Search Result

Results for "

U-2OS

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Amine N-methyltransferase (4) AMPK (1) Apoptosis (6) Autophagy (1) Bacterial (2) c-Myc (1) Calcium Channel (2) CDK (4) DNA/RNA Synthesis (2) Drug Derivative (1) DYRK (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (2) Estrogen Receptor/ERR (2) Fungal (1) G protein-coupled Bile Acid Receptor 1 (2) GPR55 (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Acetyltransferase (1) Histone Methyltransferase (5) IGF-1R (1) IKK (1) Keap1-Nrf2 (1) Microtubule/Tubulin (2) MMP (1) mTOR (1) MyD88 (1) NAMPT (2) NF-κB (2) Notch (1) Nuclear Factor of activated T Cells (NFAT) (1) PERK (1) PROTACs (3) Quinone Reductase (1) RANKL/RANK (1) Reactive Oxygen Species (ROS) (2) Reference Standards (1) SGK (1) Sirtuin (1) SOD (1) Toll-like Receptor (TLR) (1) Topoisomerase (1) VDAC (1) VEGFR (1) Wnt (2) β-catenin (1)
By Research Areas:	Cancer (31) Endocrinology (1) Infection (2) Inflammation/Immunology (3) Metabolic Disease (7) Neurological Disease (1)

By Targets:

Amine N-methyltransferase (4)

AMPK (1)

Apoptosis (6)

Autophagy (1)

Bacterial (2)

c-Myc (1)

Calcium Channel (2)

CDK (4)

DNA/RNA Synthesis (2)

Drug Derivative (1)

DYRK (1)

E1/E2/E3 Enzyme (1)

Epigenetic Reader Domain (2)

Estrogen Receptor/ERR (2)

Fungal (1)

G protein-coupled Bile Acid Receptor 1 (2)

GPR55 (1)

HIF/HIF Prolyl-Hydroxylase (1)

Histone Acetyltransferase (1)

Histone Methyltransferase (5)

IGF-1R (1)

IKK (1)

Keap1-Nrf2 (1)

Microtubule/Tubulin (2)

MMP (1)

mTOR (1)

MyD88 (1)

NAMPT (2)

NF-κB (2)

Notch (1)

Nuclear Factor of activated T Cells (NFAT) (1)

PERK (1)

PROTACs (3)

Quinone Reductase (1)

RANKL/RANK (1)

Reactive Oxygen Species (ROS) (2)

Reference Standards (1)

SGK (1)

Sirtuin (1)

SOD (1)

Toll-like Receptor (TLR) (1)

Topoisomerase (1)

VDAC (1)

VEGFR (1)

Wnt (2)

β-catenin (1)

By Research Areas:

Cancer (31)

Endocrinology (1)

Infection (2)

Inflammation/Immunology (3)

Metabolic Disease (7)

Neurological Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-19979

RCM-1 5+ Cited Publications	DNA/RNA Synthesis	Cancer
RCM-1 is a forkhead box M1 (FOXM1) inhibitor with an EC₅₀ of 0.72 μM in U2OS cells. RCM-1 blocks the nuclear localization and increased the proteasomal degradation of FOXM1. RCM-1 can be used for asthma and other chronic airway diseases research .

HY-14229

TGR5 Receptor Agonist 3 Publications Verification CCDC	G protein-coupled Bile Acid Receptor 1 Calcium Channel	Metabolic Disease
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC₅₀s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca ²⁺ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity ^[2] .

HY-151500

JBSNF-000028 free base	Amine N-methyltransferase	Metabolic Disease
JBSNF-00002 free base is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC₅₀ values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 free base can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC₅₀ being 2.5 μM. JBSNF-00002 free base exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 free base can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .

HY-169053

SU1261	IKK NF-κB	Cancer
SU1261 is an IKK inhibitor with K_i values of 10 nM and 680 nM for IKKα and IKKβ, respectively. SU1261 can inhibit non-canonical NF-κB signaling in U2OS osteosarcoma cells .

