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Results for "

Smarca Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Epigenetic Reader Domain (27) Ligands for Target Protein for PROTAC (3) Oxidative Phosphorylation (1) Pim (1) PROTACs (9) SWI/SNF Complex (9)
By Research Areas:	Cancer (32) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1)

Targets Recommended: Serpin

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-144835

Camibirstat 2 Publications Verification FHD-286	Oxidative Phosphorylation Epigenetic Reader Domain	Cancer
FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia .

HY-119374

BRM/BRG1 ATP Inhibitor-1 Maximum Cited Publications 40 Publications Verification	Epigenetic Reader Domain	Cancer
BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 *(SMARCA2)* and brahma related gene 1 *(BRG1)/SMARCA4* ATPase activity inhibitor, both IC₅₀s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity .

HY-145446

SGC-SMARCA-BRDVIII	Epigenetic Reader Domain	Metabolic Disease
SGC-SMARCA-BRDVIII, a chemical probe, is a potent and selective inhibitor of *SMARCA2/4* and PB1(5), with K_ds of 35 nM, 36 nM, and 13 nM, respectively. SGC-SMARCA-BRDVIII also inhibits PB1(2) and PB1(3), with K_ds of 3.7 and 2.0 μM, respectively. SGC-SMARCA-BRDVIII can block adipogenesis of 3T3-L1 murine fibroblasts .

HY-159607

PRT3789	PROTACs SWI/SNF Complex	Cancer
PRT3789 is a selective SMARCA2 PROTAC degrader (DC₅₀ in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric cancer .

HY-12409

PFI-3 5 Publications Verification	Epigenetic Reader Domain	Cancer
PFI-3, a chemical probe, is a selective, potent and cell-permeable *SMARCA2/4* bromodomain inhibitor with a K_d of 89 nM.

HY-153361

YD23	PROTACs Epigenetic Reader Domain	Inflammation/Immunology Cancer
YD23 is a selective SMARCA2 PROTAC degrader with DC₅₀ values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) .

HY-144896

FHT-1015 2 Publications Verification	Epigenetic Reader Domain	Cancer
FHT-1015 is a selective *SMARCA4* (IC₅₀ = 4 nM) and *SMARCA2* (IC₅₀ = 5 nM) (also known as BRG1 and BRM) inhibitor. FH-1015 is an allosteric inhibitor that causes conformation change in the BRG1/BRM protein upon interaction with an allosteric site, inhibiting ATPase activity. FH-1015 interferes with tumor cell growth and migration. FH-1015 can be studied in research for uveal melanoma and hematologic cancer .

HY-156568

SMD-3040	PROTACs Epigenetic Reader Domain	Cancer
SMD-3040 is a potent and selective SMARCA2 PROTAC degrader (DC₅₀: 12 nM; D_max: 91%). SMD-3040 can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 can be used in the study of tumors such as melanoma . (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

HY-144897

FHT-1204	Epigenetic Reader Domain	Cancer
FHT-1204 is a potent SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor with IC₅₀s of ≤10 nM (WO2020160180A1; compound 70) .

HY-149458

FHT-2344	Epigenetic Reader Domain	Cancer
FHT-2344, a chemical probe, is a SMARCA4/SMARCA2 ATPase inhibitor with IC₅₀ values of 0.026 μM and 0.013 μM, respectively. FHT-2344 has anticancer activity .

HY-170824

SMD-3236	PROTACs SWI/SNF Complex Epigenetic Reader Domain	Cancer
SMD-3236 is a *SMARCA2* PROTAC degrader with a DC₅₀ of 0.5 nM, a D_max 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 .

HY-149026

GNE-064	Epigenetic Reader Domain	Others
GNE-064 (compound 5) is a selective, orally active and highly soluble inhibitor of *SMARCA4, SMARCA2* and PBRM1 bromodomains 5. GNE-064 inhibits SMARCA4 with an IC₅₀ of 0.035 μM and inhibits SMARCA2 with an EC₅₀ of 0.10 μM. GNE-064 possess K_ds with 0.01, 0.016, 0.018 and 0.049 μM for SMARCA4, SMARCA2, PBRM1 bromodomains 5 and PBRM1 bromodomains 2, repectively. GNE-064 can be used as a chemical probe for the research of agent synthesis .

