MCE | 1月新品快報

MCE | 1月新品快報

2023.01.31

MedChemExpress - Master of Bioactive Molecules (Inhibitors. Screening Libraries. Proteins)

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 50,000 種生物活性分子化合物的庫存

 

• 超過針對20多種訊號傳遞路徑中的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)

• 每月發佈超過1000 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.: 2488952-40-3

EEDi-5285

Research Area: EED Inhibitor/Lymphoma

EEDi-5285 structure

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A potent and orally active embryonic ectoderm development (EED) inhibitor with an IC50 of 0.2 nM.

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Efficaciously inhibits Pfeiffer and KARPAS422 lymphoma cancer cells with IC50 values of 20 pM and 0.5 nM, respectively.

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Significantly induces tumor regression in KARPAS422 xenograft mouse models.

Solubility: DMSO : 125 mg/mL (260.67 mM; Need ultrasonic)

CAS No.: 859525-02-3

Cadisegliatin

Research Area: Glucokinase Activator/Type 1 and 2 Diabetes

Cadisegliatin structure

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An orally active and liver-selective glucokinase (GK) activator.

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Increases glucose metabolism in rat hepatocytes with EC50 values of 2.39 μM and 2.64 μM for lactate and glycogen, respectively.

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Reduces blood glucose, lactate and triglyceride concentrations in ob/ob mouse models with severe diabetes.

Solubility: DMSO : 125 mg/mL (274.35 mM; Need ultrasonic)

CAS No.: 371217-32-2

A-317567

Research Area: ASIC-3 Inhibitor/Depression and Pain

A-317567 structure

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A potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM.

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Dose-dependently inhibits all ASIC currents (IC50s of 2-30 µM).

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Shows fully analgesic effects in Complete Freund’s adjuvant (CFA)-induced inflammatory thermal hyperalgesia rat models.

Solubility: DMSO : 125 mg/mL (314.42 mM; Need ultrasonic)

CAS No.: 2758364-02-0

CAM833

Research Area: BRCA2-RAD51 Interaction Inhibitor/Cancer

CAM833 structure

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A selective orthosteric inhibitor of BRCA2-RAD51 interaction with a Kd of 366 nM.

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Dose-dependently decreases RAD51 nuclear foci and inhibits DNA repair.

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Induces cell-cycle arrest and cell apoptosis.

Solubility: DMSO : 125 mg/mL (236.31 mM; Need ultrasonic)

CAS No.: 1375752-78-5

BMS-984923

Research Area: mGluR5 Silent Allosteric Modulator/Alzheimer’s Disease

BMS-984923 structure

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An orally active and BBB penetrable mGluR5 silent allosteric modulator (SAM) with a Ki value of 0.6 nM.

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Prevents amyloid-β oligomer (Aβo) mediated toxicity and Aβo-induced signal transduction in brain slices.

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Rescues memory deficits and synaptic depletion in Alzheimer’s disease transgenic mouse models.

Solubility: DMSO : 100 mg/mL (266.79 mM; Need ultrasonic)

MCE分子膠化合物庫

靶向蛋白質降解Targeted protein degradation(TPD)是一種新型且有潛力的新藥發現和開發方法,其顯示出治療具有“非藥性”致病蛋白靶標的疾病和克服抗藥性的巨大潛力。分子膠和PROTACs都是最受關注的靶向蛋白降解劑。

分子膠是小分子降解劑,主要誘導 E3 ligase與靶蛋白之間的相互作用並形成復合物,進而導致蛋白質泛素化和隨後的蛋白酶體降解。與 PROTAC 相比,分子膠通常具有更有利的類藥物特性,如: 更低的分子量、更高的細胞滲透性和更好的吸收,分子膠正在成為一種有前途的新治療策略。

MCE 提供獨特的 30 多種針對各種蛋白質的分子膠,MCE分子膠化合物庫是進行科學研究和疾病機制研究的最強工具。

MCE 同位素標記化合物

Product Name

Cas No.

Structure

L-Arginine-13C6, 15N4 hydrochloride

202468-25-5

L-Arginine-13C6, 15N4 hydrochloride structure

L-Glutamine-d5

14341-78-7

L-Glutamine-d5 structure

最新文獻引用MCE產品

Covers of Recent Publications

Nature.
2022 Dec;612(7940):555-563.

Science.
2022 Dec 2;378(6623):eabo5503.

Cell.
2022 Nov 10;185(23):4347-4360.e17.

Cell.
2022 Dec 8;185(25):4801-4810.e13.

Cell Signaling Pathway

 

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