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AB120859

PP 1, Src family tyrosine kinase inhibitor

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(1 Publication)

MW 281.36 Da, Purity >98%. Potent Src family tyrosine kinase inhibitor. Inhibits a multitude of kinases (IC50 values are 0.05 (LCK), 0.52 (CSK), 0.64 (p38α) and 1.06 (CK1δ) μM). Inhibits Bcr-Abl kinase and induces apoptosis.

View Alternative Names

ABL, ABL proto oncogene 1 non receptor tyrosine kinase, ABL1_HUMAN, AI838772, ASV, AW259666, AW493413, Abelson murine leukemia viral oncogene homolog 1, Abelson tyrosine protein kinase 1, Angiopoietin-1 receptor, Avian erythroblastic leukemia viral (v erb b) oncogene homolog, Avian sarcoma virus, Bcr/c abl oncogene protein, C SRC, C ret, C syn protooncogene, C-SRC kinase, C-kit ligand, CARD 3, CARD carrying kinase, CARD containing ICE associated kinase, CARD containing interleukin 1 beta converting enzyme (ICE) associated kinase, CARD-containing IL-1 beta ICE-kinase, CARD-containing interleukin-1 beta-converting enzyme-associated kinase, CARDIAK, CD 140B, CD117, CD140A, CD140a antigen, CD140b antigen, CD202b, CD202b antigen, CD309, CD309 antigen, CDHF 12, CDHR16, CDNA FLJ14219 fis clone NT2RP3003800 highly similar to Rattus norvegicus tyrosine protein kinase pp60 c src mRNA, CKI-delta, CKId, CLARP kinase, CSAID Binding Protein 1, CSAID-binding protein, CSBP, CSBP 1, CSBP 2, CSK_HUMAN, CSNK 1D, CSPB1, CYTOPLASMIC TYROSINE KINASE, Cadherin family member 12, Cadherin related family member 16, Casein Kinase 1 delta, Casein kinase I delta isoform, Casein kinase I isoform delta, Cell growth inhibiting protein 40, Cell proliferation inducing protein 61, Cellular Yes 1 protein, Csaids binding protein, Csk A, Cytokine suppressive anti-inflammatory drug-binding protein, EC 2.7.10.1, EC 2.7.10.2, EGFR_HUMAN, ELKS Fusion gene, ERBB, ERBB1, EXIP, Endothelial tyrosine kinase, Endothelium specific receptor tyrosine kinase 2, Epidermal growth factor receptor, Epidermal growth factor receptor (avian erythroblastic leukemia viral (v erb b) oncogene homolog), Epidermal growth factor receptor (erythroblastic leukemia viral (v erb b) oncogene homolog avian), Errp, FK506 binding protein 12 rapamycin associated protein 1, FK506 binding protein 12 rapamycin associated protein 2, FK506-binding protein 12-rapamycin complex-associated protein 1, FKBP rapamycin associated protein, FKBP12-rapamycin complex-associated protein, FKBP12-rapamycin complex-associated protein 1, FLJ11090, FLJ44809, FLK-1, FLK1, mouse, homolog of, FRAP, FRAP1, FRAP2, FYN oncogene related to SRC FGR YES, FYN_HUMAN, Fetal liver kinase 1, GIG 30, Growth inhibiting gene 30, HCKID, HER1, HSCR 