HY-N2896

Arjunolic acid	Reactive Oxygen Species (ROS) Apoptosis Fungal Bacterial NF-κB SOD AMPK mTOR Notch Toll-like Receptor (TLR) Wnt MyD88 Sirtuin	Infection Neurological Disease Inflammation/Immunology Cancer
Arjunolic acid is an orally active, multifunctional bioactive compound. Arjunolic acid exhibits free radical scavenging activity, as well as fungal and bacterial activities. Arjunolic acid induces apoptosis (Apoptosis) in various cancer cells. Arjunolic acid protects hepatocytes against induced oxidative stress and apoptosis by reducing reactive oxygen species and inhibiting NF-κB activation. Arjunolic acid regulates pancreatic dysfunction in type 2 diabetic rats by blocking the activation of the TLR-4/MyD88 and canonical Wnt pathways. Arjunolic acid inhibits neuroinflammation and ameliorates depressive behaviors via the SIRT1/AMPK/Notch1 signaling pathway in microglia. Arjunolic acid improves Crohn's disease-like colitis by restoring gut microbiota composition and inhibiting TLR4 signaling. Arjunolic acid suppresses osteosarcoma progression by inhibiting Wnt3a-mediated M2 polarization of macrophages. Arjunolic acid ameliorates diabetic retinopathy via the autophagy pathway regulated by AMPK/mTOR/HO-1. Arjunolic acid is applicable to research related to type 2 diabetes, organ toxicity, depression, Crohn's disease, osteosarcoma, diabetic retinopathy, and testicular dysfunction ^[2] .

HY-111083

ML191 CID23612552	GPR55	Others
ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC₅₀=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC₅₀=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .

HY-157251

UNC8153 TFA	Histone Methyltransferase	Cancer
UNC8153 TFA is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d of 24 nM. UNC8153 TFA reduces the cellular levels of both NSD2 protein (DC₅₀ in cell U2OS is 0.35 μM) and the *H3K36me2* chromatin mark. UNC8153 TFA contains a simple warhead that confers proteasome-dependent degradation of NSD2 .

HY-147066

Dyrk1A-IN-4	DYRK	Cancer
Dyrk1A-IN-4 is a potent and orally active Dyrk1A inhibitor. Dyrk1A-IN-4 exhibits IC₅₀s against DYRK1A and *DYRK2* of 2 nM and 6 nM. Dyrk1A-IN-4 exhibits the inhibition of the DYRK1A pSer520 autophosphorylation in U2OS cells with an IC₅₀ of 28 nM. Dyrk1A-IN-4 can be used for the studies of ovarian adenocarcinoma, neuroblastoma and cervical squamous cell carcinoma .

HY-136726

CGP-82996 CINK4	CDK	Cancer
GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC₅₀s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer ^[2].

HY-151500B

JBSNF-000028 hydrochloride	Amine N-methyltransferase	Metabolic Disease
JBSNF-00002 hydrochloride is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC₅₀ values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 hydrochloride can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC₅₀ being 2.5 μM. JBSNF-00002 hydrochloride exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 hydrochloride can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .

HY-P10426

cyclo(CLLFVY)	HIF/HIF Prolyl-Hydroxylase VEGFR	Cancer
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC₅₀ of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .

HY-114208A

BI-9321 trihydrochloride	Histone Methyltransferase	Cancer
BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a K_d value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC₅₀ of 1.2 μM in U2OS cells .

HY-174996

NEP162	PROTACs Epigenetic Reader Domain Apoptosis	Cancer
NEP162 is a BRD4 PROTAC degrader with DC₅₀s of 1.2 and 1.6 μM in SW480 and U2OS cells. NEP162 exhibits antiproliferative activity, effectively inhibits tumor growth and induces apoptosis. NEP162 can be used for the study of osteosarcoma, colorectal cancer and non-small cell lung cancer, etc. (Pink: BRD4 ligand : (HY-78695), Blue: E3 ligase Ligand (HY-D2259), BLACK: Linker, E3 ligase ligand-linker conjugate (HY-174997)) .

HY-157251A

UNC8153	Histone Methyltransferase	Cancer
UNC8153 is a potent and selective nuclear receptor-binding SET domain-containing 2 (NSD2)-targeted degrader with a K_d of 24 nM. UNC8153 reduces the cellular levels of both NSD2 protein (DC₅₀ in cell U2OS is 0.35 μM) and the *H3K36me2* chromatin mark. UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 .

HY-P3730

Cdk2/Cyclin Inhibitory Peptide I	CDK	Cancer
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG), a *CDK2* inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .

HY-N6611

Chimaphilin	IGF-1R	Infection Inflammation/Immunology Cancer
Chimaphilin is an IGF-1R inhibitor (IC₅₀: 0.086 μM). Chimaphilin has antifungal, antioxidant and anticancer activities. Chimaphilin inhibits the growth of both drug-sensitive and drug-resistant osteosarcoma cell lines. Chimaphilin can induce cancer cell apoptosis. Chimaphilin is a main component of pyrola ^[2].

