells.
SB-505124
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
| 更新日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS編號(hào) | 包裝 | 價(jià)格 |
|---|
| 2026/07/06 | S2186 | SB-505124
SB505124 | 694433-59-5 | 10mg | 1375.11元 |
| 2026/07/06 | S2186 | SB-505124
SB505124 | 694433-59-5 | 10mM(1mL in DMSO) | 1815.87元 |
694433-59-5, SB-505124 相關(guān)搜索:
2-溴-N-[4-氯-3-[[(3R)-1-甲基-3-吡咯烷基]氧基]苯基]-4,5-二甲氧基-苯磺酰胺 N-[2-(Dimethylamino)ethyl]-N-[[4′-[[(2-phenylethyl)amino]methyl][1,1′-biphenyl]-4-yl]methyl]-cyclopentanepropanamidedihydrochloride 6-氯-2,3-二氫-5-甲基-N-[6-[(2-甲基-3-吡啶基)氧]-3-吡啶基]-1H-吲哚-1-酰胺鹽酸鹽 3-[(3-氯-4-羥苯基)氨基]-4-(2-硝苯基)-1H-吡咯-2,5-二酮 4-(4-氟苯基)-2-(4-羥基苯基)-5-(4-吡啶基)-1H-咪唑 SB-431542 5-[2-[4-[2-(二甲基氨基)乙氧基]苯基]-5-(4-吡啶基)-1H-咪唑-4-基]-2,3-二氫-1-茚酮肟 SB269970鹽酸鹽 14-甲基-20-氧雜-5,7,14,27-四氮雜四環(huán)[19.3.1.1(2,6).1(8,12)]二十七碳-1(25),2,4,6(27),8,10,12(26),16,21,23-十烯 6-[2-(1,1-二甲基乙基)-5-(6-甲基-2-吡啶基)-1H-咪唑-4-基]喹喔啉 3-(4-氯苯基)-N-(3-甲氧基苯基)-2-丙烯酰胺 SB-705498 4-(4-氟苯基)-2-(4-甲基亞磺酰基苯基)-5-(4-吡啶基)-1H-咪唑 4-[4-(4-氟苯基)-1-(4-哌啶基)-1H-咪唑-5-基]-2-甲氧基嘧啶 伊斯平斯 MK-22062HCl LY2109761 維利帕尼
- Tyrosine Kinase Inhibitors
- Pharmaceuticals
- Intermediates & Fine Chemicals
- Heterocycles
- Aromatics
- TGF-beta
- Smad
- Inhibitors
- 化學(xué)試劑
- 抑制劑
- 藥靶配體
- 小分子抑制劑，天然產(chǎn)物
- 小分子抑制劑
- 2-[4-(1,3-苯并二氧戊環(huán)-5-基)-2-(1,1-二甲基乙基)-1H-咪唑-5-基]-6-甲基吡啶
- 抑制劑SB-505124
- SB505124 ,S2186
- 抑制劑SB-505124
- 化合物SB-505124,10 MM DMSO 溶液
- SB 505124,ALK5抑制劑
- SB505124,競(jìng)爭(zhēng)性ALK5抑制劑
- 2-(5-(苯并[D][1,3]二氧雜環(huán)戊烯-5-基)-2-(叔丁基)-1H-咪唑-4-基)-6-甲基吡啶
- 2-(4-(苯并[D][1,3]二氧雜戊環(huán)-5-基)-2-(叔丁基)-1H-咪唑-5-基)-6-甲基吡啶
- 化合物SB-505124
- SB-505124, 一種選擇性TGFΒ受體ALK4和ALK5抑制劑
- 2-[4-(1,3-苯并二惡英-5-基)-2-(1,1-二甲基乙基)-1H-咪唑-5-基]-6-甲基吡啶
- 2-[4-(1,3-苯并二氧雜環(huán)戊烷-5-基)-2-(1,1- 二甲基乙基)-1H-咪唑-5-基]-6-甲基-吡啶
- 2-[4-(1,3-苯并二惡茂-5-基)-2-(叔丁基)-1H-咪唑-5-基]-6-甲基吡啶
- 694433-59-5
- SB-505124 hydrochloride hydrate
- SB505124 ，S2186
- SB-505124, 10 mM in DMSO
- SB 505124, ALK5 inhibitor
- SB-505124 hydrochloride hydrate SB505124
- 2-[5-(Benzo[d][1,3]dioxol-5-yl)-2-(tert-butyl)-1H-imidazol-4-yl]-6-methylpyridine
- Pyridine, 2-[4-(1,3-benzodioxol-5-yl)-2-(1,1-dimethylethyl)-1H-imidazol-5-yl]-6-methyl-
- CS-872
- SB-505124, 98%, a selective inhibitor of TGFβR for ALK4, ALK5
- SB505124;SB505124
- 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrochloride hydrate
- 2-[4-(1,3-Benzodioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl]-6-methylpyridine SB505124
- 2-(4-(benzo[d][1,3]dioxol-5-yl)-2-tert-butyl-1H-imidazol-5-yl)-6-methylpyridine
- 2-[4-(1,3-Benzodioxol-5-yl)-2-(tert-butyl)-1H-imidazol-5-yl]-6-methylpyridine
- 2-[4-(1,3-Benzodioxol-5-yl)-2-(1,1- diMethylethyl)-1H-iMidazol-5-yl]-6-Methyl-pyridine
- 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-iMidazol-4-yl)-6-Methylpyridine
- SB-505124 hydrate hydrochloride
- 2-(5-Benzo[1,3]dioxol-5-yl-2-tert-butyl-3H-imidazol-4-yl)-6-methylpyridine hydrate hydrochloride