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HT1080

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75

Inhibitors & Agonists

11

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1

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2

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N9596
    Stigmasta-4,22-dien-3-one

    		Bacterial Infection Cancer
    Stigmasta-4,22-dien-3-one is an antitubercular agent. Stigmasta-4,22-dien-3-one shows cytotoxicity against human HT1080 tumoral cell line with an IC50 of 0.3 mM .
    Stigmasta-4,22-dien-3-one
  • HY-50908
    Ridaforolimus
    5+ Cited Publications

    MK-8669; Deforolimus; AP23573

    		 mTOR Autophagy Bacterial Cancer
    Ridaforolimus (MK-8669) is a potent and selective mTOR inhibitor; inhibits ribosomal protein S6 phosphorylation with an IC50 of 0.2 nM in HT-1080 cells .
    Ridaforolimus
  • HY-133887
    Methotrexate α-tert-butyl ester

    		Antifolate DNA/RNA Synthesis Cancer
    Methotrexate α-tert-butyl ester, capped by OtBu, significantly reduces tumor growth in HT1080 tumor bearing mice. Methotrexate is an antimetabolite and antifolate agent and is also an immunosuppressant and antineoplastic agent .
    Methotrexate α-tert-butyl ester
  • HY-W047478
    3-Methylcarbazole

    NSC 10154

    		 Interleukin Related Cancer
    3-Methylcarbazole is an carbazole alkaloid compound with anticancer effects. 3-Methylcarbazole shows growth inhibitory activity (IC50 of 25 μg/mL) on human fibrosarcoma HT-1080 cells .
    3-Methylcarbazole
  • HY-156879
    Antiproliferative agent-40

    		Drug Derivative Cancer
    Antiproliferative agent-40 (Compound 9) inhibits proliferation of HT1080 and MCF-7 with IC50s of 52 and 8.2 μM respectively .
    Antiproliferative agent-40
  • HY-161930
    PROTAC GPX4 degrader-3

    		PROTACs Ferroptosis Cancer
    PROTAC GPX4 degrader-3 is a potent PROTAC GPX4 degrader with a DC50 (24h) of 0.019 μM and an IC50 of 0.024 μM in HT1080 cell .
    PROTAC GPX4 degrader-3
  • HY-162718
    GPX4-IN-12

    		Ferroptosis Cancer
    GPX4-IN-12 (compound I22) is a non-covalent GPX4 inhibitor. GPX4-IN-12 induces ferroptosis and inhibits cell growth of HT1080 cells .
    GPX4-IN-12
  • HY-162716
    GPX4-IN-10

    		Ferroptosis Cancer
    GPX4-IN-10 (compound I20) is a non-covalent GPX4 inhibitor. GPX4-IN-10 induces ferroptosis and inhibits cell growth of HT1080 cells .
    GPX4-IN-10
  • HY-156878
    Antiproliferative agent-39

    		Others Cancer
    Antiproliferative agent-39 (Compound 12) inhibits proliferation of A549, SNU-638, Col2, HT1080, MCF-7 with IC50s of 11, 25, 14, 11, 6.3 μM respectively .
    Antiproliferative agent-39
  • HY-121085
    CID-663143

    		Microtubule/Tubulin Cancer
    CID-663143 targets microtubule-associated proteins, not tubulin itself, to inhibit the polymerization process within cells. CID-663143 inhibits cancer cell growth (IC50: <100 nM for HT-1080, BJeLR, MCF10A cells) .
    CID-663143
  • HY-116087
    SRS11-92

    		Ferroptosis Neurological Disease Cancer
    SRS11-92, a Ferrostatin-1 (Fer-1) analogue, is a potent ferroptosis inhibitor. SRS11-92 inhibits ferroptotic cell death induced by Erastin in HT-1080 human fibrosarcoma cells (EC50=6 nM) .
    SRS11-92
  • HY-149236
    PROTAC GPX4 degrader-1

    		PROTACs Glutathione Peroxidase Ferroptosis Cancer
    PROTAC GPX4 degrader-1 (DC-2) is a PROTAC-based GPX4 degrader, with a DC50 of 0.03 μM in HT1080 cells .
    PROTAC GPX4 degrader-1
  • HY-159567
    Ferroptosis-IN-11

    		Ferroptosis Cardiovascular Disease Neurological Disease
    Ferroptosis-IN-11 (compound 43) is a ferroptosis inhibitor. Ferroptosis-IN-11 can inhibit Erastin (HY-15763) induced ferroptosis in HT-1080 human fibroblasts (EC50=36 nM). Ferroptosis-IN-11 can be used in the study of cardiovascular disease and neurodegeneration .
    Ferroptosis-IN-11
  • HY-153698
    CC-3060

