| Identification | Back Directory | [Name]
SID 3712249 | [CAS]
522606-67-3 | [Synonyms]
miR544-IN-1
SID 3712249
MiR-544 Inhibitor 1
SID 3712249 >=95% (HPLC)
1,8-diamino-3,6-di(1-pyrrolidinyl)[2,7]naphthyridine-4-carbonitrile
2,7-Naphthyridine-4-carbonitrile, 1,8-diamino-3,6-di-1-pyrrolidinyl- | [Molecular Formula]
C17H21N7 | [MOL File]
522606-67-3.mol | [Molecular Weight]
323.4 |
| Chemical Properties | Back Directory | [Boiling point ]
669.0±55.0 °C(Predicted) | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml | [form ]
A crystalline solid | [pka]
8.83±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer[1]. | [Biological Activity]
SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544). MiR-544 represses expression of mTORpromoting tumor cell survival in a hypoxic environment. Inhibition of miR-544 processing with MiR-544 Inhibitor 1 caused apoptosis in triple negative breast cancer cells in response to hypoxic stresssensitized their response to 5-fluorouraciland blocked their growth after transplantion into immunodeficient mice. SID 3712249 (MiR-544 Inhibitor 1) is believed to bind directly to the precursor miRNAblocking production of the mature microRNA and resulting in decreased miR-544HIF-1αand ATM transcripts. MiR-544 Inhibitor 1 was as selective and 25-fold more potent than a 2μ-O-methyl RNA antagomir. | [in vivo]
SID 3712249 (compound 1, 100 μL of 40 μM, intraperitoneal injection) inhibited tumor growth in MDA-MB-231-GFP-luc tumor model[1].
SID 3712249 (20 nM, pre-treated GFP-labeled MDA-MB-231 cells, intraperitoneal injection) inhibited tumor growth in MDA-MB-231-GFP-luc tumor model[1]. | Animal Model: | MDA-MB-231-GFP-luc tumor model[1] | | Dosage: | 100 μL of 40 μM | | Administration: | Intraperitoneal injection | | Result: | Inhibited tumor growth (evidenced by live animal bioluminescent imaging) with no overt side effects.
Decreased levels of miR-544, ATM, and HIF-1α and increased levels of mTOR (resected tumor samples).
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| [storage]
Store at -20°C | [References]
[1] Christopher L Haga, et al. Small Molecule Inhibition of miR-544 Biogenesis Disrupts Adaptive Responses to Hypoxia by Modulating ATM-mTOR Signaling. ACS Chem Biol. 2015 Oct 16;10(10):2267-76. DOI:10.1021/acschembio.5b00265 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|