WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H401483
CAS#: 220904-83-6
Description: GW5074 is a c-Raf inhibitor. GW5074 has no direct effect on the activities of several apoptosis-associated kinases when assayed in vitro. In contrast to its effect in vitro, treatment of neurons with GW5074 causes c-Raf activation (when measured in vitro in the absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW5074 prevents neurodegeneration and improves behavioral outcome in an animal model of Huntington's disease. GW5074 could have therapeutic value against neurodegenerative pathologies in humans.
Hodoodo Cat#: H401483
Name: GW5074
CAS#: 220904-83-6
Chemical Formula: C15H8Br2INO2
Exact Mass: 518.80
Molecular Weight: 520.947
Elemental Analysis: C, 34.58; H, 1.55; Br, 30.68; I, 24.36; N, 2.69; O, 6.14
Synonym: GW5074; GW 5074; GW-5074;
IUPAC/Chemical Name: 3-(3,5-Dibromo-4-hydroxy-benzylidene)-5-iodo-1,3-dihydro-indol-2-one
InChi Key: LMXYVLFTZRPNRV-KMKOMSMNSA-N
InChi Code: InChI=1S/C15H8Br2INO2/c16-11-4-7(5-12(17)14(11)20)3-10-9-6-8(18)1-2-13(9)19-15(10)21/h1-6,20H,(H,19,21)/b10-3-
SMILES Code: O=C1NC2=C(C=C(I)C=C2)/C1=C/C3=CC(Br)=C(O)C(Br)=C3
Appearance: solid powder
Purity: >98%
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >5 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 520.95 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Suenkel B, Fischer F, Steegborn C. Inhibition of the human deacylase Sirtuin 5 by the indole GW5074. Bioorg Med Chem Lett. 2013 Jan 1;23(1):143-6. doi: 10.1016/j.bmcl.2012.10.136. Epub 2012 Nov 12. PubMed PMID: 23195732.
2: Li J, Fan Y, Zhang YN, Sun DJ, Fu SB, Ma L, Jiang LH, Cui C, Ding HF, Yang J. The Raf-1 inhibitor GW5074 and the ERK1/2 pathway inhibitor U0126 ameliorate PC12 cells apoptosis induced by 6-hydroxydopamine. Pharmazie. 2012 Aug;67(8):718-24. PubMed PMID: 22957439.
3: Lei Y, Cao YX, Xu CB, Zhang Y. The Raf-1 inhibitor GW5074 and dexamethasone suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res. 2008 Nov 3;9:71. doi: 10.1186/1465-9921-9-71. PubMed PMID: 18976506; PubMed Central PMCID: PMC2599896.
4: Chen HM, Wang L, D'Mello SR. Inhibition of ATF-3 expression by B-Raf mediates the neuroprotective action of GW5074. J Neurochem. 2008 May;105(4):1300-12. doi: 10.1111/j.1471-4159.2008.05226.x. Epub 2008 Jan 10. PubMed PMID: 18194435.
5: Yue X, Varga EV, Stropova D, Vanderah TW, Yamamura HI, Roeske WR. Chronic morphine-mediated adenylyl cyclase superactivation is attenuated by the Raf-1 inhibitor, GW5074. Eur J Pharmacol. 2006 Jul 1;540(1-3):57-9. Epub 2006 May 3. PubMed PMID: 16750187.
6: Chin PC, Liu L, Morrison BE, Siddiq A, Ratan RR, Bottiglieri T, D'Mello SR. The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism. J Neurochem. 2004 Aug;90(3):595-608. PubMed PMID: 15255937.
