LC-1028
LC-1028 (Compound 20) is an irreversible, non-competitive, covalent p97 inhibitor with a Kiapp 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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- CAS No.: 2324158-08-7
- 화학식: C28H27N5O
- 분자량:449.55
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
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] |
LC-1028 (33.2 nM; 20 min, 16 h + 6 h) irreversibly inhibits purified wild-type human p97 ATPase activity with a Kiapp 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.
-
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
-
분자량 449.55
-
화학식 C28H27N5O
-
SMILES
CC#CC(NC1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C5CCCCC5=N3)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)