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| | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Basic information |
| Product Name: | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide | | Synonyms: | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide;BX 795;N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)aMino]propyl]aMino]-2-pyriMidinyl]aMino]phenyl]-1-pyrrolidin;BX795/BX-795;N-(3-(5-IODO-4-(3-(THIOPHENE-2-CARBOXAMIDO)PROPYLAMINO)PYRIMIDIN-2-YLAMINO)PHENYL)PYRROLIDINE-1-CARBOXAMIDE;N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide BX-795;BX-795 hydrochloride;N-[3-[[5-iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-Pyrrolidinecarboxamide hydrochloride | | CAS: | 702675-74-9 | | MF: | C23H26IN7O2S | | MW: | 591.47 | | EINECS: | 200-256-5 | | Product Categories: | Inhibitors;Akt;mTOR;PI3K;API | | Mol File: | 702675-74-9.mol | ![N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Structure](CAS/GIF/702675-74-9.gif) |
| | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Chemical Properties |
| Melting point | >163°C (dec.) | | density | 1.644 | | storage temp. | 2-8°C | | solubility | DMSO: soluble15mg/mL, clear | | form | powder | | pka | 12.57±0.70(Predicted) | | color | white to light brown | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. | | InChIKey | VAVXGGRQQJZYBL-UHFFFAOYSA-N |
| | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Usage And Synthesis |
| Description | 3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC. BX-795 is a potent, ATP-competitive inhibitor of PDK1 in vitro (IC50 = 11 nM) and in cells (IC50 = 300 nM). At comparable concentrations, BX-795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1, IκB kinase ε, and additional kinases. | | Uses | BX-795 hydrochloride has been used to study the effect of kinase inhibition on human endogenous retroviruses (HERVs) transcription activation. | | Definition | ChEBI: N-[3-[[5-iodo-4-[3-[[oxo(thiophen-2-yl)methyl]amino]propylamino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide is a member of ureas. | | Biochem/physiol Actions | BX-795 competes for the ATP (adenosine triphosphate) binding pocket of 3-phosphoinositide-dependent kinase-1 (PDK1) with its substrate ATP. In vitro assays reveal that BX-795 might inhibit Unc-51 (serine/threonine-protein kinase)-like autophagy activating kinase (ULK1). | | storage | Store at -20°C | | References | Feldman et al. (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1; J. Biol. Chem.?280 19867
Bain et al. (2007) The selectivity of protein kinase inhibitors: a further update; Biochem.? J. 408 297
Clark et al. (2009) Use of the Pharmacological Inhibitor BX795 to Study the Regulation and Physiological Roles of TBK1 and IkB Kinase ε; J.? Biol. Chem.?284 14136
Bai et al. (2015) BX795, a TBK1 inhibitor, exhibits antitumor activity in human oral squamous cell carcinoma through apoptosis induction and mitotic phase arrest; Eur.? J. Pharmacol.?769 287
Choi et al. (2019) A pharmacogenomic analysis using L1000CDS2 identifies BX-795 as a potential anticancer drug for primary pancreatic ductal adenocarcinoma cells; Cancer Lett.?465 82
Scuderi et al. (2021) TBK1 Inhibitor Exerts Antiproliferative Effect on Glioblastoma Multiforme Cells; Oncol.? Res.?28 779
Sutlu et al. (2012) Inhibition of Intracellular Antiviral Defense Mechanisms Augments Lentiviral Transduction of Human Natural Killer Cells: Implications for Gene Therapy; Hum. Gene Ther.?23 1090
Allan et al. (2021) Systematic improvements in lentiviral transduction of primary human natural killer cells undergoing e4x vivo expansion; Mol. Ther. Methods Clin. Dev.?20 559
Chockley et al. (2021) Transient blockade of TBK1/IKKε allows efficient transduction of primary human natural killer cells with vesicular stomatitis virus G-pseudotyped lentiviral vectors; Cytotherapy?23 787
Lingyu et al. (2020) Lentiviral delivery of combinatorial CAR/CRISPRi circuit into human primary T cells is enhanced by TBK1/IKKε complex inhibitor BX795; J. Transl. Med.?18 363 |
| | N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Preparation Products And Raw materials |
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