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Chemical Structure| 172889-26-8 Chemical Structure| 172889-26-8

Structure of PP1
CAS No.: 172889-26-8

Chemical Structure| 172889-26-8

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PP1 is a selective inhibitor of Src and Lck/Fyn with IC50 of 5 nM, 6 nM, respectively.

Synonyms: EI 275; AGL 1872; PP1 (Src Inhibitor)

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Product Details of PP1

CAS No. :172889-26-8
Formula : C16H19N5
M.W : 281.36
SMILES Code : NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(C)C=C3)=NC=N1
Synonyms :
EI 275; AGL 1872; PP1 (Src Inhibitor)
MDL No. :MFCD01076570
InChI Key :ZVPDNRVYHLRXLX-UHFFFAOYSA-N
Pubchem ID :1400

Safety of PP1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Related Pathways of PP1

RTK

Isoform Comparison

Biological Activity

Target
  • Fyn

    Fyn, IC50:6 nM

  • Lck

    LCK, IC50:5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
NRK-49F cells 1 μM, 2 μM, 5 μM 24 hours PP1 dose-dependently inhibited TGF-β1-induced expression of α-SMA, fibronectin, and collagen I, with maximum inhibition at 5 μM. PMC4824676
HUES8, HUES49, H9, iPSC 11b hPSCs 25 µM 24 hours PP1 treatment significantly improved the differentiation capacity of multiple hPSC lines, increasing the percentage and total number of Brachy+ cells. PMC4586752
HUES6 hPSCs 25-50 µM 24 hours PP1 treatment significantly improved the differentiation capacity of HUES6 hPSCs, increasing the percentage and total number of Brachy+ cells in a dose-dependent manner. PMC4586752
H460 non-small cell lung cancer cells 5 μM 48 hours PP1 inhibited the proliferation, migration, and invasion of H460 cells and reversed the morphine-induced antiapoptotic effect PMC8613927

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Unilateral ureteral obstruction (UUO) model Intraperitoneal injection 2 mg/kg Once daily for 7 or 14 days PP1 significantly reduced ECM deposition in fibrotic kidneys, inhibited the expression of fibronectin, α-SMA, and collagen I, and attenuated renal interstitial fibrosis. PMC4824676

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00797797 Fibromyalgia Phase 3 Completed - -
NCT02431702 Schizophrenia ... More >> Psychotic Disorders Less << Phase 3 Active, not recruiting October 26, 2019 -
NCT03072355 Healthy Volunteers Not Applicable Completed - Brazil ... More >> Carlos Pastre, PhD Presidente Prudente, Brazil, +551832295528 Less <<
NCT02185339 Laparoscopic Renal Surgery ... More >> Laparoscopy Muscle Relaxation Less << Phase 4 Completed - Korea, Republic of ... More >> Seoul St. Mary's Hospital Seoul, Korea, Republic of, 137-701 Less <<
NCT03206359 - Completed - -
NCT00797797 - Completed - -
NCT01406496 Type 1 Diabetes Mellitus Not Applicable Unknown December 2013 Israel ... More >> Pediatric Endocrinology Unit, Kaplan Medical Center Recruiting Rehovot, Israel, 76100 Contact: Amnon Zung, MD    972-8-9441260    amnon_z@clalit.org.il    Principal Investigator: Amnon Zung, MD          Sub-Investigator: Nitza Vazana, RN          Sub-Investigator: Lilach Hofi, R.Nutr Less <<
NCT02185339 - Completed - -
NCT01047605 Healthy Phase 1 Completed - Germany ... More >> Neurocode AG Wetzlar, Germany, D-35578 Less <<
NCT01515423 Schizophrenia Phase 3 Completed - -
NCT01515423 - Completed - -
NCT00791843 Congestive Heart Failure Phase 2 Completed - United States, Massachusetts ... More >> Massachusetts General Hospital/ Geriatric Research Boston, Massachusetts, United States, 02114 Less <<
NCT03713658 Schizophrenia Phase 4 Recruiting April 10, 2020 Rwanda ... More >> CARAES Ndera Neuro-Psychiatric Hospital Recruiting Kigali, Rwanda, 423 University Teaching Hospital of Kigali Not yet recruiting Kigali, Rwanda, 655 Ruhengeri Referral Hospital, Public Hospital Recruiting Musanze District, Rwanda, 57 Kibungo Referral Hospital Not yet recruiting Ngoma District, Rwanda, 10 Less <<
NCT03666715 - Recruiting August 15, 2019 Portugal ... More >> Neurobios , Instituto De Neurociências Recruiting Porto, Portugal, Portugal, 4200 - 117 Less <<
NCT02713282 Schizophrenia Phase 3 Completed - -
NCT03345342 Schizophrenia Phase 3 Recruiting August 31, 2020 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.54mL

7.11mL

3.55mL

References

 

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