MCE |1月新品快報

MCE |1月新品快報

2022.01.19

 

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

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

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

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

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

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

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

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

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

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

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

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

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.

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

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

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).

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:

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

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.

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

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

包括2,400多種化合物,涵蓋1,000多種異構體

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。

提供詳細的生物活性資料

具有全面靶標覆蓋的小分子化合物。

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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