YTHu78
YTHu78 is a KDM5B PROTAC degrader. YTHu78 induces KDM5B degradation via the ubiquitin-proteasome system and CRBN E3 ligase, and triggers lytic apoptosis in hematologic malignant cells. YTHu78 can be used in studies related to hematologic malignancies.
(Pink: KDM5 ligand (HY-116761); Blue: Cereblon ligand (HY-14658); Black: linker).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C33H28N8O6
- Peso molecular:632.63
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Almacenamiento:
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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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
KDM5B |
Caspase 3 |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
1.34 μM
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Antiproliferative activity against human myeloid monocytic leukemia MV-4-11 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human myeloid monocytic leukemia MV-4-11 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| HL-60 | IC50 |
6.583 μM
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Antiproliferative activity against human hematologic malignancy HL-60 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human hematologic malignancy HL-60 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| MM.1S | IC50 |
1.036 μM
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Antiproliferative activity against human hematologic malignancy MM.1S cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human hematologic malignancy MM.1S cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| MV4-11 | IC50 |
1.489 μM
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Antiproliferative activity against human hematologic malignancy MV-4-11 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human hematologic malignancy MV-4-11 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| OCI-AML-3 | IC50 |
9.074 μM
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Antiproliferative activity against human hematologic malignancy OCI-AML3 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human hematologic malignancy OCI-AML3 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| HUVEC | IC50 |
>20 μM
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Antiproliferative activity against normal human HUVEC cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against normal human HUVEC cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| HaCaT | IC50 |
>20 μM
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Antiproliferative activity against normal human HaCaT cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against normal human HaCaT cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| GES1 | IC50 |
>20 μM
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Antiproliferative activity against normal human GES-1 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against normal human GES-1 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| HEK293 | IC50 |
>20 μM
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Antiproliferative activity against normal human HEK293 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against normal human HEK293 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| Huh-7 | IC50 |
6.04 μM
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Antiproliferative activity against human solid tumor Huh-7 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor Huh-7 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| PANC-1 | IC50 |
17.67 μM
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Antiproliferative activity against human solid tumor PANC-1 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor PANC-1 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| HCC1937 | IC50 |
15.41 μM
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Antiproliferative activity against human solid tumor HCC1937 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor HCC1937 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| SNU-387 | IC50 |
>20 μM
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Antiproliferative activity against human solid tumor SNU-387 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor SNU-387 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| A 172 | IC50 |
>20 μM
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Antiproliferative activity against human solid tumor A-172 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor A-172 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| U-87MG ATCC | IC50 |
>20 μM
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Antiproliferative activity against human solid tumor U87MG cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor U87MG cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
| MDA-MB-468 | IC50 |
>20 μM
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Antiproliferative activity against human solid tumor MDA-MB-468 cells assessed by CCK-8 assay after 72 h incubation.
Antiproliferative activity against human solid tumor MDA-MB-468 cells assessed by CCK-8 assay after 72 h incubation.
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40578256 |
In Vitro
YTHu78 (0.03 µM-20 µM; 24-48 h) significantly inhibits cell viability, markedly increases the proportion of cells at the late apoptotic stage, induces mild G0/G1 cell cycle arrest, activates Caspase-3, triggers the cleavage of PARP, GSDMD and GSDME, and induces significant lactate dehydrogenase (LDH) release in MV-4-11 (IC50 = 1.34 µM) and MM.1S (IC50 = 1.036 µM) cells[1].
YTHu78 (0.03 µM-20 µM; 1-24 h) effectively induces time-dependent degradation of KDM5B protein without significantly affecting its mRNA level in MV-4-11 and MM.1S cells, exerts no obvious effect on KDM5A, and additionally increases the expression level of H3K4me3[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, HL60, MM.1S, and OCI-AML3 cell lines
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Concentration:0.03, 0.08, 0.25, 0.74, 2.2, 6.7, 20 µM
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Incubation Time:72 h
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Result:Significantly inhibited the proliferation of hematologic malignancy cells.
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Cell Line:MV-4-11 and MM.1S cell lines
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Concentration:0.03, 0.08, 0.25, 0.74, 2.2, 6.7, 20 µM (and 5 µM alone)
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Incubation Time:1, 3, 6, 12, 24, 48 h
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Result:Effectively induced KDM5B protein degradation, increased H3K4me3 levels, and activated apoptosis and pyroptosis-related executors (such as Caspase-3, GSDMD, and GSDME cleavage).
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Cell Line:MV-4-11 and MM.1S cell lines
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Concentration:0.03, 0.08, 0.25, 0.74, 2.2, 6.7, 20 µM
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Incubation Time:48 h
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Result:Significantly increased the proportion of late-stage apoptotic cells and compromised cell membrane integrity.
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Cell Line:MV-4-11 and MM.1S cell lines
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Concentration:0.03, 0.08, 0.25, 0.74, 2.2, 6.7, 20 µM
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Incubation Time:24 h
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Result:Induced a mild G0/G1 phase cell cycle arrest.
Chemical Information
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Peso molecular 632.63
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
YTHu78 Related Classifications
HY-175036 Related Classifications
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