EPZ-5676 30μM R05 exp233
Mechanism of Action
Inhibits DOT1L lysine methyltransferase (H3K79me2)
- Class / Subclass 1: Gene Regulation / Epigenetic Inhibitor
Technical Notes
Compound References
- PubChem Name: Pinometostat
- Synonyms: EPZ-5676
- CAS #: 1380288-87-8
- PubChem CID: 57345410
- IUPAC: (2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol
- INCHI Name: InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17?,19?,22-,25-,26-,29-/m1/s1
- INCHI Key: LXFOLMYKSYSZQS-XKHGBIBOSA-N
- Molecular Weight: 562.7
- Canonical SMILES: CC(C)N(CC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
- Isomeric SMILES: CC(C)N(C[C@@H]1[C@H]([C@H]([C@@H](O1)N2C=NC3=C(N=CN=C32)N)O)O)C4CC(C4)CCC5=NC6=C(N5)C=C(C=C6)C(C)(C)C
- Molecular Formula: C30H42N8O3
Compound Supplier
- Supplier Name: N/A
- Catalog #: N/A
- Lot #: N/A
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C30H42N8O3 563.34526; found 563.34668
Dose Response Curve
- Platform ID: EPZ-5676
- Min: -0.8707; Max: 35.7028
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | N/A |
| IC30 | N/A |
| IC40 | N/A |
| IC50 | N/A |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 05
- Dose: 30µM
- Days of incubation: 8
- Doublings: 6.2
- Numbers of reads: 16438702
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 |
|---|---|---|---|---|---|---|
| 15/6 | Scores |