PP1 172889-26-8

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Molecular Weight:

281.36 PP1 is a potent and selective Src Inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.


Biological Activity


PP1 is a nano-molar inhibitor of Lck and FynT, inhibits anti-CD3-induced
protein-tyrosine kinase activity in T cells (IC50, 0.5 μM),
demonstrates selectivity for Lck and FynT over ZAP-70, and
preferentially inhibits T cell receptor-dependent anti-CD3-induced T
cell proliferation (IC50, 0. 5 μM) over non-T cell receptor-dependent
phorbol 12-myristate 13-acetate/interleu-kin-2 (IL-2)-induced T cell
proliferation. PP1 (1 μM) selectively inhibits the induction of the IL-2
gene, but not the granulocyte-macrophage colony-stimulating factor or
IL-2 receptor genes. PP1 also inhibits Src (IC50, 170 nM) and Hck (IC50,
20 nM).


PP1 is 50–100-fold less active in the inhibition of A-431
epidermal growth factor receptor autophosphorylation (IC50, 0.25 μM). [1] PP1 also inhibits Kit and Bcr-Abl tyrosine kinases with IC50 of ∼75 nM
and 1 μM, respectively. PP1 completely abrogates the proliferation of
M07e cells in response to SCF with IC50 of 0.5–1 μM. PP1 (1 μM)
inhibits SCF-induced c-Kit autophosphorylation in intact cells and
blocks the activation of mitogen-activated protein kinase and Akt.


PP1
inhibits the activity of mutant constitutively active forms of c-Kit
(D814V and D814Y) found in mast cell disorders, and triggers Apoptosis
in the rat basophilic leukemia cell line RBL-2H3 that expresses mutant
c-Kit. PP1 reduces the constitutive activation of signal transducer and
activators of transcription 5 and mitogen-activated protein kinase and
triggeres apoptosis in FDCP1 cells expressing Bcr-Abl. [2]


Protocol(Only for Reference)


Kinase Assay: [1]

Immune complex enzyme assays

The acid-treated enolase is diluted 1:20 with 1× PBS before aliquoting 100 mL/well into a Nunc 96-well high protein binding assay plate. Assay wells are then aspirated; blocked with 0.5% bovine serum, 1× PBS for 1 h at 37 ℃;and then washed five times with 300 mL of 1× PBS/well. The source of Lck is either LSTRA cells or Lck expressed in HeLa cells using a vaccinia expression system. FynT is expressed in HeLa cells using the vaccinia system. Cells (12.5× 106/mL) are lysed in lysis buffer (20 mM Tris, pH 8.0, 150 mM NaCl, 0.5% Nonidet P-40, and 23 trypsin inhibitory units/mL aprotinin), and the lysates are clarified by centrifugation at 14,000 cpm for 15 min at 4 ℃ in an Eppendorf tube. The clarified lysates are then incubated with the appropriate anti-kinase antibody at 10 μg/mL for 2 h at 4 ℃. Protein A-Sepharose beads are added to the antibody/lysate mixture at 250 μL/mL and allowed to incubate for 30 min at 4 ℃. The beads are then washed twice in 1 mL of lysis buffer and twice in 1 mL of kinase buffer (25 mM HEPES, 3 mM MnCl2, 5mM MgCl2, and 100 μM sodium orthovanadate) and resuspended to 50% (w/v) in kinase buffer. Twenty-five microliters of the bead suspension is added to each well of the enolase-coated 96-well high protein binding plate together with an appropriate concentration of compound and [γ-32P]ATP (25 μL/well of a 200 μCi/mL solution in kinase buffer). After incubation for 20 min at 20 ℃, 60 μLl of boiling 2× solubilization buffer containing 10 mM ATP is added to the assay wells to terminate the reactions. Thirty microliters of the samples is removed from the wells, boiled for 5 min, and run on a 7.5% SDS-polyacrylamide gel. The gels are subsequently dried and exposed to Kodak X-AR film. For quantitation, films are scanned using a Molecular Dynamics laser scanner, and the optical density of the major substrate band, enolase p46, is determined. In companion experiments for measuring the activity of compounds against Lck, the assay plate is washed with two wash cycles on a Skatron harvester using 50 mM EDTA, 1 mM ATP. Scintillation fluid (100 μL) is then added to the wells, and 32P incorporation is measured using a micro-β-counter.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	281.36
Formula	C16H19N5
CAS No.	172889-26-8

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	AGL 1872,EI 275

Solubility (25°C) *	In vitro	DMSO	4 mg/mL (14.21 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	1H-Pyrazolo[3,4-d]pyrimidin-4-amine, 1-(1,1-dimethylethyl)-3-(4-methylphenyl)-

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