1, HsT441, Hyk, IMD22, JTK7, KC1D_HUMAN, KIT ligand, KIT oncogene, KIT proto oncogene receptor tyrosine kinase, KIT_HUMAN, KRD1, Kdr, Kinase insert domain receptor, Kinase insert domain receptor (a type III receptor tyrosine kinase), LCK proto-oncogene, Src family tyrosine kinase, LCK_HUMAN, LSK, Lck p56, Leukocyte C-terminal Src kinase, Ly73, Lymphocyte cell-specific protein-tyrosine kinase, Lymphocyte specific protein tyrosine kinase, MAP kinase 14, MAP kinase MXI2, MAP kinase p38 alpha, MAPK 14, MAX-interacting protein 2, MEN2A, MEN2B, MGC104252, MGC112732, MGC112926, MGC117393, MGC154049, MGF, MK14_HUMAN, MTC 1, MTOR_HUMAN, Mammalian target of rapamycin, Mast cell growth factor receptor, Mast/stem cell growth factor receptor Kit, Mechanistic target of rapamycin, Membrane associated protein tyrosine kinase, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase p38 alpha, Multiple endocrine neoplasia and medullary thyroid carcinoma 1, Mxi 2, NISBD2, Neuronal CSRC tyrosine specific protein kinase, Neuronal SRC, Neuronal proto-oncogene tyrosine-protein kinase Src, OKT3 induced calcium influx regulator, OTTHUMP00000001983, OTTHUMP00000174476, OTTHUMP00000174477, Oncogen ERBB, Oncogene RET, Oncogene SRC, Oncogene lck, P150, P38, PBT, PDGF Receptor alpha + beta, PDGF-R-alpha, PDGF-R-beta, PDGFR 2, PDGFRA, PDGFRB, PIG61, PRKM14, PRKM15, PTC, Piebald trait protein, Platelet derived growth factor receptor alpha, Platelet derived growth factor receptor beta, Protein YT16, Protein kinase CK1 delta, Protein tyrosine kinase fyn, Protein-tyrosine kinase CYL, Protein-tyrosine kinase receptor flk-1, Proto oncogene tyrosine protein kinase, Proto oncogene tyrosine protein kinase ABL1, Proto oncogene tyrosine protein kinase Kit, Proto oncogene tyrosine protein kinase LCK, Proto oncogene tyrosine protein kinase YES, Proto oncogene tyrosine protein kinase fyn, Proto-oncogene Lck, Proto-oncogene Syn, Proto-oncogene c-Abl, Proto-oncogene c-ErbB-1, Proto-oncogene c-Fyn, Proto-oncogene c-Kit, Proto-oncogene c-Ret, Proto-oncogene c-Src, Proto-oncogene c-Yes, Proto-oncogene tyrosine-protein kinase Src, Proto-oncogene tyrosine-protein kinase receptor ret, Protooncogene SRC, Protooncogene SRC Rous sarcoma, RAFT1, RAPT1, RET ELE1, RET transforming sequence, RET51, RET9, RET_HUMAN, RICK, RIP-like-interacting CLARP kinase, RIPK2_HUMAN, RK, RP24-311F12.2, Rapamycin and FKBP12 target 1, Rapamycin associated protein FRAP2, Rapamycin target protein, Rapamycin target protein 1, Receptor interacting protein (RIP) like interacting caspase like apoptosis regulatory protein (CLARP) kinase, Receptor interacting serine threonine kinase 2, Receptor tyrosine-protein kinase ErbB-1, Receptor-interacting protein 