GW5074
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 401483

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.


Chemical Structure

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GW5074
CAS# 220904-83-6

Theoretical Analysis

MedKoo Cat#: 401483
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

Price and Availability

Size Price Availability Quantity
100mg USD 850
200mg USD 1450
500mg USD 2150
1g USD 2950
2g USD 4250
5g USD 6450
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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:         

Product Data:
Biological target: GW 5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, and has no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms.
In vitro activity: These studies showed that GW5074 exhibited selective antimicrobial activity toward Gram-positive micro-organisms with MICs ranging from 2 to 8 μg/ml, compared with the >64 μg/ml for all Gram-negative bacteria tested (Tables 2 & 3). Reference: Future Med Chem. 2016 Oct;8(16):1941-1952. https://pubmed.ncbi.nlm.nih.gov/27652456/
In vivo activity: As shown in Fig. 10 (top panel), mice administered 3-NP display extensive bilateral striatal lesions. This degeneration is completely prevented by GW5074 when administered at a concentration of 5 mg/kg body weight. Administration of GW5074 alone had no discernible effect on the animals as judged by behavior and cell morphology of brain sections (data not shown). Reference: Neurochem. 2004 Aug;90(3):595-608. https://pubmed.ncbi.nlm.nih.gov/15255937/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 15.0 28.79
DMSO 73.0 140.13
DMSO:PBS (pH 7.2) (1:8) 0.1 0.19

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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: 1. Johnston T, Hendricks GL, Shen S, Chen RF, Kwon B, Kelso MJ, Kim W, Burgwyn Fuchs B, Mylonakis E. Raf-kinase inhibitor GW5074 shows antibacterial activity against methicillin-resistant Staphylococcus aureus and potentiates the activity of gentamicin. Future Med Chem. 2016 Oct;8(16):1941-1952. doi: 10.4155/fmc-2016-0104. Epub 2016 Sep 21. PMID: 27652456; PMCID: PMC5619112. 2. 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. doi: 10.1111/j.1471-4159.2004.02530.x. PMID: 15255937.
In vitro protocol: 1. Johnston T, Hendricks GL, Shen S, Chen RF, Kwon B, Kelso MJ, Kim W, Burgwyn Fuchs B, Mylonakis E. Raf-kinase inhibitor GW5074 shows antibacterial activity against methicillin-resistant Staphylococcus aureus and potentiates the activity of gentamicin. Future Med Chem. 2016 Oct;8(16):1941-1952. doi: 10.4155/fmc-2016-0104. Epub 2016 Sep 21. PMID: 27652456; PMCID: PMC5619112. 2. 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. doi: 10.1111/j.1471-4159.2004.02530.x. PMID: 15255937.
In vivo protocol: 1. Johnston T, Hendricks GL, Shen S, Chen RF, Kwon B, Kelso MJ, Kim W, Burgwyn Fuchs B, Mylonakis E. Raf-kinase inhibitor GW5074 shows antibacterial activity against methicillin-resistant Staphylococcus aureus and potentiates the activity of gentamicin. Future Med Chem. 2016 Oct;8(16):1941-1952. doi: 10.4155/fmc-2016-0104. Epub 2016 Sep 21. PMID: 27652456; PMCID: PMC5619112. 2. 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. doi: 10.1111/j.1471-4159.2004.02530.x. PMID: 15255937.

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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.