PROTAC SMARCA2/4 degrader-36
PROTAC SMARCA2/4 degrader-36 is a bifunctional PROTAC degrader that degrades SMARCA2 and SMARCA4. PROTAC SMARCA2/4 degrader-36 hijacks the ubiquitin-proteasome system to mediate the degradation of SMARCA2/4 by binding to the VHL E3 ubiquitin ligase. PROTAC SMARCA2/4 degrader-36 downregulates SMARCA2/4 in tumor tissues in mouse xenograft models. PROTAC SMARCA2/4 degrader-36 can be used in studies related to non-small cell lung cancer.
(Pink: SMARCA2 and SMARCA4 ligand (HY-170354); Blue: VHL ligand (HY-170353); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3033588-00-7
- Formula: C53H62ClN9O4S
- Molecular Weight:956.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
SMARCA2 0.22 nM (DC50) |
SMARCA4 0.85 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HT-1080 | DC50 |
0.22 nM
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Degradation of SMARCA2 protein in HT1080 cells genetically modified to express SMARCA2-HiBiT, assessed using Nano-Glo HiBiT Lytic Detection Assay after 6 h incubation.
Degradation of SMARCA2 protein in HT1080 cells genetically modified to express SMARCA2-HiBiT, assessed using Nano-Glo HiBiT Lytic Detection Assay after 6 h incubation.
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39570797 |
| HT-1080 | DC50 |
0.85 nM
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Degradation of SMARCA4 protein in HT1080 cells genetically modified to express SMARCA4-HiBiT, assessed using Nano-Glo HiBiT Lytic Detection Assay after 6 h incubation.
Degradation of SMARCA4 protein in HT1080 cells genetically modified to express SMARCA4-HiBiT, assessed using Nano-Glo HiBiT Lytic Detection Assay after 6 h incubation.
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39570797 |
In Vitro
PROTAC SMARCA2/4 degrader-36 (compound 29) binds to VHL E3 ubiquitin ligase with an IC50 of 2.1 nM[1].
PROTAC SMARCA2/4 degrader-36 potently degrades SMARCA2 (DC50 = 0.22 nM, Dmax = 98%) and SMARCA4 (DC50 = 0.85 nM, Dmax = 97%) in HT1080 cells[1].
PROTAC SMARCA2/4 degrader-36 potently inhibits the proliferation of SMARCA4-deficient NCIH838 cells (gIC50 = 3.0 nM) and SMARCA4 wild-type Calu-6 cells (gIC50 = 280 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c Nude mice were subcutaneously inoculated with HT‑1080 tumor cells (2 × 106 cells per mouse in 0.1 mL PBS)[1]
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Dosage:1 mg/kg; 10 mg/kg
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Administration:i.v.; single dose
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Result:Reduced SMARCA2 protein levels in tumor tissue by 94% and SMARCA4 protein levels by 54% relative to vehicle control.
Reduced SMARCA2 protein levels by >95% and SMARCA4 protein levels by 93% relative to vehicle control.
Chemical Information
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CAS No. 3033588-00-7
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Molecular Weight 956.64
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Formula C53H62ClN9O4S
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SMILES
ClC1=CC=CC(N(C(C=CC(C2CCN(C[C@H]3CC[C@H](C4=CN([C@H](C(N5C[C@H](O)C[C@H]5C(N[C@@H](C)C6=CC=C(C7=C(C)N=CS7)C=C6)=O)=O)C(C)C)N=N4)CC3)CC2)=C8)=C8C9(C)C)C9=N%10)=C1C%10=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC SMARCA2/4 degrader-36 Related Classifications
HY-170347 Related Classifications
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