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Results for "

human oral tumor

" in MedChemExpress (MCE) Product Catalog:

142

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2

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21

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1

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4

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2

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10254
    Mirdametinib
    Maximum Cited Publications
    154 Publications Verification

    PD0325901; PD325901

    		 MEK Autophagy Apoptosis Cancer
    Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Ki app of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts .
    Mirdametinib
  • HY-136927
    MSA-2
    25+ Cited Publications

    		 STING Inflammation/Immunology Cancer
    MSA-2, a potent and orally available non-nucleotide STING agonist, is bound to STING as a noncovalent dimer with nanomolar affinity. MSA-2 shows EC50s of 8.3 and 24 μM for human STING isoforms WT and HAQ, respectively. MSA-2 stimulates interferon-β secretion in tumors, induces tumor regression with durable antitumor immunity, and synergizes with anti-PD-1 in syngeneic mouse tumor models .
    MSA-2
  • HY-153811
    IAG933
    3 Publications Verification

    YAP-TEAD-IN-3

    		 YAP Apoptosis Cancer
    IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD 4217-434, with an IC50 value of 9 nM .
    IAG933
  • HY-145923
    Osunprotafib
    5 Publications Verification

    ABBV-CLS-484

    		 Phosphatase STAT JAK Cancer
    Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction .
    Osunprotafib
  • HY-156633
    Rezatapopt
    3 Publications Verification

    PC14586

    		 MDM-2/p53 Cancer
    Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
    Rezatapopt
  • HY-148669
    Bleximenib
    1 Publications Verification

    JNJ-75276617; Menin-MLL inhibitor 24

    		 Apoptosis Histone Methyltransferase FLT3 Cancer
    Bleximenib (JNJ-75276617) is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib can be used in the research of tumors such as leukemia .
    Bleximenib
  • HY-N0034
    Arctiin
    5 Publications Verification

    Arctii; NSC 315527; Arctigenin-4-glucoside

    		 NF-κB Inflammation/Immunology Cancer
    Arctiin is an orally active inhibitor of NF-κB. Arctiin suppresses cyclin D1 protein expression in human tumor cells. Arctiin also reduces malondialdehyde and pro-in ammatory cytokines levels. Arctiin can used in study glomerulonephritis .
    Arctiin
  • HY-148669A
    Bleximenib oxalate
    1 Publications Verification

    JNJ-75276617 oxalate; Menin-MLL inhibitor 24 oxalate

    		 Apoptosis Histone Methyltransferase FLT3 Cancer
    Bleximenib (JNJ-75276617) oxalate is an orally active and selective menin-KMT2A inhibitor, with IC50 values of 0.1 nM, 0.045 nM, and ≤0.066 nM for humans, mice, and dogs, respectively. Bleximenib oxalate can inhibit the proliferation and induce apoptosis and differentiation of tumor cells. Bleximenib oxalate can be used in the research of tumors such as leukemia .
    Bleximenib oxalate
  • HY-148807
    Zavondemstat

    QC8222 free base; TACH 101 free base

    		 Histone Demethylase Apoptosis Cancer
    Zavondemstat (QC8222 free base; TACH 101 free base) is an orally active pan-KDM4 inhibitor, with a IC50 ≤ 0.08 μM against human KDM4A-D and a Kᵢ of 0.52 μM against human KDM4C. Zavondemstat induces cell apoptosis, causes S-phase cell cycle arrest, reduces the population of tumor-initiating cells and inhibits cancer cell proliferation. Zavondemstat suppresses tumor growth and induces tumor regression in mouse xenograft models. Zavondemstat can be used for the research of various cancers including colorectal cancer, esophageal squamous cell carcinoma and triple-negative breast cancer .
    Zavondemstat
  • HY-14949
    Cevipabulin
    2 Publications Verification

    TTI-237

    		 Microtubule/Tubulin Cancer
    Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [ 3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line .
    Cevipabulin
  • HY-119272
    EF24
    2 Publications Verification

