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MDA-MB-468、NCI-H1975、HT1080

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N9596

    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

    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

    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

    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

    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

    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

    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

    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-176772

    Others Cancer
    QHL-1618 is a tumor microenvironment-activated drug conjugate. QHL-1618 inhibits the tumor growth in various tumor models, such as HT-1080 xenograft, CT-26 xenograft .
    QHL-1618
  • HY-101447

    EPH 116

    Src Apoptosis Cancer
    SI-2 (EPH 116) is an inhibitor for steroid receptor coactivator-3 (SRC-3), which reduces the transcriptional activity and protein concentration of SRC-3 in cells, exhibits cytotoxicity in cancer cell, inhibits migration of MDA-MB-468, induces apoptosis of MDA-MB-468. SI-2 inhibits the tumor growth in mouse models, without significant toxicity for heart and other major organs (20 mg/kg) .
    SI-2
  • HY-121085

    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-149236

    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 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-164384

    PI3K Akt mTOR Apoptosis Cancer
    DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
    DFX117
  • HY-153698

    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

    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-11038B
    Zelavespib hydrochloride
    5+ Cited Publications

    PU-H71 hydrochloride

    HSP Cancer
    Zelavespib (PU-H71) hydrochloride is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
    Zelavespib hydrochloride
  • HY-11038
    Zelavespib
    5+ Cited Publications

    PU-H71

    HSP Cancer
    Zelavespib (PU-H71) is a potent Hsp90 inhibitor, with an IC50 of 51 nM in MDA-MB-468 cells.
    Zelavespib
  • HY-158170

    CDK Cancer
    CDK7-IN-28 (CDK7-1276) is a potent CDK7 inhibitor(IC50<5 nM). CDK7-IN-28 can inhibit proliferation of MDA-MB-468 cell line by blocking cell cycle and inhibiting DNA replication .
    CDK7-IN-28
  • HY-155787

    CDK Cancer
    SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM) .
    SHR5428
  • HY-173002

    DNA Methyltransferase Cancer
    MS9024 is the degrader for DNA methyltransferase 1 that degrades DNMT1 in cell HCT116 through the ubiquitin-proteasome pathway with a DC50 of 35 nM (DC50 in MDA-MB-468 and H1299 is 254 nM and 101 nM). MS9024 also inhibits DNMT1 with an IC50 of 0.43 μM .
    MS9024
  • HY-100579
    Ferrostatin-1
    Maximum Cited Publications
    1232 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-N8187

    Apoptosis Cancer
    Eupalinolide O is a sesquiterpene lactone with anticancer activities. Eupalinolide O induces cell apoptosis in human MDA-MB-468 breast cancer cells .
    Eupalinolide O
  • HY-172957

    JAK Cancer
    JNN-5 is a potent and selective JAK2 inhibitor with an IC50 of 0.41 nM. JNN-5 shows strong antiproliferative activities in the TNBC cell lines (MDA-MB-468, MDA-MB-213, HCC70, MDA-MB-157) .
    JNN-5
  • HY-159990

    Glutathione Peroxidase Cancer
    GPX4-IN-15 (Compound C1) is an inhibitor for GPX4, that inhibits 19.8% GPX4 at 1 μM. GPX4-IN-15 inhibits the proliferation of cancer cell MDA-MB-468, BT-549 and MDA-MB-231 with IC50 of 0.86, 0.96 and 0.48 μM .
    GPX4-IN-15
  • HY-N15614

    Others Cancer
    Cassamine is a diterpenoid compound that can be isolated from the bark of Erythrophleum fordii. Cassamine exhibits certain cytotoxicity against non-small cell lung cancer cell lines, with IC50 values of 3.4, 2.1, and 1.9 μM against A549, NCI-H1975, and NCI-H1299, respectively. Cassamine has antitumor activity and can be used in the research of lung cancer and other tumors .
    Cassamine
  • HY-173029

    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

    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-146132

    EGFR Cancer
    EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
    EGFR-IN-55
  • HY-11038D
    Zelavespib formic
    5+ Cited Publications

    PU-H71 formic

    HSP Cancer
    Zelavespib formic (PU-H71 formic) is a potent Hsp90 inhibitor with an IC50 value of 51 nM for Hsp90 in MDA-MB-468 cells .
    Zelavespib formic
  • HY-114459

    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-159576

    O-Me B1939; O-Me E7389; O-Me ER-086526

    ADC Payload Cancer
    O-Me Eribulin is a derivative of Eribulin and is an ADC cytotoxin that can be used for ADC synthesis. O-Me Eribulin can inhibit the cell viability of SKBR3, MDA-MB-468, and A549 cells, with IC50 values of 0.2052, 0.1827, and 0.5151 nM, respectively. O-Me Eribulin can be used for tumor research .
    O-Me Eribulin
  • HY-143293

