Heat shock protein (Hsp) inhibitor II is the active form of Hsp inhibitor I and a benzylidene lactam compound that prevents the synthesis of inducible Hsps, such as Hsp105, Hsp72, and Hsp40. Hsp inhibitor II decreases Hsp72 synthesis in vivo and reduces thermotolerance of tumors in SCC VII tumor-containing mice. At 100 μM, it inhibits the development of thermotolerance in COLO 320 DM cells. Inhibition of Hsp70 with Hsp inhibitor II in combination with amphotericin B increases susceptibility of AmB-susceptible (MICs = 0.058 versus 0.27 μg ml for combined and AmB alone, respectively) and AmB-resistant (MICs = 21.33 versus >32 μg ml for combined and AmB alone, respectively) strains of A. fumigatus.
Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibiting Ca2+ calmodulin-dependent protein kinase II.
Calmodulin-Dependent Protein Kinase II (281-309) is a synthetic peptide phosphorylatable at Thr286 by PKC, inhibiting CaM kinase II with an IC50 of 80 nM.
[Ala286]-Calmodulin-Dependent Protein Kinase II (281-302) 是CaMKII活性区域的一段,经特别设计,在第286位点上的丙氨酸替代增强了其结构.这一修饰使得[Ala286]-Calmodulin-Dependent Protein Kinase II (281-302) 成为开发更高效CaMKII抑制剂的理想候选.
GPllb is composed of a 125 Kd heavy chain that is disulfide-linked to a 23 Kd light chain. Hydropathicity analysis of the cDNA sequence indicates that GPllb is anchored to the platelet through a single transmembrane domain located within 20 amino acids of
Doxorubicin hydrochloride (Adriamycin) 属于蒽环类抗生素,是人类 DNA 拓扑异构酶 I II 抑制剂 (IC50=0.8 2.67 μM)。Doxorubicin hydrochloride 具有细胞毒性和抗肿瘤活性。Doxorubicin hydrochloride 可降低 AMPK 及其下游靶蛋白乙酰辅酶 A 羧化酶的磷酸化,还可诱导凋亡和自噬。
Bisindolylmaleimide VIII (Ro-31-7549) 是一种具有选择性和高效性的蛋白激酶 C (PKC) 抑制剂,对 PKC-α,PKC-β我,PKC-β第二,PKC-γ,PKC-ε 均具有较好的抑制作用。Bisindolylmaleimide VIII 抑制 T 细胞介导的自身免疫性疾病,可通过蛋白激酶 C 非依赖性机制增强 Fas 介导的细胞凋亡。
K-252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi. K-252a inhibits protein kinase (IC50: 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+ calmodulin-dependent kinase type II, and phosphorylase kinase, respectively).