LLC0424
Based on 1 Customer Validation
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)).
(Pink: Histone Methyltransferase ligand (HY-161575); Blue: Cereblon ligand (HY-14658); Black: linker (HY-40002)).
For research use only. We do not sell to patients.
- Purity: 98.41%
- CAS No.: 3061315-33-8
- Formula: C45H41N7O9
- Molecular Weight:823.85
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
|
Cereblon |
NSD2 20 nM (DC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RPMI 8402 | IC50 |
0.56 μM
Compound: 10l; LLC0424
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Cytotoxicity against human RPMI 8402 cells assessed as inhibition of cell growth measured after 7 days by Celltiter-glo assay
Cytotoxicity against human RPMI 8402 cells assessed as inhibition of cell growth measured after 7 days by Celltiter-glo assay
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[PMID: 38687638] |
| SEM | IC50 |
3.56 μM
Compound: 10l; LLC0424
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Cytotoxicity against human SEM cells assessed as inhibition of cell growth measured after 7 days by Celltiter-glo assay
Cytotoxicity against human SEM cells assessed as inhibition of cell growth measured after 7 days by Celltiter-glo assay
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[PMID: 38687638] |
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.
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Cell Line:SEM or RPMI-8402 cells
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Concentration:5 μM
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Incubation Time:9 days (every 4 days)
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Result:Significantly inhibited the growth of SEM and RPMI-8402 cells.
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Cell Line:RPMI-8402 cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM, and 10 μM
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Incubation Time:1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 24 h
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Result:Reduced the protein level of both NSD2 isoforms in a concentration- and time-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-8 weeks old male CB17 severe combined immunodeficiency (SCID) mice injected with 22RV1 cells were injected[1]
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Dosage:60 mg/kg
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Administration:Intravenous injection or intraperitoneal injection; for five consecutive days
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Result:Significantly downregulated the protein levels of NSD2.
Chemical Information
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CAS No. 3061315-33-8
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Appearance Solid
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Molecular Weight 823.85
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Formula C45H41N7O9
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Color Light yellow to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
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 |
LLC0424 Related Classifications
HY-161574 Related Classifications
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