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MW 301.77 Da, Purity >98%. Inhibitor of the Src family of kinases. Inhibits Src and Lck kinase (IC50 values are 36 and 31 nM, respectively). Also shown to inhibit RIP2 and CK1δ (IC50 values are 19 and 41 nM, respectively).

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Images

Chemical Structure - PP2, Src and RIP2 kinase inhibitor (AB120308), expandable thumbnail
  • Functional Studies - PP2, Src and RIP2 kinase inhibitor (AB120308), expandable thumbnail

Publications

Key facts

CAS number

172889-27-9

Purity

> 98%

Form

Solid

Molecular weight

301.77 Da

Molecular formula

C15H16ClN5

PubChem identifier

4878

Nature

Synthetic

Alternative names

Recommended products

MW 301.77 Da, Purity >98%. Inhibitor of the Src family of kinases. Inhibits Src and Lck kinase (IC50 values are 36 and 31 nM, respectively). Also shown to inhibit RIP2 and CK1δ (IC50 values are 19 and 41 nM, respectively).

Key facts

Purity

> 98%

PubChem identifier

4878

Solubility

Soluble in DMSO to 50 mM. Soluble in ethanol to 10 mM.

Biochemical name

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

Biological description

Inhibitor of the Src family of kinases. Inhibits Src and Lck kinase (IC50 values are 36 and 31 nM, respectively). Also shown to inhibit RIP2 and CK1δ (IC50 values are 19 and 41 nM, respectively).

Canonical SMILES

CC(C)(C)N1C2=NC=NC(=C2C(=N1)C3=CC=C(C=C3)Cl)N

InChI

InChI=1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)

InChIKey

PBBRWFOVCUAONR-UHFFFAOYSA-N

IUPAC name

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

Storage

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 info

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

Activity summary

Src RIP2 and Lck are important components of the non-receptor tyrosine kinase family. Src also known as proto-oncogene tyrosine-protein kinase has a mass of approximately 60 kDa. It is widely expressed in many tissue types including epithelial and immune cells. RIP2 receptor-interacting serine/threonine-protein kinase 2 has a mass of about 61 kDa and is mainly present in immune system cells. Lck lymphocyte-specific protein tyrosine kinase weighs around 56 kDa and is predominantly in T cells. These kinases phosphorylate tyrosines on substrates modulating downstream signaling pathways and influence cell growth differentiation and survival.

Biological function summary

Src RIP2 and Lck contribute to signal transduction processes critical for cellular functions. Src commonly integrates into multi-protein complexes modulating pathways linked to cell cycle progression and proliferation. RIP2 is essential for activating nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and mitogen-activated protein kinase (MAPK) signaling pathways important in inflammation and immune responses. Lck plays a pivotal role in T cell receptor (TCR) signaling initiating adaptive immune responses. These kinases often work together with other signaling proteins to ensure proper cellular outcomes in health and disease.

Pathways

Src RIP2 and Lck serve key roles in the regulation of two significant biological pathways: the NF-κB pathway and TCR signaling. Src kinase's activity modulates the activation of downstream proteins like STAT3 and FAK which influence cell adhesion and migration. RIP2 interacts with proteins such as NOD2 during innate immune responses facilitating the activation of NF-κB pathway. Lck functions upstream in TCR signaling where it is essential for phosphorylating ZAP-70 a step important for triggering downstream signaling cascades critical for T cell activation.

Associated diseases and disorders

Dysregulation of Src RIP2 and Lck links to various pathological states. Src is notably implicated in cancer cell proliferation and metastasis making it a target in cancer therapies with PP2 Src inhibitors showing potential in treatment. RIP2 pathways are associated with inflammatory diseases like Crohn's disease as NOD2 mutations affect its interaction influencing NF-κB activation. Lck-related anomalies can contribute to immune disorders as improper TCR signaling can result in autoimmune conditions. Understanding these kinase interactions with proteins in disorders could lead to new therapeutic avenues.

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2 product images

  • Chemical Structure - PP2, Src and RIP2 kinase inhibitor (ab120308), expandable thumbnail

    Chemical Structure - PP2, Src and RIP2 kinase inhibitor (ab120308)

    2D chemical structure image of ab120308, PP2, Src and RIP2 kinase inhibitor

  • Functional Studies - PP2, Src and RIP2 kinase inhibitor (ab120308), expandable thumbnail

    Functional Studies - PP2, Src and RIP2 kinase inhibitor (ab120308)

    Anti-E Cadherin antibody [DECMA-1] - Intercellular Junction Marker ab11512 staining E-Cadherin in SW480 cells treated with PP2 (ab120308), by ICC/IF. Increase in E-cadherin expression correlates with increased concentration of PP2, as described in literature.
    The cells were incubated at 37°C for 24h in media containing different concentrations of ab120308 (PP2) 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 Anti-E Cadherin antibody [DECMA-1] - Intercellular Junction Marker ab11512 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rat polyclonal antibody (ab96971) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.

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