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PP1

Product Name
PP1
CAS No.
172889-26-8
Chemical Name
PP1
Synonyms
PP1;PPEN;CS-716;EI 275;AGL 1872;PP1 Base;PP1 USP/EP/BP;PP1, Free Base;PP1 (AGL 1872);AGL 1872,EI 275
CBNumber
CB8472133
Molecular Formula
C16H19N5
Formula Weight
281.36
MOL File
172889-26-8.mol
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PP1 Property

Melting point:
205-207°C
storage temp. 
room temp
solubility 
DMSO: >20mg/mL
form 
powder
color 
white to off-white
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
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Safety

Hazard Codes 
Xn
Risk Statements 
22
RIDADR 
UN 2811 6.1 / PGIII
WGK Germany 
3
HS Code 
2933599590
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
P0040
Product name
PP1
Purity
≥98% (HPLC)
Packaging
5mg
Price
$211
Updated
2024/03/01
Cayman Chemical
Product number
14244
Product name
PP1 (Src Inhibitor)
Purity
≥98%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
14244
Product name
PP1 (Src Inhibitor)
Purity
≥98%
Packaging
5mg
Price
$120
Updated
2024/03/01
Sigma-Aldrich
Product number
P0040
Product name
PP1
Purity
≥98% (HPLC)
Packaging
25mg
Price
$848
Updated
2024/03/01
Cayman Chemical
Product number
14244
Product name
PP1 (Src Inhibitor)
Purity
≥98%
Packaging
10mg
Price
$172
Updated
2024/03/01
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PP1 Chemical Properties,Usage,Production

Description

PP1 (172889-26-8) is a potent and selective inhibitor of Src family tyrosine kinases. IC50=5 nM (p65lck), IC50=6 nM(P59fynT), IC50=170 nM (p60src). Cell permeable.

Chemical Properties

Off-White to Grey Solid

Uses

A highly potent and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase

Uses

PP1 has been used as:

  • an inhibitor of sarcoma (Src) family kinases (SFK) like hematopoietic cell kinase (hck) and fyn
  • a selective Src tyrosine kinase inhibitor in hippocampal neuronal cultures to test its effect on neurite growth
  • a Src-kinase blocker to test its effect on brimonidine (BMD)-induced phosphorylation in extracellular signal-activated kinases(ERK1/2)

Biological Activity

Potent inhibitor of Src-family tyrosine kinases. Inhibits p56 lck and p59 fynT (IC 50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl.

Biochem/physiol Actions

PP1 is a pyrazolopyrimidine compound that acts as a competitive inhibitor of adenosine triphosphate (ATP) binding. It also inhibits protein tyrosine kinase (PTK6) and may be useful in the therapeutic management of PTK6 positive based breast cancer malignancy.

in vitro

it was reported that pp1 specifically inhibited the expression and activity of lyn, a src family kinase, in rbl-2h3 cells. based on the immune-complex kinase assays in vitro, pp1 suppressed the activity of lyn at nanomolar levels without any effect on syk kinase activity. in contrast, phosphorylation of both syk and lyn kinases were both blocked in rbl cells. fcεri- and thy-1-mediated early and late activation events were also interrupted by pp1 in a similar mannar. moreover, pp1 was found to inhibited ret-derived oncoproteins with ic50 of 80 nm. ret/ptc3-transformed cells received pp1 treatment with a dose of 5 μm lost proliferative autonomy and showed morphological reversion. [2, 3]

in vivo

under in vivo conditions pp1 was suggested to suppress tyrosine phosphorylation and proliferation in t cells stimulated with anti-cd3 and mitogen. studies using mice tumor model also showed that pp1 upregulated the expression of the il-2 gene rather than the granulocyte macrophage colony-stimulating factor or the il-2 receptor genes. based on these, pp1 could be adopted as a useful agent to investigate the role of lck and fyn t cell activation. [2]

IC 50

a potent and selective inhibitor of src-family tyrosine kinases, with an ic50 of 5 and 6 nm respectively for p56lck and p59fynt.

storage

+4°C (desiccate)

References

1) Hanke et al. (1996), Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation; J. Biol. Chem., 271 695

PP1 Preparation Products And Raw materials

Raw materials

Preparation Products

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PP1 Suppliers

MedChemexpress LLC
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View Lastest Price from PP1 manufacturers

Career Henan Chemical Co
Product
PP1 172889-26-8
Price
US $1.00/KG
Min. Order
1KG
Purity
97%-99.9%
Supply Ability
200kg
Release date
2020-03-05

172889-26-8, PP1Related Search:


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  • C16H19N5
  • 多肽抗原
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  • Inhibitors
  • Heterocyclic Compounds
  • Bases & Related Reagent
  • Heterocycles
  • Nucleotides
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  • Protein Kinase