2. Epigenetics Apoptosis
  3. Histone Acetyltransferase c-Myc
  4. P300-IN-6

P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma.

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

P300-IN-6

P300-IN-6 Chemical Structure

CAS No. : 3034595-62-2

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

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

P300-IN-6 Related Antibodies

Top Publications Citing Use of Products

View All Histone Acetyltransferase Isoform Specific Products:

View All Isoforms
CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma[1].

IC50 & Target[1]

p300-HAT

7 nM (IC50)

In Vitro

P300-IN-6 (Compound B6) potently inhibits the recombinant human p300 HAT domain with an IC50 of 7 nM[1].
P300-IN-6 potently inhibits the proliferation of human multiple myeloma OPM-2 cells with an IC50 of 8.8 nM[1].
P300-IN-6 (100 nM; 6 days) inhibits the proliferation of human prostate cancer 22RV1 cells, achieving 70-80% growth inhibition at 100 nM[1].
P300-IN-6 (1-20 nM; 24 h) dose-dependently suppresses c-Myc expression and reduces H3K18ac/H3K27ac levels in OPM-2 and 22RV1 cells[1].

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

P300-IN-6 Related Antibodies

Western Blot Analysis[1]

Cell Line: OPM-2 cells，22RV1 cells
Concentration: 1, 5, 10, 15, 20 nM
Incubation Time: 24 h
Result: Dose-dependently suppressed c-Myc expression as early as 6 h, and c-
Myc remained markedly suppressed through 12-24 h.
Reduced H3K18ac and H3K27ac levels.
Showed active inhibitory effect at 5-10 nM.
Parmacokinetics
Species Dose Route T1/2 AUC0-last CL MRT Vss Tmax Cmax F
Mice[1] 0.5 mg/kg p.o. 3.77 h 7.45 ng·h/mL / 4.16 h / 0.25 h 9.30 ng/mL 9.9 %
Mice[1] 0.5 mg/kg i.v. 0.26 h 75.1 ng·h/mL 118 mL/min/kg 0.26 h 1886 mL/kg / / /
In Vivo

P300-IN-6 (Compound B6) (20 mg/kg; i.g.; once daily; 17 days) achieves 60% tumor growth inhibition in a mouse OPM-2 multiple myeloma xenograft model[1].

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

Animal Model: BALB/c nude mice (female, 6 weeks old)[1]
Dosage: 20 mg/kg
Administration: I.g.; once daily; 17 consecutive days
Result: Achieved a tumor growth inhibition (TGI) value of 60%.
Showed good tolerability, with no mortality and only a slight decrease in body weight over the dosing period.
Molecular Weight

454.52

Formula

C26H26N6O2
CAS No.
SMILES

CN1C2=CC=C(NC([C@@H](C3=CC=CC=C3)NC[C@@H](C)C4=CC=C(C#N)C=C4)=O)N=C2N(C)C1=O
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.

P300-IN-6 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:

P300-IN-63034595-62-2Histone Acetyltransferasec-MycHATsHATMycxenograft mouse models22RV1 cellsOPM-2 cellsp300 HAT domainH3K27acH3K18acprostate cancermultiple myelomahistone acetyltransferaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
P300-IN-6
Cat. No.:
HY-181669
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

SAFETY DATA SHEET (SDS)

Request for HNMR Report

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