2. Protein Tyrosine Kinase/RTK Epigenetics TGF-beta/Smad
  3. SHP2 PKC
  4. PF-04577806

PF-04577806 是一种有效、选择性和 ATP 竞争性的 PKC 抑制剂。PF-04577806 对 PKCα，PKCβI，PKCβII，PKCγ 和 PKCθ 显示出有效的抑制活性，IC50 值分别为 2.4 nM、8.1 nM、6.9 nM、45.9 nM 和 29.5 nM。PF-04577806 可以逆转糖尿病大鼠的视网膜血管渗漏。

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PF-04577806 Chemical Structure

PF-04577806 Chemical Structure

CAS No. : 1072100-81-2

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PF-04577806 相关抗体

Top Publications Citing Use of Products

查看 PKC 亚型特异性产品:

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKCι

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats[1].

IC50 & Target[1]

PKCα

2.4 nM (IC50)

PKCβI

8.1 nM (IC50)

PKCβII

6.9 nM (IC50)

PKCγ

45.9 nM (IC50)

PKCδ

586 nM (IC50)

PKCθ

29.5 nM (IC50)

PKCε

522 nM (IC50)

体外研究
(In Vitro)

PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC50 of 0.18 μM[1].
PF-04577806 (0.12-10 μM; pretreated for 60 min) inhibits phorbol myristate acetate-stimulated phosphorylation of ERK1/2 in Jurkat cells, with an IC50 of 0.28 μM[1].
PF-04577806 (0.001-10 μM; pretreated for 1 h) inhibits phosphorylation of SHP2 in HEK293 cells, with an IC50 of 5.8 nM. PF-04577806 concentration-dependently inhibits interleukin 8 release from phorbol myristate acetate-stimulated HEK293 cells, with an IC50 of 0.12 μM[1].
PF-04577806 (1 μM; 48 h) shows low cytotoxicity against human umbilical vein endothelial cells with remaining cell viability at 100.5% viable[1].

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

PF-04577806 相关抗体:

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 0, 0.12, 0.37, 1.11, 3.33, 10.0 μM
Incubation Time: Pretreated for 1 hours
Result: Showed a dose-dependent decrease in phospho-ERK1/2 but not total ERK1/2.
分子量

495.62

Formula

C26H37N7O3
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

PF-04577806 相关分类

  • 摩尔计算器

  • 稀释计算器

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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× = ×
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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:

PF-045778061072100-81-2PF04577806PF 04577806SHP2PKCSrc homology phosphatase 2PTPN11Protein kinase CretinalvascularleakagediabeticInhibitorinhibitorinhibit

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产品名称：
PF-04577806
目录号：
HY-139467
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