PDK4-IN-1 hydrochloride

Product Name: PDK4-IN-1 hydrochloride
CAS No.: 2310262-11-2
Chemical Name: PDK4-IN-1 hydrochloride
Synonyms: PDK4-IN-1 HCl;PDK4-IN-1 hydrochloride;PDK4-IN-1 hydrochloride, 10 mM in DMSO;1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride;inhibit,anti-allergic,Pyruvate dehydrogenase kinase,PDHE1α,antidiabetic,p53,BCL-xL,PARP1,caspase-3,BAX,Inhibitor,p-Akt,Apoptosis,PDK4,PDK4 IN 1 hydrochloride,PDK4IN1 hydrochloride,PDK-4-IN-1 hydrochloride,PDHK,metabolites,PDH kinase,anticancer
CBNumber: CB98044775
Molecular Formula: C22H20ClN3O2
Formula Weight: 393.87
MOL File: 2310262-11-2.mol

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PDK4-IN-1 hydrochloride Property

storage temp.: Inert atmosphere,Room Temperature
solubility: DMSO: 125 mg/mL (317.36 mM)
form: Solid
color: Light yellow to yellow
Water Solubility: H2O: 2mg/mL, clear (Warmed)
InChIKey: ZIMLKZKPNALXKK-UHFFFAOYSA-N
SMILES: Cl.[n]2(ncc(c2)c3c4c(ccc3)C(=O)c5c(cccc5)C4=O)C1CCNCC1

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Safety

WGK Germany: WGK 3
Storage Class: 11 - Combustible Solids

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene

Product number: CS-0116441
Product name: PDK4-IN-1(hydrochloride)
Purity: 99.48%
Packaging: 5mg
Price: $380
Updated: 2021/12/16

ChemScene

Product number: CS-0116441
Product name: PDK4-IN-1(hydrochloride)
Purity: 99.48%
Packaging: 10mg
Price: $580
Updated: 2021/12/16

ChemScene

Product number: CS-0116441
Product name: PDK4-IN-1(hydrochloride)
Purity: 99.48%
Packaging: 50mg
Price: $1650
Updated: 2021/12/16

ChemScene

Product number: CS-0116441
Product name: PDK4-IN-1(hydrochloride)
Purity: 99.48%
Packaging: 100mg
Price: $2350
Updated: 2021/12/16

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PDK4-IN-1 hydrochloride Chemical Properties,Usage,Production

Uses

PDK4-IN-1 hydrochloride 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 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity[1].

Biological Activity

PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent, orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with IC50 of 84 nM. It effectively inhibits cell transformation and cell proliferation and induces apoptosis. It has antidiabetic, anticancer and antiallergic effects.

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. 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 Ser ²³² , Ser ²⁹³ , and Ser ³⁰⁰ of PDHE1α.
10 μM of PDK4-IN-1 (Compound 8c) significantly increased 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.

Cell Viability Assay

td>

Cell Line:	HCT116 and RKO cells
Concentration:	50 μM
Incubation Time:	0 hour, 24 hours, 48 hours, 72hours
Result:	Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO.

Apoptosis Analysis

< td class="col2"> 24 hours

Cell Line:	HCT116 and RKO cells
Concentration:	10 μM, 25 μM, 50 μM
Incubation Time:
Result:	Dose-depend ently increased apoptosis.

Western Blot Analysis < /p>

Cell Line:	HEK293T human embryonic kidney cells
Concentration:	10 μM
Incubation Time: < /td>	24 hours
Result:	Inhibited phosphorylation of Ser ²³² , Ser ²⁹³ , and Ser ³⁰⁰ of PDHE1α.

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 it (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.

td>

Animal Model:	C57BL/6J mice (8 -week old) fed with high-fat diet
Dosage:	100 mg/kg
Administration:	Oral adminis tration; daily; for 1 week
Result:	Significantly improved glucose tolerance.

target

IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4))

References

[1] Lee D, et al. Discovery of Novel Pyruvate Dehydrogenase Kinase 4 Inhibitors for Potential Oral Treatment of Metabolic Diseases. J Med Chem. 2019 Jan 24;62(2):575-588. DOI:10.1021/acs.jmedchem.8b01168

PDK4-IN-1 hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

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PDK4-IN-1 hydrochloride Suppliers

China 29 United States 3 Global 32

Bide Pharmatech Ltd.

Tel: 400-400-164-7117 18317119277
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Shanghai Beckham Medical Technology Co., Ltd

Tel: 13816613772
Fax: QQ: 12922499
Email: huahero21@sina.com
Country: China
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Shanghai Rechem science Co., Ltd.

Tel: 021-31433387 15618786686
Fax: QQ:1369748377
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Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840 18892239720
Fax: 010-60605840
Email: psaitong@jm-bio.com
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MQ (shanghai) Pharmaceuticals Co., Ltd.

Tel: 13761635123
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TargetMol Chemicals Inc.

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Changzhou Chenhong Biotechnology Co., Ltd.

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ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Tel: 18818260767
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Shandong Territorial sea Biological Technology Co., LTD

Tel: 15092083467
Email: 18660263263@163.com
Country: China
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Beijing Jin Ming Biotechnology Co., Ltd.

Tel: 010-60605840 15801484223;
Email: psaitong@jm-bio.com
Country: China
ProdList: 29757
Advantage: 58

2310262-11-2, PDK4-IN-1 hydrochlorideRelated Search:

PDK4-IN-1 hydrochloride

1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride

inhibit,anti-allergic,Pyruvate dehydrogenase kinase,PDHE1α,antidiabetic,p53,BCL-xL,PARP1,caspase-3,BAX,Inhibitor,p-Akt,Apoptosis,PDK4,PDK4 IN 1 hydrochloride,PDK4IN1 hydrochloride,PDK-4-IN-1 hydrochloride,PDHK,metabolites,PDH kinase,anticancer

PDK4-IN-1 hydrochloride, 10 mM in DMSO

PDK4-IN-1 HCl

2310262-11-2