N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide

Product Name: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
CAS No.: 702675-74-9
Chemical Name: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Synonyms: BX 795;CS-544;BX795, >97%;BX795/BX-795;BX 795, >=98%;BX-795 hydrochloride;BX-795; BX 795; BX795.;BX-795 - CAS 702675-74-9 - Calbiochem;IKK,Inhibitor,BX795,BX-795,I kappa B kinase,inhibit,IκB kinase,PDK-1,BX 795,Autophagy;N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrr
CBNumber: CB42484697
Molecular Formula: C23H26IN7O2S
Formula Weight: 591.47
MOL File: 702675-74-9.mol

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N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Property

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

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Safety

WGK Germany: 3

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0694
Product name: BX-795 hydrochloride
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $105
Updated: 2024/03/01

Sigma-Aldrich

Product number: 204001
Product name: BX-795
Packaging: 10mg
Price: $225
Updated: 2024/03/01

Cayman Chemical

Product number: 14932
Product name: BX-795
Purity: ≥98%
Packaging: 5mg
Price: $81
Updated: 2024/03/01

Cayman Chemical

Product number: 14932
Product name: BX-795
Purity: ≥98%
Packaging: 10mg
Price: $152
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0694
Product name: BX-795 hydrochloride
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $255
Updated: 2024/03/01

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N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Chemical Properties,Usage,Production

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

Raw materials

Preparation Products

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N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide Suppliers

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Shanghai Boyle Chemical Co., Ltd.

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View Lastest Price from N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.

Product: BX-795 702675-74-9
Price: US $0.00/kg
Min. Order: 1kg
Purity: 99% HPLC
Supply Ability: 1000kg
Release date: 2022-11-09

Career Henan Chemical Co

Product: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide 702675-74-9
Price: US $5.00/KG
Min. Order: 1KG
Purity: 99%
Supply Ability: 1ton
Release date: 2019-09-03

Career Henan Chemical Co

Product: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide 702675-74-9
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-24

702675-74-9, N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamideRelated Search:

NOTUMib-1 N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Dequalinium chloride NORFLUOXETINE HYDROCHLORIDE Iodine solution Sotrastaurin xav-939 MK-2206 2HCl Saracatinib Panobinostat LY 294002 HYDROCHLORIDE

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

BX795N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide

BX 795, >=98%

BX-795; BX 795; BX795.

CS-544

BX-795 - CAS 702675-74-9 - Calbiochem

BX795, >97%

N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrr

1-Pyrrolidinecarboxamide,N-[3-[[5-iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-

N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide

N-{3-[(5-iodo-4-{[3-(thiophen-2-ylformamido)propyl]amino}pyrimidin-2-yl)amino]phenyl}pyrrolidine-1-carboxamide

N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide USP/EP/BP

IKK,Inhibitor,BX795,BX-795,I kappa B kinase,inhibit,IκB kinase,PDK-1,BX 795,Autophagy

702675-74-9

C23H26IN7O2S

Inhibitors

Akt

mTOR

PI3K

API