2. NPC-15437

NPC-15437 是一种选择性 PKC 抑制剂，其 IC50 为 19 µM。NPC-15437 竞争性抑制佛波酯诱导的 (Ki 为 5 µM) 和磷脂丝氨酸诱导的 (Ki 为 12 µM) PKC 活性。NPC-15437 不抑制 cAMP 依赖性或钙/钙调蛋白依赖性蛋白激酶。NPC-15437 可增强 TRAIL 诱导的非小细胞肺癌和髓母细胞瘤细胞的细胞死亡。NPC-15437 可用于非小细胞肺癌、髓母细胞瘤和神经系统疾病的研究。

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NPC-15437

NPC-15437 Chemical Structure

CAS No. : 136449-85-9

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NPC-15437 的其他形式现货产品:

Customer Review

Other Forms of NPC-15437:

NPC-15437 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NPC-15437 is a selective PKC inhibitor with an IC50 of 19 µM. NPC-15437 competitively inhibits phorbol ester- (Ki of 5 µM) and phosphatidylserine-induced (Ki of 12 µM) PKC activity. NPC-15437 does not inhibits cAMP-dependent or calcium/calmodulin-dependent protein kinases. NPC-15437 augments TRAIL-induced cell death in non-small cell lung cancer and medulloblastoma cells. NPC-15437 can be used for the research of non-small cell lung cancer, medulloblastoma, and neurological disease[1][2][3][4].

IC50 & Target

PKC

19 μM (IC50)

体外研究
(In Vitro)

NPC-15437 (4-10 μM；24-48 h) 可增强 TRAIL 诱导的 A549 和 DAOY 细胞死亡及线粒体膜电位丧失 (48 小时时细胞死亡率分别高达 69% 和 76%)，但对 TNFα 无增敏作用；该效应在 A549 细胞中依赖于半胱天冬酶[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NPC-15437 相关抗体:
体内研究
(In Vivo)

NPC-15437 (0.1-1.0 μg/0.5 μL/侧；内侧伏隔核注射；在第 1、3、5、7 天的条件化训练期间给药) 可阻断精神物质诱导的雄性 Wistar 大鼠 (225-250 g) 与奖赏相关学习有关的条件性位置偏爱[1]。
NPC-15437 (0.01-10 mg/kg；i.p.；单次) 在雄性瑞士小鼠 (2 月龄，30-40 g) 记忆障碍模型中，可选择性诱导 Y 迷宫主动回避任务时间成分保留的剂量依赖性缺陷[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats (male, 225-250 g) bearing reward-related learning[1]
Dosage: 0.1, 0.5, 1.0 μg/0.5 μL/side
Administration: intra-NAc; during conditioning sessions on days 1, 3, 5, 7
Result: Dose-dependently blocked amphetamine-induced conditioned place preference: the 0.1 μg dose did not block the preference (significant increase in drug-paired compartment time from pre-conditioning to test), the 0.5 μg dose partially blocked it (no significant increase in drug-paired compartment time), and the 1.0 μg dose fully blocked it (no significant increase in drug-paired compartment time).
Did not produce a place preference or aversion when administered alone (1.0 μg, no significant change in drug-paired compartment time from pre-conditioning to test).
Animal Model: Swiss mice (male, 2 months old, 30-40 g)[2]
Dosage: 0.01, 0.1, 1, 10 mg/kg (post-training); 1 mg/kg (pre-training and pre-retention for some groups)
Administration: i.p.; single injection (immediately post-training, 30 minutes pre-training, 48 hours later pre-retention for some groups)
Result: Significantly impaired retention of the temporal component with more avoidance errors versus controls at 0.1, 1, 10 mg/kg post-training; Made more avoidance errors than discrimination errors at 1 and 10 mg/kg post-training; Did not affect acquisition performance with 1 mg/kg pre-training; Impaired temporal component retention when 1 mg/kg given before acquisition regardless of pre-retention injection.
分子量

438.70

Formula

C25H50N4O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NPC-15437 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NPC-15437136449-85-9NPC15437NPC 15437conventional PKCcPKCTRAILDAOYneurological diseasenovel PKCA549non-small cell lung cancerPKCεnPKCmale Wistar ratsTNFαY-maze active avoidance taskmicePKCratsmedulloblastomamale Swiss miceprotein kinase CInhibitorinhibitorinhibit

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