GW5074 - Moligand™, 10mM in DMSO , Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase, CAS No.220904-83-6, Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase

CAS: 220904-83-6 Cat. No.: G408888 Formula: C₁₅H₈Br₂INO₂ Peso molecolare: 520.94

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2H-Indol-2-one, 3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-1,3-dihydro-5-iodo-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Panoramica

Information

GW5074 is a potent and selectivec-Rafinhibitor withIC50of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-inducedapoptosis.
In vitro

GW5074 is a potent and specific inhibitor of c-Raf with IC50 of 9 nM and has no effect of MKK6, MKK7, p38 MAP kinase and cdks in vitro. However, treatment of neuronal cultures with GW5074 permits accumulation of activating modifications on c-Raf and also B-Raf. The inhibition of LK-induced apoptosis by GW5074 in cerebellar granule neurons is not MEK-ERK-dependent. GW5074 delays down-regulation of Akt activity but inhibits apoptosis by an Akt-independent mechanism. GW5074 affects Ras, nuclear factor-kappa B and c-jun. GW5074 inhibits cell death caused by neurotoxins in granule cells and other neuronal types.

In vivo

GW5074 is protective in an in vivo experimental model of Huntington’s disease. GW5074 (5 mg/Kg) completely prevented extensive bilateral striatal lesions induced by 3-NP in mice. GW5074 completely abolishes chronic morphine-mediated AC superactivation I in CHO cells stably expressing the humanμ-opioid receptor. GW5074 suppresses sidestream smoke-induced airway hyperresponsiveness in mice.
Cell Data

cell lines：

Concentrations：~5 μM

Incubation Time：24 hours

Powder Purity:≥99%

Specifications

Sinonimi

2H-Indol-2-one, 3-[(3,5-dibromo-4-hydroxyphenyl)methylene]-1,3-dihydro-5-iodo-

Specifiche e purezza

Moligand™, 10mM in DMSO

Meccanismi biochimici e fisiologici

GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis.

Condizioni di conservazione di stoccaggio

Store at -80°C

Spedito in

Dry ice packs + Cold packs

Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.

Grado

Moligand™

Tipo di azione

INHIBITOR

Meccanismo d'azione

Inhibitor of Raf-1 proto-oncogene; serine/threonine kinase

Nomi e identificatori

• Isomeri SMILES: C1=CC2=C(C=C1I)/C(=C/C3=CC(=C(C(=C3)Br)O)Br)/C(=O)N2
• Peso molecolare: 520.94
• Reaxy-Rn: 8641129
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8641129&ln=

Obiettivi associati (umani)

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RAF1 Tclin RAF proto-oncogene serine/threonine-protein kinase (4 Activities)

Discover Target: RAF1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRAF Tclin Serine/threonine-protein kinase B-raf (9 Activities)

Discover Target: BRAF

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ARAF Tchem Serine/threonine-protein kinase A-Raf (1 Activities)

Discover Target: ARAF

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Proprietà chimiche e fisiche

• Solubilità: Solubility (25°C) In vitro DMSO: 71 mg/mL (198.64 mM); Water: Insoluble; Ethanol: Insoluble

Riferimenti

1. Jiao Ma, Zhechun Hu, Huimin Yue, Yujian Luo, Chao Wang, Xuan Wu, Yan Gu, Lang Wang.  (2023)  GRM2 Regulates Functional Integration of Adult-Born DGCs by Paradoxically Modulating MEK/ERK1/2 Pathway.  JOURNAL OF NEUROSCIENCE,  43  (16): (2822-2836).  [PMID:36878727] [10.1523/JNEUROSCI.1886-22.2023]

2. Xiaoli Ling, Zhipeng Tian, Dong Chen, Yujia Zhang, Ziyan Dong, Dan He, Jiayu Li, Zhidi He, Jiaxin Li, Fang Chen, Qin He, Man Li.  (2024)  Functionalized aluminum hydroxide-based self-adjuvanted nanovaccine orchestrates antitumor immune responses via Dectin-1 signaling.  JOURNAL OF CONTROLLED RELEASE,      [PMID:39716663] [10.1016/j.jconrel.2024.12.035]

Domande frequenti

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 220904-83-6, the molecular formula is C15H8Br2INO2, and the molecular weight is 520.94 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.