2. PROTAC Epigenetics
  3. Ligands for Target Protein for PROTAC Epigenetic Reader Domain
  4. 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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CBP/p300 ligand 4 Chemical Structure

CBP/p300 ligand 4 Chemical Structure

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CBP/p300 ligand 4 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 91.4 nM (CBP/p300 bromodomain)
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.

CBP/p300 ligand 4 Related Antibodies

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
Molecular Weight

563.60

Formula

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
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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CBP/p300 ligand 4 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:

CBP/p300 ligand 4Ligands for Target Protein for PROTACEpigenetic Reader DomainTarget Protein-binding MoietyXYD190AMLNOD-SCID miceMV4;11 AMLMOLM-13MOLM-16Inhibitorinhibitorinhibit

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CBP/p300 ligand 4
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