HY-163499

NAMPT activator-7	NAMPT	Cancer
NAMPT activator-7 (Compound 232) is an activator for nicotinamide phosphoribosyltransferase (NAMPT), with EC₅₀ < 0.5 μM. NAMPT activator-7 activates NAMPT in cells U2OS with cellular EC₅₀ of < 0.5 μM .

HY-163500

NAMPT activator-8	NAMPT	Cancer
NAMPT activator-8 (Compound 278) is an activator for nicotinamide phosphoribosyltransferase (NAMPT), with EC₅₀ < 0.5 μM. NAMPT activator-8 activates NAMPT in cells U2OS with cellular EC₅₀ of < 0.5 μM .

HY-I0450

Anticancer agent 265	Drug Derivative	Cancer
Anticancer agent 265 (compound 1) is an anticancer compound. Anticancer agent 265 exhibits in vitro anticancer activity against three human bone cancer lines, U2OS, Saos-2, and GC9811, with IC₅₀ values of 13.1, 11.7, and 14.6 μM, respectively .

HY-128221

SGK1-IN-5	SGK	Inflammation/Immunology
SGK1-IN-5 (Compound 1) is an inhibitor for serum and glucocorticoid regulated kinase SGK 1 with an IC₅₀ of 3 nM. SGK1-IN-5 inhibits SGK-1 dependent phosphorylation of GSK3β in U2OS cells with an IC₅₀ of 1.4 μM. SGK1-IN-5 can be used in research about osteoarthritis or rheumatism .

HY-114208

BI-9321	Histone Methyltransferase	Cancer
BI-9321, a chemical probe, is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a K_d value of 166 nM. BI-9321 is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC₅₀ of 1.2 μM in U2OS cells .

HY-151500A

JBSNF-000028 TFA	Amine N-methyltransferase	Metabolic Disease
JBSNF-00002 TFA is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC₅₀ values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 TFA can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC₅₀ being 2.5 μM. JBSNF-00002 TFA exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 TFA can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .

HY-N10073

Eupahualin C	Others	Cancer
Eupahualin C is a sesquiterpene lactone that can be isolated from Eupatorium hualienense. Eupahualin C shows cytotoxicity to K562 and U2OS cancer cells .

HY-151500C

JBSNF-000028	Amine N-methyltransferase	Metabolic Disease
JBSNF-00002 is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC₅₀ values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC₅₀ being 2.5 μM. JBSNF-00002 exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .

HY-14229R

TGR5 Receptor Agonist (Standard) CCDC (Standard)	G protein-coupled Bile Acid Receptor 1 Calcium Channel Reference Standards	Metabolic Disease
TGR5 Receptor Agonist (Standard) is the analytical standard of TGR5 Receptor Agonist. This product is intended for research and analytical applications. TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity ^[2] .

HY-124132

Autophagy-IN-4	Autophagy	Cancer
Autophagy-IN-4 (Compound 34) is an autophagy inhibitor, with an EC₅₀ of 0.5 μM and a LD50 of 27 μM for U2OS cells .

HY-P3731

Cdk2/Cyclin Inhibitory Peptide II	CDK	Cancer
Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL), a *CDK2* inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .

HY-161628

Tapcin	Topoisomerase	Cancer
Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC₅₀ of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC₅₀s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .

HY-161863

Tubulin polymerization-IN-67	Microtubule/Tubulin Reactive Oxygen Species (ROS) Apoptosis	Cancer
Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC₅₀ of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC₅₀s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice

HY-163518

Antitumor agent-153	E1/E2/E3 Enzyme	Cancer
Antitumor agent-153 (compound 11b) is an optimized *H2A* histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity .

HY-103453

(R)-DPN	Estrogen Receptor/ERR	Endocrinology
(R)-DPN (compound 3) is a selective ERβ ligand with EC₅₀s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC₅₀s of 286, 205 nM, respectively .

HY-169418

Tubulin polymerization-IN-71	Microtubule/Tubulin Apoptosis	Cancer
Tubulin polymerization-IN-71 (Compound 4k) is an inhibitor for tubulin polymerization with an IC₅₀ of 3.06 μM. Tubulin polymerization-IN-71 inhibits the proliferation of cancer cell MG-63 and U2OS with IC₅₀ of 0.08-0.14 μM. Tubulin polymerization-IN-71 arrests the cell cycle at G2/M phase, and induces apoptosis in MG-63 .