    		 ERK Caspase NF-κB Apoptosis p38 MAPK Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
    EF24
  • HY-14153
    Tegaserod
    4 Publications Verification

    		 5-HT Receptor Apoptosis Metabolic Disease Cancer
    Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
    Tegaserod
  • HY-14153A
    Tegaserod maleate
    4 Publications Verification

    SDZ-HTF-919; HTF-919

    		 5-HT Receptor Apoptosis Neurological Disease Metabolic Disease Cancer
    Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research .
    Tegaserod maleate
  • HY-152293
    EVT801

    		VEGFR ERK Cancer
    EVT801 is an orally active and selective inhibitor of VEGFR-3 (IC50=11 nM), which has antitumor effects. EVT801 inhibits not only VEGF-C-induced human endothelial cell proliferation, but also tumor (lymphatic) angiogenesis in tumor mouse models. EVT801 can reduce tumor hypoxia, immunosuppressive cytokines (CCL4, CCL5) and myeloid derived suppressor cells (MDSC) production. EVT801 has synergistic effect with immune checkpoint therapy (ICT), which improves ICT response rate and has better inhibitory effect on cancer mouse models . EVT801 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    EVT801
  • HY-13241A
    Ralimetinib
    10+ Cited Publications

    LY2228820

    		 p38 MAPK Autophagy Cancer
    Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
    Ralimetinib
  • HY-15790
    Elobixibat
    1 Publications Verification

    A 3309; AZD 7806

    		 Apical Sodium-Dependent Bile Acid Transporter Metabolic Disease Inflammation/Immunology Cancer
    Elobixibat (A 3309; AZD 7806) is an orally active, bile acid transporter (IBAT) inhibitor with IC50 values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to study metabolic syndrome. Elobixibat can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly .
    Elobixibat
  • HY-13208
    Xevinapant hydrochloride
    10+ Cited Publications

    AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride

    		 IAP Apoptosis Cancer
    Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors .
    Xevinapant hydrochloride
  • HY-W015635
    Diallyl disulfide
    1 Publications Verification

    		 Environmental Pollutants Cancer
    Diallyl disulfide, an active compound in garlic oil, is an orally active human squalene monooxygenase inhibitor with an IC50 of 400 μM for squalene epoxidation. Diallyl disulfide exhibits obvious anti-inflammatory, anti-oxidative, antidepressant and anti-tumor activities .
    Diallyl disulfide
  • HY-142118
    Trabedersen
    1 Publications Verification

    AP 12009

    		 TGF-beta/Smad Cancer
    Trabedersen (AP 12009) is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
    Trabedersen
  • HY-116073
    L-Penicillamine

    		Acyltransferase Infection Cancer
    L-Penicillamine is an orally active serine palmitoyltransferase (SPT) inhibitor. L-Penicillamine inactivates the PLP cofactor by forming adducts, thereby inhibiting SPT activity and reducing sphingolipid biosynthesis. L-Penicillamine not only blocks tumor access to vitamin B6, but also stabilizes the human papillomavirus 16 E6 oncoprotein monomer and inhibits its polymerization, exhibiting a unique anticancer mechanism. L-Penicillamine effectively delays the growth of Sarcoma-180, induces tumor necrosis and prolongs survival (though long-term use may lead to Pyridoxine (HY-B1328) deficiency and weight loss) .
    L-Penicillamine
  • HY-123981
    5MPN
    3 Publications Verification

    		 Phosphatase Cancer
    5MPN is a first-in-class, potent, orally active and selective 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4 (PFKFB4) inhibitor. 5MPN appears to be a competitive inhibitor of the F6P binding site (Ki=8.6 μM). 5MPN does not inhibit PFK-1 or PFKFB3. 5MPN targets the sugar metabolism of tumors and suppresses proliferation of multiple human cancer cell lines .
    5MPN
  • HY-137438
    Edralbrutinib

