1030203-81-6
中文名稱
2-[[1-(3-Chlorophenyl)-4-oxo-5H-pyrazolo[5,4-d]pyrimidin-6-yl]sulfanyl]propanamide
CAS
1030203-81-6
分子式
C14H12ClN5O2S
分子量
349.8
MOL 文件
1030203-81-6.mol
更新日期
2024/10/22 08:53:00
1030203-81-6 結構式
基本信息
英文別名
HS38HS-38 (HS38)
HS38 >=95% (HPLC)
NASYEGAVCTZSDO-UHFFFAOYSA-N
2-[[1-(3-Chlorophenyl)-4-oxo-5H-pyrazolo[5,4-d]pyrimidin-6-yl]sulfanyl]propanamide
2-[[1-(3-Chlorophenyl)-4,5-dihydro-4-oxo-1H-pyrazolo[3,4-d]pyrimidin-6-yl]thio]-propanamide
Propanamide, 2-[[1-(3-chlorophenyl)-4,5-dihydro-4-oxo-1H-pyrazolo[3,4-d]pyrimidin-6-yl]thio]-
常見問題列表
生物活性
HS38 是一種高效、選擇性的，ATP 競爭性的 DAPK1 和 ZIPK (DAPK3) 抑制劑，Kd 值分別為 300 nM 和 280 nM。HS38 也是 PIM3 的抑制劑，其 IC50 值為 200 nM。HS38 可用于平滑肌相關疾病的研究。靶點
Kd: 300 nM (DAPK1), 79 nM (DAPK2), 280 nM (ZIPK), IC50: 200 nM (DAPK1), 200 nM (PIM3)
體外研究
HS38 displays high affinity toward DAPK2, with a K
d
of 79 nM. DAPK2 is not implicated in smooth muscle contractility.
HS38 significantly reduces relative RLC20 phosphorylation in both the basal and sphingosine 1-phosphate (S1P) activated states in human aortic SM cells.
HS38 reduces contractile forces generated by intact mouse aorta in aortic tissue.
HS38 reduces the contractile force, RLC20 phosphorylation, and MYPT1 phosphorylation in Ca
2+
-sensitized rabbit ileum.
Western Blot Analysis
| Cell Line: | CA-VSMCs |
| Concentration: | 10 μM |
| Incubation Time: | 40 minutes |
| Result: | Reduced relative RLC20 phosphorylation in both the basal and S1P activated states. |