2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs SWI/SNF Complex
  4. PROTAC SMARCA2 degrader-36

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers.
(Pink: SMARCA2 ligand (HY-181910); Blue: VHL ligand (HY-112078); Black: linker).

For research use only. We do not sell to patients.

PROTAC SMARCA2 degrader-36

PROTAC SMARCA2 degrader-36 Chemical Structure

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PROTAC SMARCA2 degrader-36 Related Antibodies

Top Publications Citing Use of Products

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SMARCA2 SMARCA4 Protein Polybromo-1

  • Biological Activity

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Description

PROTAC SMARCA2 degrader-36 (Compound 26) is a selective and potent SMARCA2 PROTAC degrader with a DC50 of 51 nM. PROTAC SMARCA2 degrader-36 promotes ubiquitination and degradation of SMARCA2. PROTAC SMARCA2 degrader-36 exhibits anticancer activity against non-small cell lung cancer. PROTAC SMARCA2 degrader-36 can be used in studies related to SMARCA4-deficient cancers[1]. (Pink: SMARCA2 ligand (HY-181910); Blue: VHL ligand (HY-112078); Black: linker).

IC50 & Target[1]

VHL

 

SMARCA2

 

Parmacokinetics
Species Dose Route T1/2 Cmax AUC0-t CL Bioavailability
Mice[1] 1 mg/kg i.v. 0.632 h 578 ng/mL 304 3323 mL/h/kg /
Mice[1] 3 mg/kg p.o. 0.963 h 8.29 ng/mL 4.38 / 0.592 %
In Vivo

PROTAC SMARCA2 degrader-36 (50-100 mg/kg; i.v.; three times per week for 21 days) significantly inhibits the growth of SMARCA4-deficient NCI-H1944 xenograft tumors in BALB/c nude mice[1].
Compound 26 (100 mg/kg; i.v.; single dose) induces sustained SMARCA2 degradation for up to 24 hours in NCI-H1944 xenograft tumors[1].

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

Animal Model: BALB/c nude SCID (female)[1]
Dosage: 100 mg/kg
Administration: i.v.; three times per week for 21 days or single
Result: Achieved a tumor/control (T/C) ratio of 48.9% at 100 mg/kg.
Achieved a tumor/control (T/C) ratio of 63.9% at 50 mg/kg.
Showed no significant body weight loss.
Confirmed degradation of target protein SMARCA2.
Molecular Weight

779.95

Formula

C42H49N7O6S
SMILES

O=C([C@H]1N(C([C@@H](NC(CN2CCC(C3=CC4=NN=C(C5=CC=CC=C5O)C=C4O3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C6=CC=C(C7=C(C)N=CS7)C=C6)C
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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PROTAC SMARCA2 degrader-36 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:

PROTAC SMARCA2 degrader-36PROTACsSWI/SNF ComplexSWI/SNF Family of Chromatin-Remodelling Complexestumor tissueSMARCA4SMARCA4-deficient cancerBALB/c nude miceNCI-H1944cancer cellVHLSMARCA2plasmaubiquitin-proteasome systemInhibitorinhibitorinhibit

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PROTAC SMARCA2 degrader-36
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HY-181909
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