2. PROTAC Epigenetics
  3. PROTACs Histone Methyltransferase
  4. LLC0424

LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)).

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

LLC0424 Chemical Structure

LLC0424 Chemical Structure

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LLC0424 Related Antibodies

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Description

LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575))[1].

IC50 & Target[1]

Cereblon

 

NSD2

20 nM (DC50)

In Vitro

In SEM and RPMI-8402 cells, LLC0424 dose-dependently suppresses the growth of these two cell lines, with IC50 values of 3.56 μM and 0.56 μM respectively[1].
LLC0424 (0.001 μM-10 μM; 1 h-24 h) induces NSD2 degradation in a concentration- and time-dependent manner, and induces NSD2 degradation in a CRBN- and proteasome-dependent manner. LLC0424 also leads to downregulation of H3K36Me2[1].

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

LLC0424 Related Antibodies

Cell Viability Assay[1]

Cell Line: SEM or RPMI-8402 cells
Concentration: 5 μM
Incubation Time: 9 days (every 4 days)
Result: Significantly inhibited the growth of SEM and RPMI-8402 cells.

Western Blot Analysis[1]

Cell Line: RPMI-8402 cells
Concentration: 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, and 10 μM
Incubation Time: 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 24 h
Result: Reduced the protein level of both NSD2 isoforms in a concentration- and time-dependent manner.
In Vivo

LLC0424 (60 mg/kg; iv or ip; for 5 consecutive days) shows potent NSD2 degradation in vivo[1].

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

Animal Model: 6-8 weeks old male CB17 severe combined immunodeficiency (SCID) mice injected with 22RV1 cells were injected[1]
Dosage: 60 mg/kg
Administration: Intravenous injection or intraperitoneal injection; for five consecutive days
Result: Significantly downregulated the protein levels of NSD2.
Molecular Weight

823.85

Formula

C45H41N7O9
SMILES

O=C(N1)COC2=C1C=CC(C(N(C3CC3)CC4=CC=C(C(NC5=CC=C(C(NC6CCN(C7=CC8=C(C(N(C(C(N9)=O)CCC9=O)C8=O)=O)C=C7)CC6)=O)C=C5)=O)C=C4)=O)=C2
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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LLC0424 Related Classifications

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

LLC0424LLC 0424LLC-0424PROTACsHistone MethyltransferaseH3K36me2NSD2 PROTAC DegradercereblonInhibitorinhibitorinhibit

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HY-161574
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