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MedKoo/GSK2606414featured/25mg/406393

  • 产品编号: 406393
  • 美  元  价: $150.00
  • 市  场  价: ¥3000.00
  • 品       牌:
  • 产       地: 美国(厂家直采)
  • 公       司: MedKoo Biosciences, Inc
  • 产品分类:
  • 公司分类: Apoptosis
MedKoo/GSK2606414featured/25mg/406393
  • MedKoo/GSK2606414featured/25mg/406393
商品介绍

GSK2606414
featured

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

MedKoo CAT#:406393

CAS#:1337531-36-8

Description:GSK2606414 is an orally available, potent, and selective PERK inhibitor. GSK2606414 inhibits PERK activation in cells and inhibits the growth of a human tumor xenograft in mice. Protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is activated in response to a variety of endoplasmic reticulum stresses implicated in numerous disease states. Evidence that PERK is implicated in tumorigenesis and cancer cell survival stimulated our search for small molecule inhibitors.

Price and Availability

SizePriceShipping out timeQuantity
25mgUSD 150Same day
50mgUSD 250Same day
100mgUSD 450Same day
200mgUSD 750Same day
500mgUSD 1550Same day
1gUSD 2450Same day
2gUSD 3950Same day
5gUSD 6950Same day
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

GSK2606414, purity > 98%, is in stock. The same day shipping after order is received.

Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 406393Name: GSK2606414CAS#: 1337531-36-8Chemical Formula: C24H20F3N5OExact Mass: 451.16199Molecular Weight: 451.44Elemental Analysis: C, 63.85; H, 4.47; F, 12.63; N, 15.51; O, 3.54

Synonym:GSK2606414; GSK-2606414; GSK 2606414; GSK PERK Inhibitor.

IUPAC/Chemical Name:1-(5-(4-amino-7-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethyl)phenyl)ethanone

InChi Key:SIXVRXARNAVBTC-UHFFFAOYSA-N

InChi Code:InChI=1S/C24H20F3N5O/c1-31-12-18(21-22(28)29-13-30-23(21)31)15-5-6-19-16(11-15)7-8-32(19)20(33)10-14-3-2-4-17(9-14)24(25,26)27/h2-6,9,11-13H,7-8,10H2,1H3,(H2,28,29,30)

SMILES Code:FC(C1=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3)=O)=CC=C1)(F)F

Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:
View CoA: current batch, Lot# APC40116 View CoA: current batch, Lot#A9T09K25

QC Data:
View QC data, current batch, Lot#APC40116View QC data: current batch, Lot#A9T09K25

Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)

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:
>2 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

Additional Information

    The chemical structures of GSK2606414  and GSK2656157 are very similar. The following graphic is a side-by-side comparison.  

References

1: Rojas-Rivera D, Delvaeye T, Roelandt R, Nerinckx W, Augustyns K, VandenabeeleP, Bertrand MJM. When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157. Cell Death Differ. 2017 Apr 28. doi: 10.1038/cdd.2017.58. [Epub ahead of print] PubMed PMID: 28452996.

2: Wen L, Xiao B, Shi Y, Han F. PERK signalling pathway mediates single prolonged stress-induced dysfunction of medial prefrontal cortex neurons. Apoptosis. 2017 Jun;22(6):753-768. doi: 10.1007/s10495-017-1371-5. PubMed PMID: 28391375.

3: Jiang X, Wei Y, Zhang T, Zhang Z, Qiu S, Zhou X, Zhang S. Effects of GSK2606414 on cell proliferation and endoplasmic reticulum stress associated gene expression in retinal pigment epithelial cells. Mol Med Rep. 2017 May;15(5):3105-3110. doi: 10.3892/mmr.2017.6418. Epub 2017 Mar 30. PubMed PMID: 28358434.

