CENP-E-IN-1
CENP-E-IN-1 is a CENP-E inhibitor. CENP-E-IN-1 acts as a Mitotic arrest inducer and Apoptosis inducer, which causes abnormal alignment of chromosomes on the metaphase plate, activates the spindle assembly checkpoint and triggers apoptosis. CENP-E-IN-1 exhibits anti-tumor activity in colorectal adenocarcinoma xenograft models. CENP-E-IN-1 can be used in cancer-related research.
For research use only. We do not sell to patients.
- CAS No.: 1446399-26-3
- Formula: C30H27F4N5O4S
- Molecular Weight:629.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[1]|
CENP-E |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | GI50 |
80 nM
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Antiproliferative activity against asynchronous human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by ATP-based cell viability assay.
Antiproliferative activity against asynchronous human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by ATP-based cell viability assay.
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26649895 |
In Vitro
CENP-E-IN-1 (Compound Cmpd-A) (200 nM; 3 h up to 12 h) induces pole-proximal chromosome misalignment, activates the SAC, and causes prolonged mitotic arrest in synchronized HeLa cells[1].
CENP-E-IN-1 (0-1000 nM; 24-72 h) potently inhibits proliferation in asynchronous HeLa cells with a GI50 of 80 nM, and its antiproliferative and pro-apoptotic effects are dependent on SAC activation via BubR1[1].
CENP-E-IN-1 (3-3000 nM; 3 days) exhibits potent antiproliferative activity across a broad range of human cancer cell lines, though sensitivity is not correlated with CENP-E mRNA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Synchronized HeLa cells
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Concentration:200 nM
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Incubation Time:3 h; up to 12 h post-thymidine block release
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Result:Caused pole-proximal chromosome misalignment in 77% of mitotic HeLa cells, compared to no misalignment in control cells.
Prevented progression to anaphase/telophase.
Reduced inter-kinetochore distances in misaligned chromosomes to 0.8 μm compared to aligned chromosomes in control or Cmpd-A-treated cells.
Arrested cells in the G2/M phase, with accumulation of pHH3-positive mitotic cells reaching 38.7% at 12 h post-release.
Induced elevated BubR1 phosphorylation and cyclin B1 accumulation, indicating spindle assembly checkpoint (SAC) activation.
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Cell Line:Asynchronous HeLa cells
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Concentration:0-1000 nM
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Incubation Time:72 h (cell viability); 24 h (pHH3, caspase-3/7, siRNA experiments)
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Result:Potently suppressed HeLa cell proliferation with a GI50 of 80 nM, and this activity correlated with increased pHH3-positive cells.
Induced dose-dependent caspase-3/7 activation and antiproliferation in non-silencing siRNA-transfected cells.
Drastically reduced both caspase-3/7 activation and antiproliferative effects in BubR1 siRNA-transfected cells, indicating dependence on SAC activation.
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Cell Line:Multiple human cancer cell lines (DU145, COLO205, NIH-OVCAR3, RKO, ES2, SK-OV3, PC-3, SW620, CAPAN-2)
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Concentration:3-3000 nM
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Incubation Time:3 days
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Result:Exhibited potent antiproliferative effects in multiple cancer cell lines including DU145, COLO205, NIH-OVCAR3, RKO, ES2, SK-OV3, and PC-3.
Showed resistance in some cell lines (SW620, CAPAN-2), with responses similar to MRC5 cells.
Demonstrated antiproliferative activity that did not significantly correlate with CENP-E mRNA expression levels in tested cancer cell lines (R2 = 0.0001).
Parmacokinetics
| Species | Dose | Route | Plasma Concentration |
|---|---|---|---|
| Mice[1] | 100 mg/kg | i.p. | 33.7 μg/mL |
In Vivo
CENP-E-IN-1 (100 mg/kg; i.p.; three doses at 0, 8, and 24 hours on day 1) produces potent antitumor activity, with a T/C % of 11% on Day 8, in COLO205 xenograft nude mice without significant body weight loss[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nude mice (subcutaneous xenograft of COLO205 human colorectal cancer cells)[1]
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Dosage:100 mg/kg
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Administration:i.p.; three doses at 0, 8, and 24 hours on day 1
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Result:Reduced mean tumor volume to approximately 400 mm3 on Day 8 post-administration, compared to over 800 mm3 in vehicle-treated mice.
Achieved a T/C % of 11% on Day 8.
Caused no significant body weight loss relative to vehicle controls.
Chemical Information
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CAS No. 1446399-26-3
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Molecular Weight 629.63
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Formula C30H27F4N5O4S
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SMILES
O=C(N(CCN(C)C)C(C1)C2=CC=C(C(C#N)=C2S1(=O)=O)C(F)(F)F)C3=C(N4C(OC)=CC=CC4=N3)C5=CC=C(C(C)=C5)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CENP-E-IN-1 Related Classifications
HY-125106 Related Classifications
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