2. PROTAC Cell Cycle/DNA Damage Epigenetics
  3. PROTACs SWI/SNF Complex Epigenetic Reader Domain
  4. SMD-3236

SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia.
(Pink: SMARCA2 ligand (HY-170817); Blue: VHL ligand (HY-170826); Black: linker (HY-170825)).

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SMD-3236

SMD-3236 Chemical Structure

CAS No. : 3033586-31-8

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SMD-3236 Related Antibodies

Top Publications Citing Use of Products

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SMARCA2 SMARCA4 Protein Polybromo-1

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Description

SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia[1]. (Pink: SMARCA2 ligand (HY-170817); Blue: VHL ligand (HY-170826); Black: linker (HY-170825)).

IC50 & Target[1]

VHL

 

SMARCA2

 

In Vitro

SMD-3236 (Compound 22) potently inhibits the proliferation of SMARCA4-deficient cell lines, with GI50 values of 1.5 nM (SK-Mel-5), 9.5 nM (NCI-H838), 2.2 nM (NCI-H1568), 9.8 nM (NCI-H1944) and 4.8 nM (NCI-H1693) (Imax: 71-95%), whereas it exhibits only extremely low activity in SMARCA4 wild-type cell lines (GI50 >10 μM)[1].

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

SMD-3236 Related Antibodies
In Vivo

SMD-3236 (10-30 mg/kg; i.v.; weekly; 3 weeks) inhibits tumor growth by 87% and 91% respectively in H838 SMARCA4-deficient xenograft tumors in SCID mice, with no observable toxicity[1].
SMD-3236 (30 mg/kg; i.v.; single dose) reduces SMARCA2 protein levels by up to 97% for at least 168 h in MV4-11 xenograft tumors in SCID mice, while increasing SMARCA4 protein levels[1].

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

Animal Model: CB.17 SCID (female, 6-8 weeks old)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: i.v.; weekly; 3 weeks
Result: Inhibited tumor growth by 87% compared to vehicle control.
Inhibited tumor growth by 91% compared to vehicle control.
Induced minimal tumor growth after treatment cessation.
Caused no significant weight loss or other signs of toxicity throughout the experiment.
Animal Model: CB.17 SCID (female, 6-10 weeks old)[1]
Dosage: 30 mg/kg
Administration: i.v.; single dose
Result: Reduced SMARCA2 protein levels in MV4-11 tumors by 97% at 24 h post-administration.
Reduced SMARCA2 protein levels in MV4-11 tumors by 85% at 96 h post-administration.
Reduced SMARCA2 protein levels in MV4-11 tumors by 89% at 168 h post-administration.
Increased SMARCA4 protein levels in MV4-11 tumors by 131% at 24 h post-administration.
Increased SMARCA4 protein levels in MV4-11 tumors by 110% at 96 h post-administration.
Increased SMARCA4 protein levels in MV4-11 tumors by 45% at 168 h post-administration.
Molecular Weight

1095.83

Formula

C61H75ClN10O5S
CAS No.
SMILES

ClC1=CC=CC(N(C(C=C(C2CCN(C[C@H]3CC[C@H](C4=CN([C@@H](C(C)(C)C)C(N5[C@H](C(N[C@@H](CN6CCOCC6)C7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C5)=O)N=N4)CC3)CC2)C=C9)=C9C%10%11CCCCC%11)C%10=N%12)=C1C%12=O
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Purity & Documentation
References
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SMD-3236 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:

SMD-32363033586-31-8SMD3236SMD 3236PROTACsSWI/SNF ComplexEpigenetic Reader DomainSWI/SNF Family of Chromatin-Remodelling ComplexesSMARCA2 PROTAC degradermelanomanon-small cell lung canceracute myeloid leukemiaSK-Mel-5 cellsNCI-H838 cellsNCI-H1568 cellsNCI-H1944 cellsNCI-H1693 cellsMV4-11 cellsCB.17 SCIDInhibitorinhibitorinhibit

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