    TG-1701

    		 Btk Cancer
    Edralbrutinib (TG-1701) is a highly selective, orally available irreversible BTK inhibitor, with an EC50 of 6.70 nM and a Kd of 3 nM against human BTK. Edralbrutinib inhibits downstream signaling of the B cell receptor, induces dephosphorylation of Ikaros Ser442/445, promotes nuclear exclusion of Ikaros, attenuates Ikaros gene signatures, and exerts anti-tumor activity. Edralbrutinib can be used in research related to B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, and diffuse large B-cell lymphoma .
    Edralbrutinib
  • HY-124179
    IT-901
    1 Publications Verification

    		 NF-κB Cancer
    IT-901 is an orally active and potent NF-κB subunit c-Rel inhibitor with an IC50 of 0.1 μM, 3 μM for NF-κB DNA binding and c-Rel DNA binding, respectively. IT-901, a bioactive naphthalenethiobarbiturate derivative, has the potential for human lymphoid tumors and ameliorate graft-versus-host disease (GVHD) .
    IT-901
  • HY-107801
    Inosine pranobex
    1 Publications Verification

    Imunovir; Delimmun; Groprinosin

    		 Interleukin Related HSV HIV HPV Infection Inflammation/Immunology
    Inosine pranobex is an orally active immunomodulator. Inosine pranobex has broad-spectrum antiviral activity. Inosine pranobex inhibits human immunodeficiency virus (HIV), herpes simplex virus (HSV), vaccinia virus (VACV), human tumor virus (HPV), Cytomegalovirus, influenza virus (INFV), parainfluenza virus (PIV), and Epstein-Barr virus .
    Inosine pranobex
  • HY-156649
    Vorbipiprant

    CR6086

    		 Prostaglandin Receptor Interleukin Related MMP PD-1/PD-L1 Cardiovascular Disease Inflammation/Immunology Cancer
    Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (Ki: 16.6 nM). Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer .
    Vorbipiprant
  • HY-144987
    RBN013209
    1 Publications Verification

    		 CD38 LAG-3 Tim3 PD-1/PD-L1 Inflammation/Immunology Cancer
    RBN013209 is an orally active small molecule inhibitor of CD38 with an IC50 of 0.01 to 0.1 μM for human CD38. RBN013209 prevents the conversion of extracellular NAD + to ADPR or cADPR in tumor cells and PBMCs. RBN013209 can be used in the study of tumor. In addition, RBN013209 enables CAR-T cells to maintain the naive state and central memory state, and decreases the expression of cell activation markers and exhaustion-related inhibitory receptors .
    RBN013209
  • HY-136780
    SEN177

    		Amyloid-β Apoptosis CD47 Huntingtin Neurological Disease Cancer
    SEN177 is an orally effect glutamine cyclase (QC) inhibitor. The Ki of SEN177 for human glutamine cyclase (hQC) is 20 nM, and the IC50 is 13 nM. SEN177 interferes with the interaction between CD47 and SIRRPα, and has anti-tumor activity. SEN177 reduces aggregation and apoptosis caused by HTT mutation in Huntington model, and can be used in the study of neurodegenerative diseases .
    SEN177
  • HY-N2123
    Neoliquiritin
    1 Publications Verification

    		 Caspase Neurological Disease Cancer
    Neoliquiritin is a flavonoid and flavanone-derived cytotoxic agent with anticancer activity and neuroprotective effects. Neoliquiritin exhibits excellent tumor specificity, exerting a more pronounced killing effect on cancer cells compared with normal oral cells. Neoliquiritin also exerts neuroprotective effects by inhibiting ATP depletion and the elevation of caspase 3/7 activity. Widely present in the roots of Glycyrrhiza uralensis, Glycyrrhiza inflata and Glycyrrhiza glabra, Neoliquiritin can be applied to studies on human oral squamous cell carcinoma, leukemia, Parkinson's disease and other conditions .
    Neoliquiritin
  • HY-15790A
    Elobixibat hydrate
    1 Publications Verification

