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Cat. No.: HY-146277

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CBP/p300-IN-19

CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC₅₀s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity.

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

CAS No.: 2592638-13-4
Formula: C₃₀H₂₇N₃O₃
Molecular Weight:477.55

Storage:

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

Data Sheet (272 KB)

CBP/p300-IN-19 Chemical Structure

CAS No.: 2592638-13-4

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Fluorescent Dye

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

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

Biological Activity

Description

CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC₅₀s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity^[1].

IC₅₀ & Target^[1]

Myst3

>100 μM (IC₅₀)

p300-HAT

1.4 μM (IC₅₀)

CBP-HAT

2.2 μM (IC₅₀)

PCAF

>100 μM (IC₅₀)

All Histone Acetyltransferase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
LNCaP	EC₅₀	6.2 μM Compound: 29	Antiproliferative activity against human LNCaP cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human LNCaP cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
MCF7	EC₅₀	5.3 μM Compound: 29	Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
MDA-MB-231	EC₅₀	8.5 μM Compound: 29	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
MOLM-13	EC₅₀	3.6 μM Compound: 29	Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
MV4-11	EC₅₀	8.7 μM Compound: 29	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
PANC-1	EC₅₀	1.2 μM Compound: 29	Antiproliferative activity against human PANC-1 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human PANC-1 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
PC-3	EC₅₀	4.4 μM Compound: 29	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]
RPMI-8226	EC₅₀	6.4 μM Compound: 29	Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 5 days by XTT assay Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 5 days by XTT assay	[PMID: 35512565]

In Vitro

CBP/p300-IN-19 (compound 29) shows antiproliferative activity with EC₅₀s of 5.3, 8.5, 6.2, 4.4, 1.2, 4.3, 3.6, 8.7, 6.4 µM for MCF-7, MDA-MB231, LNCaP, PC-3, PANC-1, MDA-PANC-28, Molm-13, MV4;11, RPMI-8226 cells, respectively^[1].
CBP/p300-IN-19 (0, 5, 10 µM; 12 h) dose-dependenly inhibits the acetylation of H3K18, H3K9 and K27^[1].

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

Western Blot Analysis^[1]

Cell Line:

Kasumi-1 leukemia cells
Concentration:

0, 5, 10 µM
Incubation Time:

12 h
Result:

Dose-dependently inhibited the acetylation of H3K18, H3K9 and K27.

Chemical Information

CAS No. 2592638-13-4
Molecular Weight 477.55
Formula C₃₀H₂₇N₃O₃
SMILES

C1(C2=CC=C(C3=COC=C3)C=C2)=NC=C(OCC4CCNCC4)N=C1C5=CC=C(C6=COC=C6)C=C5
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]. Nie S, et al. Structure-activity relationship and antitumor activity of 1,4-pyrazine-containing inhibitors of histone acetyltransferases P300/CBP. Eur J Med Chem. 2022 Jul 5;237:114407. [Content Brief]

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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.

Keywords

100 mg

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

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CBP/p300-IN-19

All Histone Acetyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

CBP/p300-IN-19 Related Classifications

HY-146277 Related Classifications