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HT1080

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102

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100579
    Ferrostatin-1
    Maximum Cited Publications
    1547 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-B1645
    Ammonium iron(III) citrate
    Maximum Cited Publications
    28 Publications Verification

    Ammonium ferric citrate; FAC

    		 Environmental Pollutants 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-13016
    Cabozantinib
    55+ Cited Publications

    XL184; BMS-907351

    		 VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
    Cabozantinib
  • HY-N2117
    Isoginkgetin
    15+ 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-B0581
    Dexrazoxane
    15+ Cited Publications

    ICRF-187; ADR-529; NSC-169780

    		 Ferroptosis Apoptosis Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Dexrazoxane, as an intracellular iron chelating agent, reduces the formation of superoxide radicals and has cardioprotective, anti-inflammatory, antioxidant, anti-tumor and neuroprotective activities. Dexrazoxane inhibits ferroptosis of H9c2 cells by inhibiting HMGB1. Dexrazoxane induces DNA damage and apoptosis in human fibrosarcoma cells .
    Dexrazoxane
  • HY-50908
    Ridaforolimus
    10+ 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-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-B1465
    1-Hexadecanol

    Palmityl alcohol

    		 Environmental Pollutants Endogenous Metabolite Others
    1-Hexadecanol is a fatty alcohol, a lipophilic substrate. 1-Hexadecanol can be used for the research of ferroptosis .
    1-Hexadecanol
  • HY-14299
    Indacaterol
    5 Publications Verification

    		 Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .
    Indacaterol
  • HY-145669
    DIF-3
    5+ Cited Publications

    		 Wnt 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-P991049
    Atrosimab

    ATM-001

    		 TNF Receptor Metabolic Disease Inflammation/Immunology
    Atrosimab is an Fv-Fc1K fusion protein with an EC50 value of 0.37 nM against humans. Atrosimab inhibits TNF-induced TNFR1 activation, release of IL-6 and IL-8, and cell death, and alleviates neuroinflammation. Atrosimab is applicable to research related to inflammatory diseases, neurodegenerative diseases, acute and chronic inflammation, experimental arthritis, non-alcoholic steatohepatitis, and experimental autoimmune encephalomyelitis .
    Atrosimab
  • HY-153698
    CC-3060

    		Molecular Glues Ligands for E3 Ligase Cancer
    CC-3060 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase and ZBTB16 degrader with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 engages structural degrons on ZBTB16’s ZnF1 or ZnF3 domains for fusion protein substrates. CC-3060 can be used for the research of acute promyelocytic leukemia .
    CC-3060
  • HY-14299A
    Indacaterol maleate
    5 Publications Verification

    QAB149

    		 Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research .
    Indacaterol maleate
  • HY-D2869
    Ac-H-FluNox

    		Fluorescent Dye Drug Intermediate Others
    Ac-H-FluNox is an acetylated cell-compatible prodrug of H-FluNox (HY-D2339). Ac-H-FluNox undergoes intracellular hydrolysis of its acetyl group by esterases to generate H-FluNox, which then undergoes a deoxygenation reaction with labile heme to form a fluorescent product. Ac-H-FluNox detects fluctuations of labile heme in living cells, acute labile heme release upon nitric oxide stimulation, and accumulation of labile heme following inhibition of heme export proteins .
    Ac-H-FluNox
  • HY-171658
    R1-ICR-5

    		PROTACs Ser/Thr Kinase TNF Receptor Toll-like Receptor (TLR) NF-κB p38 MAPK Inflammation/Immunology Cancer
    R1-ICR-5 is a highly selective RIPK1 PROTAC degrader. Mediated by VHL, R1-ICR-5 induces the degradation of RIPK1, which in turn dysregulates the TNFR1 and TLR3/4 signaling hubs, enhances the signaling outputs of NF-κB, MAPK and IFN, and simultaneously promotes RIPK3 activation and necroptosis (necroptosis). R1-ICR-5 can be used in the research of triple-negative breast cancer and skin inflammation .
    R1-ICR-5
  • 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-N2497
    Isoliquiritin apioside
    2 Publications Verification

