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BX-795 - ≥97%, high purity , CAS No.702675-74-9, 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

  • Moligand™
  • ≥97%
Item Number
B126947
Grouped product items
SKUSizeAvailabilityPrice Qty
B126947-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$18.90
B126947-10mg
10mg
In stock
$142.90
B126947-50mg
50mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$482.90
B126947-100mg
100mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$652.90

PDK1 inhibitor. Potent TBK1 and IKKε inhibitor

Basic Description

Synonyms702675-74-9|BX795|BX-795|BX 795|N-[3-[[5-IODO-4-[[3-[(2-THIENYLCARBONYL)AMINO]PROPYL]AMINO]-2-PYRIMIDINYL]AMINO]PHENYL]-1-PYRROLIDINECARBOXAMIDE|N-(3-((5-iodo-4-((3-(thiophene-2-carboxamido)propyl)amino)pyrimidin-2-yl)amino)phenyl)pyrrolidine-1-carboxamid
Specifications & PurityMoligand™, ≥97%
Biochemical and Physiological MechanismsBX 795 is shown to be a specific and potent inhibitor of IκB kinase ε (IKKε), phosphoinositide 3-kinase 1 (PDK1), and TANK-binding kinase 1 (TBK1). These protein kinases regulate production of type 1 interferons during certain infections. BX 795 has been
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor 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
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

BX795 is a potent and specific PDK1 inhibitor with IC50 of 6 nM, 140- and 1600-fold more selective for PDK1 than PKA and PKC, respectively. Meanwhile, in comparison to GSK3β more than 100-fold selectivity observed for PDK1.
An inhibitor of PDK1, TBK1, and IKK&epsilon

Names and Identifiers

IUPAC Name N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide
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)
InChi Key VAVXGGRQQJZYBL-UHFFFAOYSA-N
Canonical SMILES C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I
Isomeric SMILES C1CCN(C1)C(=O)NC2=CC=CC(=C2)NC3=NC=C(C(=N3)NCCCNC(=O)C4=CC=CS4)I
PubChem CID 10077147
Molecular Weight 591.47

Certificates

Certificate of Analysis(COA)

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3 results found

Lot NumberCertificate TypeDateItem
B1512010Certificate of AnalysisJun 03, 2024 B126947
H2409680Certificate of AnalysisApr 01, 2024 B126947
L2219182Certificate of AnalysisJan 10, 2023 B126947

Chemical and Physical Properties

SolubilityDMSO 100 mg/mL Water <1 mg/mL Ethanol <1 mg/mL

Related Documents

References

1. Feldman RI, Wu JM, Polokoff MA, Kochanny MJ, Dinter H, Zhu D, Biroc SL, Alicke B, Bryant J, Yuan S et al..  (2005)  Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1..  J Biol Chem,  280  (20): (19867-74).  [PMID:15772071]
2. Clark K, Plater L, Peggie M, Cohen P.  (2009)  Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IkappaB kinase epsilon: a distinct upstream kinase mediates Ser-172 phosphorylation and activation..  J Biol Chem,  284  (21): (14136-46).  [PMID:19307177]
3. Hasan M, Yan N.  (2016)  Therapeutic potential of targeting TBK1 in autoimmune diseases and interferonopathies..  Pharmacol Res,  111  (3): (336-42).  [PMID:27353409]

Solution Calculators