2. PROTAC Cell Cycle/DNA Damage
  3. Molecular Glues SWI/SNF Complex
  4. SMARCA2/4 degrader-1

SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4DCAF16 and CRL1FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer.

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SMARCA2/4 degrader-1

SMARCA2/4 degrader-1 Chemical Structure

CAS No. : 2901804-87-1

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SMARCA2/4 degrader-1 Related Antibodies

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SMARCA2 SMARCA4 Protein Polybromo-1

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Description

SMARCA2/4 degrader-1 is a SMARCA2/4 molecular glue degrader with a DCAF16 EC50 of 110 nM. SMARCA2/4 degrader-1 covalently adducts at cysteine to form a ternary complex with SMARCA2/4 and recruits CUL4DCAF16 and CRL1FBXO22 E3 ligase complexes. SMARCA2/4 degrader-1 induces ubiquitination and proteasomal degradation of SMARCA2/4. SMARCA2/4 degrader-1 can be used for research of SMARCA4-deficient malignancies, non-small cell lung cancer (NSCLC), and colorectal cancer[1].

IC50 & Target[1]

Brd

 

In Vitro

SMARCA2/4 degrader-1 (Compound 1) (10-7-1 μM; 12-24 h) induces potent, proteasome-dependent degradation of SMARCA2, SMARCA4, and PBRM1 in HEK293T and HCT-116 cells[1].
SMARCA2/4 degrader-1 (16-25 h) induces SMARCA4 degradation in HEK293T cells with a DC50 of 2.2 nM, relying redundantly on both CRL4DCAF16 and CRL1FBXO22 E3 ligase complexes[1].
SMARCA2/4 degrader-1 forms ternary complexes with SMARCA2 bromodomain and CRL4DCAF16 (EC50 = 110 nM) or CRL1FBXO22 (EC50 > 1 μM)[1].
SMARCA2/4 degrader-1 (1 μM; 24 h) relies on DCAF16 residues C173 and Y62 for SMARCA2 degradation in DCAF16+FBXO22 double KO HEK293T cells, with C173 being a critical covalent binding site[1].
SMARCA2/4 degrader-1 forms a covalent ternary complex with SMARCA2 bromodomain and DCAF16:DDB1(ΔBPB):DDA1, with the degrader covalently bound to DCAF16 C173 and forming multiple stabilizing non-covalent interactions[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SMARCA2/4 degrader-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: HEK293T, HCT-116
Concentration: 10-7, 10-6, 10-5, 10-4, 10-3, 10-2, 10-1, 1 μM (immunoblot) 0.1, 1 μM (co-treatment with inhibitors)
1 μM (proteomic analysis)
Incubation Time: 24 h (immunoblot)
18 h (co-treatment with inhibitors)
12 h (proteomic analysis)
Result: Induced potent degradation of SMARCA2 and SMARCA4 in both cell lines.
Had its degradation of SMARCA2 and SMARCA4 blocked when cells were co-treated with ubiquitin-activating enzyme inhibitor TAK243, neddylation inhibitor MLN4924, or proteasome inhibitor Carfilzomib.
Induced selective degradation of SMARCA2, SMARCA4, and PBRM1.
Molecular Weight

509.65

Formula

C30H35N7O
CAS No.
SMILES

OC1=CC=CC=C1C2=CC(N3CC4N(C5=CC(C#CCN6CCCCCC6)=NC=C5)C(CC4)C3)=C(N)N=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SMARCA2/4 degrader-1 Related Classifications

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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:

SMARCA2/4 degrader-12901804-87-1Molecular GluesSWI/SNF ComplexSWI/SNF Family of Chromatin-Remodelling ComplexesCUL4DCAF16DCAF16FBXO22HEK293T cellsSMARCA2CRL1FBXO22PBRM1SMARCA4Cullin Ring LigaseHCT-116 cellsnon-small cell lung cancerInhibitorinhibitorinhibit

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