HY-170301

Keap1-IN-1	Quinone Reductase Keap1-Nrf2	Others
Keap1-IN-1 (Compound 27) is the inhibitor for Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE)-dependent gene NQO1 with an EC₅₀ of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC₅₀ of 527 nM .

HY-161860

Antibacterial agent 233	Bacterial	Cancer
Antibacterial agent 233 (Compound 7c) exhibits inhibitory efficacy against Helicobacter pylori with MIC of 0.4-1.6 μg/mL. Antibacterial agent 233 inhibits jack bean urease (IC₅₀ is 0.27 μg/mL), changes the permeability of H. pylori cell membrane, causes the leakage of cellular contents. Antibacterial agent 233 exhibits metabolic stability in whole blood and artificial gastric fluid. Antibacterial agent 233 exhibits antitumor efficacy against U2OS in mice .

HY-146080

Antitumor agent-61	Apoptosis	Cancer
Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC₅₀s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways .

HY-P3730A

Cdk2/Cyclin Inhibitory Peptide I acetate	CDK	Cancer
Cdk2/Cyclin Inhibitory Peptide I (Tat-LFG) acetate, a *CDK2* inhibitor, kills U2OS osteosarcoma cells in a dose-dependent manner .

HY-103455

ZK164015	Estrogen Receptor/ERR	Others
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.

HY-183802

PROTAC CBP/P300 Degrader-4	PROTACs Histone Acetyltransferase	Cancer
PROTAC CBP/P300 Degrader-4 is a p300/CBP PROTAC degrader with DC₅₀ of 17.4 nM and 10.2 nM against p300 and CBP in U2OS cells, respectively. PROTAC CBP/P300 Degrader-4 forms ternary complexes with p300 or CBP and an E3 ligase, drives ubiquitination, and mediates proteasomal degradation. PROTAC CBP/P300 Degrader-4 can be used for the research of hematological malignancies .

HY-123599

IACS-4619	DNA/RNA Synthesis	Cancer
IACS-4619 (compound 4) is a highly selective 2-aminopyrimidine-based MTH1 (MutT homolog 1) inhibitor (IC₅₀=0.2 nM). IACS-4619 inhibits MTH1 by blocking its hydrolysis of oxidized purine nucleotides such as 8-oxo-dGTP, thereby preventing MTH1 from inhibiting the incorporation of oxidized nucleotides into DNA. IACS-4619 significantly inhibits endogenous MTH1 activity in MTH1-overexpressing U2OS cells, but without antiproliferative or cytotoxic effects on various human cancer and normal cell lines. IACS-4619 can be used in oncology research related to the MTH1 target .

HY-179650

NSD2-PWWP1-IN-5	Histone Methyltransferase Apoptosis	Cancer
NSD2-PWWP1-IN-5 (Compound 13) is an effective *NSD2-PWWP1* inhibitor with a K_d value of 78 nM. NSD2-PWWP1-IN-5 competitively blocks the recognition of H3K36me2 and DNA by NSD2-PWWP1, thereby weakening its binding ability to nucleosomes. NSD2-PWWP1-IN-5 inhibits the proliferation of U2OS osteosarcoma cells and induces cell cycle arrest and apoptosis. NSD2-PWWP1-IN-5 can be used for the study of osteosarcoma .

HY-179588

PROTAC BET Degrader-14	PROTACs Epigenetic Reader Domain c-Myc	Cancer
PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC₅₀ = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC₅₀ = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma .

HY-W185542

E09241	Wnt β-catenin Nuclear Factor of activated T Cells (NFAT) MMP RANKL/RANK	Metabolic Disease
E09241 is an orally active osteoclastogenesis inhibitor. E09241 reduces the RANKL-induced expression of NFATc1 and MMP-9 by activating Wnt/β-catenin. E09241 increases the OPG/RANKL ratio by upregulating OPG expression, inhibits bone resorption, promotes bone formation and prevents ovariectomy-related bone loss. E09241 can be used in the research of osteoporosis .

HY-181529

NCATS-SM0225	VDAC PERK	Cancer
NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, *VDAC2* and VDAC3. NCATS-SM0225 exhibits an IC₅₀of 1.02 μM for ERAD and a K_d of 3.13 μM for human VDAC1 binding. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling and activating PERK. NCATS-SM0225 selectively kills cancer cells, exhibits tumor growth inhibitory effects in melanoma xenograft models. NCATS-SM0225 can be used for research on multiple cancers including melanoma, as well as the molecular mechanisms of ERAD and calcium homeostasis regulation .

Cat. No.	Product Name	Target	Research Area