    		 NF-κB MMP p38 MAPK Cancer
    Isoliquiritin apioside significantly decreases PMA-induced increases in MMP9 activities and suppresses PMA-induced activation of MAPK and NF-κB. Isoliquiritin apioside auppresseses invasiveness and angiogenesis of cancer cells and endothelial cells .
    Isoliquiritin apioside
  • HY-123242
    FTI-2153

    		Farnesyl Transferase Cancer
    FTI-2153 is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity .
    FTI-2153
  • HY-14454
    TPh A
    2 Publications Verification

    Triphenyl Compound A

    		 Biochemical Assay Reagents Cancer
    TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells .
    TPh A
  • HY-12475
    Mutant IDH1-IN-1
    2 Publications Verification

    Agios 135

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1 R132H and IDH1 R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research .
    Mutant IDH1-IN-1
  • HY-161929
    GPX4 activator 2

    		Glutathione Peroxidase Ferroptosis Cardiovascular Disease
    GPX4 activator 2 is a GPX4 activator with a Ka value of 0.426 μM for human GPX4. GPX4 activator 2 reduces lipid hydroperoxide levels, prevents lipid peroxide accumulation, and inhibits ferroptosis. GPX4 activator 2 rescues cell death induced by Erastin (HY-15763). GPX4 activator 2 exerts cardioprotective effects in a mouse model of doxorubicin (HY-15142A)-induced myocardial injury .
    GPX4 activator 2
  • 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-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-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-122862
    RAS inhibitor Abd-7
    3 Publications Verification

    		 Ras Cancer
    RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
    RAS inhibitor Abd-7
  • HY-116474
    Viridicatol

    		ERK JNK MMP p38 MAPK STAT Fungal Bacterial NO Synthase PGE synthase NF-κB Wnt β-catenin Infection Metabolic Disease Inflammation/Immunology
    Viridicatol is a quinolone alkaloid with anti-inflammatory, antibacterial, antifungal, osteogenic and chondrogenic activities. Viridicatol reduces the phosphorylation levels of ERK, JNK, p38 and STAT6; inhibits MMP-2, MMP-9, NF-κB signaling pathway and PTP1B; downregulates genes related to mast cell activation; and binds to SHN3 to activate the Wnt/SHN3 signaling pathway. Viridicatol inhibits the expression of pro-inflammatory mediators and cytokines, and promotes osteogenic/chondrogenic differentiation. Viridicatol can be used in studies related to fibrosarcoma, allergy, bacterial infection, fungal infection and osteoporosis .
    Viridicatol
  • 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-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-175649
    LATS1/2-IN-1

    		Large Tumor Suppressor (LATS) YAP Cancer
    LATS1/2-IN-1 is a potent and selective LATS1 and LATS2 inhibitor. LATS1/2-IN-1 exhibits potent inhibitory activity against LATS1 and LATS2 with IC50 values of 4.4 nM and 5.5 nM as determined via r 33P functional assay. LATS1/2-IN-1 displays cellular IC50 values of 136 nM for LATS1 and 36.0 nM for LATS2 as determined via NanoBRET assay. LATS1/2-IN-1 reduces phosphorylation of YAP1 in mouse liver. LATS1/2-IN-1 demonstrates wound healing activity in HT-1080 scratch assay and in vivo SKH1 mouse punch biopsy model. LATS1/2-IN-1 can be used for the study of regenerative medicine indications such as wound healing .
    LATS1/2-IN-1
  • HY-153339
    E235

    		Eukaryotic Initiation Factor (eIF) Cancer
    E235 is an expression regulator of activates transcription factor 4 (ATF4). E235 reduces cell viability by activating integrated stress response (ISR) and DNA damage response signals. E235 has anti-proliferative activity and can be used for tumor research .
    E235
  • HY-176772
    QHL-1618

    		Drug-Linker Conjugates for ADC Topoisomerase 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-176869
    EMC-AANL-DOX

