MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

PDK4-IN-1 hydrochloride

產(chǎn)品活性：PDK4-IN-1 hydrochloride 是一種蒽醌衍生物，也是一種有效的，口服活性的丙酮酸脫氫酶激酶 4 (PDK4) 抑制劑，IC₅₀ 值為 84 nM。PDK4-IN-1 hydrochloride 有效抑制細(xì)胞轉(zhuǎn)化和細(xì)胞增殖并誘導(dǎo)細(xì)胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病，抗癌和抗過敏作用。

研究領(lǐng)域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶點(diǎn)：PDHK  |  Apoptosis

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 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.

相關(guān)產(chǎn)品：Natural Product-like Compound Library  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Immunology/Inflammation Compound Library  |  Kinase Inhibitor Library  |  Metabolism/Protease Compound Library  |  Anti-Cancer Compound Library  |  Anti-diabetic Compound Library  |  Glycolysis Compound Library  |  Orally Active Compound Library  |  Anti-Cancer Metabolism Compound Library  |  Mitochondria-Targeted Compound Library  |  Glucose Metabolism Compound Library  |  Targeted Diversity Library  |  Heterocyclic Compound Library  |  TCA Cycle Compound Library  |  SY-5609  |  BRD4 Inhibitor-18  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  AAPK-25  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  Abacavir sulfate  |  Meloxicam-d₃-1  |  Thailanstatin D  |  SB-218078  |  Toyocamycin  |  Sorafenib-d₄  |  Busulfan  |  PTC-028  |  Dinaciclib  |  CR-1-31-B  |  AZD7545  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  AZA1  |  Bleomycin A5  |  Xevinapant  |  Mangiferin  |  Cambinol  |  hGGPPS-IN-1  |  Bafetinib

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種全球僅有化合物庫，我們致力于為全球科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項(xiàng)目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團(tuán)隊(duì)跟蹤最新的制藥及生命科學(xué)研究進(jìn)展，為您提供全球新的活性化合物；
•   與世界各大制藥公司及著名科研機(jī)構(gòu)建立了長期的合作。