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Results for "

U2OS

" in MedChemExpress (MCE) Product Catalog:

70

Inhibitors & Agonists

1

Biochemical Assay Reagents

3

Peptides

9

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-169053
    SU1261

    		IKK NF-κB Cancer
    SU1261 is an IKK inhibitor with Ki values of 10 nM and 680 nM for IKKα and IKKβ, respectively. SU1261 can inhibit non-canonical NF-κB signaling in U2OS osteosarcoma cells .
    SU1261
  • 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 .
    Anticancer agent 265
  • 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 .
    Autophagy-IN-4
  • 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 .
    Cdk2/Cyclin Inhibitory Peptide I
  • 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 .
    Cdk2/Cyclin Inhibitory Peptide II
  • 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 .
    Eupahualin C
  • 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 .
    NAMPT activator-7
  • 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 .
    NAMPT activator-8
  • HY-161863
    Tubulin polymerization-IN-67

    		Microtubule/Tubulin Reactive Oxygen Species 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
    Tubulin polymerization-IN-67
  • 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 .
    Tubulin polymerization-IN-71
  • 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 .
    cyclo(CLLFVY)
  • HY-170301
    Keap1-IN-1

    		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 .
    Keap1-IN-1
  • 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 .
    (R)-DPN
  • 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 .
    Antibacterial agent 233
  • 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 .
    Tapcin
  • HY-19979
    RCM-1
    3 Publications Verification

    		 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 .
    RCM-1
  • 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 .
    Antitumor agent-153
  • 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 .
    ML191
  • 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 .
    SGK1-IN-5
  • HY-W018158
    DHICA

    5,6-Dihydroxyindole-2-carboxylic acid

    		 Endogenous Metabolite GPR35 Arrestin Others
    DHICA (5,6-Dihydroxyindole-2-carboxylic acid) is an intermediate in melanin synthesis and a component of true black pigment, and it’s also a moderately potent GPR35 agonist. DHICA shows an ability to stimulate β-arrestin translocation signaling with an EC50 value of 23.2 μM in the U2OS cell line. DHICA plays a significant role in promoting and protecting against DNA damage [2].
    DHICA
  • 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 .
    Antitumor agent-61
  • HY-14229
    TGR5 Receptor Agonist
    2 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] .
    TGR5 Receptor Agonist
  • 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.
    ZK164015
  • HY-114208
    BI-9321

    		Histone Methyltransferase Cancer
    BI-9321 is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a Kd 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 .
    BI-9321
  • 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 Kd 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 .
    BI-9321 trihydrochloride
  • 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].
    CGP-82996
  • 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 Kd of 124, 262 and 417 nM .
    SMARCA2-IN-4
  • HY-158318
    NUDT5/14 antagonist 1

    		DNA/RNA Synthesis Cancer
    NUDT5/14 antagonist 1 (Compound 9) is a selective, dual antagonist for nucleotide diphosphate kinase NUDT5 and NUDT14, with IC50 of 0.27 and 0.16 μM, respectively. NUDT5/14 antagonist 1 binds to Bruton’s tyrosine kinase (BTK) with an IC50 of 0.377 μM .
    NUDT5/14 antagonist 1
  • HY-117846
    MLAF50

    		DNA/RNA Synthesis Cancer
    MLAF50 is apotent REV1 UBM2-Ubiquitin interaction inhibitor. MLAF50 inhibits chromatin co-localization of REV1 with PCNA following DNA-damage induction .
    MLAF50
  • HY-144650
    Hsp90-Cdc37-IN-3

    		Apoptosis HSP Cancer
    Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol−imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90−Cdc37 by covalent-binding, and induces apoptosis .
    Hsp90-Cdc37-IN-3
  • HY-163460
    MS8535

    		Epigenetic Reader Domain Others
    MS8535 is a SPIN1 selective inhibitor, with an IC50 of 0.2 μM .
    MS8535
  • HY-W011215
    Dihexyl phthalate

    		Apoptosis Reactive Oxygen Species Inflammation/Immunology
    Dihexyl phthalate is one of the commonly used phthalate esters in various plastics and consumer products. Dihexyl phthalate is classified as a priority pollutant and an endocrine disruptor. Dihexyl phthalate can induce reactive oxygen species (ROS) accumulation, promote inflammation, and lead to significant increases in apoptosis and inflammation-related gene expression levels. Dihexyl phthalate can cause testicular atrophy and is a reproductive toxicant [2].
    Dihexyl phthalate
  • HY-P10286
    Phage-derived 12/1 peptide

    		MDM-2/p53 Cancer
    Phage-derived 12/1 peptide exhibits antitumor activity by targeting MDM2 and MDMX, an thus disrupt the MDM2-p53 and MDMX-p53 interaction, with IC50 of 0.15 and 1.25 μM .
    Phage-derived 12/1 peptide
  • HY-115570A
    (Z/E)-GW406108X

