Cyclopamine inhibitor 1
IRAK inhibitor 1
CAS: 1042224-63-4
Molecular Formula: C17H19N5
Cyclopamine inhibitor 1 - Names and Identifiers
Cyclopamine inhibitor 1 - Physico-chemical Properties
| Molecular Formula | C17H19N5 |
| Molar Mass | 293.37 |
| Density | 1.32 |
| Solubility | DMSO: 12.2 mg/mL |
| pKa | 9.94±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | IRAK inhibitor 1 possesses significant potency in an IRAK-4 enzyme assay but is poorly active against JNK-1 and JNK-2. IRAK-4 is a novel member of the IRAK family with unique functional properties. IRAK-4 is the closest human homolog to Pelle. Endogenous IRAK-4 interacts with IRAK-1 and TRAF6 in an IL-1-dependent manner, and overexpression of IRAK-4 can activate NF-κB as well as mitogen-activated protein (MAP) kinase pathways. Most strikingly, and in contrast to the other IRAKs, IRAK-4 depends on its kinase activity to activate NF-κB. In addition, IRAK-4 is able to phosphorylate IRAK-1, and overexpression of dominant-negative IRAK-4 is blocking the IL-1-induced activation and modification of IRAK-1, suggesting a role of IRAK-4 as a central element in the early signal transduction of Toll/IL-1 receptors, upstream of IRAK-1. IRAK-4 shares the domain structure of the other IRAKs and it is able to activate similar signal transduction pathways, namely NF-κB and MAPK pathways. It rapidly and transiently associates with IRAK-1 and TRAF6 in an IL-1-dependent manner but it is not functionally redundant with IRAK-1. IRAK-4 is an active protein kinase and requires its kinase activity to activate NF-κB. IRAK-4 might act upstream of IRAK-1 as an IRAK-1 activator. |
Cyclopamine inhibitor 1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.409 ml | 17.044 ml | 34.087 ml |
| 5 mM | 0.682 ml | 3.409 ml | 6.817 ml |
| 10 mM | 0.341 ml | 1.704 ml | 3.409 ml |
| 5 mM | 0.068 ml | 0.341 ml | 0.682 ml |
Last Update：2024-01-02 23:10:35
Cyclopamine inhibitor 1 - Reference Information
| Overview | Cyclopamine (cyclopamine) is a isosteroidal alkaloid, which was discovered in the 1960 s due to its teratogenic effect. The latest research shows that it is a Hedgehog pathway inhibitor and has a good inhibitory effect on various tumors. Cyclopamine, as a potential anti-tumor drug, has attracted extensive attention and research at home and abroad. In the mid-20th century, the deformity rate of lambs born in some areas of Idaho in the United States was much higher than that in other areas, and most of them showed monocular deformity of the head. Keeler and others of the U.S. Toxic Plant Research Laboratory conducted a long-term study on this phenomenon, and in 1964 confirmed that a steroidal alkaloid in the veratrum genus Veratrum (Veratrumcalifornicum) was the main teratogenic component, and its structure was confirmed in 1967. This alkaloid is the same substance as the alkaloid isolated from Veratrum (Veratrumgrandiflorum) by Japanese scholar Masamune et al. in 1964. The discovery of cyclosamine stems from its teratogenic effect, so the research on cyclosamine from the 1960s to the 1980s was limited to teratogenic effects. Until the mid-1990s, cyclosamine was discovered to be an inhibitor of the hedgehog signaling pathway, which essentially explained its teratogenic effect. Because mutations in the hedgehog signaling pathway are associated with the pathogenesis of a variety of tumors, cyclosamine As a potential new anti-tumor drug, it has set off a research boom worldwide. Cyclobamide inhibitor 1 is a cycloapamine derivative. |
| biological activity | IRAK inhibitor 1 is an effective IRAK-4 inhibitor, IC50 is 216 nM, weakly inhibits JNK-1 and JNK-2,IC50 is 3.801 μM and> 10 μM respectively. |
| target | IC50: 216 nM (IRAK-4), 3.801 μM (JNK-1), >10 μM (JNK-2) |
| in vitro study | IRAK inhibitor 1 possesses significant potency in an IRAK-4 enzyme say but is a valuable active against JNK-1 and JNK-2. IRAK-4 is a novel member of the IRAK family with unique functional properties. IRAK-4 is the closest human homolog to Pelle. Endogenous IRAK-4 interacts with IRAK-1 and TRAF6 in an IL-1-dependent manner, and overexpression of IRAK-4 can activate NF-κB as well as mitogen-activated protein (MAP) kinase pathways. Most strikingly, and in contrast to the other IRAKs, IRAK-4 depends on its activity to activate NF-κB. In addition, IRAK-4 is able to phosphorylate IRAK-1, and overexpression of dominant-negative IRAK-4 is blocking the IL-1-induced activation and modification of IRAK-1, suggesting a role of IRAK-4 as a central element in the early signal transduction of Toll/IL-1 receptors, upstream of IRAK-1. IRAK-4 shares of the domain structure of the other IRAKs and it is able to activate similar signal transduction pathways, namely NF-κB and MAPK pathways. It rapidly and transiently associates with IRAK-1 and TRAF6 in an IL-1-dependent banner but it is not functionally redundant with IRAK-1. IRAK-4 is an active protein kinase and requires its activity to activate NF-κB. IRAK-4 might act upstream of IRAK-1 as an IRAK-1 activator. |
Last Update：2024-04-09 21:54:55
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Product Name: 6-Imidazo[1,2-a]pyridin-3-yl-N-4-piperidinyl-2-pyridinamine Visit Supplier Webpage Request for quotationCAS: 1042224-63-4
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Product Name: IRAK inhibitor 1 Visit Supplier Webpage Request for quotation
CAS: 1042224-63-4
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CAS: 1042224-63-4
Tel: 18301782025
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