pka/pkg

HA-1004是一种 PKG，PKA，PKC 和 MLC 的激酶抑制剂。

H-1152 dihydrochloride (H-1152 2HCl) 是 Rho 相关蛋白激酶 (ROCK) 的特异性抑制剂，IC50 为 12 nM，Ki 为 1.6 nM。 H-1152 dihydrochloride 抑制 PKA、PKC、PKG、Aurora A 和 CaMKII，IC50 值分别为 3.03 μM、5.68 μM、0.360 μM、0.745 μM 和 0.180 μM。

Fasudil (HA-1077) 是一种非特异性 RhoA ROCK 抑制剂，也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用，ROCK1 的 Ki 值为 0.33 μM，ROCK2 和 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。

Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA ROCK 抑制剂，也抑制蛋白激酶，对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。

H-89 dihydrochloride (5-Isoquinolinesulfonamide) 是一种选择性 cAMP 依赖性蛋白激酶A(PKA) 抑制剂，IC50值为 48 nM。也可轻微抑制 PKG、PKC 和酪蛋白激酶活性。

HA-100 是蛋白激酶和ROCK 抑制剂，抑制PKG，PKA，PKC 和MLC 激酶的IC50值分别为 4、8、12 和 240 μM。

KT5823 是一种具有选择性和有效性的 cGMP 依赖性蛋白激酶 (PKG) 抑制剂，对 PKA 和 PKG 有抑制作用。KT5823 在甲状腺细胞中通过调节碘化钠交感蛋白的表达和活性来增加甲状腺刺激激素诱导的 (Na+ I- symporter) NIS 表达和碘离子摄取。 KT5823 诱导细胞凋亡。

HA-100 hydrochloride is a powerful protein kinase inhibitor, exhibiting IC50 values of 4 μM, 8 μM, 12 μM, and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC), and MLC-kinase, respectively. Additionally, HA-100 hydrochloride is utilized as a ROCK inhibitor.

Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].

Fasudil hydrochloride semihydrate 是一种有用的有机化合物，可用于生命科学领域的相关研究，其产品编号为 T64582。

Fasudil hydrochloride hydrate is an HCl salt of Fasudil -- a Rho-kinase (ROCK) inhibitor that has been shown to be effective in hindering the development of mature Cerebral Cavernous Malformation (CCM) lesions as well as reducing portal venous pressure in cirrhotic rats.

H-1152 是一种膜通透的选择性ROCK 抑制剂，Ki 为 1.6 nM，对ROCK2的IC50为 12 nM。

2-Chloroadenosine 5-triphosphate (2-chloro ATP), an analog of ATP and adenine nucleotide, functions as an antagonist of the purinergic P2Y1 receptor, inhibiting ADP-induced intracellular calcium mobilization in Jurkat cells with a Ki value of 2.3 µM. Additionally, 2-chloro ATP acts as an agonist of purinergic P2X receptors, demonstrated by inducing inward currents in HEK293 cells expressing either human bladder smooth muscle or rat PC12 receptor forms, with EC50 values of 0.5 and 2.5 µM, respectively. It also triggers relaxation in precontracted isolated guinea pig taenia caeci strips in a concentration-dependent fashion. Furthermore, 2-chloro ATP has been employed in research to investigate the substrate specificity of cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG.

Fasudil mesylate (HA-1077; AT877) 是一种口服有效的非特异性RhoA ROCK抑制剂，同时能够抑制多种蛋白激酶。该化合物对ROCK1的Ki值为0.33 μM，对ROCK2、PKA、PKC和PKG的IC50值分别为0.158 μM、4.58 μM、12.30 μM和1.650 μM。此外，Fasudil mesylate 还作为Ca2+通道拮抗剂和血管扩张剂，表现出良好的药效。

8-pCPT-5'-AMP 作为 5'-AMP 的类似物，兼具亲脂性，能激活 PKA、PKG 及 Epac（cAMP 激活的交换蛋白）。

Sp-8-pCPT-cGMPS 是一种对CNG通道具有高激活作用的化合物(cyclic guanosine monophosphate-gated channel)，并且作为 PKG (I α、I β 和 II 型) 以及 PKA II 型的疏水性活化剂显示出色的细胞膜穿透能力和对磷酸二酯酶的高稳定性。此外，Sp-8-pCPT-cGMPS 还常用于探究 cGMP 在神经可塑性及突触功能中的调控机制。

Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by