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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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SMARCA2 1.3 nM (DC50) |
SMARCA4 94 nM (DC50) |
VHL |
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.
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.
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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