    		Ligands for E3 Ligase Cancer
    CC-3060 is a Cereblon modulator that promotes ZBTB16 degradation. CC-3060 degrades ZBTB16 with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 targets ZBTB16 for degradation by primarily engaging distinct structural degrons on different zinc finger domains .
    CC-3060
  • HY-N10158
    1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one

    		Others Cancer
    1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one (compound 39), a diarylheptanoid, exhibits antiproliferative activity towards human HT-1080 fibrosarcoma and murine colon 26-L5 carcinoma cells .
    1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one
  • HY-100579
    Ferrostatin-1
    Maximum Cited Publications
    862 Publications Verification

    Fer-1

    		 Ferroptosis Fungal Cancer
    Ferrostatin-1 (Fer-1), a potent and selective ferroptosis inhibitor, suppresses Erastin-induced ferroptosis in HT-1080 cells (EC50=60 nM). Ferrostatin-1, a synthetic antioxidant, acts via a reductive mechanism to prevent damage to membrane lipids and thereby inhibits cell death. Ferrostatin-1 exhibits antifungal activity .
    Ferrostatin-1
  • HY-173029
    UAMC-4821

    		Ferroptosis Cancer
    UAMC-4821 is an inhibitor for ferroptosis with an IC50 of 5.2 nM. UAMC-4821 scavenges free radicals, blocks the lipid peroxidation, inhibits ML162 (HY-100002)-induced ferroptosis, and exhibits protective effect in HT-1080 cell. UAMC-4821 exhibits good pharmacokinetics characteristics in mouse with an oral bioavailability of 63%. UAMC-4821 can cross blood-brain barrier .
    UAMC-4821
  • HY-139248
    Paclitaxel octadecanedioate

    		Drug Derivative Cancer
    Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively) .
    Paclitaxel octadecanedioate
  • HY-114459
    Mutant IDH1-IN-4

    		Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells .
    Mutant IDH1-IN-4
  • HY-111844
    PROTAC RAR Degrader-1

    		PROTACs SNIPERs RAR/RXR Neurological Disease Metabolic Disease Cancer
    PROTAC RAR degrader-1 (Compound 9) is a potent and selective RAR PROTAC Degrader consisting of apoptotic protein inhibitors (IAPs) ligands. IAPs-based degraders are also known as SNIPERs. PROTAC RAR Degrader-1 reduces RARα levels in HT1080 cells in a concentration-dependent manner but is blocked by the proteasome inhibitor MG132 (HY-13259). PROTAC RAR Degrader-1 can be used in the study of nuclear receptor-related diseases. (Pink: RAR ligand 1 (HY-111843); Black: Linker (HY-140189); Blue: IAPs Ligand (HY-B0134)) .
    PROTAC RAR Degrader-1
  • HY-161948
    Ferroptosis inducer-4

    		Ferroptosis Cancer
    Ferroptosis inducer-4 (Compound 5) is a ferroptosis (Ferroptosis) inducer with a structure featuring terminal double bonds introduced at the sn-2 position of phospholipids. Ferroptosis inducer-4 exhibits significant cytotoxicity towards HT-1080 cells, with an IC50 of 18 μM. This cytotoxic mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane triggered by the terminal double bonds. Ferroptosis inducer-4 can be used for research on ferroptosis regulation .
    Ferroptosis inducer-4
  • HY-168093
    Cetzole

    		Ferroptosis Cancer
    Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
    Cetzole
  • HY-170959
    NYY-6a

    		Ferroptosis Neurological Disease Metabolic Disease
    NYY-6a is a Ferroptosis inhibitor. NYY-6a shows significant inhibitory activity against RSL3-induced ferroptosis across 786-O and HT-1080 cells with EC50s of 52 and 50 nM, respectively. NYY-6a functions as a radical trapping antioxidant (RTA) with efficacy of diminishing lipid peroxidation comparable to ferrostatin-1 and liproxtatin-1. NYY-6a is potential for ferroptosis related pathologies reasearch .
    NYY-6a
  • HY-169133
    GDCNF-11

