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Cat. No.: HY-179427

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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.

Formula: C₄₁H₅₉ClN₂O₅
Molecular Weight:695.37

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (281 KB)

NSD2/H3K36me2 modulator-1 Chemical Structure

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

NSD2

All Histone Methyltransferase Isoforms :

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.

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.

Chemical Information

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Lv L, et al. Synthesis of amide-linked panaxadiol-indolinedione derivatives: A novel NSD2/H3K36me2 epigenetic modulator with significant antitumor efficacy. Eur J Med Chem. 2026 Jan 15;302(Pt 1):118275. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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NSD2/H3K36me2 modulator-1

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

NSD2/H3K36me2 modulator-1 Related Classifications

HY-179427 Related Classifications