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Cat. No.: HY-139467

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PF-04577806

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.

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CAS No.: 1072100-81-2
화학식: C₂₆H₃₇N₇O₃
분자량:495.62

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

PF-04577806 Chemical Structure

CAS No.: 1072100-81-2

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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)

All PKC Isoforms :

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].

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

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.

Chemical Information

CAS No. 1072100-81-2
분자량 495.62
화학식 C₂₆H₃₇N₇O₃
SMILES

O=C(C1=CC=CC=N1)NC2=NNC3=C2CN(C(N4[C@H](CN([C@@H](C4)C)CC5CCOCC5)C)=O)C3(C)C
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Grant S, et, al. Discovery of a novel class of targeted kinase inhibitors that blocks protein kinase C signaling and ameliorates retinal vascular leakage in a diabetic rat model. Eur J Pharmacol. 2010 Feb 10;627(1-3):16-25. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
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PF-04577806

All PKC Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

PF-04577806 Related Classifications

HY-139467 Related Classifications