MW 294.3 Da, Purity >99%. JAK2/3 inhibitor (IC50 values are ~10 and 25 μM, respectively). Inhibits downstream activation of STAT5a/b. Effects synaptic plasticity and cytokine-independent cell growth in vitro and spatial learning, memory and tumor cell invasion in vivo.
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- Journal of neuroinflammation 18:1502021Red nucleus IL-33 facilitates the early development of mononeuropathic pain in male rats by inducing TNF-α through activating ERK, p38 MAPK, and JAK2/STAT3.Applications:Unspecified applicationReactive species:Unspecified reactive speciesHao-Nan Li,Qing-Qing Yang,Wen-Tao Wang,Xue Tian,Fan Feng,Shu-Ting Zhang,Yu-Tong Xia,Jia-Xue Wang,Yuan-Wu Zou,Jun-Yang Wang,Xiao-Yan ZengPubMed 34225736
- Journal of molecular endocrinology 66:259-2722021Neuritin inhibits astrogliosis to ameliorate diabetic cognitive dysfunction.Applications:Unspecified applicationReactive species:Unspecified reactive speciesZuo Zhang,Hongli Zhou,Jiyin ZhouPubMed 33729996
- Journal of neuroscience research 96:1847-18612018Red nucleus interleukin-1β evokes tactile allodynia through activation of JAK/STAT3 and JNK signaling pathways.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYi-Jie Guo et. al.PubMed 30216497
- RSC advances 8:8164-81722018MiR-29c inhibits HCV replication activation of type I IFN response by targeting STAT3 in JFH-1-infected Huh7 cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYanjing Wang,Yuanyuan LiPubMed 35542013
- Carcinogenesis 35:2244-532014Inhibition of STAT5a by Naa10p contributes to decreased breast cancer metastasis.Applications:Unspecified applicationReactive species:Unspecified reactive speciesYan Zeng et. al.PubMed 24925029
Key facts
- CAS number
- 133550-30-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 294.3 Da
- Molecular formula
- C17H14N2O3
- PubChem identifier
- 5328779
- Nature
- Synthetic
Target data
Alternative names
EC 2.7.10.2, JAK L, JAK2_HUMAN, JAK3 HUMAN, JAK3_HUMAN, JTK 10, Janus Activating Kinase 2, Janus kinase 2, Janus kinase 2 (a protein tyrosine kinase), Janus kinase 3, Janus kinase 3 (a protein tyrosine kinase, leukocyte), L-JAK, Leukocyte janus kinase, OTTHUMP00000043260, Protein tyrosine kinase leukocyte, THCYT3, Tyrosine-protein kinase JAK2, Tyrosine-protein kinase JAK3, kinase Jak2
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MW 294.3 Da, Purity >99%. JAK2/3 inhibitor (IC50 values are ~10 and 25 μM, respectively). Inhibits downstream activation of STAT5a/b. Effects synaptic plasticity and cytokine-independent cell growth in vitro and spatial learning, memory and tumor cell invasion in vivo.
Key facts
- CAS number
- 133550-30-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 294.3 Da
- Molecular formula
- C17H14N2O3
- PubChem identifier
- 5328779
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
Soluble in ethanol to 25 mM.
- Biochemical name
- Tyrphostin B42
- Biological description
JAK2/3 inhibitor (IC50 values are ~10 and 25 μM, respectively). Inhibits downstream activation of STAT5a/b. Effects synaptic plasticity and cytokine-independent cell growth in vitro and spatial learning, memory and tumor cell invasion in vivo.
- Canonical SMILES
- C1=CC=C(C=C1)CNC(=O)C(=CC2=CC(=C(C=C2)O)O)C#N
- Isomeric SMILES
- C1=CC=C(C=C1)CNC(=O)/C(=C/C2=CC(=C(C=C2)O)O)/C#N
- InChI
- InChI=1S/C17H14N2O3/c18-10-14(8-13-6-7-15(20)16(21)9-13)17(22)19-11-12-4-2-1-3-5-12/h1-9,20-21H,11H2,(H,19,22)/b14-8+
- InChIKey
- TUCIOBMMDDOEMM-RIYZIHGNSA-N
- IUPAC name
- (E)-N-benzyl-2-cyano-3-(3,4-dihydroxyphenyl)prop-2-enamide
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- -20°C
- Appropriate long-term storage conditions
- -20°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
JAK2 and JAK3 are key members of the Janus kinase family with JAK2 often referred to as Janus kinase 2. JAK2 has a molecular mass of approximately 130 kDa and is widely expressed in hematopoietic cells whereas JAK3 weighing about 125 kDa is predominantly found in immune cells such as T and B lymphocytes. These kinases function as intracellular non-receptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT signaling pathway. They possess distinct domains: the JH1 domain responsible for kinase activity and the JH2 domain providing a regulatory role.
- Biological function summary
JAK2 and JAK3 transmit signals from various cytokine receptors to modulate important cellular functions like proliferation differentiation and apoptosis. They do not operate in isolation; these kinases are part of large complexes that include specific receptor subunits and downstream signal transducers known as STATs (Signal Transducer and Activator of Transcription proteins). As part of these complexes they ensure the precise transmission of extracellular cytokine signals to the nucleus altering gene expression patterns to affect cellular responses.
- Pathways
These kinases have essential roles in the JAK-STAT signaling pathway and the PI3K-AKT pathway. JAK2 and JAK3 activation leads to the phosphorylation of STAT proteins which then dimerize and translocate to the nucleus to modulate gene expression. In these pathways they interact with various proteins like STAT5 and STAT1 that facilitate their signaling roles. Their activity is tightly regulated and their dysregulation can lead to implicating pathological conditions.
- Associated diseases and disorders
JAK2 and JAK3 are closely associated with myeloproliferative disorders and immunodeficiencies. Mutations in JAK2 such as the JAK2 V617F mutation are linked to conditions like polycythemia vera and essential thrombocythemia where unchecked cell proliferation occurs. JAK3 deficiencies or mutations often lead to severe combined immunodeficiency (SCID) affecting immune cell development. These conditions highlight the therapeutic potential of JAK2 inhibitors and JAK3 inhibitors to modulate abnormal kinase activity with agents like AG-490 being notable for their inhibitory effects on JAK2.
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Chemical Structure - AG 490, JAK2/3 inhibitor (ab120950)
2D chemical structure image of ab120950, AG 490, JAK2/3 inhibitor
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