1. Apoptosis
  2. MDM-2/p53
  3. SP-141

SP-141 

Cat. No.: HY-110182
Handling Instructions

SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells.

For research use only. We do not sell to patients.

SP-141 Chemical Structure

SP-141 Chemical Structure

CAS No. : 1253491-42-7

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Description

SP-141 is a specific inhibitor of MDM2. SP-141 promotes MDM2 auto-ubiquitination and degradation. SP-141 might be used for the research of pancreatic cancer and breast cancer cells[1].

IC50 & Target

MDM2[1]

In Vitro

SP-141 (0.01-10 μM; 72 hours) inhibits human pancreatic cancer cell growth with IC50 values of less than 0.5 μM (0.38-0.50 μM) in a p53-independent manner. The IMR90 cells are much less sensitive to SP141 than the pancreatic cancer cells, suggesting that SP141 has a selective cytotoxicity for cancer cells[1].
SP141 induces MDM2 auto-ubiquitination and proteasomal degradation in both HPAC and Panc-1 cells[1].

Cell Viability Assay[1]

Cell Line: HPAC, Panc-1, AsPC-1, and Mia-Paca-2 pancreatic cancer cell lines. Human primary fibroblasts (IMR90)
Concentration: 0.01, 0.1, 1, and 10 μM
Incubation Time: 72 hours
Result: IC50s of 0.38, 0.50, 0.36, 0.41, and 13.22 μM for HPAC, Panc-1, AsPC-1, Mia-Paca-2, and IMR90, respectively.

Western Blot Analysis[1]

Cell Line: HPAC and Panc-1 cells
Concentration: 0.5 μM
Incubation Time: 120 minutes
Result: Reduced the MDM2 protein levels.
Increased the degradation rate of the MDM2 protein in the presence of Cycloheximide (15 μg/mL).
In Vivo

SP-141 (40 mg/kg; administered by i.p. injection; 5 d/wk for about three weeks) suppresses pancreatic tumor growth in both xenograft and orthotopic mouse models[1].

Animal Model: Nude mice bearing Panc-1 xenograft tumors[1]
Dosage: 40 mg/kg
Administration: Administered by i.p. injection; 5 d/wk for about three weeks
Result: Significantly suppressed the growth of pancreatic xenograft tumors. On Day 18, the tumor volume in the treated group was reduced by 75% compared with that in the control group. There were no significant differences in the body weight compared with the control group.
Molecular Weight

324.38

Formula

C₂₂H₁₆N₂O

CAS No.

1253491-42-7

SMILES

COC1=CC2=C(NC3=C2C=CN=C3C4=C5C=CC=CC5=CC=C4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

SP-141SP141SP 141MDM-2/p53auto-ubiquitinationdegradationpancreaticcancerbreastInhibitorinhibitorinhibit

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