4: Zhang J, Feng Z, Wang C, Zhou H, Liu W, Kanchana K, Dai X, Zou P, Gu J, Cai L, Liang G. Curcumin derivative WZ35 efficiently suppresses colon cancer progression through inducing ROS production and ER stress-dependent apoptosis. Am J Cancer Res. 2017 Feb 1;7(2):275-288. eCollection 2017. PubMed PMID: 28337376; PubMed Central PMCID: PMC5336501.

5: Sharma R, Quilty F, Gilmer JF, Long A, Byrne AM. Unconjugated secondary bile acids activate the unfolded protein response and induce golgi fragmentation via a src-kinase-dependant mechanism. Oncotarget. 2017 Jan 3;8(1):967-978. doi: 10.18632/oncotarget.13514. PubMed PMID: 27888615; PubMed Central PMCID: PMC5352210.

6: Abhishek K, Sardar AH, Das S, Kumar A, Ghosh AK, Singh R, Saini S, Mandal A, Verma S, Kumar A, Purkait B, Dikhit MR, Das P. Phosphorylation of Translation Initiation Factor 2-Alpha in Leishmania donovani under Stress Is Necessary for Parasite Survival. Mol Cell Biol. 2016 Dec 19;37(1). pii: e00344-16. Print 2017 Jan 1. PubMed PMID: 27736773; PubMed Central PMCID: PMC5192082.

7: Wu WS, Chien CC, Chen YC, Chiu WT. Protein Kinase RNA-Like Endoplasmic Reticulum Kinase-Mediated Bcl-2 Protein Phosphorylation Contributes to Evodiamine-Induced Apoptosis of Human Renal Cell Carcinoma Cells. PLoS One. 2016Aug 2;11(8):e0160484. doi: 10.1371/journal.pone.0160484. eCollection 2016. PubMed PMID: 27483435; PubMed Central PMCID: PMC4970736.

8: Celardo I, Costa AC, Lehmann S, Jones C, Wood N, Mencacci NE, Mallucci GR, Loh SH, Martins LM. Mitofusin-mediated ER stress triggers neurodegeneration in pink1/parkin models of Parkinson"s disease. Cell Death Dis. 2016 Jun 23;7(6):e2271. doi: 10.1038/cddis.2016.173. PubMed PMID: 27336715; PubMed Central PMCID: PMC5143399.

9: Guthrie LN, Abiraman K, Plyler ES, Sprenkle NT, Gibson SA, McFarland BC, Rajbhandari R, Rowse AL, Benveniste EN, Meares GP. Attenuation of PKR-like ER Kinase (PERK) Signaling Selectively Controls Endoplasmic Reticulum Stress-induced Inflammation Without Compromising Immunological Responses. J Biol Chem. 2016 Jul22;291(30):15830-40. doi: 10.1074/jbc.M116.738021. Epub 2016 May 23. PubMed PMID: 27226638; PubMed Central PMCID: PMC4957064.

10: Zhou Y, Qi B, Gu Y, Xu F, Du H, Li X, Fang W. Porcine Circovirus 2 Deploys PERK Pathway and GRP78 for Its Enhanced Replication in PK-15 Cells. Viruses. 2016 Feb 20;8(2). pii: E56. doi: 10.3390/v8020056. PubMed PMID: 26907328; PubMed Central PMCID: PMC4776210.

11: Chen TC, Chien CC, Wu MS, Chen YC. Evodiamine from Evodia rutaecarpa inducesapoptosis via activation of JNK and PERK in human ovarian cancer cells. Phytomedicine. 2016 Jan 15;23(1):68-78. doi: 10.1016/j.phymed.2015.12.003. Epub 2015 Dec 22. PubMed PMID: 26902409.

12: Yan F, Cao S, Li J, Dixon B, Yu X, Chen J, Gu C, Lin W, Chen G. Pharmacological Inhibition of PERK Attenuates Early Brain Injury After Subarachnoid Hemorrhage in Rats Through the Activation of Akt. Mol Neurobiol. 2017 Apr;54(3):1808-1817. doi: 10.1007/s12035-016-9790-9. Epub 2016 Feb 18. PubMed PMID: 26887383.

