EN6
- Product Name
- EN6
- CAS No.
- 1808714-73-9
- Chemical Name
- EN6
- Synonyms
- EN6;EN-6;EN 6;EN6 (>95%);EN6, 10 mM in DMSO;Autophagy,inhibit,Inhibitor,Proton Pump,EN-6,EN 6,EN6;N-(3-Acrylamido-4-fluorophenyl)-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide;N-[4-Fluoro-3-(prop-2-enamido)phenyl]-1-(2-fluorophenyl)-1H-pyrazole-4-carboxamide;1H-Pyrazole-4-carboxamide, N-[4-fluoro-3-[(1-oxo-2-propen-1-yl)amino]phenyl]-1-(2-fluorophenyl)-
- CBNumber
- CB85440948
- Molecular Formula
- C19H14F2N4O2
- Formula Weight
- 368.34
- MOL File
- 1808714-73-9.mol
EN6 Property
- Boiling point:
- 484.1±45.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:10): 0.09 mg/ml; DMSO: 15 mg/ml
- form
- A crystalline solid
- pka
- 11.27±0.70(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H301Toxic if swalloed
H311Toxic in contact with skin
H331Toxic if inhaled
H341Suspected of causing genetic defects
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P308+P313IF exposed or concerned: Get medical advice/attention.
P310Immediately call a POISON CENTER or doctor/physician.
P330Rinse mouth.
P361Remove/Take off immediately all contaminated clothing.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- SML2689
- Product name
- EN6
- Purity
- ≥98% (HPLC)
- Packaging
- 5MG
- Price
- $94.2
- Updated
- 2024/03/01
- Product number
- SML2689
- Product name
- EN6
- Purity
- ≥98% (HPLC)
- Packaging
- 25MG
- Price
- $381
- Updated
- 2024/03/01
- Product number
- 28715
- Product name
- EN6
- Packaging
- 5mg
- Price
- $85
- Updated
- 2024/03/01
- Product number
- 28715
- Product name
- EN6
- Packaging
- 25mg
- Price
- $234
- Updated
- 2024/03/01
- Product number
- 28715
- Product name
- EN6
- Packaging
- 10mg
- Price
- $136
- Updated
- 2024/03/01
EN6 Chemical Properties,Usage,Production
Uses
EN6 is a small-molecule in vivo autophagy activator that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal v-ATPase. EN6-mediated modification of ATP6V1A uncouples v-ATPase from Rag, leading to inhibition of mTORC1 signalling, increased lysosomal acidification, and activation of autophagy. EN6 also scavenges TDP-43 aggregates (causative agents of frontotemporal dementia) in a lysosome-dependent manner[1].
Biological Activity
EN6 is an autophagy activator th at simultaneously upregulates lysosomal vacuolar H(+)-ATPase (v-ATPase) activity and induces its decoupling from the Rag GTPases by covalently targeting v-ATPase subunit ATP6V1A Cys277. EN6 blocks mTORC1 lysosomal recruitment & activation (1-4 hr 25 μM EN6 pretreatment prior to 10-min amino acids (AA) stimulation of AA-starived HEK293) and clears cellular TDP-43 aggregates (25 μM; U2OS with inducible TDP-43). When administered in mice in vivo (50 mg/kg ip.), EN6 inhibits mTORC1 signaling and activates autophagy in both skeletal muscle and heart tissue. Unlike bafilomycin A1 (BafA1), EN6 activates, but not inhibits v-ATPase catalytic activity.
in vivo
EN6 (50 mg/kg; i.p.; single) inhibits mTORC1 and activates autophagy in vivo[1].
| Animal Model: | Six-week-old male C57BL/6 mice[1]. |
| Dosage: | 50 mg/kg |
| Administration: | Intraperitoneal injection; single |
| Result: | Significantly inhibited mTORC1 signaling in both skeletal muscle and heart, as demonstrated by reduced phosphorylation of S6, 4EBP1 and ULK1. Strongly activated autophagy as shown by heightened LC3BII levels and reduced p62 levels. |
storage
Store at -20°C
References
[1] Chung CY, et al. Covalent targeting of the vacuolar H+-ATPase activates autophagy via mTORC1 inhibition. Nat Chem Biol. 2019 Aug;15(8):776-785. DOI:10.1038/s41589-019-0308-4
EN6 Preparation Products And Raw materials
Raw materials
Preparation Products
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