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Referencia número: HY-161495

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CBP/p300 ligand 4

CBP/p300 ligand 4 (Compound 4) is an orally active inhibitor for CBP/p300 bromodomain, with IC₅₀ of 91.4 nM. CBP/p300 ligand 4 serves as a ligand for target protein XYD190 (HY-161495). XYD190 is a PROTAC degrader for CBP/p300.

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No. CAS: 3040120-71-3
Fòrmula: C₃₀H₃₁F₂N₅O₄
Peso molecular:563.60

Almacenamiento:

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

Data Sheet (278 KB)

CBP/p300 ligand 4 Chemical Structure

No. CAS: 3040120-71-3

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Use of MCE Products

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
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Actividad biológica

Descripciòn

IC₅₀ & Target

CBP/p300

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In Vitro

CBP/p300 ligand 4 (0-1 μM, 72-120 h) inhibits proliferations of AML cells MV4;11, MOLM-13 and MOLM-16, with the IC₅₀ of 20.4, 102 and 12.9 nM, respectively, through degradation of CBP, p300 and c-Myc proteins^[1].

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

Cell Viability Assay^[1]

Cell Line:

MV4;11 AML, MOLM-13 and MOLM-16
Concentration:

0-1 μM
Incubation Time:

3 days for MOLM-13, 4 days for MV4;11 AML and MOLM-16
Result:

Inhibited cell proliferation.

Western Blot Analysis^[1]

Cell Line:

MV4;11 AML, MOLM-13 and MOLM-16
Concentration:

50 nM
Incubation Time:

24 h
Result:

Degraded CBP, p300 and c-Myc proteins.

In Vivo

CBP/p300 ligand 4 (10 mg/kg, p.o., once daily for 2 weeks) exhibits antitumor activity in MV4;11 xenograft mice model, with a tumor growth inhibition rate TGI of 65%^[1].

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

Animal Model:

MV4;11 xenograft NOD-SCID mice model^[1]
Dosage:

10 mg/kg
Administration:

p.o., once every day for 2 weeks
Result:

Inhibited tumor growth

Chemical Information

No. CAS 3040120-71-3
Peso molecular 563.60
Fòrmula C₃₀H₃₁F₂N₅O₄
SMILES

O=C1CCC[C@H](N1C2=CC=C(C(F)=C2)F)C3=NC4=C(C=CC(C5=C(ON=C5C)C)=C4)N3C6CCN(CC(O)=O)CC6
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (278 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Hu J, et al., Discovery of Highly Potent and Efficient CBP/p300 Degraders with Strong In Vivo Antitumor Activity. J Med Chem. 2024 May 9;67(9):6952-6986. [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.

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100 mg

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Actividad biológica
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- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

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CBP/p300 ligand 4

Ver todos los productos específicos de isoformas Epigenetic Reader Domain

Ver todos los productos específicos de isoformas Histone Acetyltransferase