13: Radford H, Moreno JA, Verity N, Halliday M, Mallucci GR. PERK inhibition prevents tau-mediated neurodegeneration in a mouse model of frontotemporal dementia. Acta Neuropathol. 2015 Nov;130(5):633-42. doi: 10.1007/s00401-015-1487-z. Epub 2015 Oct 8. PubMed PMID: 26450683; PubMed Central PMCID: PMC4612323.

14: Johari YB, Estes SD, Alves CS, Sinacore MS, James DC. Integrated cell and process engineering for improved transient production of a "difficult-to-express" fusion protein by CHO cells. Biotechnol Bioeng. 2015 Dec;112(12):2527-42. doi: 10.1002/bit.25687. Epub 2015 Sep 7. PubMed PMID: 26126657.

15: Jamison S, Lin Y, Lin W. Pancreatic endoplasmic reticulum kinase activation promotes medulloblastoma cell migration and invasion through induction of vascular endothelial growth factor A. PLoS One. 2015 Mar 20;10(3):e0120252. doi:10.1371/journal.pone.0120252. eCollection 2015. PubMed PMID: 25794107; PubMed Central PMCID: PMC4368580.

16: Halliday M, Radford H, Sekine Y, Moreno J, Verity N, le Quesne J, Ortori CA,Barrett DA, Fromont C, Fischer PM, Harding HP, Ron D, Mallucci GR. Partial restoration of protein synthesis rates by the small molecule ISRIB prevents neurodegeneration without pancreatic toxicity. Cell Death Dis. 2015 Mar 5;6:e1672. doi: 10.1038/cddis.2015.49. PubMed PMID: 25741597; PubMed Central PMCID: PMC4385927.

17: Moon HS, Kim B, Gwak H, Suh DH, Song YS. Autophagy and protein kinase RNA-like endoplasmic reticulum kinase (PERK)/eukaryotic initiation factor 2 alpha kinase (eIF2α) pathway protect ovarian cancer cells from metformin-induced apoptosis. Mol Carcinog. 2016 Apr;55(4):346-56. doi: 10.1002/mc.22284. Epub 2015Feb 7. PubMed PMID: 25663310.

18: Lin LC, Sibille E. Somatostatin, neuronal vulnerability and behavioral emotionality. Mol Psychiatry. 2015 Mar;20(3):377-87. doi: 10.1038/mp.2014.184. Epub 2015 Jan 20. PubMed PMID: 25600109; PubMed Central PMCID: PMC4355106.

19: Ounallah-Saad H, Sharma V, Edry E, Rosenblum K. Genetic or pharmacological reduction of PERK enhances cortical-dependent taste learning. J Neurosci. 2014 Oct 29;34(44):14624-32. doi: 10.1523/JNEUROSCI.2117-14.2014. PubMed PMID: 25355215.

20: Axten JM, Romeril SP, Shu A, Ralph J, Medina JR, Feng Y, Li WH, Grant SW, Heerding DA, Minthorn E, Mencken T, Gaul N, Goetz A, Stanley T, Hassell AM, Gampe RT, Atkins C, Kumar R. Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development. ACS Med Chem Lett. 2013 Aug 12;4(10):964-8. doi: 10.1021/ml400228e. eCollection 2013 Oct 10. PubMed PMID: 24900593; PubMed Central PMCID: PMC4027568.

品牌介绍


MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务。

MedKoo是世界领先的供应商之一的抗癌化学试剂和激酶抑制剂。我们制造、销售和分发高质量的抗癌小分子肿瘤学研究试剂。我们的使命是建立世界上最全面的抗癌小分子的集合。我们也为医药行业提供高质量的研究服务、医学研究机构和学术机构。我们致力于提供优质的服务和分子有竞争力的价格。MedKoo是您可靠的合作伙伴采购药物发现和药物分子。




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MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
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