1. Epigenetics
    PI3K/Akt/mTOR
    Autophagy
    Metabolic Enzyme/Protease
  2. AMPK
    Mitophagy
    E1/E2/E3 Enzyme
  3. BC1618

BC1618 

Cat. No.: HY-134656 Purity: 99.83%
Handling Instructions

BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.

For research use only. We do not sell to patients.

BC1618 Chemical Structure

BC1618 Chemical Structure

CAS No. : 2222094-18-8

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 220 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
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10 mg USD 350 In-stock
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25 mg USD 650 In-stock
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50 mg USD 950 In-stock
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100 mg USD 1350 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity[1].

In Vitro

BC1618 enhances pAmpkα protein stability during CHX treatment[1].
BC1618 displays more than 1,000-fold enhanced activity to stimulate pAmpkα in cells than metformin[1].
BC1618 (0.1-2 μM, 16 h) induced dose- and time-dependent increases in pAmpkα and pACC protein levels are also confirmed in human primary-like hepatocytes[1].
BC1618 (1 μM) effectively disrupts the interaction between Fbxo48 and pAmpkα, and has no effect on Fbxo48, Ampkα1 or Ampkα2 messenger RNAs[1].
BC1618 increases the abundance of a series of autophagic marker proteins during glucose depletion. BC1618 induces phosphorylation of the mTORC1 associated protein Raptor, reducing pS6 levels, all consistent with the known mTOR inhibitory effects exerted by activated Ampk[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: BEAS-2B cells.
Concentration: 0-2 μM.
Incubation Time: 16 h.
Result: Induced pAmpkα and pACC protein levels dose-dependently.
In Vivo

BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity in high-fat-diet-induced obese mice[1].
BC1618, appears to be ~1,000-fold more potent than metformin and is extremely well tolerated in mice[1].
BC1618 displays excellent oral bioavailability with a peak of 2,000 ng/mL within 0.5h and 500 ng/mL in plasma at 4h after an oral load of 20mg/kg[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1].
Dosage: 2 or 10 mg/kg (challenged with LPS (3 mg/kg) for an additional 18 h).
Administration: IP, once.
Result: Reduced lung inflammation in endotoxin treated mice.
Animal Model: C57BL/6 mice[1].
Dosage: 15 and 30 mg/kg/d.
Administration: Drinking water for 3 months.
Result: Exhibited no obvious toxicity.
Molecular Weight

415.45

Formula

C₂₄H₂₄F₃NO₂

CAS No.

2222094-18-8

SMILES

OC(COC1=CC=C(C(F)(F)F)C=C1)CN(CC2=CC=CC=C2)CC3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (240.70 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4070 mL 12.0351 mL 24.0703 mL
5 mM 0.4814 mL 2.4070 mL 4.8141 mL
10 mM 0.2407 mL 1.2035 mL 2.4070 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (6.02 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.02 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BC1618BC 1618BC-1618AMPKMitophagyE1/E2/E3 EnzymeAMP-activated protein kinaseMitochondrial AutophagyE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligasepAmpkFbxo48mTORCLPSpS6metformininsulinmitochondrialfissionInhibitorinhibitorinhibit

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