Table of Contents
UMK57 1μM R01 exp59
Mechanism of Action
Potentiates kinesin-13 (MCAK), destabilizes kinetochore-MT attachment, suppresses chromosome mis-segregation
- Class / Subclass 1: Cell Cycle / Mitotic Inhibitor
- Class / Subclass 2: Organelle Function / Cytoskeletal Inhibitor
Technical Notes
Protein References
- PubChem Name: 5-(4-Methylphenyl)-4-pyrrolidinylthiopheno[2,3-d]pyrimidine
- Synonyms: N/A
- CAS #: 342595-74-8
- PubChem CID: 693939
- IUPAC: 5-(4-methylphenyl)-4-pyrrolidin-1-ylthieno[2,3-d]pyrimidine
- INCHI Name: InChI=1S/C17H17N3S/c1-12-4-6-13(7-5-12)14-10-21-17-15(14)16(18-11-19-17)20-8-2-3-9-20/h4-7,10-11H,2-3,8-9H2,1H3
- INCHI Key: VOAWQTDHSSKEKA-UHFFFAOYSA-N
- Molecular Weight: 295.4
- Canonical SMILES: CC1=CC=C(C=C1)C2=CSC3=NC=NC(=C23)N4CCCC4
- Isomeric SMILES: N/A
- Molecular Formula: C17H17N3S
Protein Supplier
- Supplier Name: In house - University of Montreal - Chemistry Platform
- Catalog #: N/A
- Lot #: N/A
Protein Characterization
- HRMS (ESI-TOF) m/z: [M+H]+ Calcd for C17H18N3S 296.1216; found 296.1142
Dose Response Curve
- Platform ID: UMK57
- Min: -2.8530; Max: 75.4945
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | 0.3698 |
| IC30 | 0.6436 |
| IC40 | 1.0136 |
| IC50 | 1.5379 |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 01
- Dose: 1µM
- Days of incubation: 8
- Doublings: 5.2
- Numbers of reads: 15049192
Screen Results
| Sensitive/Resistant hits (FDR<0.05) | CRANKS | Score Plot | Top 30 Genes | Screen Similarity | Top 30 Sensitive GO terms | Top 30 Resistant GO terms |
|---|---|---|---|---|---|---|
| 27/49 | Scores |
UMK57 1μM R01 exp59
UMK57 1μM R01 exp59 vs Vinblastine 0.002μM R01 exp60
UMK57 1μM R01 exp59 vs Vincristine 0.0005μM R04 exp190
Mdivi-1 15μM R05 exp217 vs UMK57 1μM R01 exp59
BML-284 0.09μM R08 exp460 vs UMK57 1μM R01 exp59
UM131593 0.2μM R03 exp106 vs UMK57 1μM R01 exp59
2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312 vs UMK57 1μM R01 exp59
HMS-I1 1μM R01 exp46 vs UMK57 1μM R01 exp59
Quercetin 20μM R08 exp517 vs UMK57 1μM R01 exp59
BVD-523 15μM R02 exp67 vs UMK57 1μM R01 exp59
Combretastatin A4 0.002 to 0.003μM day4 R04 exp179 vs UMK57 1μM R01 exp59
Colchicine 0.009μM R05 exp215 vs UMK57 1μM R01 exp59
Demecolcine 0.03μM R05 exp228 vs UMK57 1μM R01 exp59
2-Methoxyestradiol 0.55 to 0.75μM on day4 R07 exp311 vs UMK57 1μM R01 exp59
Taxol 0.004μM R03 exp103 vs UMK57 1μM R01 exp59
Ixabepilone 0.004 to 0.005μM on day4 R04 exp184 vs UMK57 1μM R01 exp59
2-Methoxyestradiol 0.55μM R07 exp310 vs UMK57 1μM R01 exp59
RO-3307 4.7μM R02 exp80 vs UMK57 1μM R01 exp59
LY2090314 0.003μM R08 exp500 no dilution day6 vs UMK57 1μM R01 exp59
Milciclib 2μM R08 exp502 vs UMK57 1μM R01 exp59
3-Bromopyruvate 7μM R04 exp175 vs UMK57 1μM R01 exp59
Hydroxyurea 100μM R07 exp329 vs UMK57 1μM R01 exp59
Pterostilbene 16μM R02 exp78 vs UMK57 1μM R01 exp59
Docetaxel 0.002μM R01 exp45 vs UMK57 1μM R01 exp59
Thimerosal 0.85μM R08 exp529 vs UMK57 1μM R01 exp59
Epothilone-B 0.0015μM R05 exp231 vs UMK57 1μM R01 exp59
Actinomycin-D 0.001μM R00 exp3 vs UMK57 1μM R01 exp59
LLY-283 2.6μM R06 exp290 vs UMK57 1μM R01 exp59
