Product Name :
PDK4-IN-1
Description:
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
CAS:
2310262-10-1
Molecular Weight:
357.41
Formula:
C22H19N3O2
Chemical Name:
1-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9, 10-dione
Smiles :
O=C1C2=CC=CC(=C2C(=O)C2C=CC=CC1=2)C1C=NN(C=1)C1CCNCC1
InChiKey:
RUCYSQLKCYBLDW-UHFFFAOYSA-N
InChi :
InChI=1S/C22H19N3O2/c26-21-17-4-1-2-5-18(17)22(27)20-16(6-3-7-19(20)21)14-12-24-25(13-14)15-8-10-23-11-9-15/h1-7,12-13,15,23H,8-11H2
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:
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM.{{Tivantinib} medchemexpress|{Tivantinib} Inducer|{Tivantinib} Epigenetics|{Tivantinib} Protocol|{Tivantinib} Formula|{Tivantinib} custom synthesis} PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis.{{SKI II} MedChemExpress|{SKI II} Stem Cell/Wnt|{SKI II} Protocol|{SKI II} In stock|{SKI II} supplier|{SKI II} Autophagy} PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.|Product information|CAS Number: 2310262-10-1|Molecular Weight: 357.41|Formula: C22H19N3O2|Chemical Name: 1-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9, 10-dione|Smiles: O=C1C2=CC=CC(=C2C(=O)C2C=CC=CC1=2)C1C=NN(C=1)C1CCNCC1|InChiKey: RUCYSQLKCYBLDW-UHFFFAOYSA-N|InChi: InChI=1S/C22H19N3O2/c26-21-17-4-1-2-5-18(17)22(27)20-16(6-3-7-19(20)21)14-12-24-25(13-14)15-8-10-23-11-9-15/h1-7,12-13,15,23H,8-11H2|Technical Data|Appearance: Solid Power|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.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PDK4-IN-1 (Compound 8c; 50 μM; 0-72 hours; HCT116 and RKO cells) treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO.PMID:24190482 The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1. PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. PDK4-IN-1 (Compound 8c; 10 μM; 24 hours; HEK293T cells) treatment inhibits phosphorylation of Ser232, Ser293, and Ser300 of PDHE1α. 10 μM of PDK4-IN-1 (Compound 8c) significantly increases p-Akt in AML12 cells. PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1.|In Vivo:|PDK4-IN-1 (Compound 8c; 100 mg/kg; oral administration; daily; for 1 week; C57BL/6J mice) treatment significantly improves glucose tolerance. Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, showing that the absorbance values are 0.26, 0.20, and 0.126 in IgE/Ag, 10 μM, and 20 μM PDK4-IN-1-treated BMMCs. The pharmacokinetic (PK) profiles of PDK4-IN-1 (compound 8c) are evaluated in rat. PDK4-IN-1 shows good bioavailability (64%), long half-life (>7 h), and moderate clearance (CL of 0.69) in rats.|Products are for research use only. Not for human use.|
