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Cat. No.: HY-128363

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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.

CAS No.: 2259641-59-1
Formula: C₂₆H₂₇F₃N₄O₄
Molecular Weight:516.51

Storage:

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

Data Sheet (272 KB)

Ep300/CREBBP-IN-2 Chemical Structure

CAS No.: 2259641-59-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EP300

0.052 μM (IC₅₀)

CREBBP

0.148 μM (IC₅₀)

All Histone Acetyltransferase Isoforms :

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.

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%.

Chemical Information

CAS No. 2259641-59-1
Molecular Weight 516.51
Formula C₂₆H₂₇F₃N₄O₄
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. NAITO Hiroyuki, et al. EP300 / CREBBP inhibitor. Patent JPWO2018235966A1.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Ep300/CREBBP-IN-2

All Histone Acetyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Ep300/CREBBP-IN-2 Related Classifications

HY-128363 Related Classifications