PROTAC KDM4 degrader-1
Based on 1 Customer Validation
PROTAC KDM4 degrader-1 is a KDM4 PROTAC degrader that degrades KDM4A-C with DC50 values of 37.53, 39.93, and 49.41 nM, respectively, while sparing KDM4D. PROTAC KDM4 degrader-1 induces cell cycle arrest, apoptosis and antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 can be used for the research of esophageal cancer.
(Pink: KDM4A and KDM4B and KDM4C ligand (HY-173136); Blue: VHL ligand (HY-112078); Black: linker (HY-W013381)).
For research use only. We do not sell to patients.
- CAS No.: 3102423-10-6
- Formula: C56H71N7O8S
- Molecular Weight:1002.27
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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KDM4A 37.53 nM (DC50) |
KDM4B 39.93 nM (DC50) |
KDM4C 49.41 nM (DC50) |
PROTAC KDM4 degrader-1 (Compound 11) (50 nM; 24 h) mediates the degradation of KDM4A in KYSE-150 esophageal cancer cells via a proteasome-dependent, Neddylation-dependent, VHL-dependent ubiquitin-proteasome pathway mechanism[1].
PROTAC KDM4 degrader-1 (12.3-1000 nM; 24 h) upregulates the level of H3K36me3 in KYSE-150 esophageal cancer cells in a dose-dependent manner after 24 hours of treatment, confirming its target-binding activity[1].
PROTAC KDM4 degrader-1 (0.0001-10 μM; 7 days) potently inhibits the proliferation of KYSE-150 esophageal cancer cells, with an IC50 of 16 nM[1].
PROTAC KDM4 degrader-1 (12.3-1000 nM; 24 h) induces G0/G1 cell cycle arrest in KYSE-150 esophageal cancer cells and MOLT-4 T lymphoblast cells after 24 h of treatment[1].
PROTAC KDM4 degrader-1 (12.3-1000 nM; 72 h) induces apoptosis in KYSE-150 esophageal cancer cells and MOLT-4 T lymphoblastoid cells in a dose-dependent manner after 72 h of treatment; at a concentration of 1000 nM, the early apoptosis rate of KYSE-150 cells is 29% and the late apoptosis rate is 48%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:KYSE-150 esophageal cancer cells
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Concentration:50 nM (with 2 h pre-treatment of 10 μM bortezomib, 1 μM MLN4924, or 5 μM Ac-VHL-Me)
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Incubation Time:24 h
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Result:Had its induced degradation of KDM4A attenuated by pre-treatment with bortezomib, MLN4924, or Ac-VHL-Me.
Increased the ubiquitination level of KDM4A compared to DMSO control at 50 nM for 24 h.
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Cell Line:KYSE-150 esophageal cancer cells
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Concentration:12.3 nM, 37 nM, 111.1 nM, 333.3 nM, 1000 nM
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Incubation Time:24 h
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Result:Induced a dose-dependent increase in H3K36me3 levels.
Increased H3K36me3 levels to approximately two-fold higher than the DMSO control at 1000 nM for 24 h.
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Cell Line:KYSE-150 esophageal cancer cells, MOLT-4 T lymphoblast cells
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Concentration:12.3 nM, 37 nM, 111.1 nM, 333.3 nM, 1000 nM
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Incubation Time:24 h
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Result:Increased the G0/G1-phase population in KYSE-150 cells from 65% (DMSO control) to 74% at 1000 nM for 24 h.
Induced similar G0/G1-phase arrest in MOLT-4 cells.
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Cell Line:KYSE-150 esophageal cancer cells, MOLT-4 T lymphoblast cells
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Concentration:12.3 nM, 37 nM, 111.1 nM, 333.3 nM, 1000 nM
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Incubation Time:72 h
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Result:Induced dose-dependent apoptosis in KYSE-150 cells, with obvious apoptosis observed at 12.3 nM.
Reached 29% early-stage apoptosis and 48% late-stage apoptosis in KYSE-150 cells at 1000 nM for 72 h.
Induced similar apoptotic effects in MOLT-4 cells.
Chemical Information
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CAS No. 3102423-10-6
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Appearance Solid
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Molecular Weight 1002.27
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Formula C56H71N7O8S
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SMILES
O=C(O)C1=CC=NC=C1NC[C@@H]2CCOC3=C2C=CC(N(C4=CC=C(OCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5[C@H](C(N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C)=O)C[C@@H](O)C5)=O)=O)C=C4)C)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC KDM4 degrader-1 Related Classifications
HY-173135 Related Classifications
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