1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. BI8622

BI8622 

Cat. No.: HY-120929 Purity: 99.35%
Handling Instructions

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.

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

BI8622 Chemical Structure

BI8622 Chemical Structure

CAS No. : 1875036-74-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM[1].

IC50 & Target

IC50: 3.1 μM (HUWE1)[1]

In Vitro

BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC50 value of 6.8 μM in HeLa cells[1].
BI8622 suppresses colony formation of Ls174T cells with estimated IC50 value of 8.4 μM[1].
BI8622 (10 μM; 1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1[1].
BI8622 (0-50 μM; 16 hours) retards the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells[1].
BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells[1].

Cell Cycle Analysis[1]

Cell Line: Ls174T cells
Concentration: 0 μM, 5 μM,10 μM, 15 μM, 20 μM
Incubation Time: 0-4 days
Result: Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 0 μM, 10 μM, 20 μM
Incubation Time: 16 hours
Result: Retarded the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells.
Molecular Weight

426.51

Formula

C₂₅H₂₆N₆O

CAS No.

1875036-74-0

SMILES

O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4

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
In Vitro: 

DMSO : 125 mg/mL (293.08 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3446 mL 11.7231 mL 23.4461 mL
5 mM 0.4689 mL 2.3446 mL 4.6892 mL
10 mM 0.2345 mL 1.1723 mL 2.3446 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

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

BI8622 | BI 8622 | BI-8622 | E1/E2/E3 Enzyme | E1 activating enzyme | E2 conjugating enzyme | E3 ligating enzyme | Ubiquitin activating enzyme | Ubiquitin conjugating enzyme | Ubiquitin ligase | Inhibitor | inhibitor | inhibit

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Product name:
BI8622
Cat. No.:
HY-120929
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