    		PROTACs Glutathione Peroxidase Ferroptosis Cancer
    GDCNF-11 is a HIM-PROTAC GPX4 degrader based on the chaperone protein HSP90. GDCNF-11 promotes the ubiquitination and degradation of GPX4 through the HSP 90 chaperone complex, reduces endogenous GPX4 expression to induce ferroptosis in HT-1080 cells, and the DC50 value is 0.08 μM (Pink: Target protein ligand (HY-153748); Blue: HSP90 ligand (HY-10212); Black: Linker (HY-W169526)) .
    GDCNF-11
  • HY-143234
    mIDH1-IN-1

    		Isocitrate Dehydrogenase (IDH) Cancer
    mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
    mIDH1-IN-1
  • HY-169382
    Melatonin-Tamoxifen Conjugate

    		Melatonin Receptor Cancer
    Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
    Melatonin-Tamoxifen Conjugate
  • HY-145669
    DIF-3
    2 Publications Verification

    		 CDK GSK-3 Infection Cancer
    DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo .
    DIF-3
  • HY-N0998
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one

    		Melanocortin Receptor Cancer
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one (compound 6) shows antiproliferative activity with ED50s of 57.7, 78.8 μM for 26-L5 and HT-1080 cells, respectively. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one inhibits melanogenesis in B16 melanoma 4A5 cells. 1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one has the potential for the research of skin disorders .
    1,7-Bis(4-hydroxyphenyl)-hepta-4E,6E-dien-3-one
  • HY-149359
    IHMT-IDH1-053

    		Isocitrate Dehydrogenase (IDH) Cancer
    IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
    IHMT-IDH1-053
  • HY-161972
    ZX782

    		PROTACs Glutathione Peroxidase Ferroptosis Cancer
    ZX782 is a Hty-type PROTAC targeting GPX4 and a ferroptosis inducer, which induces GPX4 degradation and significantly increases lipid ROS accumulation in HT1080 cells. ZX782 can be used to treat AD by reducing the size and/or number of brain amyloid plaques and by inhibiting the spread of IL-1beta-positive microglial-like cells around amyloid plaques. ZX782 is labeled with hydrophobic benzyl alcohol (HBA) and appears bright blue under acidic conditions, which can be used for quantitative determination . ZX782 is composed of target protein ligand (red part) ML-210 (HY-100003), PROTAC linker (black part) Bromo-PEG2-CH2-Boc (HY-141371) and Hty molecule (blue part) Adamantan-1-ylmethanamine (HY-W037848). The conjugate consisting of Hyt and linker parts is Adamantan-C-amide-PEG2-C-Br (HY-161974), and the activity control of the target protein ligand is Hydroxyl-ML-210 (HY-161973).
    ZX782
  • HY-149670
    Ferroptosis-IN-3

    		Ferroptosis Inflammation/Immunology
    Ferroptosis-IN-3 (Compound 25) is a ferroptosis inhibitor. Ferroptosis-IN-3 inhibits RSL3-induced ferroptosis (EC50: 8.6?nM in HT-1080?cells). Ferroptosis-IN-3 scavenges DPPH and ABTS radicals (EC50: 3.94?and 6.3 μM respectively). Ferroptosis-IN-3 decreases lipid peroxidation .
    Ferroptosis-IN-3
  • HY-168236
    PROTAC SMARCA2 degrader-28

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC SMARCA2 degrader-28 (Compound 158) is a PROTAC degrader for SMARCA2, that degrades SMARCA2 with a DC50 of 3 nM in HiBiT A549 cells. (Pink: Ligand for target protein (HY-168237); Black: Linker (HY-168238); Blue: Ligand for E3 ligase (HY-W087383))
    PROTAC SMARCA2 degrader-28
  • HY-B1645
    Ammonium iron(III) citrate
    25+ Cited Publications

    Ammonium ferric citrate; FAC

    		 Ferroptosis Cancer
    Ammonium iron(III) citrate (Ammonium ferric citrate), a physiological form of nonetransferrin-bound iron, induces intracellular iron overload to cause ferroptosis . Ammonium iron(III) citrate can enhance protein production .
    Ammonium iron(III) citrate
  • HY-170349
    SMARCA2 ligand-11

    		Ligands for Target Protein for PROTAC SWI/SNF Complex Cancer
    SMARCA2 ligand-11 is the ligand for SMARCA2, and can be used for synthesis of PROTAC SMARCA2 degrader-32 (HY-170343) as ligand for target protein .
    SMARCA2 ligand-11
  • HY-170352
    E3 Ligase Ligand-linker Conjugate 150

