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Cat. No.: 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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

CAS No.: 2324158-08-7
Formule: C₂₈H₂₇N₅O
Masse moléculaire:449.55

Stockage:

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

LC-1028 Chemical Structure

CAS No.: 2324158-08-7

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Fluorescent Dye

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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]

In Vitro

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.

Chemical Information

CAS No. 2324158-08-7
Masse moléculaire 449.55
Formule C₂₈H₂₇N₅O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

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

Calculators

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Help & FAQs

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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