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871543-07-6

中文名稱 871543-07-6
英文名稱 H1152, DIHYDROCHLORIDE
CAS 871543-07-6
分子式 C16H21N3O2S
分子量 319.422
MOL 文件 871543-07-6.mol
更新日期 2024/11/15 18:20:29
871543-07-6 結構式 871543-07-6 結構式

基本信息

中文別名
H-1152雙鹽酸鹽
RHO激酶抑制劑(H-1152 DIHYDROCHLORIDE)
英文別名
H-1152 2HCl
H1152, DIHYDROCHLORIDE
H 1152 DIHYDROCHLORIDE
H1152 DIHYDROCHLORIDE
4-methyl-5-[[(2S)-2-methyl-1,4-diazepan-1-yl]sulfonyl]isoquinoline
5-[[(2S)-Hexahydro-2-Methyl-1H-1,4-diazepin-1-yl]sulfonyl]-4-Methylisoquinoline
H1152P2HCl,(S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazineDihydrochloride
H1152P Dihydrochloride, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolynyl)sulfonyl]homopiperazine Dihydrochloride
所屬類別
生物化工:激動劑抑制劑

物理化學性質

熔點182-184°C
儲存條件Hygroscopic, -20°C Freezer, Under Inert Atmosphere
溶解度溶于甲醇、水
形態(tài)固體
顏色白色至灰白色
穩(wěn)定性吸濕性
871543-07-6價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2024/11/08HY-15720A871543-07-6
H-1152 dihydrochloride
871543-07-62mg950元
2024/11/08HY-15720A871543-07-6
H-1152 dihydrochloride
871543-07-65mg1800元
2024/11/08HY-15720A871543-07-6
H-1152 dihydrochloride
871543-07-610mM * 1mLin DMSO1980元

常見問題列表

生物活性
H-1152 dihydrochloride 是一種膜通透的,選擇性的 ROCK 抑制劑,Ki 值為 1.6 nM,對 ROCK2 的 IC50 值為 12 nM。
靶點

ROCKII

12 nM (IC 50 )

CaMKII

0.18 μM (IC 50 )

PKG

0.36 μM (IC 50 )

AuroraA

0.745 μM (IC 50 )

PKA

3.03 μM (IC 50 )

Src

3.06 μM (IC 50 )

PKC

5.68 μM (IC 50 )

Abl

7.77 μM (IC 50 )

MKK4

16.9 μM (IC 50 )

MLCK

28.3 μM (IC 50 )

EGFR

50 μM (IC 50 )

GSK3α

60.7 μM (IC 50 )

AMPK

100 μM (IC 50 )

P38α

100 μM (IC 50 )

體外研究

H-1152 dihydrochloride is an inhibitor of Rho-kinase, with an IC 50 of 12 nM for ROCK2. H-1152 (H-1152P) also shows less inhibitory activities against CaMKII, PKG, AuroraA, PKA, Src, PKC, MLCK, Abl, EGFR, MKK4, GSK3α, AMPK, and P38α, with IC 50 s of 0.180, 0.360, 0.745, 3.03, 3.06, 5.68, 28.3, 7.77, 50.0, 16.9, 60.7, 100, and 100 μM, respectively. H-1152 potently inhibits Rho kinase, with a K i of 1.6 nM, and slightly suppresses PKA, PKC and MLCK, with K i s of?0.63, 9.27, and 10.1 μM, respectively. H-1152 (0.1-10 μM) highly inhibits MARCKS phosphorylation, with an IC 50 value of 2.5 μM in LPA-treated cells, but shows no such obvious effects in PDBu-treated cells. H-1152 (0.5-10 μM) cuases no decreased neuronal survival. H-1152 (1, 5 or 10 μM) also exerts no alterations in the ratios of different neuronal morphologies. Furthermore, H-1152 (10 μM) increases neurite length in both BMP4 and LIF cultures.

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