Rapamycin 0.001μM R08 exp429
Mechanism of Action
Allosteric mTORC1 inhibitor, forms ternary complex with FKBP12 and mTOR, attenuates protein synthesis and metabolism
- Class / Subclass 1: Signal Transduction / Kinase Inhibitor
- Class / Subclass 2: Proteostasis / mTOR inhibitor
Technical Notes
Compound References
- PubChem Name: Sirolimus
- Synonyms: Sirolimus; AY 22989
- CAS #: 53123-88-9
- PubChem CID: 5284616
- IUPAC: (1R,9S,12S,15R,16E,18R,19R,21R,23S,24E,26E,28E,30S,32S,35R)-1,18-dihydroxy-12-[(2R)-1-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]propan-2-yl]-19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-azatricyclo[30.3.1.04,9]hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone
- INCHI Name: InChI=1S/C51H79NO13/c1-30-16-12-11-13-17-31(2)42(61-8)28-38-21-19-36(7)51(60,65-38)48(57)49(58)52-23-15-14-18-39(52)50(59)64-43(33(4)26-37-20-22-40(53)44(27-37)62-9)29-41(54)32(3)25-35(6)46(56)47(63-10)45(55)34(5)24-30/h11-13,16-17,25,30,32-34,36-40,42-44,46-47,53,56,60H,14-15,18-24,26-29H2,1-10H3/b13-11+,16-12+,31-17+,35-25+/t30-,32-,33-,34-,36-,37+,38+,39+,40-,42+,43+,44-,46-,47+,51-/m1/s1
- INCHI Key: QFJCIRLUMZQUOT-HPLJOQBZSA-N
- Molecular Weight: 914.2
- Canonical SMILES: CC1CCC2CC(C(=CC=CC=CC(CC(C(=O)C(C(C(=CC(C(=O)CC(OC(=O)C3CCCCN3C(=O)C(=O)C1(O2)O)C(C)CC4CCC(C(C4)OC)O)C)C)O)OC)C)C)C)OC
- Isomeric SMILES: C[C@@H]1CC[C@H]2C[C@@H](/C(=C/C=C/C=C/[C@H](C[C@H](C(=O)[C@@H]([C@@H](/C(=C/[C@H](C(=O)C[C@H](OC(=O)[C@@H]3CCCCN3C(=O)C(=O)[C@@]1(O2)O)[C@H](C)C[C@@H]4CC[C@H]([C@@H](C4)OC)O)C)/C)O)OC)C)C)/C)OC
- Molecular Formula: C51H79NO13
Compound Supplier
- Supplier Name: LC Laboratories
- Catalog #: R-5000
- Lot #: ASW-130
Compound Characterization
- HRMS (ESI-TOF) m/z: (M+Na)+ Calcd for C51H79NO13 936.54436; found 936.54366
Dose Response Curve
- Platform ID: Rapamycin_old
- Min: -12.4006; Max: 41.8376
| IC | Concentration (µM) |
|---|---|
| IC10 | 6.9560 |
| IC20 | 8.3100 |
| IC30 | 9.3520 |
| IC40 | 10.3000 |
| IC50 | 11.2600 |
| IC60 | 12.3100 |
| IC70 | 13.5600 |
| IC80 | 15.2600 |
| IC90 | 18.2400 |
Screen Summary
- Round: 08
- Dose: 1nM
- Days of incubation: 8
- Doublings: 5.6
- Numbers of reads: 17160031
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 |
|---|---|---|---|---|---|---|
| 3/13 | Scores |
Rapamycin 0.001μM R08 exp429
Rapamycin 0.001μM R08 exp429 vs Rapamycin 1μM R00 exp29
Rapamycin 0.001μM R08 exp429 vs Rapamycin 10μM R00 exp30
Rapamycin 0.001μM R08 exp429 vs Rapamycin 2μM R07 exp306
Rapamycin 0.001μM R08 exp429 vs Rapamycin 2μM plus Cyclosporin-A 3μM R07 exp307
Rapamycin 0.001μM R08 exp429 vs Rapamycin 2μM plus FK-506 5μM R07 exp308
Rapamycin 0.001μM R08 exp429 vs Torin1 0.08μM R02 exp82
Dexamethasone 0.006 to 0.015μM on day4 R07 exp352 vs Rapamycin 0.001μM R08 exp429
Dimethyloxaloylglycine 100μM R05 exp229 vs Rapamycin 0.001μM R08 exp429
Dexamethasone 0.006μM R07 exp351 vs Rapamycin 0.001μM R08 exp429
MK2206 4μM R08 exp504 vs Rapamycin 0.001μM R08 exp429
