MCE | 12月最新快報

MCE | 12月最新快報

2022.12.15

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,包括超過 40,000 種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。

CAS No.: 1398695-47-0

GSK2646264

Research Area: SYK Inhibitor/Inflammatory Skin Disease

GSK2646264 structure

A selective and skin permeable spleen tyrosine kinase (Syk) inhibitor with a pIC50 of 7.1, and exhibits >300-fold selectivity over Aurora B.

Has the potential for chronic spontaneous urticaria, cold urticaria, and cutaneous lupus erythematosus research.

Solubility: DMSO : 50 mg/mL (133.52 mM; ultrasonic and warming and heat to 60°C)

CAS No.: 2406278-81-5

OM-153

Research Area: Tankyrase Inhibitor/Colon Cancer

OM-153 structure

A potent, orally active Tankyrase 1 and Tankyrase 2 (TNKS1/TNKS2) inhibitor with IC50 values of 13 nM and 2 nM, respectively.

Shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM cells or in COLO 320DM mouse colon carcinoma xenografts.

Demonstrates antitumor efficacy in COLO 320DM mouse colon carcinoma and B16-F10 mouse melanoma models.

Solubility: DMSO : 100 mg/mL (196.26 mM; Need ultrasonic)

CAS No.: 2102192-68-5

Envafolimab

Research Area: PD-L1 Antibody/Advanced Solid Tumors

Envafolimab structure

A fusion protein of a humanized single-domain anti-PD-L1 antibody fused with a human IgG1 Fc fragment.

Blocks interaction between PD-L1 and PD-1, resulting in T cell-mediated immune response to neoplasms.

Used in the research of advanced solid tumors, biliary tract carcinoma and sarcoma.

Solubility: Solution: 9.8 mg/mL

CAS No.: 1517965-94-4

Vornorexant

Research Area: OX1R/OX2R Antagonist/Insomnia and Sleep Apnoea Syndrome

Vornorexant structure

An orally active, dual OX1R and OX2R antagonist with IC50 values of 1.05 nM and 1.27 nM, respectively.

Exhibits potent sleep-promoting effects in a rat polysomnogram study, and optimal pharmacokinetic properties with rapid Tmax and short half-lives are observed in rats and dogs.

Solubility: DMSO : ≥ 100 mg/mL (223.48 mM)

CAS No.: 2784577-71-3

RLX-33

Research Area: RXFP3 Antagonist/Metabolic Syndrome

RLX-33 structure

Selective and CNS-penetrant relaxin family peptide 3 (RXFP3) non-peptide antagonist.

Inhibits relaxin-3-induced ERK1/2 phosphorylation, and decreases cAMP accumulation.

Blocks the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats.

Solubility: DMSO : 125 mg/mL (270.04 mM; Need ultrasonic)

MCE海洋天然產品:

近年來,海洋天然物質已成為發現新藥的重要來源,例如:抗病毒藥物 Vidarabine 以及抗腫瘤藥物 Cytarabine 是由海綿中分離出的spongothymidine和spongouridine、 用於治療乳腺癌和脂肪肉瘤的 Eribulin 是來自 Halichondria okadai Kadota的 Halichondrin B 衍生物。

Product Name

Description

Structure

Didemnin B

Shows activity against miirine B16 melanoma, P388 leukemia, and M5076 sarcoma.

Aaptamine

A competitive antagonist of α-adrenoceptor.

Jasplakinolide

A potent actin polymerization inducer with fungicidal and anti-cancer activities.

Aeroplysinin 1

Exerts anti-HIV-1, anti-inflammatory, anti-angiogenic and anti-tumor activities.

Psammaplin A

A potent inhibitor of HDAC and DNA methyltransferases.

MCE可提供magnetic beads 和agarose beads:

Product Name

Technical Improvement

Experimental Type

Protein A/G Magnetic Beads (1 μm)

More uniform and better dispersion;
higher protein binding capacity;
more specific.

Purification of small amount protein;
IP/Co-IP/CHIP;
Pull Down etc.

Anti-HA Magnetic Beads (1 μm)

Anti-c-Myc Magnetic Beads (1 μm)

Anti-Flag Magnetic Beads (1 μm)

Streptavidin Agarose 6FF

Better pressure resistance and compatibility;
compatible with ÄKTA chromatography columns;
higher binding capacity.

Purification of large-scale protein.

最新文獻引用MCE產品

Covers of Recent Publications

Nature.
2022 Nov;611(7936):603-613.

Cell.
2022 Nov 10;185(23):4361-4375.e19.

Nat Genet.
2022 Nov;54(11):1702-1710.

Cancer Discov.
2022 Nov 4:CD-22-0535.

 

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