BX-795 - Moligand™, 10mM in DMSO , Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of aurora kinase B;Inhibitor of checkpoint kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of in, Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of aurora kinase B;Inhibitor of checkpoint kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of inhibitor of nuclear factor kappa B k

CAS: 702675-74-9 Cat. No.: B408917 Molecular Weight: 591.47
AVAILABLE TO ORDER
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
N-(3-(5-iodo-4-(3-(thiophene-2-carboxamido)propylamino)pyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
 ·  off list, applied to all prices below.
Size
Status
Price
Qty
1ml
B408917-1ml
2

$187.90

$219.90
Save $32.00 (14.55%)
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 1 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

Information

BX-795 BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. B
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/IKKɛ, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation.

In vivo


Cell Data

cell lines:

Concentrations:~10 μM

Incubation Time:72 hours

Powder Purity:≥97%

Specifications

Synonyms
N-(3-(5-iodo-4-(3-(thiophene-2-carboxamido)propylamino)pyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
Specifications & Purity
Moligand™, 10mM in DMSO
Biochemical and Physiological Mechanisms
BX-795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC in cell-free assays, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1. BX-795 mod
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
This product requires cold chain shipping. Ground and other economy services are not available.
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of 3-phosphoinositide dependent protein kinase 1;Inhibitor of aurora kinase B;Inhibitor of checkpoint kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of glycogen synthase kinase 3 beta;Inhibitor of inhibitor of nuclear factor kappa B k
Names and Identifiers
Isomeric SMILES C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I
Molecular Weight 591.47
Reaxy-Rn 15690029
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15690029&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Associated Targets(Human)
CGAS Tchem Cyclic GMP-AMP synthase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CDK2 Tchem Cyclin-dependent kinase 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
IKBKE Tchem Inhibitor of nuclear factor kappa-B kinase subunit epsilon (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TBK1 Tchem Serine/threonine-protein kinase TBK1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CHEK1 Tchem Serine/threonine-protein kinase Chk1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GSK3B Tclin Glycogen synthase kinase-3 beta (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PDPK1 Tchem 3-phosphoinositide-dependent protein kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificates(CoA,COO,BSE/TSE and Analysis Chart)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Documents & Articles
Citations of This Product
References
1. Jingyun Li, Siqi Zeng, Enyuan Zhang, Ling Chen, Jingbin Jiang, Jun Li.  (2024)  Spatial metabolomics to discover hypertrophic scar relevant metabolic alterations and potential therapeutic strategies: A preliminary study.  BIOORGANIC CHEMISTRY,      [PMID:39383811] [10.1016/j.bioorg.2024.107873]
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