Product Name :
BX-795
Description:
BX-795 is a potent PDK1 inhibitor. BX-795 also suppresses MARK1, MARK2, MARK4, NUAK1,
CAS:
702675-74-9
Molecular Weight:
591.47
Formula:
C23H26IN7O2S
Chemical Name:
N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Smiles :
O=C(NC1=CC(=CC=C1)NC1=NC(NCCCNC(=O)C2=CC=CS2)=C(I)C=N1)N1CCCC1
InChiKey:
VAVXGGRQQJZYBL-UHFFFAOYSA-N
InChi :
InChI=1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{ALC-0159} web|{ALC-0159} Liposome|{ALC-0159} Immunology/Inflammation|{ALC-0159} Technical Information|{ALC-0159} In stock|{ALC-0159} custom synthesis}
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
BX-795 is a potent PDK1 inhibitor. BX-795 also suppresses MARK1, MARK2, MARK4, NUAK1,|Product information|CAS Number: 702675-74-9|Molecular Weight: 591.47|Formula: C23H26IN7O2S|Synonym:|BX 795|BX795|BX-795|Chemical Name: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide|Smiles: O=C(NC1=CC(=CC=C1)NC1=NC(NCCCNC(=O)C2=CC=CS2)=C(I)C=N1)N1CCCC1|InChiKey: VAVXGGRQQJZYBL-UHFFFAOYSA-N|InChi: InChI=1S/C23H26IN7O2S/c24-18-15-27-22(30-20(18)25-9-5-10-26-21(32)19-8-4-13-34-19)28-16-6-3-7-17(14-16)29-23(33)31-11-1-2-12-31/h3-4,6-8,13-15H,1-2,5,9-12H2,(H,26,32)(H,29,33)(H2,25,27,28,30)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: Soluble in DMSO, not in water|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Citric acid} medchemexpress|{Citric acid} Endogenous Metabolite|{Citric acid} Purity & Documentation|{Citric acid} Formula|{Citric acid} custom synthesis|{Citric acid} Cancer} |Shelf Life: ≥12 months if stored properly.PMID:24187611 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|BX-795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX-795 potently inhibits tumor cell growth on plastic with IC50 of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX-795 displays higher growth inhibition with IC50 of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively. In addition, BX-795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. In platelet physiological responses, BX-795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation.|References:|Miyabe H, Hyodo M, Nakamura T, Sato Y, Hayakawa Y, Harashima H. A new adjuvant delivery system ‘cyclic di-GMP/YSK05 liposome’ for cancer immunotherapy. J Control Release. 2014 Jun 28;184:20-7. doi: 10.1016/j.jconrel.2014.04.004. Epub 2014 Apr 13. PubMed PMID: 24727060.Dangelmaier C, Manne BK, Liverani E, Jin J, Bray P, Kunapuli SP. PDK1 selectively phosphorylates Thr(308) on Akt and contributes to human platelet functional responses. Thromb Haemost. 2014 Mar 3;111(3):508-17. doi: 10.1160/TH13-06-0484. Epub 2013 Dec 19. PubMed PMID: 24352480; PubMed Central PMCID: PMC4079046.Parsons KS, Hsu AC, Wark PA. TLR3 and MDA5 signalling, although not expression, is impaired in asthmatic epithelial cells in response to rhinovirus infection. Clin Exp Allergy. 2014 Jan;44(1):91-101. doi: 10.1111/cea.12218. PubMed PMID: 24131248.Sun Q, Sammut B, Wang FM, Kurihara N, Windle JJ, Roodman GD, Galson DL. TBK1 mediates critical effects of measles virus nucleocapsid protein (MVNP) on pagetic osteoclast formation. J Bone Miner Res. 2014 Jan;29(1):90-102. doi: 10.1002/jbmr.2026. PubMed PMID:23794264; PubMed Central PMCID: PMC3870038.Minegishi Y, Iejima D, Kobayashi H, Chi ZL, Kawase K, Yamamoto T, Seki T, Yuasa S, Fukuda K, Iwata T. Enhanced optineurin E50K-TBK1 interaction evokes protein insolubility and initiates familial primary open-angle glaucoma. Hum Mol Genet. 2013 Sep 1;22(17):3559-67. doi: 10.1093/hmg/ddt210. Epub 2013 May 12. PubMed PMID: 23669351.Awe JP, Crespo AV, Li Y, Kiledjian M, Byrne JA. BAY11 enhances OCT4 synthetic mRNA expression in adult human skin cells. Stem Cell Res Ther. 2013 Feb 6;4(1):15. doi: 10.1186/scrt163. PubMed PMID: 23388106; PubMed Central PMCID: PMC3706837.Products are for research use only. Not for human use.|
