2. Epigenetics Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Histone Methyltransferase Apoptosis Reactive Oxygen Species (ROS)
  4. NSD2/H3K36me2 modulator-1

NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC).

For research use only. We do not sell to patients.

NSD2/H3K36me2 modulator-1

NSD2/H3K36me2 modulator-1 Chemical Structure

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NSD2/H3K36me2 modulator-1 Related Antibodies

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

NSD2/H3K36me2 modulator-1 is an orally active NSD2/H3K36me2 modulator. NSD2/H3K36me2 modulator-1 competitively binds to the SAM pocket of NSD2, potently inhibits NSD2 expression and suppresses H3K36me2 methylation. NSD2/H3K36me2 modulator-1 reverses epithelial-mesenchymal transition (EMT), inhibits cell migration, and induces G0/G1 phase arrest and apoptosis. NSD2/H3K36me2 modulator-1 induces decreased Mitochondrial membrane potential (MMP) and subsequent Reactive oxygen species (ROS) generation. NSD2/H3K36me2 modulator-1 can be used to research the NSD2-targeting epigenetic anticancer strategies for hepatocellular carcinoma (HCC)[1].

IC50 & Target[1]

NSD2

 

In Vitro

NSD2/H3K36me2 modulator-1 (Compound 5b) (24 h) displays IC50 < 5 μM against all five cancer cell lines (IC50 values of 4.67, 2.12, 2.64, 4.56, 4.99 μM in A549, HepG-2, PC-3, HCT-116, MCF-7 cells respectively), confirming its exceptional broad-spectrum antitumor activity[1].
NSD2/H3K36me2 modulator-1 exhibits a high tumor selectivity for HepG-2 cells over HaCaT cells (IC50 = 19.2 μM) (selectivity index (SI) = 9.06)[1].
NSD2/H3K36me2 modulator-1 (2 μM, 24 h , 37-62°C) effectively binds to NSD2 within HepG-2 cells[1].
NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 h) inhibits NSD2 and selectively downregulates its mediated H3K36me2 in HepG-2 cells[1].
NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 h) reverses EMT at the molecular level, likely through NSD2 inhibition and subsequent TWIST1 downregulation, leading to altered expression of Epithelial-mesenchymal transition (EMT) master regulators[1].
NSD2/H3K36me2 modulator-1 (2, 4 μM, 18, 36 h) significantly inhibits migration and proliferation of HepG-2 cells[1].
NSD2/H3K36me2 modulator-1 (2, 4 μM, 24 h) exerts multiple regulatory effects on HepG-2 cells, including effectively inducing apoptosis, triggering concentration-dependent G0/G1 phase arrest, reducing mitochondrial membrane potential (MMP) dose-dependently, and efficiently promoting the generation of ROS[1].

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

NSD2/H3K36me2 modulator-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HepG-2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Suppressed NSD2 expression in a dose-dependent manner, with notably strong inhibition at 4 μM.
Exhibited high selective inhibition of H3K36me2.
Bound effectively to NSD2 within cells.

Apoptosis Analysis[1]

Cell Line: HepG-2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Significantly increased the total apoptosis rate in HepG-2 cells with the elevation of the concentration.
Exhibited slightly superior apoptosis-inducing capacity at the concentration of 4 μM.

Western Blot Analysis[1]

Cell Line: HepG-2 cells
Concentration: 2, 4 μM
Incubation Time: 24 h
Result: Significantly suppressed TWIST1 expression.
Dose-dependently downregulated N-Cadherin and Vimentin.
Upregulated E-Cadherin and Occludin in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HepG-2 cells
Concentration: 0, 2, 4 μM
Incubation Time: 24 h
Result: Elevated the proportion of HepG-2 cells in G0/G1 phase from 53.8 % to 65.7 %, with the concentration increasing from 0 to 2 μM.
Increased the G0/G1 subpopulation to 79.6 %, with the concentration reaching 4 μM, and exceeded that of 5-Fluorouracil (HY-90006) (73.5 %).
Induced a marked decrease in the levels of cell cycle regulators CDK2, CDK4, and CDK6, effectively blocking cell cycle progression in a concentration-dependent manner.
In Vivo

NSD2/H3K36me2 modulator-1 (Compound 5b) (20, 40 mg/kg, daily p.o. for 18 consecutive days) exerts robust antitumor effects with effective tumor growth inhibition and an acceptable safety profile in a HepG-2 cell xenograft model, as evidenced by the absence of significant differences in the body weight, organ indices, and morphological features[1].

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

Animal Model: An HepG-2 xenograft model established in female BALB/c nude mice (6-8 weeks old)[1]
Dosage: 20, 40 mg/kg
Administration: daily oral gavage (p.o.) for 18 consecutive days
Result: Significantly suppressed tumor growth in a dose-dependent manner.
Exhibited the strongest antitumor effect at 40 mg/kg.
Molecular Weight

695.37

Formula

C41H59ClN2O5
SMILES

ClC1=CC(N(CC(N[C@@H]2C(C)(C)[C@@](CC[C@]3(C)[C@@]4([H])C[C@@H](O)[C@@]5([H])[C@@]3(C)CC[C@]5([H])[C@@]6(C)CCCC(C)(C)O6)(C)[C@]4(C)CC2)=O)C(C7=O)=O)=C7C=C1
Shipping

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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NSD2/H3K36me2 modulator-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:

NSD2/H3K36me2 modulator-1Histone MethyltransferaseApoptosisReactive Oxygen Species (ROS)Panaxadiol derivativesNSD2H3K36me2EMTEpigenetic modulatorsAntitumor agentsHepatocellular carcinomaInhibitorinhibitorinhibit

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