Did you know ? If you order before Friday 14h we deliver 90PCT of the the time next Tuesday, GENTAUR another in time delivery

Pubmed ID :28657677
Publication Date : 2017/06/28

Effects of Pimozide Derivatives on pSTAT5 in K562 Cells.


STAT5 is a transcription factor, a member of the STAT family of signaling proteins. STAT5 is involved in many types of cancer, including chronic myelogenous leukemia (CML), in which this protein is found constitutively activated as a consequence of BCR-ABL expression. The neuroleptic drug pimozide was recently reported to act as an inhibitor of STAT5 phosphorylation and is capable of inducing apoptosis in CML cells in vitro. Our research group has synthesized simple derivatives of pimozide with cytotoxic activity and that are able to decrease the levels of phosphorylated STAT5. In this work we continued the search for novel STAT5 inhibitors, synthesizing compounds in which the benzoimidazolinone ring of pimozide is either maintained or modified, in order to obtain further structure-activity relationship information for this class of STAT5 inhibitors. Two compounds of the series showed potent cytotoxic activity against BCR-ABL-positive and pSTAT5-overexpressing K562 cells and were able to markedly decrease the levels of phosphorylated STAT5.

Authors : Rondanin Riccardo , Simoni Daniele , Maccesi Martina , Romagnoli Romeo , Grimaudo Stefania , Pipitone Rosaria Maria , Meli Maria , Cascio Antonio , Tolomeo Manlio ,

Related products :

Catalog number Product name Quantity
SL100489-K562 Transfection Reagents and Kits, GenJet™ DNA In Vitro Tranfection Reagent for K562 was pre_optimized for most efficiently transfecting K562 cells. 1 ml
orb61300 Vorinostat Vorinostat is a histone deacetylase inhibitor and causes growth arrest and death of some transformed cells both in vitro and in vivo, with little or no toxic effects on normal cells. For re 1 g
SL100489-K562 TRANSFECTION REAGENTS AND KITS, GENJET™ DNA TRANFECTION REAGENT PRE-OPTIMIZED FOR K562, EA, 1.0ML 5x1ML
SL100489-K562 TRANSFECTION REAGENTS AND KITS, GENJET™ DNA TRANFECTION REAGENT PRE-OPTIMIZED FOR K562, EA, 1.0ML 1ML
YM8070 CD55, K562 cells, Mab anti_Human; Clone 67 0.1 mg.
30-204 Retinoids exert biologic effects such as potent growth inhibitory and cell differentiation activities and are used in the treatment of hyperproliferative dermatological diseases. These effects are med 0.1 mg
31-058 CXCL3 may play a role in inflammation and exert its effects on endothelial cells in an autocrine fashion. 0.1 mg
orb82630 Cys Protein G GCSF is a pleiotropic cytokine best known for its specific effects on the proliferation, differentiation, and activation of hematopoietic cells of the neutrophilic granulocyte lineage. I 5 mg
orb84800 G-CSF protein GCSF is a pleiotropic cytokine best known for its specific effects on the proliferation, differentiation, and activation of hematopoietic cells of the neutrophilic granulocyte lineage. I 10
orb60536 Ubenimex Ubenimex is a competitive aminopeptidase B inhibitor with an IC50 of 100 mg_ml for K562 cells. For research use only. 10 mg
orb82832 Rhesus macaque GCSF protein RGCSF is a pleiotropic cytokine best known for its specific effects on the proliferation, differentiation, and activation of hematopoietic cells of the neutrophilic granulo 1 mg
orb60893 Matrine((+)-Matrine) Matrine((+)-Matrine) is an alkaloid found in plants from the Sophora family. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opio 50 mg
orb82613 Human GCSF protein GCSF is a pleiotropic cytokine best known for its specific effects on the proliferation, differentiation, and activation of hematopoietic cells of the neutrophilic granulocyte linea 2
LR-2072 pTF-LucTM Name: pStat5-Luc 2ug
LR-2072 pTF-LucTM: pStat5-Luc 2ug
LR-2072 pStat5-Luc report vector 2ug
LR-2072 pTF-LucTM pStat5-Luc report vector 2ug
SCH-LYS004B K562 CELL TOTAL PROTEIN LYSATE, Product Type Cell Lysate, Specificity K562 LYSATE, Target Species Human, Host N_A, Format Total Protein Lysate, Isotypes , Applications WB, Clone 1 mg
SCH-LYS004A K562 CELL TOTAL PROTEIN LYSATE, Product Type Cell Lysate, Specificity K562 LYSATE, Target Species Human, Host N_A, Format Total Protein Lysate, Isotypes , Applications WB, Clone 0.5 mg
LYS004B K562 CELL TOTAL PROTEIN LYSATE, Product Type Cell Lysate, Specificity K562 LYSATE, Target Species Human, Host N_A, Format Total Protein Lysate, Isotypes , Applications WB, Clone 1 mg
SCH-LYS004 K562 CELL TOTAL PROTEIN LYSATE, Product Type Cell Lysate, Specificity K562 LYSATE, Target Species Human, Host N_A, Format Total Protein Lysate, Isotypes , Applications WB, Clone 0.1 mg
LYS004 K562 CELL TOTAL PROTEIN LYSATE, Product Type Cell Lysate, Specificity K562 LYSATE, Target Species Human, Host N_A, Format Total Protein Lysate, Isotypes , Applications WB, Clone 0.1 mg
LYS004A K562 CELL TOTAL PROTEIN LYSATE, Product Type Cell Lysate, Specificity K562 LYSATE, Target Species Human, Host N_A, Format Total Protein Lysate, Isotypes , Applications WB, Clone 0.5 mg
1887-250 Pimozide 250 mg
1887-50 Pimozide 50 mg