    		Drug Derivative Cancer
    EMC-AANL-DOX is a legumain-activated prodrug conjugate of Doxorubicin (DOX) (HY-15142A). EMC-AANL-DOX shows antitumor activity in mouse models of neuroblastoma (NB), breast cancer (4T1), fibrosarcoma (HT1080), and colorectal cancer liver metastases (CT26). EMC-AANL-DOX can be used for cancer research .
    EMC-AANL-DOX
  • 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-13016R
    Cabozantinib (Standard)

    XL184 (Standard); BMS-907351 (Standard)

    		 Reference Standards VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
    Cabozantinib (Standard)
  • HY-110147B
    SSM3 tetraTFA hydrate

    		Furin Infection
    SSM3 tetraTFA hydrate is a potent synthetic furin inhibitor with an EC50 and a Ki of 54 nM and 12 nM, respectively. SSM3 tetraTFA hydrate is able to block furin-dependent cell surface processing of anthrax protective antigen-83 in vitro .
    SSM3 tetraTFA hydrate
  • HY-14299AR
    Indacaterol maleate (Standard)

    QAB149 (Standard)

    		 Reference Standards Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol (maleate) (Standard) is the analytical standard of Indacaterol (maleate). This product is intended for research and analytical applications. Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research .
    Indacaterol maleate (Standard)
  • HY-N10158
    1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one

    		Drug Derivative 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-125964
    LLP-3

    		Survivin Cancer
    LLP-3 is a potent Survivin inhibitor that disrupts the Survivin-Ran interaction in cancer cells. LLP-3 can be used in the research of Glioblastoma multiforme (GBM) .
    LLP-3
  • HY-14299R
    Indacaterol (Standard)

    		Reference Standards Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Indacaterol (Standard) is the analytical standard of Indacaterol. This product is intended for research and analytical applications. Indacaterol is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol can also be used in cardiovascular disease research .
    Indacaterol (Standard)
  • HY-170027
    LW1564

    		HIF/HIF Prolyl-Hydroxylase AMPK Cancer
    LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
    LW1564
  • 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-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-178370
    Ferroptosis inducer-12

    		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-175041
    GPX4-IN-18

    		Glutathione Peroxidase Reactive Oxygen Species (ROS) Cannabinoid Receptor Ferroptosis Cancer
    GPX4-IN-18 (Compound 17) is a ferrocene-containing inhibitor of glutathione peroxidase 4 (GPX4). GPX4-IN-18 is also an inducer of ferroptosis. GPX4-IN-18 can increase the production of ROS and malondialdehyde (MDA) levels in OS-RC-2 clear cell renal cell carcinoma cells. GPX4-IN-18 induces ferroptosis in HT-1080 cells with IC50s of 0.007 μM (absence of ferrostatin-1) and 1.486 μM (presence of ferrostatin-1). GPX4-IN-18 reduces in vivo tumor volume and intratumoral GPX4 levels in OS-RC-2 xenograft murine model .
    GPX4-IN-18
  • 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-175213
    Mutant IDH1-IN-7

    		Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
    Mutant IDH1-IN-7
  • HY-B1465R
    1-Hexadecanol (Standard)

    Palmityl alcohol (Standard)

    		 Reference Standards Endogenous Metabolite Others
    1-Hexadecanol (Standard) is the analytical standard of 1-Hexadecanol. This product is intended for research and analytical applications. 1-Hexadecanol is a fatty alcohol, a lipophilic substrate. 1-Hexadecanol can be used for the research of ferroptosis .
    1-Hexadecanol (Standard)
  • 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-N10229
    Harzianum A

    		Fungal Infection
    Harzianum A is a trichothecene compound. Harzianum A has no antibacterial activity against Gram-negative and Gram-positive bacteria, but has antifungal activity. In addition, Harzianum A is cytotoxic to tumor cells .
    Harzianum A
  • HY-13016A
    Cabozantinib hydrochloride

    XL184 hydrochloride; BMS-907351 hydrochloride

    		 VEGFR c-Met/HGFR c-Kit TAM Receptor FLT3 Apoptosis Cancer
    Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
    Cabozantinib hydrochloride

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