Determine the necessary mass, volume, or concentration for preparing a solution.
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SKU | Size | Availability | Price | Qty |
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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
Synonyms | 5-bromo-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]pyrimidine-2,4-dione | AKOS016369934 | AS-16196 | 4-(2-bromoethyloxy)-nitrobenzene | CS-0259 | HMS3672K09 | BX-795, 3 | N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimid |
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Specifications & Purity | Moligand™, ≥97% |
Biochemical and Physiological Mechanisms | BX 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 Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
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 |
Note | Wherever 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. |
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IUPAC Name | N-[3-[[5-iodo-4-[3-(thiophene-2-carbonylamino)propylamino]pyrimidin-2-yl]amino]phenyl]pyrrolidine-1-carboxamide |
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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 |
PubChem CID | 10077147 |
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ChEMBL Ligand | CHEMBL577784 |
CAS Registry No. | 702675-74-9 |
RCSB PDB Ligand | BX7 |
Enter Lot Number to search for COA:
Solubility | DMSO 100 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
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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] |