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AB120308

PP2, Src and RIP2 kinase inhibitor

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(17 Publications)

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).

View Alternative Names

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

2 Images
Functional Studies - PP2, Src and RIP2 kinase inhibitor (AB120308)
  • FuncS

Unknown

Functional Studies - PP2, Src and RIP2 kinase inhibitor (AB120308)

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 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.

Chemical Structure - PP2, Src and RIP2 kinase inhibitor (AB120308)
  • Chemical Structure

Lab

Chemical Structure - PP2, Src and RIP2 kinase inhibitor (AB120308)

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

Key facts

CAS number

172889-27-9

Purity

>98%

Form

Solid

form

Molecular weight

301.77 Da

Molecular formula

C<sub>1</sub><sub>5</sub>H<sub>1</sub><sub>6</sub>ClN<sub>5</sub>

PubChem

4878

Nature

Synthetic

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

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.

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.

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.

Product protocols

Publications (17)

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

JCI insight 10: PubMed40493407

2025

Csk-mediated Src family kinase regulation dampens neutrophil infiltration during pulmonary infection.

Applications

Unspecified application

Species

Unspecified reactive species

Wida Amini,Lena Schemmelmann,Jan-Niklas Heming,Marina Oguama,Katharina Thomas,Helena Block,Pia Lindental,Bernadette Bardel,Andreas Margraf,Oliver Soehnlein,Anika Cappenberg,Alexander Zarbock

Glia 72:916-937 PubMed38372375

2024

Axon-derived PACSIN1 binds to the Schwann cell survival receptor, LRP1, and transactivates TrkC to promote gliatrophic activities.

Applications

Unspecified application

Species

Unspecified reactive species

Stefano Martellucci,Andreas Flütsch,Mark Carter,Masaki Norimoto,Donald Pizzo,Elisabetta Mantuano,Mahrou Sadri,Zixuan Wang,Daisy Chillin-Fuentes,Sara Brin Rosenthal,Pardis Azmoon,Steven L Gonias,Wendy M Campana

Proceedings of the National Academy of Sciences of the United States of America 120:e2316456120 PubMed38055737

2023

Coupling during collective cell migration is controlled by a vinculin mechanochemical switch.

Applications

Unspecified application

Species

Unspecified reactive species

T Curtis Shoyer,Evan M Gates,Jolene I Cabe,Aarti N Urs,Daniel E Conway,Brenton D Hoffman

Mediators of inflammation 2021:6639252 PubMed33927570

2021

Toll-Like Receptor 4 Mediated Oxidized Low-Density Lipoprotein-Induced Foam Cell Formation in Vascular Smooth Muscle Cells via Src and Sirt1/3 Pathway.

Applications

Unspecified application

Species

Unspecified reactive species

Zhongli Chen,Qiqi Xue,Lijuan Cao,Yanpin Wang,Yuanyuan Chen,Xiaojie Zhang,Fan Xiao,Ying Yang,Melvin R Hayden,Yan Liu,Ke Yang

Cell reports 33:108245 PubMed33086058

2020

LPS-Induced Acute Kidney Injury Is Mediated by Nox4-SH3YL1.

Applications

Unspecified application

Species

Unspecified reactive species

Jung-Yeon Yoo,Dae Ryong Cha,Borim Kim,Eun Jung An,Sae Rom Lee,Jin Joo Cha,Young Sun Kang,Jung Yeon Ghee,Jee Young Han,Yun Soo Bae

Cell reports 29:4144-4158.e7 PubMed31851939

2019

Discrimination of Dormant and Active Hematopoietic Stem Cells by G Marker Reveals Dormancy Regulation by Cytoplasmic Calcium.

Applications

Unspecified application

Species

Unspecified reactive species

Tsuyoshi Fukushima,Yosuke Tanaka,Fiona K Hamey,Chih-Hsiang Chang,Toshihiko Oki,Shuhei Asada,Yasutaka Hayashi,Takeshi Fujino,Taishi Yonezawa,Reina Takeda,Kimihito Cojin Kawabata,Tomofusa Fukuyama,Terumasa Umemoto,Keiyo Takubo,Hitoshi Takizawa,Susumu Goyama,Yasushi Ishihama,Hiroaki Honda,Berthold Göttgens,Toshio Kitamura

FASEB journal : official publication of the Federa 33:12812-12824 PubMed31469589

2019

The neuronal oxygen-sensing pathway controls postnatal vascularization of the murine brain.

Applications

Unspecified application

Species

Unspecified reactive species

Emil Nasyrov,Karen A Nolan,Roland H Wenger,Hugo H Marti,Reiner Kunze

eLife 8: PubMed30947808

2019

Light-based tuning of ligand half-life supports kinetic proofreading model of T cell signaling.

Applications

Unspecified application

Species

Unspecified reactive species

Doug K Tischer,Orion David Weiner

Biomaterials 161:164-178 PubMed29421553

2018

Hacking macrophage-associated immunosuppression for regulating glioblastoma angiogenesis.

Applications

Unspecified application

Species

Unspecified reactive species

Xin Cui,Renee-Tyler Tan Morales,Weiyi Qian,Haoyu Wang,Jean-Pierre Gagner,Igor Dolgalev,Dimitris Placantonakis,David Zagzag,Luisa Cimmino,Matija Snuderl,Raymond H W Lam,Weiqiang Chen

eLife 6: PubMed29271742

2017

Paxillin facilitates timely neurite initiation on soft-substrate environments by interacting with the endocytic machinery.

Applications

Unspecified application

Species

Unspecified reactive species

Ting-Ya Chang,Chen Chen,Min Lee,Ya-Chu Chang,Chi-Huan Lu,Shao-Tzu Lu,De-Yao Wang,Aijun Wang,Chin-Lin Guo,Pei-Lin Cheng
View all publications

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