PROTAC SMARCA2 degrader-32
PROTAC SMARCA2 degrader-32 is a potent, selective SMARCA2 PROTAC degrader, with DC50 values of 1.3 nM and 94 nM against SMARCA2 and SMARCA4, respectively. PROTAC SMARCA2 degrader-32 exhibits IC50 against SMARCA2, SMARCA4 and the VHL E3 ubiquitin ligase of 30 nM, 63 nM and 25 nM, respectively. PROTAC SMARCA2 degrader-32 inhibits the growth of SMARCA4-deficient cancer cells. It can be used in research on cancers such as fibrosarcoma.
(Pink: SMARCA2 ligand (HY-170349); Blue: VHL ligand (HY-170348); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3033586-50-1
- Formula: C54H64ClN9O4S
- Molecular Weight:970.66
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
SMARCA2 1.3 nM (DC50) |
SMARCA4 94 nM (DC50) |
VHL |
In Vitro
PROTAC SMARCA2 degrader-32 (Compound 27) (0.02-1000 nM; 6-24 h) potently and selectively degrades SMARCA2 over SMARCA4 in HT1080 cells via a ubiquitin-proteasome system-dependent mechanism, with a SMARCA2 DC50 of 1.3 nM and 72-fold degradation selectivity[1].
PROTAC SMARCA2 degrader-32 (10-point 3-fold dilution series; 6 days) potently inhibits the growth of SMARCA4 loss-of-function NCIH838 cells with a gIC50 of 34 nM, while having no antiproliferative effect on SMARCA4 wild-type Calu-6 cells[1].
PROTAC SMARCA2 degrader-32 (10-point 3-fold dilution series; 6 days) selectively inhibits the growth of SMARCA4 loss-of-function cancer cell lines while having minimal effect on SMARCA4 wild-type cancer cell lines, with gIC50 >1000 nM for Calu-6 and NCIH1373, and gIC50 ~100 nM for HT1080[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Chemical Information
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CAS No. 3033586-50-1
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Molecular Weight 970.66
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Formula C54H64ClN9O4S
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SMILES
CC1(C(N(C2=CC=CC(Cl)=C23)C4=CC(C5CCN(CC5)C[C@@H]6CC[C@@H](C7=CN(N=N7)[C@@H](C(C)(C)C)C(N8[C@@H](C[C@H](C8)O)C(N[C@H](C9=CC=C(C%10=C(N=CS%10)C)C=C9)C)=O)=O)CC6)=CC=C41)=NC3=O)C
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC SMARCA2 degrader-32 Related Classifications
HY-170343 Related Classifications
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