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Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是蛋白激酶 C(PKC) 的同工酶选择性抑制剂,竞争性且可逆地抑制 PKCβI 和 PKCβII,IC50 值分别为 4.7 和 5.9 nM。
Ruboxistaurin hydrochloride (LY 333531 hydrochloride) 是蛋白激酶 C(PKC) 的同工酶选择性抑制剂,竞争性且可逆地抑制 PKCβI 和 PKCβII,IC50 值分别为 4.7 和 5.9 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 453 | 现货 | |
2 mg | ¥ 659 | 现货 | |
5 mg | ¥ 1,470 | 现货 | |
10 mg | ¥ 2,490 | 现货 | |
25 mg | ¥ 4,260 | 现货 | |
50 mg | ¥ 6,070 | 现货 | |
100 mg | ¥ 8,370 | 现货 | |
500 mg | ¥ 16,700 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,680 | 现货 |
产品描述 | Ruboxistaurin hydrochloride (LY 333531 hydrochloride) is an Isozyme-selective inhibitor of protein kinase C (PKC); competitively and reversibly inhibits PKCβI and PKCβII (IC50 values are 4.7 and 5.9 nM respectively). Selective for PKCβ over other PKC isozymes (IC50values are 0.052, 0.25, 0.30, 0.36, 0.60 and >100 μM for PKCη, -δ, -γ, -α, -ε and -ζ respectively). Exhibits selectivity for PKC over other ATP-dependent kinases, including protein kinase A, casein kinase and src). |
靶点活性 | PKCβ1:4.7 nM, PKCγ:0.3 μM, PKCδ:0.25 μM, PKCβ2:5.9 nM, PKCη:0.052 μM |
体外活性 | Ruboxistaurin显著降低HUVEC存活率,并且与AGEs组相比,Ruboxistaurin在促进HUVEC细胞凋亡方面的效果显著增强。PKC-beta的阻断上调Bax和Bad蛋白表达,下调Bcl-2蛋白表达。此外,Ruboxistaurin降低Bcl-2/Bax比率。Ruboxistaurin还能进一步促进AGEs诱导的内皮细胞凋亡。Bax、Bad的表达增加和Bcl-2的表达减少以及Bcl-2/Bax比率降低与凋亡过程相关[3]。 |
体内活性 | 在糖尿病大鼠中观察到TGF-b1、Smad2和Smad3 mRNA表达的显著上调,而通过给予ruboxistaurin治疗后,这一现象得到了缓解。 |
细胞实验 | HUVECs are seeded into 96-well plates in low glucose DMEM with 10% FBS for 12 h. Afterwards, HUVECs are starved for 12 h and incubated with BSA (200 μg/ml), AGEs (200 μg/ml) and LY333531 (200 nM)+AGEs (200 μg/ml) for 48 h. Then, the medium is replaced with 0.5 mg/ml MTT and at 37 ?C in a 95% air/5% CO2 incubator for 4 h. Finally, the medium containing MTT is aspirated and replaced by dimethyl sulphoxide (DMSO). OD is measured with a Microplate spectrophotometer. AGEs:advanced glycation end products.(Only for Reference) |
别名 | 芦布妥林, Ruboxistaurin, LY333531 HCl, LY 333531 hydrochloride |
分子量 | 505.01 |
分子式 | C28H28N4O3·HCl |
CAS No. | 169939-93-9 |
Smiles | Cl.CN(C)CC1CCn2cc(C3=C(C(=O)NC3=O)c3cn(CCO1)c1ccccc31)c1ccccc21 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (108.91 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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