2, Receptor-interacting serine/threonine-protein kinase 2, Ret Proto oncogene, SA7, SAPK2A, SCAN1, SCF Receptor, SCFR, SRC Oncogene, SRC proto oncogene non receptor tyrosine kinase, SRC_HUMAN, SYN, Serine/threonine-protein kinase mTOR, Soluble TIE2 variant 1, Soluble TIE2 variant 2, Species antigen 7, Src yes related novel gene, Src-like kinase, Src/yes related novel, Steel Factor Receptor, Stem cell factor receptor, Stress-activated protein kinase 2a, T cell-specific protein-tyrosine kinase, T lymphocyte specific protein tyrosine kinase p56lck, TEK tyrosine kinase endothelial, TIE2_HUMAN, TNFRSF, TYDP, TYDP1_HUMAN, Tek, Tunica interna endothelial cell kinase, Tyr-DNA phosphodiesterase 1, Tyrosine kinase growth factor receptor, Tyrosine kinase p59fyn T, Tyrosine kinase p59fyn(T), Tyrosine kinase pp60c src, Tyrosine kinase with Ig and EGF homology domains-2, Tyrosine protein kinase SRC 1, Tyrosine-protein kinase ABL1, Tyrosine-protein kinase CSK, Tyrosine-protein kinase Fyn, Tyrosine-protein kinase Kit, Tyrosine-protein kinase Lck, Tyrosine-protein kinase RIPK2, Tyrosine-protein kinase Yes, Tyrosine-protein kinase receptor TEK, Tyrosine-protein kinase receptor TIE-2, Tyrosyl-DNA phosphodiesterase 1, UNQ277/PRO314/PRO34092, Urogastrone, V src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog (avian), VEGFR, VEGFR-2, VGFR2_HUMAN, VMCM, VMCM 1, Vascular endothelial growth factor receptor 2, Venous malformations multiple cutaneous and mucosal, Viral oncogene yes 1 homolog 1, Wa5, YES proto oncogene 1, Src family tyrosine kinase, YES1 proto oncogene, Src family tyrosine kinase, YES_HUMAN, YT 16, Yamaguchi sarcoma oncogene, Yes 1, bcr/abl, c ABL, c Yes, c abl oncogene 1 non receptor tyrosine kinase, c abl oncogene 1 receptor tyrosine kinase, c-Kit, c-src tyrosine kinase, dJ576K7.1 (FK506 binding protein 12 rapamycin associated protein 1), erb-b2 receptor tyrosine kinase 1, hTIE 2, hydroxyaryl-protein kinase, mENA, p140 TEK, p145 c-kit, p38 ALPHA, p38 MAP kinase, p38 MAPK, p38 mitogen activated protein kinase, p38alpha Exip, p56(LSTRA) protein tyrosine kinase, p56-LCK, p59-Fyn, p60-Src, p60c-src, p61-Yes, pp58 lck, pp60c-src, soluble KIT variant 1, soluble VEGFR2, tek tyrosine kinase, tyrosine-protein kinase receptor ret, v abl, v abl Abelson murine leukemia viral oncogene homolog 1, v kit Hardy Zuckerman 4 feline sarcoma viral oncogene like protein, v src avian sarcoma (Schmidt Ruppin A2) viral oncogene homolog, v src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog avian, v yes 1 Yamaguchi sarcoma viral oncogene homolog 1, v-erb-b Avian erythroblastic leukemia viral oncogen homolog, v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog, wa2, zgc:154049

