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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1 mg USD 420 In-stock
5 mg USD 1060 In-stock
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Based on 1 publication(s) in Google Scholar

LLC0424 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All Histone Methyltransferase Isoform Specific Products:

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

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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
Appearance

Solid

Color

Light yellow to yellow

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

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (121.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2138 mL 6.0691 mL 12.1381 mL
5 mM 0.2428 mL 1.2138 mL 2.4276 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2138 mL 6.0691 mL 12.1381 mL 30.3453 mL
5 mM 0.2428 mL 1.2138 mL 2.4276 mL 6.0691 mL
10 mM 0.1214 mL 0.6069 mL 1.2138 mL 3.0345 mL
15 mM 0.0809 mL 0.4046 mL 0.8092 mL 2.0230 mL
20 mM 0.0607 mL 0.3035 mL 0.6069 mL 1.5173 mL
25 mM 0.0486 mL 0.2428 mL 0.4855 mL 1.2138 mL
30 mM 0.0405 mL 0.2023 mL 0.4046 mL 1.0115 mL
40 mM 0.0303 mL 0.1517 mL 0.3035 mL 0.7586 mL
50 mM 0.0243 mL 0.1214 mL 0.2428 mL 0.6069 mL
60 mM 0.0202 mL 0.1012 mL 0.2023 mL 0.5058 mL
80 mM 0.0152 mL 0.0759 mL 0.1517 mL 0.3793 mL
100 mM 0.0121 mL 0.0607 mL 0.1214 mL 0.3035 mL
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LLC0424 Related Classifications

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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