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製品番号: HY-125472

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LC-1028

LC-1028 (Compound 20) is an irreversible, non-competitive, covalent p97 inhibitor with a Ki^app value of 33.2 nM. LC-1028 covalently modifies the cysteine residues (Cys105, Cys522, Cys535) of p97. LC-1028 can be used in the research of pancreatic cancer.

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CAS 番号: 2324158-08-7
分子式: C₂₈H₂₇N₅O
分子量:449.55

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

LC-1028 構造式

CAS 番号: 2324158-08-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

Cellular Effect

Cell Line	Type	Value	Description	References
MIA PaCa-2	EC₅₀	0.436 μM Compound: 20	Antiproliferative activity against human MIAPaCa2 cells Antiproliferative activity against human MIAPaCa2 cells	[PMID: 30830772]

体外実験

LC-1028 (33.2 nM; 20 min, 16 h + 6 h) irreversibly inhibits purified wild-type human p97 ATPase activity with a K_i^app of 33.2 nM, with only 3% activity recovered after dialysis, and completely inhibits p97 delta N activity irreversibly^[1].
LC-1028 (1 μM; up to 24 h) reacts covalently with GSH with a half-life of 16.4 h, forming a detectable adduct^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

A373 cells stably expressing US11 and HA-tagged MHC class I heavy chain
Concentration:

2 μM
Incubation Time:

1 h treatment, followed by 0-3 h chase in inhibitor-free medium
Result:

Caused a drastically reduced rate of MHC class I heavy chain turnover after agent washout compared to cells treated with the reversible p97 inhibitor NMS-873.

化学情報

CAS 番号 2324158-08-7
分子量 449.55
分子式 C₂₈H₂₇N₅O
SMILES

CC#CC(NC1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C5CCCCC5=N3)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Ding R, et al. Discovery of Irreversible p97 Inhibitors. J Med Chem. 2019;62(5):2814-2829. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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