Cellagen Technology LLC
 
작성일 : 14-08-11
[Cellagen Technology LLC] UCH-L1 inhibitor & other new products of Cellagen Tech.
UCH-L1 / Tyrosine kinase / Wnt inhibitor | CFTR potentiator | ER agonist


UCH-L1 inhibitor & other new products of Cellagen Technology


Product Name: LDN-57444 | UCH-L1inhibitor (#C5574)


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LDN-57444 is a specific inhibitor (Ki = 0.4 ?M) against Ubiquitin carboxy-terminal hydrolase L1 (UCH-L1), a

member of deubiquitinating enzymes (DUBs). LDN-57444 increased proliferation of SH-SY5Y cells, a UCH-

L1-expressing neuroblastoma line. [1]

 

As expression of UCH-L1 is highly specific to neurons and to cells of the diffuse neuroendocrine system and

their tumors, LDN-57444 is a useful tool for studying the roles of UCH-L1 in Alzheimer’s disease,

Parkinson’s disease, and other neurological disorders. [2,3]

 

Details

Chemical Formula:

 

C17H11Cl3N2O3

CAS No.:

 

668467-91-2

Molecular weight:

 

397.64

Purity:

> 98%

Appearance:

 

Yellow

Chemical name:

 

 1H-Indole-2,3-dione, 5-chloro-1-[(2,5-dichlorophenyl)methyl]-, 3-(O-acetyloxime)

Solubility:

 

Up to 25 mM in DMSO

Synonyms:

 

LDN-57444, LDN57444

Storage:

For longer shelf life, store solid powder or DMSO solution at -20oC


References

1. Liu Y, et al. Discovery of inhibitors that elucidate the role of UCH-L1 activity in the H1299 lung cancer cell

   line. Chem Biol. 2003; 10(9):837-46. Pubmed ID: 14522054

2. Cartier AE, et al. Regulation of synaptic structure by ubiquitin C-terminal hydrolase L1. J Neurosci. 2009; 29

   (24):7857-68. Pubmed ID: 19535597

3. Zhang M, et al. Control of BACE1 degradation and APP processing by ubiquitin carboxyl-terminal

   hydrolase L1. J Neurochem. 2012; 120(6):1129-38. Pubmed ID: 22212137


 

Product Name: VX-770 (Ivacaftor) | CFTR potentiator (#C8770)


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VX-770 (Ivacaftor) is a CFTR potentiator and has been shown to potentiate normal CFTR, as well as CFTR

with G551D and F508-del mutations. Ivacaftor directly binds to the ion channel, causes conformation change

and open the ion channel to improve chloride transportation. In primary cultured human CF bronchial epithelia

(HBE) carrying the G551D and F508del CFTR mutations, Ivacaftor (10 ?M) potently increases the forskolin-

stimulated Cl- secretion with an EC50 of 236 nM. [1]

 

VX-770 (Ivacaftor) is approved for cystic fibrosis patients with G551D mutation, and has shown efficacy in a

patient with S549N mutation. [2]


Details

Chemical Formula:

 

C24H28N2O3

CAS No.:

 

873054-44-5

Molecular weight:

 

392.49

Purity:

> 98%

Appearance:

 

Off-white

Chemical name:

 

N-(2,4-di-tert-butyl-5-hydroxyphenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide

Solubility:

 

Up to 100 mM in DMSO

Storage:

For longer shelf life, store solid powder or DMSO solution at -20oC


References

1. Van Goor F et al. Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770. , Proc

   Natl Acad Sci U S A. 2009; 106(44):18825-30. Pubmed ID: 19846789

2. McGarry ME and Nielson DW. Normalization of sweat chloride concentration and clinical improvement with

   ivacaftor in a patient with cystic fibrosis with mutation S549N. Chest. 2013; 144(4):1376-8.

   Pubmed ID: 24081349


 

Product Name: BAY-73-4506 (Regorafenib) | Tyrosine kinase inhibitor (#C2734)


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BAY-73-4506 (Regorafenib) is an orally active and highly potent inhibitor against multiple tyrosine kinases,

including VEGFR1/2/3, PDGFR?, Kit, RET and Raf-1. Regorafenib inhibits the proliferation of HUVEC cells

stimulated with VEGF, and inhibits FGFR signaling in breast cancer MCF-7 cells stimulated with FGF.

Regorafenib is anti-angiogenic due to its inhibitions against VEGFR2-TIE2 tyrosine kinase. [1]

Co-administration of Regorafenib and a PI3K/Akt inhibitor (MK-2206) clearly demonstrated synergistic effect

in a HCT116 xenocraft mouse model [2]. Regorafenib is currently being studied as a potential treatment

option in multiple tumor types, and has recently be approved in treating patients with Metastatic Colorectal

cancer. [3]


Details

Chemical Formula:

 

C21H15CIF4N4O3

CAS No.:

 

755037-03-7

Molecular weight:

 

482.82

Purity:

> 98%

Appearance:

 

White

Chemical name:

 

1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-

4-yloxy)phenyl)urea

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

BAY-73-4506, BAY73-4506, Regorafenib, Fluoro-Sorafenib

Storage:

