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).
172889-27-9
> 98%
Solid
301.77 Da
C15H16ClN5
4878
Synthetic
ASV, AW259666, Avian sarcoma virus, C SRC, 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, CDNA FLJ14219 fis clone NT2RP3003800 highly similar to Rattus norvegicus tyrosine protein kinase pp60 c src mRNA, CLARP kinase, EC 2.7.10.2, GIG 30, Growth inhibiting gene 30, IMD22, LCK proto-oncogene, Src family tyrosine kinase, LCK_HUMAN, LSK, Lck p56, Leukocyte C-terminal Src kinase, Lymphocyte cell-specific protein-tyrosine kinase, Lymphocyte specific protein tyrosine kinase, Membrane associated protein tyrosine kinase, Neuronal CSRC tyrosine specific protein kinase, Neuronal SRC, Neuronal proto-oncogene tyrosine-protein kinase Src, OTTHUMP00000174476, OTTHUMP00000174477, Oncogene SRC, Oncogene lck, Protein YT16, Proto oncogene tyrosine protein kinase LCK, Proto-oncogene Lck, Proto-oncogene c-Src, Proto-oncogene tyrosine-protein kinase Src, Protooncogene SRC, Protooncogene SRC Rous sarcoma, RICK, RIP-like-interacting CLARP kinase, RIPK2_HUMAN, Receptor interacting protein (RIP) like interacting caspase like apoptosis regulatory protein (CLARP) kinase, Receptor interacting serine threonine kinase 2, Receptor-interacting protein 2, Receptor-interacting serine/threonine-protein kinase 2, SRC Oncogene, SRC proto oncogene non receptor tyrosine kinase, SRC_HUMAN, T cell-specific protein-tyrosine kinase, T lymphocyte specific protein tyrosine kinase p56lck, TNFRSF, Tyrosine kinase pp60c src, Tyrosine protein kinase SRC 1, Tyrosine-protein kinase Lck, Tyrosine-protein kinase RIPK2, UNQ277/PRO314/PRO34092, V src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog (avian), YT 16, p56(LSTRA) protein tyrosine kinase, p56-LCK, p60-Src, p60c-src, pp58 lck, pp60c-src, v src avian sarcoma (Schmidt Ruppin A2) viral oncogene homolog, v src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog avian
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).
172889-27-9
> 98%
Solid
301.77 Da
C15H16ClN5
4878
Synthetic
Soluble in DMSO to 50 mM. Soluble in ethanol to 10 mM.
1-tert-butyl-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine
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).
CC(C)(C)N1C2=NC=NC(=C2C(=N1)C3=CC=C(C=C3)Cl)N
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)
PBBRWFOVCUAONR-UHFFFAOYSA-N
1-tert-butyl-3-(4-chlorophenyl)pyrazolo[3,4-d]pyrimidin-4-amine
Ambient - Can Ship with Ice
+4°C
+4°C
Store under desiccating conditions, The product can be stored for up to 12 months
This supplementary information is collated from multiple sources and compiled automatically.
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.
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.
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.
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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2D chemical structure image of ab120308, PP2, Src and RIP2 kinase inhibitor
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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