    VEGFR Apoptosis Cancer
    VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. VEGFR-IN-3 inhibits OVCAR-4 and MDA-MB-468 cancer cells growth with IC50s of 0.29 and 0.35 μM, respectively. VEGFR-IN-3 can be used for the research of cancer .
    VEGFR-IN-3
  • HY-111844

    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 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-175023

    Phosphatase Cancer
    OncoACP3 (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 can be used for prostate cancer research .
    OncoACP3
  • HY-175023A

    Phosphatase Cancer
    OncoACP3 TFA (Compound s43) is a high affinity ligand for prostatic acid phosphatase (ACP3). OncoACP3 TFA, radiolabelled with Lu-177, selectively accumulates in enzyme-expressing tumors and shows a potent anti-tumor activity with excellent tumor-selective payload deposition in HT1080.hACP3 and PC3.hACP3 tumor-bearing mice model. OncoACP3 TFA can be used for prostate cancer research .
    OncoACP3 TFA
  • HY-178370

    Ferroptosis Reactive Oxygen Species (ROS) Cancer
    Ferroptosis inducer-12 is a potent and selective ferroptosis inducer. Ferroptosis inducer-12 exhibits potent antiproliferative activity against HT1080 and OS-RC-2, with IC50 values of 3 nM and 5 nM, respectively. Ferroptosis inducer-12 strongly inhibits GPX4 enzymatic activity, induces intracellular ROS and elevates intracellular Fe 2+ levels in OS-RC-2 cells. Ferroptosis inducer-12 significantly inhibits tumor growth in BALB/c nude mice bearing OS-RC-2 xenografts. Ferroptosis inducer-12 can be used for the study of cancer .
    Ferroptosis inducer-12
  • HY-P10760

    Peptide-Drug Conjugates (PDCs) Cancer
    PhAc-ALGP-Dox, a peptide-drug conjugate, is a novel anticancer prodrug, with IC50 values ranged from 311 nM to 34.25 μM for TNBC (E0771), normal murine epithelium (HC-11), human TNBC (MDA-MB-231 and MDA-MB-468), human CrC (LS 174T), normal human epithelium (HME-1) cells .
    PhAc-ALGP-Dox
  • HY-168093

    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

    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

    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-173038

    EGFR ERK STAT Apoptosis Cancer
    EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC50s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975 .
    EGFR-IN-151
  • HY-147858A

    PROTACs Cancer
    PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
    PROTAC EGFR degrader 7 diTFA
  • HY-151630

    Carbonic Anhydrase Cancer
    hCAIX-IN-16 (Compound 12d) is hCA IX inhibitor, with Ki values of 190.0 and 187.9 nM for hCA IX and hCA XII, respectively. hCAIX-IN-16 can arrest the cell cycle of breast cancer MDA-MB-468 in G0-G1 and S phase and induce apoptosis. hCAIX-IN-16 shows good broad-spectrum anticancer activity and can be used for cancer research .
    hCAIX-IN-16
  • HY-168037

    PROTACs PIN1 Cancer
    PROTAC PIN1 degrader-1 (compound D4) is a PROTAC targeting PIN1, with a DC50=1.8 nM. The GI50 of PROTAC PIN1 degrader-1 to MDA-MB-468 is >30 μM. PROTAC PIN1 degrader-1 is composed of target protein ligand PIN1 ligand-1 (HY-168038) (red part), E3 ligase ligand Thalidomide (HY-14658) (blue part), and PROTAC linker (black part) [1] .
    PROTAC PIN1 degrader-1
  • HY-143234

    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-160899A

    Drug-Linker Conjugates for ADC Cancer
    Thailanstatin A cyclohexane diamine formic is an analog of Spliceostatin (HY-16466). Thailanstatin A cyclohexane diamine formic inhibits proliferations of cells N87 (IC50 is 0.33 μM), BT474 (IC50 is 0.34 μM), MDA-MB-361-DYT2 (IC50 is 0.88 μM) and MDA-MB-468 (IC50 is 0.27 μM). Thailanstatin A cyclohexane diamine formic is used as a drug-linker conjugate for ADC molecule .
    Thailanstatin A cyclohexane diamine formic
  • HY-145860

    Phosphoglycerate Dehydrogenase (PHGDH) Cancer
    PHGDH-IN-2 is a potent and NAD + competitive PHGDH inhibitor with an IC50 of 5.2 µM. PHGDH-IN-2 inhibits the serine synthetic pathway in MDA-MB-468 cells. PHGDH-IN-2 inhibits the growth of PHGDH-dependent cancer cells .
    PHGDH-IN-2

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