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Results for "

SMARCA2/4-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E3 Ligase Ligand-Linker Conjugates (1) Epigenetic Reader Domain (6) Ligands for Target Protein for PROTAC (2) Molecular Glues (1) PROTAC Linkers (2) PROTACs (3) SWI/SNF Complex (4)
By Research Areas:	Cancer (14)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Click Chemistry

Art. -Nr.	Produktname	Target	Forschungsgebiete	Chemical Structure

HY-175756

**SMARCA2/4 degrader-1**	Molecular Glues SWI/SNF Complex	Cancer
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 CUL4 ^DCAF16 and CRL1 ^FBXO22 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 .

HY-161884

*SMARCA2/4-IN-1*	Epigenetic Reader Domain	Cancer
SMARCA2/4-IN-1 (compound 1) is a potent *SMARCA2* inhibitor with IC₅₀ values of 3.8, 1.7 µM for SMARCA2, SMARCA4, respectively .

HY-161885

SMARCA2/4-IN-4	SWI/SNF Complex	Cancer
SMARCA2-IN-6 is a *SMARCA2* and SMARCA4 inhibitor, with an IC₅₀ value of <0.005 μM for both *SMARCA2* and SMARCA4. SMARCA2-IN-6 exerts anticancer activity against BRG1-mutant melanoma. SMARCA2-IN-6 can be used for research related to Brg1/Smarca4-mutant cancers .

HY-171774

PBRM1/SMARCA2,4-ligand-1	Ligands for Target Protein for PROTAC Epigenetic Reader Domain	Cancer
PBRM1/SMARCA2,4-ligand-1 (Compound 4) is a Ligand for Target Protein for PROTAC that binds to PBRM1, *SMARCA2, and SMARCA4*. PBRM1/SMARCA2,4-ligand-1 is a potent SMARCA4 bromodomain inhibitor. PBRM1/SMARCA2,4-ligand-1 can be used to synthesize PROTAC AU-24118 (HY-163410) .

HY-178225

PROTAC SMARCA2/4 degrader-39	PROTACs Epigenetic Reader Domain	Cancer
PROTAC SMARCA2/4 degrader-39 (Compound 7) is a selective degrader of SMARCA2 (BRM) and SMARCA4 (BRG1) PROTAC. PROTAC SMARCA2/4 degrader-39 is promising for research of oncology, such as non-small cell lung cancer and colorectal cancer . (Pink: BRM/BRG1 ligand 5 (HY-178886); Black: Linker Piperazine (HY-B0912); Blue: (S)-Deoxy-thalidomide (HY-168055))

HY-159452

PROTAC SMARCA2/4-degrader-1	PROTACs	Cancer
SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting *SMARCA2* and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC₅₀s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .

HY-174237

PBRM1/SMARCA2,4 binder-1	Epigenetic Reader Domain	Cancer
PBRM1/SMARCA2,4 binder-1 (Compound 17) is a binder of PBRM1, *SMARCA2, and SMARCA4* (IC₅₀: 0.083, 0.153, and 0.046 μM, respectively) .

HY-161889

DCSM06-05	Epigenetic Reader Domain	Cancer
DCSM06-05 is a potent *SMARCA2-BRD* inhibitor with an IC₅₀ value of 9 µM, a K_d value of 22.4 µM .

HY-159592

Piperazine-Pyrimidine-Cyclohexane-COOEt	PROTAC Linkers	Cancer
Piperazine-Pyrimidine-Cyclohexane-COOEt is a PROTAC linker. Piperazine-Pyrimidine-Cyclohexane-COOEt can be used in the synthesis of PROTAC SMARCA2/4-degrader-1 (HY-159452) .

HY-162815

PROTAC SMARCA2/4-degrader-26	PROTACs Epigenetic Reader Domain	Cancer
PROTAC SMARCA2/4-degrader-26 (compound 6) is a PROTAC targeting SMARCA2/4. SMARCA2 and SMARCA4 are genes and cancer targets with complementary functions that catalyze nucleosome movement. PROTAC SMARCA2/4-degrader-25 is composed of PROTAC target protein ligand 2-(4-(3-Amino-6-(2-hydroxyphenyl)pyridazin-4-yl)piperazin-1-yl)acetic acid (HY-46618) (red part), E3 ligase ligand (2S,4R)-4-Hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (HY-W998248) (blue part), PROTAC linker (S)-2-Amino-3,3-dimethylbutanoic acid (HY-59140) (black part), and the conjugate composed of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC (HY-125845) ^{[1] ^.}

HY-162791

(1s,4s)-C1-Piperidine-C1-cyclohexane-C1	PROTAC Linkers	Cancer
(1s,4s)-C1-Piperidine-C1-cyclohexane-C1 is a PROTAC linker. (1s,4s)-C1-Piperidine-C1-cyclohexane-C1 can be used to synthesize PROTAC SMARCA2/4-degrader-33 (HY-162741) .

HY-182987

SMARCA2/SMARCA4 ligand-1	Ligands for Target Protein for PROTAC SWI/SNF Complex	Cancer
SMARCA2/SMARCA4 ligand-1 is a *SMARCA2/SMARCA4* ligand with K_D values of 1.2 and 10.3 nM. SMARCA2/SMARCA4 ligand-1 binds SMARCA2/4 bromodomain via hydrogen bonds with asparagine and tyrosine residues, and a salt bridge with a glutamate residue. SMARCA2/SMARCA4 ligand-1 shows antiproliferative activity against cancer cells. SMARCA2/SMARCA4 ligand-1 can be used for the research of cancer, such as smarca4 mutant nonsmall cell lung cancer .

HY-159593

Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo	E3 Ligase Ligand-Linker Conjugates	Cancer
Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo is an E3 Ligase Ligand-Linker Conjugate. Ac-NH-(S,R,S)-AHPC-CO-cyclohexane-pyrimidine-diazabicyclo can be used to synthesize PROTAC SMARCA2/4-degrader-1 (HY-159452) .

HY-185075

FHD-909 LY4050784	SWI/SNF Complex	Cancer
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC₅₀ of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified *SMARCA4* (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders .

Art. -Nr.	Produktname		Classification

HY-159452

PROTAC SMARCA2/4-degrader-1		Azide
SMARCA2/4-degrader-1 (compound I-430) is a PROTAC degrader targeting *SMARCA2* and SMARCA4; it degrades SMARCA2/4 proteins in A549 cells with the DC₅₀s <100 nM, and the maximum degradation rate (Dmax%) >90 after 24 h of treatment .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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