2. Epigenetics
  3. Histone Acetyltransferase
  4. Ep300/CREBBP-IN-2

Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer.

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

Ep300/CREBBP-IN-2 Chemical Structure

Ep300/CREBBP-IN-2 Chemical Structure

CAS No. : 2259641-59-1

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Ep300/CREBBP-IN-2 Related Antibodies

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Description

Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer[1].

IC50 & Target[1]

EP300

0.052 μM (IC50)

CREBBP

0.148 μM (IC50)

In Vitro

Ep300/CREBBP-IN-2 (Example 73) inhibits intracellular H3K27Ac activity with an IC50 of 0.070 μM[1].
Ep300/CREBBP-IN-2 (38 nM-10 mM; 3 days) inhibits LK2 and TE-8 cell growth with GI50s of 610.15 and 619.505 μM, respectively[1].

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

Ep300/CREBBP-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: LK2 and TE-8 cells
Concentration: 38 nM-10 mM
Incubation Time: 3 days
Result: Inhibited LK2 and TE-8 cell growth with GI50s of 610.15 and 619.505 μM, respectively.
In Vivo

Ep300/CREBBP-IN-2 (Example 73; 2 mg/kg/day; oral; twice daily for 9 days) inhibits tumor proliferation in mice[1].

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

Animal Model: Female BALB/c-nu/nu mice, TE-8 cell subcutaneous transplant model[1]
Dosage: 2 mg/kg/day
Administration: Oral administration, twice a day for 9 days
Result: Inhibited tumor volume by 65%.
Molecular Weight

516.51

Formula

C26H27F3N4O4
CAS No.
SMILES

O=C([C@@H]1N(C(C2(C3=CC=C(OC)C=C3)CCC(F)(F)CC2)=O)C[C@H](F)C1)NC4=CC=C(NC(C5)=O)C5=N4
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
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Ep300/CREBBP-IN-2 Related Classifications

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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:

Ep300/CREBBP-IN-22259641-59-1Histone AcetyltransferaseHATsHATH3K27AcLK2TE-8Inhibitorinhibitorinhibit

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