    A 3309 hydrate; AZD 7806 hydrate

    		 Apical Sodium-Dependent Bile Acid Transporter Metabolic Disease Cancer
    Elobixibat (A 3309; AZD 7806) hydrate is an orally active, bile acid transporter (IBAT) inhibitor with IC50 values ??of 0.53 nM (human IBAT), 0.13 nM (mouse IBAT), and 5.8 nM (canine IBAT). Elobixibat hydrate can lower LDL cholesterol, increase serum GLP-1, promote colonic motility, and has the potential to study metabolic syndrome. Elobixibat hydrate can be used in the study of chronic functional constipation (CIC), dyslipidemia, non-alcoholic hepatitis, and liver tumors in the elderly .
    Elobixibat hydrate
  • HY-15163
    Zotiraciclib
    2 Publications Verification

    TG02; SB1317

    		 JAK CDK FLT3 Cancer
    Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
    Zotiraciclib
  • HY-153793
    Alcudacigib

    DGKζ-IN-1

    		 DGK IFNAR Interleukin Related ERK Cancer
    Alcudacigib (ASP1570; DGKζ-IN-1) is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against human DGKζ and an IC50 of 3.0 nM against mouse DGKζ. Alcudacigib selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib enhances the anti-tumor functions of T cells and NK cells. Alcudacigib can be used for the research of advanced/metastatic solid tumors .
    Alcudacigib
  • HY-N0475
    Triptophenolide

    Hypolide; (+)-Triptophenolide

    		 Androgen Receptor Pyroptosis Caspase Bcl-2 Family Apoptosis Inflammation/Immunology Cancer
    Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
    Triptophenolide
  • HY-111254
    GQ-16

    		PPAR NF-κB JNK Inflammation/Immunology
    GQ-16 is an orally active PPARγ partial agonist with an IC50 of 1.84 μM and a Ki of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer .
    GQ-16
  • HY-157231A
    HC-5404-Fu

    		PERK Cancer
    HC-5404-Fu is an orally active PERK inhibitor with an IC50 of 0.001 μM against human PERK. HC-5404-Fu blocks PERK activation induced by VEGFR-TKI and disrupts the adaptive stress response triggered by VEGFR-TKI. HC-5404-Fu enhances anti-angiogenic effects by inhibiting newly formed and mature tumor blood vessels in renal cell carcinoma models. HC-5404-Fu can be used in research related to renal cell carcinoma .
    HC-5404-Fu
  • HY-12182A
    ONO-8711 dicyclohexylamine

    		Prostaglandin Receptor Cancer
    ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer .
    ONO-8711 dicyclohexylamine
  • HY-145734
    AMXI-5001

    		Microtubule/Tubulin Cancer
    AMXI-5001 is a potent, orally active, and dual parp1/2 and microtubule polymerization inhibitor. MXI-5001 exhibits selective antitumor cytotoxicity across a wide variety of human cancer cells with much lower IC50s than existing clinical PARP1/2 inhibitors. AMXI-5001 induces complete regression of established tumors, including exceedingly large tumors .
    AMXI-5001
  • HY-168022
    CAM2602
    1 Publications Verification

    		 Aurora Kinase Cancer
    CAM2602 is an orally active Aurora A-TPX2 protein−protein interaction inhibitor with a human Kd of 19 nM for Aurora A. CAM2602 increases the proportion of PH3 positive cells while reducing P-T288 Aurora A levels. CAM2602 arrests tumor xenograft growth in mice. CAM2602 can be used for the research of cancer, such as acute T cell leukemia .
    CAM2602
  • HY-P2302
    Defensin HNP-3 human

