2. Epigenetics
  3. Epigenetic Reader Domain
    Histone Acetyltransferase
  4. GNE-272

GNE-272 

Cat. No.: HY-100726 Purity: 99.76%
COA Handling Instructions

GNE-272 est un inhibiteur CBP / EP300 puissant et sélectif avec des valeurs IC50 de 0,02, 0,03 et 13 μM pour CBP, EP300 et BRD4, respectivement. GNE-272 est également une sonde sélective in vivo pour CBP/EP300.

GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.

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

GNE-272 Chemical Structure

GNE-272 Chemical Structure

CAS No. : 1936428-93-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 213 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 213 In-stock
Estimated Time of Arrival: December 31
Solid
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 228 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GNE-272

WB

    GNE-272 purchased from MCE. Usage Cited in: J Transl Med. 2023 Mar 17;21(1):201.  [Abstract]

    GNE-272 downregulates the expression of SNAI2 both in BxPC-3 and PANC1.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300[1].

    IC50 & Target

    IC50: 0.02 μM (CBP), 0.03 μM (EP300), 13 μM (BRD4)[1]
    In Vitro

    GNE-272 is exquisitely selective for CBP/ EP300 and remarkably selective (650-fold) over BRD4. When tested at 10 μM in 35 kinase panel and 42 receptors off-target screening panel, GNE-272 does not inhibit any target at >30%. In addition, GNE-272 does not inhibit (>10 μM, top concentration) several cytochrome P450s (3A4, 1A2, 2C9, 2C19, 2D6). The compound has good potency in the BRET cellular assay. In an orthogonal measure of the target engagement, GNE-272 is shown to inhibit the expression of MYC10 (MV4−11 cell line) with an EC50 of 0.91 μM and good correlation between the BRET and MYC cellular assays is observed[1].

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

    GNE-272 demonstrates low clearance following a 1 mg/ kg intravenous dose in a mouse PK experiment and good oral bioavailability when dosed at 100 mg/kg, reaching an unbound Cmax of 26 μM. GNE-272 shows a marked antiproliferative effect in hematologic cancer cell lines and modulates MYC expression in vivo that corresponds with antitumor activity in an AML tumor model[1].

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

    424.47

    Appearance

    Solid

    Formula

    C22H25FN6O2
    CAS No.
    SMILES

    CC(N1CCC2=C(C(NC3=C(F)C=C(C4=CN(C)N=C4)C=C3)=NN2[[email protected]@H]5COCC5)C1)=O
    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 : 100 mg/mL (235.59 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3559 mL 11.7794 mL 23.5588 mL
    5 mM 0.4712 mL 2.3559 mL 4.7118 mL
    10 mM 0.2356 mL 1.1779 mL 2.3559 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: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
    Cell Assay
    [1]

    Human cancer cell lines (MOLM-16, HL-60, LP-1, KMS-34, Pfeiffer, DOHH-2) are treated for 4 h with 5 μM GNE-272 or DMSO control. After 6 days, cell viability is measured by CellTiter-Glo[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice: Mice are given 0 (vehicle, 0.5% methylcellulose; 0.2% Tween-80), 12.5, 25, and 50 mg/kg of GNE-272 by gavage, twice daily (BID) for 21 days in a volume of 100 μL. Tumor volumes are measured in two dimensions (length and width) using Ultra CalIV calipers and analyzed using Excel, version 11.2[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    GNE-2721936428-93-1GNE272GNE 272Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email address *

    Phone number *

    		 

    Organization name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GNE-272
    Cat. No.:
    HY-100726
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email address *

    Phone number

    		 

    Department *

    Organization name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.