UNC1999 2μM R03 exp155
Mechanism of Action
Inhibits EZH2 catalytic subunit of PRC2 histone methyltransferase (H3K27me3)
- Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor
Technical Notes
Compound References
- PubChem Name: N-[(6-Methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide
- Synonyms: N/A
- CAS #: 1431612-23-5
- PubChem CID: 72551585
- IUPAC: N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-1-propan-2-yl-6-[6-(4-propan-2-ylpiperazin-1-yl)pyridin-3-yl]indazole-4-carboxamide
- INCHI Name: InChI=1S/C33H43N7O2/c1-7-8-24-15-23(6)37-33(42)28(24)19-35-32(41)27-16-26(17-30-29(27)20-36-40(30)22(4)5)25-9-10-31(34-18-25)39-13-11-38(12-14-39)21(2)3/h9-10,15-18,20-22H,7-8,11-14,19H2,1-6H3,(H,35,41)(H,37,42)
- INCHI Key: DPJNKUOXBZSZAI-UHFFFAOYSA-N
- Molecular Weight: 569.7
- Canonical SMILES: CCCC1=C(C(=O)NC(=C1)C)CNC(=O)C2=C3C=NN(C3=CC(=C2)C4=CN=C(C=C4)N5CCN(CC5)C(C)C)C(C)C
- Isomeric SMILES: N/A
- Molecular Formula: C33H43N7O2
Compound Supplier
- Supplier Name: Structural Genomics Consortium
- Catalog #: N/A
- Lot #: N/A
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C33H43N7O2 570.3551; found 570.35617
Dose Response Curve
- Platform ID: UNC1999
- Min: -5.1046; Max: 98.9328
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | 1.4722 |
| IC30 | 2.1540 |
| IC40 | 2.9427 |
| IC50 | 3.9181 |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 03
- Dose: 2µM
- Days of incubation: 8
- Doublings: 7.0
- Numbers of reads: 10487296
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 |
|---|---|---|---|---|---|---|
| 2/0 | Scores |