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Ruboxistaurin HCl

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Chemical Structure| 169939-93-9 同义名 : LY333531 Hydrochloride;LY333531 (hydrochloride);Ruboxistaurin;Ruboxistaurin hydrochloride
CAS号 : 169939-93-9
货号 : A280932
分子式 : C28H29ClN4O3
纯度 : 99%+
分子量 : 505.008
MDL号 : MFCD00940226
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(9.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PKCη

    PKCη, IC50:0.052 μM

  • PKCβ

    PKCβ1, IC50:4.7 nM

    PKCβ2, IC50:5.9 nM

  • PKCγ

    PKCγ, IC50:0.3 μM

  • PKCα

    PKCα, IC50:0.36 μM

  • PKCδ

    PKCδ, IC50:0.25 μM
描述 LY333531 is a selective PKCβinhibitor with IC50 values of 4.7nM and 5.9nM for PKCβI and PKCβII isozyme, respectively, 76- and 61-fold selective for inhibition of PKCβI and PKCβII in comparison to PKCα(IC50=360nM). Oral administration of 1mg/kg LY333531 for a duration of 4 weeks prevented excessive PKCβ2 activation induced by hyperglycemia and attenuated cardiac diastolic dysfunction in rats with streptozotocin-induced diabetes. Also it suppressed the decreased expression of myocardial NO, Cav-3, phosphorylated p-Akt, and p-eNOS and also mitigated the augmentation of O2-, nitrotyrosine, Cav-1, and iNOS expression).
作用机制 LY333531 is an ATP-competitive inhibitor.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.90mL

1.98mL

0.99mL

19.80mL

3.96mL

1.98mL
参考文献

[1]Jirousek MR, Gillig JR, et al. (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J Med Chem. 1996 Jul 5;39(14):2664-71.

[2]Faul MM, Gillig JR, et al. Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9.

[3]Lei S, Li H, et al. Hyperglycemia-induced protein kinase C β2 activation induces diastolic cardiac dysfunction in diabetic rats by impairing caveolin-3 expression and Akt/eNOS signaling. Diabetes. 2013 Jul;62(7):2318-28.