2. PROTAC Cell Cycle/DNA Damage Apoptosis
  3. PROTACs SWI/SNF Complex Apoptosis
  4. ACBI1

ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis.
(Pink: SMARCA2 and SMARCA4 and PBRM1 ligand (HY-44012); Blue: VHL ligand (HY-125905); Black: linker).

Para uso exclusivo en investigación. No vendemos a pacientes.

The ACBI1 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

No. CAS : 2375564-55-7

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Revisión del cliente

Based on 11 publication(s) in Google Scholar

ACBI1 Related Antibodies

Top Publications Citing Use of Products

    ACBI1 purchased from MedChemExpress. Usage Cited in: Nat Genet. 2023 Mar;55(3):471-483.  [Abstract]

    ACBI1 (1.25, 2.5 μM; 2 days) inhibits ACE2 expression in both Vero E6 and Huh7.5 cells.

    ACBI1 purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.  [Abstract]

    Immunofluorescence of MBD constructs (V5, cyan) and SS18-SSX1 (HA), SMARCA2 or SMARCC1 (magenta) in HS-SY-II cells not treated (MBD-Luc) or treated with DMSO or 500 nM ACBI1 (MBD-KDM2B).

    ACBI1 purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.  [Abstract]

    Immunofluorescence of HEK293T cells expressing eGFP-SS18-SSX1 (cyan) treated with DMSO (top) or 500 nM ACBI1 (bottom) stained for BAF subunits (magenta) SMARCA2 (BRM, left), ARID1A (middle) or SMARCC1 (right). Images are representative of two biological replicates.

    ACBI1 purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.  [Abstract]

    Western Blot of whole cell extracts from HS-SY-II or HEK293T cells collected 72 h without or with 500 nM ACBI1 treatment.

    ACBI1 purchased from MedChemExpress. Usage Cited in: Nat Struct Mol Biol. 2023 Nov;30(11):1640-1652.  [Abstract]

    H3K27ac immunofluorescence of HEK293T cells expressing eGFP-EWSR1-SSX1 (left) or eGFP-MN1-SSX1 (right) treated with DMSO (top) or 500 nM ACBI1 (bottom) for SMARCA2 (BRM, left), ARID1A (middle) or SMARCC1 (right). Merge channels display eGFP (cyan) and BAF H3K27ac (magenta) overlays. Images are representative of three biological replicates.

    ACBI1 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2022 Jun 1;11(1):30.  [Abstract]

    G401 cells were treated with 250 nM ACBI1 for the indicated times and protein lysates were probed for expression of BRG1, pBAF-specific subunits PBRM1, ARID2, and BRD7, and MYC. DMSO control is matched to longest treatment. GAPDH is used as a loading control.

    ACBI1 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2022 Jun 1;11(1):30.  [Abstract]

    G401 cells in c were allowed to grow for 4 days in the presence of ACBI1 or DMSO control and cells counted at this timepoint.

    ACBI1 purchased from MedChemExpress. Usage Cited in: Oncogenesis. 2022 Jun 1;11(1):30.  [Abstract]

    Total number of differentially expressed genes that were increased in expression ("up") or decreased ("down") in response to 24 h ACBI1 treatment. FDR < 0.05 was used for determining significantly changed genes.

    Ver todos los productos específicos de isoformas PROTACs:

    Ver todas las isoformas
    von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

    Ver todos los productos específicos de isoformas SWI/SNF Complex:

    Ver todas las isoformas
    SMARCA2 SMARCA4 Protein Polybromo-1

    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis[1]. (Pink: SMARCA2 and SMARCA4 and PBRM1 ligand (HY-44012); Blue: VHL ligand (HY-125905); Black: linker).

    IC50 & Target[1]

    VHL

     

    SMARCA2

     

    SMARCA4

     

    PBRM1

     

    Cellular Effect
    Cell Line Type Value Description References
    MV4-11 IC50
    28 nM
    Compound: 25
    Antiproliferative activity against human MV4-11 cells assessed as growth inhibition
    Antiproliferative activity against human MV4-11 cells assessed as growth inhibition
    		[PMID: 32858471]
    In Vitro

    ACBI1 (1-10000 nM； 3-7 days) shows anti-proliferative activity[1].
    ACBI1 (0.3 μM; 100 h) induces apoptosis in SK-MEL-5 cells[1].
    ACBI1 is composed of a bromodomain ligand, a linker, and the E3 ubiquitin ligase von Hippel-Lindau[1].

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

    ACBI1 Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: MV-4-11, NCI-H1568 cells
    Concentration: 0-1000 nM
    Incubation Time: 3-7 days
    Result: Showed anti-proliferative activity with IC50 of 29, 68 nM for MV-4-11, NCI-H1568 cells, respectively.

    Apoptosis Analysis[1]

    Cell Line: SK-MEL-5 cells
    Concentration: 0.3 µM
    Incubation Time: 100 h
    Result: Induced apoptosis in SK-MEL-5 cells.
    Peso molecular

    936.10

    Fòrmula

    C49H58FN9O7S
    No. CAS
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CC(N=CS1)=C1C2=CC=C(CNC([C@@H]3C[C@@H](O)CN3C([C@H](C(C)(C)C)NC(C4(CC4)F)=O)=O)=O)C(OCCOC5=CC=C(CN6CCN(C7=CC(C8=C(O)C=CC=C8)=NN=C7N)CC6)C=C5)=C2
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento

    -20°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvente y solubilidad
    In Vitro: 

    DMSO : ≥ 100 mg/mL (106.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.0683 mL 5.3413 mL 10.6826 mL
    5 mM 0.2137 mL 1.0683 mL 2.1365 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Calculadora de molaridad

    • Calculadora de dilución

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (2.67 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Pureza y Documentación

    Purity: 99.92%

    SDS (393 KB)

    COA (252 KB) HNMR (598 KB) LCMS (99 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.0683 mL 5.3413 mL 10.6826 mL 26.7065 mL
    5 mM 0.2137 mL 1.0683 mL 2.1365 mL 5.3413 mL
    10 mM 0.1068 mL 0.5341 mL 1.0683 mL 2.6707 mL
    15 mM 0.0712 mL 0.3561 mL 0.7122 mL 1.7804 mL
    20 mM 0.0534 mL 0.2671 mL 0.5341 mL 1.3353 mL
    25 mM 0.0427 mL 0.2137 mL 0.4273 mL 1.0683 mL
    30 mM 0.0356 mL 0.1780 mL 0.3561 mL 0.8902 mL
    40 mM 0.0267 mL 0.1335 mL 0.2671 mL 0.6677 mL
    50 mM 0.0214 mL 0.1068 mL 0.2137 mL 0.5341 mL
    60 mM 0.0178 mL 0.0890 mL 0.1780 mL 0.4451 mL
    80 mM 0.0134 mL 0.0668 mL 0.1335 mL 0.3338 mL
    100 mM 0.0107 mL 0.0534 mL 0.1068 mL 0.2671 mL
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    ACBI1 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    ACBI12375564-55-7ACBI 1ACBI-1PROTACsSWI/SNF ComplexApoptosisSWI/SNF Family of Chromatin-Remodelling ComplexesMV-4-11 cellsSK-MEL-5 cellsanti-proliferativeapoptosisInhibitorinhibitorinhibit

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    Nombre del producto:
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