2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. XYD190

XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496)).

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XYD190 Chemical Structure

XYD190 Chemical Structure

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XYD190 Related Antibodies

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Description

XYD190 (Compound 14g) is an orally active degrader for CBP/p300. XYD190 inhibits CBP/p300 bromodomain with IC50 of 483.7 nM. XYD190 exhibits antitumor activity against acute myeloid leukemia. (Structure: Pink, CBP/p300 ligand 4 (HY-161495); Blue, E3 ligase ligand (HY-14658); Black: linker (HY-161496))[1].

In Vitro

XYD190 (0-1 μM, 72-120 h) inhibits proliferations of acute myeloid leukemia (AML) cells MV4;11, MOLM-13 and MOLM-16, with the IC50 of 1.8, 26.9 and 4.6 nM, respectively[1].
XYD190 (0-150 nM, 6 h) induces CBP and p300 degradation in bromodomain family proteins in a CRBN- and proteasome-dependent manner[1].

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

XYD190 Related Antibodies

Cell Proliferation 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: 0-150 nM
Incubation Time: 6 h
Result: Degraded CBP and p300 proteins.
In Vivo

CBP/p300 ligand 4 (5 mg/kg, p.o., every other day for 2 weeks) exhibits antitumor activity in MV4;11 xenograft mice model, with a tumor growth inhibition rate TGI of 88%[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: 5 mg/kg
Administration: p.o., every other day for 2 weeks
Result: Inhibited tumor growth with a TGI of 88%.
Molecular Weight

1001.05

Formula

C55H50F2N10O7
SMILES

O=C1CCC[C@H](N1C2=CC=C(C(F)=C2)F)C3=NC4=C(C=CC(C5=C(ON=C5C)C)=C4)N3C6CCN(CC6)CC(NC7=CC=C(N=C7)C8=CC=C(C=C8)CNC9=CC=CC(C(N%10C%11C(NC(CC%11)=O)=O)=O)=C9C%10=O)=O
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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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XYD190 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:

XYD190XYD 190XYD-190PROTACsEpigenetic Reader DomainAMLNOD-SCID miceMV4;11MOLM-13MOLM-16leukemiaInhibitorinhibitorinhibit

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