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MedChemExpress-Master of Small Molecules (Inhibitors, Agonists, Screening Libraries)

MedChemExpress - New Products January 2022

亞旭所代理的MedChemExpress (MCE) 提供多元的高品質研究化學品和生物化學品,包括用於實驗室和科學用途的新型生物活性化合物、染劑、胜肽和天然化合物。

 

• 超過 30,000 種生物活性分子化合物的庫存

• 超過針對 20 多種信號通路中的 500 多種關鍵目標蛋白的化合物

• 產品均附上品質報告書(LC/MS、NMR 和 HPLC)

• 每月發布超過500 種最新的產品

• 提供詳細Datasheet的資訊

• 高純度和有競爭力的價格

• 快速到貨

CAS No.: 2621928-55-8

MRTX1133

Research Area: KRAS G12D Inhibitor/Diverse Cancers

MRTX1133 structure

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Noncovalent, potent, and selective KRAS G12D inhibitor (KD=0.2 pM).

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Inhibits mutant KRAS-dependent signal and selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.

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Efficacious in a KRAS G12D mutant xenograft mouse tumor model.

Solubility: DMSO : 50 mg/mL (83.25 mM; Need ultrasonic)

Ivaltinostat formic

Research Area: HDAC Inhibitor/Prostate Cancer/Cholangiocarcinoma

Ivaltinostat formic structure

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An orally active, potent hydroxamate-based pan-HDAC inhibitor with antitumor effects.

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Enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-FU, thereby decreasing cell viability and inducing apoptosis.

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Inhibits deacetylation of histone H3 and tubulin in prostate cancer cells and induces clonogenic cell death by modulating acetylation of p53 in cancer cells.

Solubility: DMSO : 50 mg/mL (105.58 mM; Need ultrasonic)

H2O : 50 mg/mL (105.58 mM; Need ultrasonic)

CAS No.: 1352914-52-3

CR-1-31-B

Research Area: eIF4A Inhibitor/Neuroblastoma/Pancreatic Ductal Adenocarcinoma

CR-1-31-B structure

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A synthetic Rocaglate and potent eIF4A inhibitor with anticancer and antimalarial activities.

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Exhibits powerful inhibitory effects over eIF4A by perturbing the interaction between eIF4A and RNA, sequentially impeding initiation during protein synthesis.

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Induces apoptosis of neuroblastoma and gallbladder cancer cells.

Solubility: DMSO : 230 mg/mL (453.18 mM; Need ultrasonic)

MRTX9768 hydrochloride

Research Area: PRMT5•MTA Inhibitor/MTAP-del Cancer

MRTX9768 hydrochloride structure

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A synthetic lethal-based orally active PRMT5•MTA inhibitor.

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Selectively inhibits symmetric dimethylarginine (SDMA) marks and shows selective antitumor activity in MTAP-del tumor cells while sparing MTAP-WT cells.

Solubility: DMSO : 90 mg/mL (195.27 mM; Need ultrasonic)

H2O : 40 mg/mL (86.79 mM; Need ultrasonic)

CAS No.: 357425-68-4

CP-601932

Research Area: α3β4 nAChR Agonist/Alcohol Dependence

CP-601932 structure

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High-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~3 μM), has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and can penetrate the CNS.

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Selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure.

Solubility: DMSO : 200 mg/mL (880.17 mM; Need ultrasonic)

CAS No.: 245520-69-8

SCH79797

Research Area: PAR1 Antagonist/Myocardial Ischemia/Reperfusion Injury

SCH79797 structure

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Highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist.

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Inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 (IC50=70 nM; Ki=35 nM) and inhibits thrombin-induced platelet aggregation (IC50=3 μM).

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Limits myocardial ischemia/reperfusion injury in rat hearts.

Solubility: DMSO : 50 mg/mL (134.60 mM; Need ultrasonic)

Kinase 篩選服務

Kinase在新陳代謝、細胞信號傳導、蛋白質調節、細胞運輸、分泌過程和許多其他細胞路徑中至關重要,這使Kinase成為細胞功能的關鍵調節劑。 如果Kinase發生問題則會導致多種人類疾病的發生, 因此Kinase具有潛力可做為藥物的靶點。 然而真核生物Kinase(尤其是催化結構域)的高度保留結構給開發抑製劑帶來了巨大挑戰。 對於許多人來說,廣泛的分析需要新的Kinase抑制劑,進而了解kinase的結構與活性之間的關係。 MCE可以提供高品質和全面的Kinase檢測平台,其化合物和Kinase之間結合親和力/活性差異的實驗數據可以評估化合物的靶標選擇性。

mce-kinase-screening-en

主要特色:

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品項齊全:400 多種Kinase,包括 AGC、CAMK、CMGC、CK1、STE、TK、TKL 和常見突變體。

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靈活且可客製化的Kinase panel:Characteristic TK, CDK kinase profiles, 60/207/302 kinase panels和客製化 panels.

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多種檢測:TR-FRET(LANCE Ultra、LathaScreen、HTRF)、螢光法(Kinase-Glo、ADP-Glo)、Z`-LYTE、binding assay。

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檢測準確,快速服務。

多樣性化合物庫

MCE提供優質且便宜的Targeted Diversity Library以進行全面篩選

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包括2,400多種化合物,涵蓋1,000多種異構體

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為每個目標和異構體選擇了 1-3 種具有高效力和選擇性的化合物。

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提供詳細的生物活性資料

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具有全面靶標覆蓋的小分子化合物。

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用於表型篩選的工具。

近期引用 MCE 產品的文獻

Covers of Recent Publications

Nat Nanotechnol. 2021 Nov;16(11):1260-1270.

Cell Metab. 2021 Nov 2;33(11):2247-2259.e6.

Cell Metab. 2021 Dec 7;33(12):2355-2366.e8.

Cancer Cell. 2021 Nov 8;39(11):1531-1547.e10.

 

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