For longer shelf life, store solid powder or DMSO solution at -20oC


References

1. Wilhelm SM et al, Regorafenib (BAY 73-4506): a new oral multi-kinase inhibitor of angiogenic, stromal and

   oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011; 129:245-55

   Pubmed ID: 21170960

2. Sajithlal GB et al. Sorafenib/regorafenib and phosphatidyl inositol 3 kinase/thymoma viral proto-oncogene

   Inhibition interact to kill tumor cells. Mol Pharmacol. 2013; 84(4):562-71. Pubmed ID: 23877009

3. Carter NJ. Regorafenib: a review of its use in previously treated patients with progressive metastatic

   colorectal cancer. Drugs Aging. 2014; 31(1):67-78. Pubmed ID: 24276917



Product Name: Zearalenone (Toxin F2) | ER agonist (#C9327)


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Zearalenone is a heat-resistant mycotoxin produced by fungi in food and animal feeds [1]. It acts as an

estrogen receptor agonist and can cause hormonal effects in animal species such as the pig [2]. Evidence

for Zearalenone effects have been observed in a wide variety of animals. The association between

Zearalenone exposure and human diseases remains speculative at present; it has been considered as a

possible causative agent in outbreaks of precocious pubertal changes in young children and has been

suggested to have a possible involvement in human cervical cancer. [3,4]


Details

Chemical Formula:

 

C18H22O5

CAS No.:

 

17924-93-4

Molecular weight:

 

318.36

Purity:

> 98%

Appearance:

 

Off-white

Chemical name:

 

(3S,?11E)-?3,?4,?5,?6,?9,?10-?hexahydro-?14,?16-?dihydroxy-?3-?methyl-?1H-?2-

?benzoxacyclotetradecin-?1,?7(8H)-?dione

Solubility:

 

Up to 50 mM in DMSO

Synonyms

 

Zearalenone, Mycotoxin F2, FES, Zenone, Toxin F2

Storage:

For longer shelf life, store solid powder or DMSO solution at -20oC


References:

1. Zinedine A, et al. Review on the toxicity, occurrence, metabolism, detoxification, regulations and intake of

   zearalenone: An oestrogenic mycotoxin. Food Chem Toxicol, 2007; 45:1-18 Pubmed ID: 17045381

2. Tiemann U. and Dänicke S. In vivo and in vitro effects of the mycotoxins zearalenone and deoxynivalenol

   on different non-reproductive and reproductive organs in female pigs: A review.Food Addit Contam, 2007;

   24:306-314 Pubmed ID: 17364934

3. Caloni F. and Cortinovis C. Effects of fusariotoxins in the equine species. Vet J, 2010; 186:157-161 Pubmed

   ID: 19837621

4. Massart F. and Saggese G. Oestrogenic mycotoxin exposures and precocious pubertal development. Int J

   Androl, 2010; 33:369-376 Pubmed ID: 17364934

 


Product Name: NVP-LGK974 | Wnt inhibitor (#C6545)


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LGK974 is a potent and orally active Wnt pathway inhibitor with an IC50<1 nM in the Wnt signaling assay [1].

It inhibits acylation of Wnt proteins by Porcupine (Porcn). LGK974 specifically blocks the proliferation of

pancreatic cancer cells that have up-regulated Wnt signaling caused by carrying inactive mutations in a

Ubiquitin E3 ligase, RNF43 [2].

 

LGK974 robustly suppressed Wnt signaling in vivo resulting in tumor regression in a murine breast cancer

model driven by MMTV-Wnt1, and showed excellent efficacy in xenograft models of head and neck

squamous cell carcinoma and pancreatic cancer [3]. Currently LGK974 is in the Phase I study to treat

patients with different types of Wnt signaling-driven cancers [4].


Details

Chemical Formula:

 

C23H20N6O

CAS No.:

 

1243244-14-5

Molecular weight:

 

396.44

Purity:

> 98%

Appearance:

 

White

Chemical name:

 

 2-(2',3-dimethyl-[2,4'-bipyridin]-5-yl)-N-(5-(pyrazin-2-yl)pyridin-2-yl)acetamide

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

NVP-LGK974, LGK974

Storage:

For longer shelf life, store solid powder or DMSO solution at -20oC


References:

1. Shifeng Pan. Discovery of LGK974: A selective Porcupine inhibitor targeting Wnt signaling in cancer. AACR

   Annual Meeting 2013.

2. Jiang X, et al. Inactivating mutations of RNF43 confer Wnt dependency in pancreatic ductal

   adenocarcinoma. Proc Natl Acad Sci USA. 2013; 110(31):12649-54. Pubmed ID: 23847203

3. Liu J, et al. Targeting Wnt-driven cancer through the inhibition of Porcupine by LGK974. Proc Natl Acad Sci

   U S A. 2013; 110(50):20224-9 Pubmed ID: 24277854

4. http://clinicaltrials.gov/show/NCT01351103


 

Ordering informations

Catalog No.

Product Name

Size

C5574

LDN-57444 | UCH-L1inhibitor

5mg, 25mg & 100mg

C8770

VX-770 (Ivacaftor) | CFTR potentiator

5mg, 25mg & 100mg

C2734

BAY-73-4506 (Regorafenib) | Tyrosine kinase inhibitor

5mg, 25mg & 100mg

C9327

Zearalenone (Toxin F2) | ER agonist

10mg, 50mg & 250mg

C6545

NVP-LGK974 | Wnt inhibitor

2mg, 10mg & 50mg


 

* 관련제품 정보

Stem Cell Pathway and Chemical Modulators

Stem Cell Pathway Modulating Compounds



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