    (Z/E)-GW108X

    		 Kinesin ULK Autophagy Cancer
    (Z/E)-GW406108X is a mixture of different configurations of GW406108X (HY-115570). GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM .
    (Z/E)-GW406108X
  • HY-171035
    PRL-295

    		Keap1-Nrf2 Aminotransferases (Transaminases) Metabolic Disease
    PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction。PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice .
    PRL-295
  • HY-124754
    Navacaprant

    BTRX-335140; CYM-53093

    		 Opioid Receptor Neurological Disease Metabolic Disease
    Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
    Navacaprant
  • HY-115570
    GW406108X
    1 Publications Verification

    GW108X

    		 Kinesin ULK Autophagy Cancer
    GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK [2].
    GW406108X
  • HY-148078
    PFM03
    1 Publications Verification

    		 Endonuclease Others
    PFM03 is a MRE11 Endonuclease inhibitor. PFM03 regulates DNA double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ) .
    PFM03
  • HY-N7385
    Nudol

    		MMP Apoptosis Cancer
    Nudol is a phenanthrene compound that has anti-cancer activity. Nudol inhibits cell proliferation, induces cell apoptosis. Nudol inhibits MMP-2M and MMP-9 activity (Ki: 988.9 nM, 1.76 μM, respectively). Nudol can be used in the research of cancers, such as osteosarcoma [2].
    Nudol
  • HY-139149
    NiCur

    		Histone Acetyltransferase Cancer
    NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC50 value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins .
    NiCur
  • HY-109015S
    Tucidinostat-d4

    Chidamide-d4; HBI-8000-d4; CS 055-d4

    		 Isotope-Labeled Compounds HDAC Cancer
    Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
    Tucidinostat-d4
  • HY-168890
    TRF2-IN-1

    		Telomerase Apoptosis Cancer
    TRF2-IN-1 (compound F2) is a potent telomere repeat-binding factor 2 (TRF2) inhibitor. TRF2-IN-1 shows antiproliferative activity. TRF2-IN-1 induces apoptosis. TRF2-IN-1 directly bind to the TRF2TRFH domain and selectively inhibits TRF2 protein expression and telomeric localization. TRF2-IN-1 shows anticancer activity. TRF2-IN-1 has the potential for the research of osteosarcoma .
    TRF2-IN-1
  • HY-148764
    M47

    		Apoptosis Cancer
    M47 is a small molecule that selectively destabilizes Cryptochrome 1 (CRY1) and increases degradation of the CRY1 in the nucleus. M47 enhances apoptosis in Ras-transformed P53-deficient mouse skin fibroblast lines and enhances life span in p53 knockout mice. M47 can be used in research of cancer .
    M47
  • HY-110315
    Ischemin sodium

    		Apoptosis MDM-2/p53 Epigenetic Reader Domain Cardiovascular Disease
    Ischemin sodium is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. Ischemin sodium salt inhibits p53-induced p21 activation with an IC50 value of 5 µM. Ischemin sodium salt also prevents apoptosis in ischemic cardiomyocytes. Ischemin sodium salt can be used in the study of cardiovascular diseases (such as myocardial ischemia) .
    Ischemin sodium
  • HY-200129
    PCNA-IN-1

    		DNA/RNA Synthesis Cancer
    PCNA-IN-1 (Compound 11) is a PCNA/PIP-box interaction inhibitor, with IC50 of >50 μM. PCNA-IN-1 can be used in research of cancer .
    PCNA-IN-1
  • HY-134828
    AZ506
    2 Publications Verification

    		 Histone Methyltransferase Cancer
    AZ506 is a potent SMYD2 inhibitor with an IC50 of 17 nM. AZ506 inhibits SMYD2 methyltransferase activity in cells, leading to a decrease in the SMYD2-mediated methylation signal .
    AZ506
  • HY-W773183
    Methyl betulonate

    Betulonic acid methyl ester; Methyl 3-oxolup-20(29)-en-28-oate

    		 Others Cancer
    Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
    Methyl betulonate
  • HY-12442
    LY5

    		STAT Apoptosis Cancer
    LY5 is a STAT3 inhibitor with an IC50 value of 0.5 μM. LY5 induces apoptosis and inhibits STAT3 phosphorylation. LY5 shows antitumor activity in vivo, it can be used for the research of cancer .
    LY5
  • HY-100789
    ON1231320
    1 Publications Verification

    		 Polo-like Kinase (PLK) Apoptosis Cancer
    ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC50 of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity [2].
    ON1231320
  • HY-159798
    NR-11c

    		PROTACs p38 MAPK Cancer
    NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)) .
    NR-11c

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