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AB282423

WH-4-023

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(3 Publications)

MW 568.7 Da, Purity >98%. Potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src.

View Alternative Names

ASV, AW259666, Avian sarcoma virus, C SRC, CD309, CD309 antigen, CDNA FLJ14219 fis clone NT2RP3003800 highly similar to Rattus norvegicus tyrosine protein kinase pp60 c src mRNA, CSAID Binding Protein 1, CSAID-binding protein, CSBP, CSBP 1, CSBP 2, CSPB1, Csaids binding protein, Cytokine suppressive anti-inflammatory drug-binding protein, EC 2.7.10.1, EC 2.7.10.2, EXIP, FLK-1, FLK1, mouse, homolog of, Fetal liver kinase 1, IMD22, 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, MK14_HUMAN, Membrane associated protein tyrosine kinase, Mitogen-activated protein kinase 14, Mitogen-activated protein kinase p38 alpha, Mxi 2, Neuronal CSRC tyrosine specific protein kinase, Neuronal SRC, Neuronal proto-oncogene tyrosine-protein kinase Src, OTTHUMP00000174476, OTTHUMP00000174477, Oncogene SRC, Oncogene lck, P38, PRKM14, PRKM15, Protein YT16, Protein-tyrosine kinase receptor flk-1, 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, RK, SAPK2A, SRC Oncogene, SRC proto oncogene non receptor tyrosine kinase, SRC_HUMAN, Stress-activated protein kinase 2a, T cell-specific protein-tyrosine kinase, T lymphocyte specific protein tyrosine kinase p56lck, Tyrosine kinase growth factor receptor, Tyrosine kinase pp60c src, Tyrosine protein kinase SRC 1, Tyrosine-protein kinase Lck, V src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog (avian), VEGFR, VEGFR-2, VGFR2_HUMAN, Vascular endothelial growth factor receptor 2, YT 16, p38 ALPHA, p38 MAP kinase, p38 MAPK, p38 mitogen activated protein kinase, p38alpha Exip, p56(LSTRA) protein tyrosine kinase, p56-LCK, p60-Src, p60c-src, pp58 lck, pp60c-src, soluble VEGFR2, v src avian sarcoma (Schmidt Ruppin A2) viral oncogene homolog, v src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog avian

Key facts

CAS number

837422-57-8

Purity

>98%

Form

Powder

form

Molecular weight

568.7 Da

Molecular formula

C<sub>3</sub><sub>2</sub>H<sub>3</sub><sub>6</sub>N<sub>6</sub>O<sub>4</sub>

PubChem

11844351

Nature

Synthetic

Solubility

Soluble in DMSO: 20 mg/ml.

Biochemical name

2,6-Dimethylphenyl (2,4-dimethoxyphenyl)(2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamate

Biological description

Potent and selective inihbitor of the tyrosine kinases Lck and Src with IC50 values of 2 nM for Lck and 6 nM for Src.

Canonical smiles

CC1=C(C(=CC=C1)C)OC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCN(CC5)C

InChi

InChI=1S/C32H36N6O4/c1-22-7-6-8-23(2)30(22)42-32(39)38(27-14-13-26(40-4)21-28(27)41-5)29-15-16-33-31(35-29)34-24-9-11-25(12-10-24)37-19-17-36(3)18-20-37/h6-16,21H,17-20H2,1-5H3,(H,33,34,35)

InChiKey

NBTNHSGBRGTFJS-UHFFFAOYSA-N

IUPAC Name

(2,6-dimethylphenyl) N-(2,4-dimethoxyphenyl)-N-[2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]carbamate

Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C

Supplementary information

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

The targets p38 Src VEGF Receptor 2 and Lck play significant roles in various cellular processes. p38 also known as MAPK14 is part of the mitogen-activated protein kinase (MAPK) family and it has a mass of about 41 kDa. It is widely expressed in many tissues like the heart skeletal muscle and liver. Src a non-receptor tyrosine kinase weighs approximately 60 kDa and resides in the cytoplasm and membranes of cells. VEGF Receptor 2 also known as KDR or FLK-1 is integral to cell signaling and shows a molecular weight of 150 kDa. It is found in endothelial cells facilitating vascular growth. Lck a lymphocyte-specific tyrosine kinase with a mass of roughly 56 kDa localizes mainly in T-cells and is important for T-cell receptor signaling.
Biological function summary

These proteins perform essential functions in cellular signaling. p38 for instance regulates inflammatory responses by activating downstream effectors in stress-stimulated pathways. Src plays a significant role in the regulation of cell division and survival by interacting with various signal transducers. VEGF Receptor 2 is fundamental to angiogenesis a process vital for new blood vessel formation. It participates in a complex with VEGF to transmit signals for endothelial cell proliferation. Lck functions in the immune system by initiating the signaling cascade necessary for T-cell activation and development.

Pathways

These proteins impact significant cellular communication networks. p38 is an important player in the MAPK pathway involved in responses to stress stimuli. It interacts with other MAPKs like JNK in controlling cytokine production. Src integrates into the Src-family kinase pathway modulating cell growth and movement by activating downstream proteins such as FAK. VEGF Receptor 2 is pivotal in the VEGF signaling pathway partnering with PI3K and AKT to promote endothelial cell responses. Lck fits into the T-cell receptor pathway where it associates with proteins like ZAP-70 to relay activation signals.

These targets link to several pathological conditions. p38 plays an essential role in inflammatory diseases like arthritis where it mediates inflammatory cytokine production. Src is implicated in cancer carrying mutations or overexpressions in various malignancies often accompanied by proteins such as FAK that drive tumor progression. VEGF Receptor 2 contributes to angiogenesis-related disorders including cancer where its pathway's overactivation supports tumor vasculature development. Lck links with immune disorders like autoimmune diseases as improper signaling here leads to abnormal T-cell responses. In these contexts therapeutic targeting of these proteins can provide compelling strategies to mitigate disease progression.

Product protocols

Publications (3)

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

Theranostics 9:646-660 PubMed30809299

2019

Nuclear Entry of CRTC1 as Druggable Target of Acquired Pigmentary Disorder.

Applications

Unspecified application

Species

Unspecified reactive species

Cheong-Yong Yun,Seung Deok Hong,Young Hee Lee,Jiyeon Lee,Da-Eun Jung,Ga Hyun Kim,Song-Hee Kim,Jae-Kyung Jung,Ki Ho Kim,Heesoon Lee,Jin Tae Hong,Sang-Bae Han,Youngsoo Kim

Oncotarget 9:10723-10733 PubMed29535838

2018

Targeting loss of the Hippo signaling pathway in -deficient papillary kidney cancers.

Applications

Unspecified application

Species

Unspecified reactive species

Carole Sourbier,Pei-Jyun Liao,Christopher J Ricketts,Darmood Wei,Youfeng Yang,Sarah M Baranes,Benjamin K Gibbs,Lernik Ohanjanian,L Spencer Krane,Bradley T Scroggins,J Keith Killian,Ming-Hui Wei,Toshiki Kijima,Paul S Meltzer,Deborah E Citrin,Len Neckers,Cathy D Vocke,W Marston Linehan

Blood 130:2750-2761 PubMed29101238

2017

Glucocorticoid resistance is reverted by LCK inhibition in pediatric T-cell acute lymphoblastic leukemia.

Applications

Unspecified application

Species

Unspecified reactive species

Valentina Serafin,Giorgia Capuzzo,Gloria Milani,Sonia Anna Minuzzo,Marica Pinazza,Roberta Bortolozzi,Silvia Bresolin,Elena Porcù,Chiara Frasson,Stefano Indraccolo,Giuseppe Basso,Benedetta Accordi
View all publications

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