- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Inhibitors
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 195514-80-8] AP20187
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-13992 |
| Brand: | MCE |
| CAS: | 195514-80-8 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 1482.75 |
| Molecular Formula | C82H107N5O20 |
| SMILES | COC1=C(OC)C=C(CC[C@H](C2=CC=CC(OCC(NCC(CN(C)C)CNC(COC3=CC=CC([C@H](OC([C@H]4N(C([C@@H](CC)C5=CC(OC)=C(OC)C(OC)=C5)=O)CCCC4)=O)CCC6=CC(OC)=C(OC)C=C6)=C3)=O)=O)=C2)OC([C@@H]7CCCCN7C([C@H](C8=CC(OC)=C(OC)C(OC)=C8)CC)=O)=O)C=C1 |
19 Publications Citing Use of MCE
- [1]Nature. 2022 Nov;611(7936):603-613.
- [2]Circulation. 2016 Jul 5;134(1):61-72.
- [3]Cell Metab. 2019 May 7;29(5):1061-1077.e8.
- [4]Cell Stem Cell. 2020 Jun 4;26(6):845-861.e12.
- [5]Nat Commun. 2019 May 7;10(1):2091.
- [6]Cell Death Differ. 2021 Jan;28(1):251-266.
- [7]EMBO J. 2021 Mar 25;e106048.
- [8]Aging Cell. 2019 Jun;18(3):e12950.
- [9]Cell Death Dis. 2021 Oct 23;12(11):994.
- [10]Cell Death Dis. 2018 Apr 27;9(5):500.
- [11]Cell Discov. 2021 Jun 1;7(1):41.
- [12]FASEB J. 2018 Jun 18:fj201800548.
- [13]J Transl Med. 2023 Feb 10;21(1):110.
- [14]Methods. 2018 May 1;140-141:40-51.
- [15]PLoS One. 2021 Mar 29;16(3):e0248996.
- [16]Microbiol Immunol. 2020 Feb;64(2):143-152.
- [17]bioRxiv. 2023 Jan 13.
- [18]Nat Cancer. 2022 Jun 30.
- [19]Harvard University. Graduate School of Arts & Sciences. 2016 Apr.
Summary
AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein ( FKBP ) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.
IC50 & Target
FKBP homodimerizer [1]
In Vitro
When LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100 nM), ro-iCaspase-9 levels are significantly reduced, and the smaller processed active caspase-9 becomes apparent [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5 mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of PLP/Fv2E-PERK mice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 (B/B Homodimerizer) treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord of PLP/Fv2E-PERK mice [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
Ethanol : 150 mg/mL ( 101.16 mM ; Need ultrasonic)
DMSO : ≥ 57 mg/mL ( 38.44 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.6744 mL | 3.3721 mL | 6.7442 mL |
| 5 mM | 0.1349 mL | 0.6744 mL | 1.3488 mL |
| 10 mM | 0.0674 mL | 0.3372 mL | 0.6744 mL |
-
1.
-
2.
Add each solvent one by one: 10% EtOH >> 90% (20% SBE-β-CD in saline)
Solubility: 6 mg/mL (4.05 mM); Suspended solution; Need ultrasonic
-
3.
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (1.69 mM); Clear solution
-
5.
Add each solvent one by one: 4% ethanol >> 10% PEG-400 >> 2% Tween-80 >> 84%water.
Solubility: 2.4 mg/mL (1.62 mM); Clear solution; Need ultrasonic
References
- [1] Ahmed S, et al. Photocleavable dimerizer for the rapid reversal of molecular trap antagonists. J Biol Chem. 2014 Feb 21;289(8):4546-52.
- [2] Lin W, et al. Oligodendrocyte-specific activation of PERK signaling protects mice against experimental autoimmune encephalomyelitis. J Neurosci. 2013 Apr 3;33(14):5980-91.
- [3] Haas ME, et al. The Role of Proprotein Convertase Subtilisin/Kexin Type 9 in Nephrotic Syndrome-Associated Hypercholesterolemia. Circulation. 2016 Jul 5;134(1):61-72.
Synonyms
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.