 

GENTAUR Belgium BVBA BE0473327336
Voortstraat 49, 1910 Kampenhout BELGIUM
Tel 0032 16 58 90 45

Fax 0032 16 50 90 45
info@gentaur.com | Gentaur





GENTAUR Ltd.
Howard Frank Turnberry House
1404-1410 High Road
Whetstone London N20 9BH
Tel 020 3393 8531 Fax 020 8445 9411
uk@gentaur.com | Gentaur

 

 




GENTAUR France SARL
9, rue Lagrange, 75005 Paris
Tel 01 43 25 01 50

Fax 01 43 25 01 60
RCS Paris B 484 237 888

SIRET 48423788800017

BNP PARIBAS PARIS PL MAUBERT BIC BNPAFRPPPRG

france@gentaur.com | Gentaur

GENTAUR GmbH
Marienbongard 20
52062 Aachen Deutschland
Support Karolina Elandt
Tel: 0035929830070
Fax: (+49) 241 56 00 47 88

Logistic :0241 40 08 90 86
Bankleitzahl 39050000
IBAN lautet DE8839050000107569353
Handelsregister Aachen HR B 16058
Umsatzsteuer-Identifikationsnummer *** DE 815175831
Steuernummer 201/5961/3925
de@gentaur.com | Gentaur

GENTAUR U.S.A
Genprice Inc, Logistics
547, Yurok Circle
San Jose, CA 95123
CA 95123
Tel (408) 780-0908,
Fax (408) 780-0908,
sales@genprice.com

Genprice Inc, Invoices and accounting
6017 Snell Ave, Ste 357
San Jose, CA 95123




GENTAUR Nederland BV
NL850396268B01 KVK nummer 52327027
Kuiper 1
5521 DG Eersel Nederland
Tel:  0208-080893  Fax: 0497-517897
nl@gentaur.com | Gentaur
IBAN: NL04 RABO 0156 9854 62   SWIFT RABONL2U






GENTAUR Spain
tel:0911876558
spain@gentaur.com | Gentaur






ГЕНТАУЪР БЪЛГАРИЯ
ID # 201 358 931 /BULSTAT
София 1000, ул. "Граф Игнатиев" 53 вх. В, ет. 2
Tel 0035924682280 Fax 0035924808322
e-mail: Sofia@gentaur.com | Gentaur
IBAN: BG11FINV91501014771636
BIC: FINVBGSF

GENTAUR Poland Sp. z o.o.


ul. Grunwaldzka 88/A m.2
81-771 Sopot, Poland
TEL Gdansk 058 710 33 44 FAX  058 710 33 48              

poland@gentaur.com | Gentaur

Other countries

Österreich +43720880899

Canada Montreal +15149077481

Ceská republika Praha +420246019719

Danmark +4569918806

Finland Helsset +358942419041

Magyarország Budapest +3619980547

Ireland Dublin+35316526556

Luxembourg+35220880274

Norge Oslo+4721031366

Sverige Stockholm+46852503438

Schweiz Züri+41435006251

US New York+17185132983

GENTAUR Italy
SRL IVA IT03841300167
Piazza Giacomo Matteotti, 6
24122 Bergamo Tel 02 36 00 65 93
Fax 02 36 00 65 94
italia@gentaur.com | Gentaur