3 Images
Functional Studies - PP 1, Src family tyrosine kinase inhibitor (AB120859)
  • FuncS

Unknown

Functional Studies - PP 1, Src family tyrosine kinase inhibitor (AB120859)

ab11512 staining E cadherin in SW480 cells treated with PP1 (ab120859), by ICC/IF. Increase of E cadherin expression correlates with increased concentration of PP1, as described in literature.
The cells were incubated at 37°C for 24h in media containing different concentrations of ab120859 (PP1) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab11512 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight® 488 anti-rat polyclonal antibody (ab98386) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.

Functional Studies - PP 1, Src family tyrosine kinase inhibitor (AB120859)
  • FuncS

PubMed

Functional Studies - PP 1, Src family tyrosine kinase inhibitor (AB120859)

Herpes simplex virus-2 regulates ER-alpha and HA via Src kinase in ECT-1 cells.

(Panel B) ECT-1 cells were treated with vehicle (DMSO) or Src inhibitor (SKI/PP1). ER-alpha was quantified using densitometry following Western blot analysis (ANOVA with Tukey's multiple comparison; NT vs VEH, n.s.; NT vs SKI/PPI, p< .02; VEH vs SKI/PPI, p< .01).

McGee et al PLoS One. 2017 Nov 30;12(11):e0188645. doi: 10.1371/journal.pone.0188645. eCollection 2017. Fig 6. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/

Chemical Structure - PP 1, Src family tyrosine kinase inhibitor (AB120859)
  • Chemical Structure

Lab

Chemical Structure - PP 1, Src family tyrosine kinase inhibitor (AB120859)

2D chemical structure image of ab120859, PP 1, Src family tyrosine kinase inhibitor

Key facts

CAS number

172889-26-8

Purity

>98%

Form

Solid

form

Molecular weight

281.36 Da

Molecular formula

C<sub>1</sub><sub>6</sub>H<sub>1</sub><sub>9</sub>N<sub>5</sub>

PubChem

1400

Nature

Synthetic

Solubility

Soluble in DMSO to 25 mM

Soluble in ethanol to 10 mM

Biochemical name

1-(tert-Butyl)-3-(p-tolyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine

Biological description

Potent Src family tyrosine kinase inhibitor. Inhibits a multitude of kinases (IC50 values are 0.05 (LCK), 0.52 (CSK), 0.64 (p38α) and 1.06 (CK1δ) μM). Inhibits Bcr-Abl kinase and induces apoptosis.

Canonical smiles

CC1=CC=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)(C)C

InChi

InChI=1S/C16H19N5/c1-10-5-7-11(8-6-10)13-12-14(17)18-9-19-15(12)21(20-13)16(2,3)4/h5-9H,1-4H3,(H2,17,18,19)

InChiKey

ZVPDNRVYHLRXLX-UHFFFAOYSA-N

IUPAC Name

1-tert-butyl-3-(4-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The biological targets p38 mTOR Src RIP2 CSNK1D Ret VEGF Receptor 2 c-Kit Fyn EGFR Lck TDP1 ABL1 PDGFR alpha + beta TIE2 and Yes1 comprise a group of proteins and kinases with significant mechanical functions in cellular processes. These targets play roles in signal transduction growth regulation and cellular differentiation. They have diverse alternate names; for example VEGF Receptor 2 is also known as KDR or Flk-1 while c-Kit is referred to as CD117. Many of these proteins are expressed in various tissues with high concentrations often found in tumor cells or critical organ systems. The masses of these proteins vary with some like mTOR being around 289 kDa reflecting their complex structures.
Biological function summary

These proteins have key roles in cellular communication and homeostasis often by activating or inhibiting signaling pathways. For instance mTOR (mechanistic target of rapamycin) is a central component of the mTOR complex which regulates cell growth and metabolism. Src (proto-oncogene tyrosine-protein kinase Src) influences cell division and adhesion. VEGF Receptor 2 through angiogenic signaling modulates blood vessel formation. Their presence within multiprotein complexes often facilitates or modulates downstream signaling effectively integrating external stimuli with cellular responses.

Pathways

A significant number of these proteins are involved in the PI3K/AKT/mTOR and MAPK/ERK pathways essential for controlling cell proliferation survival and apoptosis. For example mTOR interacts closely with AKT and PI3K regulating cell growth and survival. Similarly the MAPK pathway involving targets like Src and p38 contributes to cellular responses to stress and growth factors. These pathways highlight intricate relationships among these proteins creating a network of interactions that affect numerous cell functions.

These proteins show strong links to cancer and inflammatory conditions. Abnormal activity of mTOR VEGF Receptor 2 and EGFR is frequently associated with various cancers where they contribute to uncontrolled cell growth and resistance to apoptosis. Src and Lck have connections to autoimmune diseases with dysregulated signaling leading to chronic inflammation and tissue damage. Through these pathological contexts the roles of these proteins in disease development are further emphasized impacting drug targeting strategies and therapeutic interventions.

Product protocols

Publications (1)

Recent publications for all applications. Explore the full list and refine your search

PloS one 12:e0188645 PubMed29190738

2017

Cervical HSV-2 infection causes cervical remodeling and increases risk for ascending infection and preterm birth.

Applications

Unspecified application

Species

Unspecified reactive species

Devin McGee,Arianna Smith,Sharra Poncil,Amanda Patterson,Alison I Bernstein,Karen Racicot
View all publications

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