Product Name :
VER-246608
Description:
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
CAS:
1684386-71-7
Molecular Weight:
552.96
Formula:
C28H23ClF2N4O4
Chemical Name:
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-({4-[(2,2-difluoroacetamido)methyl]phenyl}methyl)-2,4-dihydroxybenzamide
Smiles :
CC1=CN=C(Cl)N=C1C1C=CC(=CC=1)N(CC1C=CC(CNC(=O)C(F)F)=CC=1)C(=O)C1=CC=C(O)C=C1O
InChiKey:
LCGNLQSOSJFLKR-UHFFFAOYSA-N
InChi :
InChI=1S/C28H23ClF2N4O4/c1-16-13-33-28(29)34-24(16)19-6-8-20(9-7-19)35(27(39)22-11-10-21(36)12-23(22)37)15-18-4-2-17(3-5-18)14-32-26(38)25(30)31/h2-13,25,36-37H,14-15H2,1H3,(H,32,38)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.|Product information|CAS Number: 1684386-71-7|Molecular Weight: 552.96|Formula: C28H23ClF2N4O4|Chemical Name: N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-({4-[(2,2-difluoroacetamido)methyl]phenyl}methyl)-2,4-dihydroxybenzamide|Smiles: CC1=CN=C(Cl)N=C1C1C=CC(=CC=1)N(CC1C=CC(CNC(=O)C(F)F)=CC=1)C(=O)C1=CC=C(O)C=C1O|InChiKey: LCGNLQSOSJFLKR-UHFFFAOYSA-N|InChi: InChI=1S/C28H23ClF2N4O4/c1-16-13-33-28(29)34-24(16)19-6-8-20(9-7-19)35(27(39)22-11-10-21(36)12-23(22)37)15-18-4-2-17(3-5-18)14-32-26(38)25(30)31/h2-13,25,36-37H,14-15H2,1H3,(H,32,38)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 100 mg/mL (180.84 mM; Need ultrasonic).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Afatinib} web|{Afatinib} Autophagy|{Afatinib} Purity & Documentation|{Afatinib} References|{Afatinib} manufacturer|{Afatinib} Epigenetics} |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|VER-246608 is a novel pan-isoform ATP competitive inhibitor of PDK.{{Allopurinol} medchemexpress|{Allopurinol} Metabolic Enzyme/Protease|{Allopurinol} Biological Activity|{Allopurinol} Formula|{Allopurinol} manufacturer|{Allopurinol} Cancer} VER-246608 demonstrates similar potency across all four PDK isoforms in a DELFIA-based enzyme functional assay in the sub 100 nM range.PMID:32180353 In terms of cellular biomarker modulation, VER-246608 suppresses the phosphorylation of the Ser293 residue of E1α (phosphorylated by all four PDK isozymes) with IC50 values of 266 nM. Treatment of PC-3 cells with 9 μM and 27 μM VER-246608 results in a 21% and 42% reduction, respectively, in media L-lactate levels following a 1 h incubation. VER-246608 also decreases D-glucose consumption at the same concentrations that result in reduced L-lactate production. An approximately 50% reduction in spheroid volume is achieved at concentrations of 10 μM and above, suggesting an increase in VER-246608 potency compared to monolayer growth.|Products are for research use only. Not for human use.|