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

LRRK2-IN-1

CAS No. : 1234480-84-2

產(chǎn)品活性：LRRK2-IN-1 is a potent and selective?LRRK2?inhibitor with?IC₅₀?of 6 nM and 13 nM for LRRK2 (G2019S) and LRRK2 (WT), respectively.

研究領域：Autophagy  |  Apoptosis

作用靶點：LRRK2  |  Apoptosis

In Vitro: Wild-type and G2019S transduction results in 2.5 fold higher TR-FRET signal which can be inhibited by LRRK2-IN-1 in a dose-dependent manner with IC₅₀ values of 0.08 µM and 0.03 µM, respectively. LRRK2-IN-1 possessed an IC₅₀ of 45 nM for inhibition of DCLK2 and exhibits an IC₅₀ of greater than 1 µM when evaluated in biochemical assays for AURKB, CHEK2, MKNK2, MYLK, NUAK1, and PLK1. LRRK2-IN-1 is confirmed to inhibit MAPK7 with an EC₅₀ of 160 nM. LRRK2-IN-1 induces a dose dependent inhibition of Ser910 and Ser935 phosphorylation accompanied by loss of 14-3-3 binding to both wild type LRRK2 and LRRK2[G2019S] stably transfected into HEK293 cells. LRRK2-IN-1 is moderately cytotoxic with IC₅₀ of 49.3 µM in HepG2 cells. LRRK2-IN-1 exhibits genotoxicity in the presence and absence of S9 at 15.6 and 3.9 µM, respectively. LRRK2-IN-1 inhibits proliferation, migration, and induces cell death with hallmarks of apoptosis of HCT116 and AsPC-1 cells.

In Vivo: LRRK2-IN-1 (100 mg/kg, i.p.) induces dephosphorylation of LRRK2 in the kidney of the mice. Peritumoral injection of LRRK2-IN-1 (100 mg/kg) results in a significant decrease in tumor volume and weight of AsPC-1 tumor xenografts.

相關產(chǎn)品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Parkinson's Disease Compound Library  |  Neurodegenerative Disease-related Compound Library  |  Targeted Diversity 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  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  AZA1  |  Bleomycin A5  |  Xevinapant  |  Mangiferin  |  Cambinol  |  hGGPPS-IN-1  |  Bafetinib  |  Dinoprost-d₄

熱門產(chǎn)品線：重組蛋白  |  化合物庫  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標記物  |  寡核苷酸  |  抗體  |  點擊化學

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

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；
•   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，廣泛應用于新藥研發(fā)、生命科學等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學分析檢測分析，藥物篩選等專業(yè)技術服務；
•   設有專業(yè)的實驗中心和嚴格的質控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質檢報告，確保產(chǎn)品的高純度、高品質；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
•   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)團隊跟蹤最新的制藥及生命科學研究進展，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構建立了長期的合作。