MedKoo Biosciences/GW5074/401483/200mg-蚂蚁淘生物

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 Huntingtons disease. GW5074 could have therapeutic value against neurodegenerative pathologies in humans.

MedKoo Cat#: 401483 Name: GW5074 CAS#: 220904-83-6 Chemical Formula: C15H8Br2INO2 Exact Mass: 518.79665 Molecular Weight: 520.94 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

Technical Data

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).

Harmonized System Code: 293490

Additional Information

References

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.

Technical Data

Additional Information

References

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