HY-170817

SMI-1074	Ligands for Target Protein for PROTAC SWI/SNF Complex	Cancer
SMI-1074, a SMARCA bromodomain inhibitor, is a PROTAC target protein ligand (Ligand for Target Protein for PROTAC). SMI-1074 can be used for synthesis SMD-3236 (HY-170824) and SMD-1087 (HY-170828). SMI-1074 can be used for the research of smarca4-deficient cancers .

HY-W494890

SMARCA2-IN-10	Epigenetic Reader Domain	Cancer
SMARCA2-IN-10 (Compound 4) is a highly selective SMARCA2 ATPase domain inhibitor (IC₅₀=17.676 μM). SMARCA2-IN-10 induces cell death in SMARCA4-deficient tumors. SMARCA2-IN-10 is promising for research of SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma .

HY-144720

BRG1-IN-1	SWI/SNF Complex	Cancer
BRG1-IN-1 (Compound 11d) is a potent inhibitor of *SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor* effect of Temozolomide on the growth of subcutaneous GBM tumors .

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-161887

SMARCA2-IN-8	Epigenetic Reader Domain	Cancer
SMARCA2-IN-8 (Compound 13) is an orally active inhibitor for SWI/SNF chromatin remodeling complexe *SMARCA2* (also known as Brahma homologue, BRM) and *SMARCA4* (also known as Brahma-related gene 1, BRG1) with IC₅₀ of 5 and 6 nM. SMARCA2-IN-8 inhibits the proliferation of SMARCA2 mutated cancer cell SKMEL5 with AAC₅₀ of 5 nM. SMARCA2-IN-8 downregulates the SMARCA2-dependent KRT80 gene expression with AAC₅₀ of 10 nM. SMARCA2-IN-8 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .

HY-122645

SMARCA2-IN-4	Epigenetic Reader Domain	Cancer
SMARCA2-IN-4 (Compound 26) is an inhibitor for SWI/SNF chromatin remodeling complexe *SMARCA* by targeting the bromodomains. SMARCA2-IN-4 exhibits high affinity for PB1(5), *SMARCA2B* and *SMARCA4* with K_d of 124, 262 and 417 nM .

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-162740

SMARCA2-IN-2	Epigenetic Reader Domain	Cancer
SMARCA2-IN-2 (Compound I-25) is a *SMARCA2* inhibitor (IC₅₀: 101-500 μM), and can be used for cancer research .

HY-161888

DCSM06	Epigenetic Reader Domain	Cancer
DCSM06 is an inhibitor for the bromodomain of SWI/SNF chromatin remodeling complexe *SMARCA2* with an IC₅₀ of 9.7 μM

HY-161886

SMARCA2-IN-7	SWI/SNF Complex Epigenetic Reader Domain	Cancer
SMARCA2-IN-7 (compound 12), a dual inhibitor of BRM and BRG1 (IC₅₀ < 0.005 for both), has an anti-tumor proliferation effect that inhibits BRG1-deleted SKMEL5 tumor proliferation with a cell proliferation activity AAC₅₀ of 13 nM in SKMEL5. The cell proliferation activity AAC₅₀ of KRT880 in H1299 cells was 42 nM .

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-162739

SMARCA2-IN-1	Epigenetic Reader Domain	Cancer
SMARCA2-IN-1 (Compound I-19) is an inhibitor for SWI/SNF chromatin remodeling complexe *SMARCA2* with IC₅₀ >1000 nM in H1299 .

HY-169273

PROTAC SMARCA2 degrader-22	PROTACs SWI/SNF Complex	Cancer
PROTAC SMARCA2 degrader-22 (Compound 5) is a PROTAC degrader for *SMARCA2* with a degradation efficacy of 94% at 100 nM. PROTAC SMARCA2 degrader-22 inhibits the proliferation of cell A549 with an EC₅₀ < 250 nM .

