YTHu78
YTHu78 is a KDM5B PROTAC-type degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and triggers apoptosis in MV-4-11 and MM.1S cell lines. YTHu78 exhibits significant antiproliferative activity against a variety of hematological cancer cell lines and can be used to study hematological cancers. (Pink: KDM5B ligand: (HY-116761); Blue: Thalidomide ligand: (HY-14658), Black + Pink: KDM5B ligand + linker: (HY-175145)).
(Pink: KDM5 ligand (HY-116761); Blue: Cereblon ligand (HY-14658); Black: linker).
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- 화학식: C33H28N8O6
- 분자량:632.63
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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Cereblon |
KDM5B |
Caspase 3 |
YTHu78 (72 h) shows antiproliferative activity against MV-4-11, HL60, MM.1S and OCI-AML3 cells, with IC50s of 1.34 μM, 6.58 μM, 1.03 μM, 9.07 μM[1].
YTHu78 (0.03-20 μM, 1-24 h) reduces KDM5B protein levels through the proteasome-mediated pathway in MV-4-11 and MM.1S cells[1].
YTHu78 (0.03-20 μM, 48 h) induces lytic apoptosis dependent on caspase in MV-4-11 and MM.1S cells[1].
YTHu78 (72 h) exhibits negligible anti-proliferative effects against primary HUVEC, GM00637 fibroblasts, HaCaT keratinocytes, GES-1, and HEK293 cells, with IC50s >20 μM[1].
YTHu78 (72 h) shows limited antiproliferative effects on refractory solid tumors and modestly sensitive solid tumor models, including HCC, PDAC, gGBM, and TNBC cells, with IC50s >20 μM and Huh-7, HCC1937, PANC-1 cells, IC50s 6-20 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11 cells, MM.1S cells
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Concentration:0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
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Incubation Time:1 h, 3 h, 6 h, 12 h, 24 h,48 h
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Result:Induced KDM5B protein degradation at a concentration of 0.74 μM and depleted KDM5B in a time-dependent manner, with maximal degradation achieved after 12 hours of treatment at a concentration of 5 μM.
Increased H3K4me3 levels.
Activated Caspase-3, induced PARP cleavage, and upregulated cleaved-GSDMD and cleaved-GSDME after 48 h of 5 μM treatment.
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Cell Line:MV-4-11 cells, MM.1S cells
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Concentration:0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
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Incubation Time:24 h
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Result:Did not affect KDM5B mRNA levels at low doses, increased mRNA levels at high concentrations in MM.1S cells.
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Cell Line:MV-4-11 cells, MM.1S cells
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Concentration:0.03 μM, 0.08 μM, 0.25 μM, 0.74 μM, 2.2 μM, 5 μM, 6.7 μM, 20 μM
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Incubation Time:48 h
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Result:Increased apoptotic population, induced mild G0/G1 cell cycle arrest at high doses, and increased LDH release.
Chemical Information
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분자량 632.63
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화학식 C33H28N8O6
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SMILES
O=C1NC(OC2=CN(CC3=CC=C(CCCNC4=CC=CC(C(N5C6CCC(NC6=O)=O)=O)=C4C5=O)C=C3)N=C2)=NC7=CN=CC=C71
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YTHu78 Related Classifications
HY-175036 Related Classifications
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