PROTAC SMARCA2/4 degrader-38

Cat. No.: HY-173333: FAQs
Data Sheet Handling Instructions Technical Support

PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC₅₀: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)).

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

PROTAC SMARCA2/4 degrader-38 Chemical Structure

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

SMARCA2

3.0 nM (DC₅₀)

SMARCA4

4.0 nM (DC₅₀)

VHL

In Vitro

PROTAC SMARCA2/4 degrader-38 (Compound A11) (25-100 nM, 3 d) inhibits the proliferation activity of MV-4-11 cell lines (IC₅₀: 4.9 nM) and MOLM-13 cell lines (IC₅₀: 23.3 nM) in AML cells, and SU-DHL-4 (IC₅₀: 87.7 nM) and WSU-DLCL-2 (IC₅₀: 336.7 nM) in diffuse large B-cell lymphoma^[1].
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 48 h) induces cell cycle arrest at G0/G1 phase in MV-4-11 and MOLM-13 cells in a concentration-dependent manner^[1].
PROTAC SMARCA2/4 degrader-38 (100-1000 nM, 72 h) induces apoptosis in MV-4-11 and MOLM-13 cells^[1].
PROTAC SMARCA2/4 degrader-38 (11.1-1000 nM, 24 h) inhibits the transcriptional expression of AML oncogenes in a concentration-dependent manner^[1].

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

Cell Cycle Analysis^[1]

Cell Line:	MV-4-11 cells and MOLM-13 cells
Concentration:	100 nM, 300 nM and 1000 nM
Incubation Time:	48 h
Result:	Induced a large accumulation of G0/G1 cells in MV-4-11 and MOLM-13 cells.

Apoptosis Analysis^[1]

Cell Line:	MV-4-11 cells and MOLM-13 cells
Concentration:	100 nM, 300 nM and 1000 nM
Incubation Time:	72 h
Result:	Induced apoptosis in MV-4-11 and MOLM-13 cells.

Western Blot Analysis^[1]

Cell Line:	MOLM-13 cells; MV-4-11 cells
Concentration:	100 nM, 300 nM and 1000 nM; 11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
Incubation Time:	72 h; 24 h
Result:	Up-regulated apoptosis-related cleaved poly ADP-ribose polymerase (PARP) and cleaved caspase-3 proteins levels. Down-regulated MYC protein level.

RT-PCR^[1]

Cell Line:	MV-4-11 cells
Concentration:	11.1 nM, 33.3 nM, 100 nM, 300 nM and 1000 nM
Incubation Time:	24 h
Result:	Down-regulated the expression of E2F1, CDC25A, TRAP1, PU. 1, CD44 and BCL-2 genes.

Parmacokinetics

Species	Dose	Route	Indicator	value
Rat	1 mg/kg	i.v.	C_max	1953 ng/mL
Rat	10 mg/kg	p.o.	C_max	6.41 ng/mL
Rat	1 mg/kg	i.v.	T_max	0.033 hr
Rat	10 mg/kg	p.o.	T_max	0.42 hr
Rat	1 mg/kg	i.v.	T_1/2	1.91 hr
Rat	10 mg/kg	p.o.	T_1/2	2.10 hr
Rat	1 mg/kg	i.v.	AUC_0-t	358 ng·h/mL
Rat	10 mg/kg	p.o.	AUC_0-t	8.22 ng·h/mL
Rat	1 mg/kg	i.v.	MRT_0-t	0.70 hr
Rat	10 mg/kg	p.o.	MRT_0-t	0.81 hr
Rat	10 mg/kg	p.o.	F	0.62 %

Molecular Weight

773.94

Formula

C₄₃H₄₇N₇O₅S

SMILES

O=C([C@H]1N(C([C@@H](NC(C2(C3=CC=C(C4=CC(C5=CC=CC=C5O)=NN=C4N)C=C3)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

Handling Instructions (2659 KB)

References

[1]. Yang T, et al. Design, synthesis and biological evaluation of 3-amino-6-(2-hydroxyphenyl)pyridazin-4-aryl derivatives as SMARCA2/4 degraders. Eur J Med Chem. 2025 Jun 5;290:117521.