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-163864

PROTAC SMARCA2/4-degrader-11	PROTACs	Cancer
SMARCA2 degrader-1 (compound I-321) is a PROTAC degrader of *SMARCA* with DC₅₀＜100nM (red: SMARCA inhibitor, black: linker (HY-Y1215), blue: E3 ligase ligand (HY-163927) ) .

HY-161881

SMARCA2-IN-9	Epigenetic Reader Domain	Cancer
SMARCA2-IN-9 (compound 11) is a *SMARCA2, PBRM1 bromodomains 2 (PBRM1(2)), and PBRM1 bromodomains 5 (PBRM1(5))* inhibitor with K_d values of 1.6 μM, 2.5 μM, and 3.95 μM, respectively .

HY-170343

PROTAC SMARCA2 degrader-32	PROTACs SWI/SNF Complex	Cancer
PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for *SMARCA2* with a DC₅₀ of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI₅₀ of 34 nM . (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))

HY-156568B

SMD-3040 formate	PROTACs Epigenetic Reader Domain	Cancer
SMD-3040 formate is a potent and selective SMARCA2 PROTAC degrader (DC₅₀: 12 nM; D_max: 91%). SMD-3040 formate can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 formate can be used in the study of tumors such as melanoma . (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

HY-156568A

SMD-3040 TFA	PROTACs Epigenetic Reader Domain	Cancer
SMD-3040 TFA is a potent and selective SMARCA2 PROTAC degrader (DC₅₀: 12 nM; D_max: 91%). SMD-3040 TFA can inhibit tumor cell proliferation and exhibits antitumor activity. SMD-3040 TFA can be used in the study of tumors such as melanoma . (SMARCA2/4-ligand (HY-171765); HY-112078 VHL ligand (HY-112078))

HY-122573

Bromodomain inhibitor-13	Epigenetic Reader Domain	Cancer
Bromodomain inhibitor-13 (Compound 1) is an analog of PFI-3 (HY-12409). Bromodomain inhibitor-13 is a bromodomain-containing protein (BCP) inhibitor. Bromodomain inhibitor-13 targets SMARCA2, SMARCA4, PB1(5), and second bromodomain of PB1 (PB1(2)) with K_D values of 37, 53, 30, and 190 nM, respectively .

HY-178488

BRM/BRG1 ATP-IN-7	Epigenetic Reader Domain	Infection Cancer
BRM/BRG1 ATP-IN-7 (Compound Cpd69) is a selective dual BRM (SMARCA2) and BRG1 (SMARCA4) inhibitor with IC₅₀ values of 12 nM and 8 nM, respectively. BRM/BRG1 ATP-IN-7 is promising for research of BRM/BRG1-dependent cancers (e.g., non-small cell lung cancer, Ewing sarcoma) and virus-associated diseases (e.g., HPV infection) .

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 .

HY-176822

SGC-BRDVIII-NC	Epigenetic Reader Domain	Others
SGC-BRDVIII-NC (Compound 35) is a negative control compound of *SMARCA2/4* and PB1 bromodomain (BRD) inhibitor. SGC-BRDVIII-NC completely abolishes protein-ligand binding capacity with the methylation of the phenolic hydroxyl moiety. SGC-BRDVIII-NC can be used for adipogenesis research .

HY-186147

SGI-1776-amide-C6-acid	Ligands for Target Protein for PROTAC Pim	Others
SGI-1776-amide-C6-acid (Compound S4) is a Target Protein Ligand-Linker Conjugate that contains a Pim inhibitor (HY-13287) and a PROTAC linker, and can recruit E3 ligase. SMARCA2 Ligand-Linker Conjugate-4 is applicable for the synthesis of PROTAC SGI-1776-VHL-02 (HY-186146) .

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Smarca Inhibitors

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