2. PROTAC Epigenetics Apoptosis
  3. PROTACs Histone Demethylase Apoptosis
  4. PROTAC KDM4 degrader-1

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.

PROTAC KDM4 degrader-1

PROTAC KDM4 degrader-1 Chemical Structure

CAS No. : 3102423-10-6

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Based on 1 publication(s) in Google Scholar

PROTAC KDM4 degrader-1 Related Antibodies

Top Publications Citing Use of Products

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

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Description

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[1]. (Pink: KDM4A and KDM4B and KDM4C ligand (HY-173136); Blue: VHL ligand (HY-112078); Black: linker (HY-W013381)).

IC50 & Target[1]

KDM4A

37.53 nM (DC50)

KDM4B

39.93 nM (DC50)

KDM4C

49.41 nM (DC50)

In Vitro

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.

PROTAC KDM4 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: KYSE-150 esophageal cancer cells
Concentration: 50 nM (with 2 h pre-treatment of 10 μM bortezomib, 1 μM MLN4924, or 5 μM Ac-VHL-Me)
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: KYSE-150 esophageal cancer cells
Concentration: 12.3 nM, 37 nM, 111.1 nM, 333.3 nM, 1000 nM
Incubation Time: 24 h
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.

Cell Cycle Analysis[1]

Cell Line: KYSE-150 esophageal cancer cells, MOLT-4 T lymphoblast cells
Concentration: 12.3 nM, 37 nM, 111.1 nM, 333.3 nM, 1000 nM
Incubation Time: 24 h
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.

Apoptosis Analysis[1]

Cell Line: KYSE-150 esophageal cancer cells, MOLT-4 T lymphoblast cells
Concentration: 12.3 nM, 37 nM, 111.1 nM, 333.3 nM, 1000 nM
Incubation Time: 72 h
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.
Molecular Weight

1002.27

Formula

C56H71N7O8S
CAS No.
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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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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PROTAC KDM4 degrader-1 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:

PROTAC KDM4 degrader-13102423-10-6PROTACsHistone DemethylaseApoptosisKDM4CKDM4BKDM4Aubiquitin-proteasome systemesophageal cancer cellsKYSE-150MOLT-4 T lymphoblast cellshistone H3 lysine demethylationcell cycle arrestKDM4DInhibitorinhibitorinhibit

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