2. Epigenetics
  3. Histone Acetyltransferase
  4. B026

B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines.

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

B026 Chemical Structure

B026 Chemical Structure

CAS No. : 2379416-48-3

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

B026 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

B026 is a selective, potent, orally active p300/CBP histone acetyltransferase (HAT) inhibitor with IC50 values of 1.8 nM and 9.5 nM for p300 and CBP enzyme, respectively. B026 has anticancer activity for androgen receptor-positive (AR+) prostate cancer cell lines[1].

IC50 & Target[1]

p300

8.1 nM (IC50)

CBP

9.5 nM (IC50)

In Vitro

B026 (0-5 μM; 12 h; cancer cell lines) has antiproliferative activity[1].
B026 (0-5 μM; 6 h; MV-4-11 cells) exhibits inhibitory effects on H3K27Ac expression[1].
B026 (0-5 μM; 12 h; MV-4-11 cells) targets the cellular p300 protein and increases the thermal stability of p300 protein in a dose-dependent manner[1].
B026 (0-1 μM; 24 h; MV-4-11 cells) decreases the expression of MYC, which a key oncogenictranscription factor that is regulated by superenhancer regions containing p300/CBP[1].

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

B026 Related Antibodies

Cell Viability Assay[1]

Cell Line: Maver-1, MV-4-11, K562, Kasumi-1, LnCaP-FGC and 22Rv1 cells
Concentration: 0-5 μM
Incubation Time: 12 hours
Result: Inhibited cell growth with IC50 values of 2.6, 4.2, 4.4, 9.8, 40.5 and 104.4 nM for Maver-1, MV-4-11, 22Rv1, LnCaP-FGC, Kasumi-1 and K562 cells, respectively.

Western Blot Analysis[1]

Cell Line: MV-4-11 cells
Concentration: 0, 0.313, 0.625, 1.25, 2.5 and 5 μM
Incubation Time: 6 hours
Result: Decreased the expression of H3K27Ac in a dose-dependent manner.
In Vivo

B026 (1-3 mg/kg; i.v. and p.o.; 0-24 h; male SD rats) has a low clearance (13.4 mL/min/kg) and good oral exposure (AUC=3.71 μM·h) with good oral bioavailability (F=56%) in rat[1].
B026 (50-100 mg/kg; p.o.; daily, for 28 days; balb/c female mice) inhibits tumor growth in a dose-dependent manner[1].

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

Animal Model: Balb/c female mice with MV-4-11 xenograft[1]
Dosage: 50 and 100 mg/kg
Administration: Oral administration; daily, for 28 days
Result: Inhibited tumor growth with TGI of 75.0% at 50 mg/kg and 85.7% at 100 mg/kg, respectively.
Animal Model: Male SD rats[1]
Dosage: 1 and 3 mg/kg
Administration: Intravenous injection and oral administration; 0.25, 0.5 , 1 , 2 , 4 , 8 and 24 hours
Result: 1.19
Administration i.v. (1 mg/kg) p.o. (3 mg/kg)
T1/2 (h) 1.5 1.02
Tmax (h) 0.83
Cmax (μM) 1.12
AUClast (μM·h) 2.22 3.71
Vdss (L/kg) 1.5
CL_obs (mL/min/kg) 13.4
PPB % 98.2
F % 56
Molecular Weight

557.50

Formula

C27H23F4N5O4
CAS No.
SMILES

O=C1[C@@]2(NC(N1CC(N3[C@@H](COC4=CC=C(F)C=C4C3)C(F)(F)F)=O)=O)C5=CC=C(C6=CN(N=C6)C)C=C5CC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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.

B026 Related Classifications

  • 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
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:

B0262379416-48-3B 026B-026Histone AcetyltransferaseHATsHATp300CBPhistone acetyltransferaseanticancerH3K27AcMYCInhibitorinhibitorinhibit

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:
B026
Cat. No.:
HY-147261
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.