    		E3 Ligase Ligand-Linker Conjugates Cancer
    E3 Ligase Ligand-linker Conjugate 150 is the conjugate of the ligand for E3 ligase VHL and the linker, that can be used for synthesis of PROTAC SMARCA2 degrader-32 (HY-170343) .
    E3 Ligase Ligand-linker Conjugate 150
  • 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))
    PROTAC SMARCA2 degrader-32
  • HY-162449
    GIC-20

    		Apoptosis Ferroptosis Cancer
    GIC-20 is a dual inducer for apoptosis and ferroptosis. GIC-20 exhibits antitumor efficacy against fibrosarcoma .
    GIC-20
  • HY-162717
    GPX4-IN-11

    		Glutathione Peroxidase Ferroptosis Cancer
    GPX4-IN-11 (compound I14) is a potent inhibitor of GPX4, with the KD of 45.7 μM. GPX4-IN-11 plays an important role in ferroptosis research .
    GPX4-IN-11
  • HY-161764
    α-Glucosidase-IN-67

    		Amylases Glycosidase Metabolic Disease
    α-Glucosidase-IN-67 (compound 5k) is a potent α-Glucosidase inhibitor with IC50 values of 0.31, 4.51 µM for alpha-glucosidase and alpha-amylase, respectively. α-Glucosidase-IN-67 has the potential for the research of type-2 diabetes .
    α-Glucosidase-IN-67
  • HY-N2117
    Isoginkgetin
    10+ Cited Publications

    		 MMP Akt NF-κB Proteasome Apoptosis Autophagy Inflammation/Immunology Cancer
    Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .
    Isoginkgetin
  • HY-162106
    PROTAC GPX4 degrader-2

    		Ferroptosis PROTACs Glutathione Peroxidase Cancer
    PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 48h value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .
    PROTAC GPX4 degrader-2
  • HY-N2117R
    Isoginkgetin (Standard)

    		MMP Akt NF-κB Proteasome Apoptosis Autophagy Inflammation/Immunology Cancer
    Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy .
    Isoginkgetin (Standard)
  • HY-147173
    FAPI-74

    		FAP Cancer
    FAPI-74 is a PET (positron emission tomography) tracer targeting the fibroblast activation protein (FAP). FAPI-74 can be used for FAP-positive tumor research .
    FAPI-74
  • HY-155602
    CDK2-IN-18

    		CDK Cancer
    CDK2-IN-18 (compound 8q) is a potent inhibitor of CDK2/E and CDK4/D1, with IC50s of 8 nM and 46 nM, respectively. CDK2-IN-18 inhibits the proliferation of tumor cells .
    CDK2-IN-18
  • HY-149923
    GPX4-IN-4

    		Glutathione Peroxidase Cancer
    GPX4-IN-4 (Compound 24) is a potent GPX4 inhibitor. GPX4-IN-4 can be used for the research of cancer .
    GPX4-IN-4
  • HY-157788
    ZX703

    		PROTACs Reactive Oxygen Species Ferroptosis Glutathione Peroxidase Cancer
    ZX703 (compound 5I) is a PROTAC that significantly degrades GPX4 in a dose- and time-dependent manner through the ubiquitin-proteasome and autophagy-lysosome pathways (DC50=0.315 µM). ZX703 induces ferroptosis by inducing Reactive Oxygen Species (ROS) accumulation in cells. ZX703 can be used for cancer research .
    ZX703
  • HY-168879
    GPX4-IN-16

    		Glutathione Peroxidase Cancer
    GPX4-IN-16 ((R)-9i) is a potent GPX4 inhibitor with an KD value of 20.4 nM. GPX4-IN-16 shows cytotoxicity. GPX4-IN-16 shows anticancer activity .
    GPX4-IN-16
  • HY-137175
    TMBIM6 antagonist-1

    		mTOR Cancer
    TMBIM6 antagonist-1, a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca 2+ .
    TMBIM6 antagonist-1
  • HY-161929
    GPX4 activator 2

    		Glutathione Peroxidase Ferroptosis Cardiovascular Disease
    GPX4 activator 2 (Compound C3) is an activator of GPX4. GPX4 activator 2 exhibits cardioprotective effects and can inhibit cellular ferroptosis (EC50 = 7.8 μM)。GPX4 activator 2 can be used in the research of myocardial injury .
    GPX4 activator 2
  • HY-169350
    EA-B2L

    		Glutathione S-transferase Cancer
    EA-B2L is a potent degrader of glutathione S-transferase (GSTP), with the DC50 of 48 μM. EA-B2L is a kind of Boc2Lys-linked Ethacrynic acid (HY-B1640). EA-B2L plays an important role in cancer research .
    EA-B2L

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