    		Antibiotic Bacterial Fungal Infection Inflammation/Immunology Cancer
    Defensin HNP-3 human is an α-defensin stored in the azurophilic granules of human neutrophils. Defensin HNP-3 human exerts broad-spectrum bactericidal, antifungal and antiviral activities mainly by forming bacterial membrane pores, and acts as a chemoattractant for monocytes and T cells. Defensin HNP-3 human maintains epithelial integrity to support periodontal tissue homeostasis, and exerts concentration-dependent effects on epithelial cell proliferation, adhesion and bacterial adhesion. Defensin HNP-3 human targets solid tumors and leukemia by inducing single-strand DNA breaks and membrane permeabilization in tumor cells via electrostatic binding and pore formation. Defensin HNP-3 human is abundant in human tongue squamous cell carcinoma and neutrophils infiltrating oral squamous cell carcinoma. Defensin HNP-3 human can be applied to research related to periodontitis and human tongue squamous cell carcinoma .
    Defensin HNP-3 human
  • HY-14949C
    Cevipabulin fumarate
    2 Publications Verification

    TTI-237 fumarate

    		 Microtubule/Tubulin Cancer
    Cevipabulin fumarate (TTI-237 fumarate) is an oral, microtubule-active, antitumor compound and inhibits the binding of [ 3H]NSC 49842 to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line .
    Cevipabulin fumarate
  • HY-16196
    ENMD-1198

    IRC-110160

    		 Microtubule/Tubulin HIF/HIF Prolyl-Hydroxylase STAT Cancer
    ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
    ENMD-1198
  • HY-122168
    AAT-008

    		Prostaglandin Receptor Inflammation/Immunology Cancer
    AAT-008 is a potent, selective, and orally active prostaglandin EP4 receptor antagonist with Kis of 0.97 and 6.1 nM for recombinant human EP4 and recombinant rat EP4, respectively. AAT-008 exerts tumor growth delay in mice bearing CT26WT colon tumors when combined with radiotherapy. AAT-008 can be used for the study of acute and chronic inflammatory pain and cancer .
    AAT-008
  • HY-149208
    HDAC-IN-53

    		HDAC Apoptosis Cancer
    HDAC-IN-53 is an orally active, and selective HDAC1-3 inhibitor with IC50 values of 47 nM, 125 nM, and 450 nM, respectively. HDAC-IN-53 does not inhibit class II HDACs (HDAC4, 5, 6, 7, 9; IC50>10 μM). HDAC-IN-53 induces caspase-dependent apoptosis. HDAC-IN-53 significantly inhibits the growth of human tumor xenografts in nude mice and murine tumor growth in immune-competent mice bearing MC38 colon cancer .
    HDAC-IN-53
  • HY-153793A
    Alcudacigib TFA

    DGKζ-IN-1 TFA

    		 DGK IFNAR Interleukin Related ERK Cancer
    Alcudacigib (ASP1570; DGKζ-IN-1) TFA is an orally active diacylglycerol kinase ζ (DGKζ) inhibitor, with an IC50 of 4.7 nM against human DGKζ and an IC50 of 3.0 nM against mouse DGKζ. Alcudacigib TFA selectively inhibits the kinase activity of DGKζ and induces proteasome-dependent degradation of DGKζ protein. Alcudacigib TFA enhances the anti-tumor functions of T cells and NK cells. Alcudacigib TFA can be used for the research of advanced/metastatic solid tumors .
    Alcudacigib TFA
  • HY-165245
    SBI-183

    		Transmembrane Glycoprotein Cancer
    SBI-183 is an orally active inhibitor of QSOX1 (Kd: 20 μM). SBI-183 suppresses the proliferative and invasive phenotype of renal cancer cell lines, including triple negative breast cancer cell line, lung adenocarcinoma cell line and pancreatic ductal adenocarcinoma. SBI-183 inhibits tumor growth in two human xenograft mouse models of renal cell carcinoma in vivo .
    SBI-183
  • HY-142118A
    Trabedersen sodium
    1 Publications Verification

    AP 12009 sodium

    		 TGF-beta/Smad Cancer
    Trabedersen (AP 12009) sodium is an orally active synthetic antisense phosphorothioate oligodeoxynucleotide that selectively targets human TGFβ2 mRNA. Trabedersen sodium blocks TGFβ2 protein production, enters the nucleus without a transfection vector, and exerts dose-dependent antitumor effects. By reversing TGFβ2-induced immunosuppression and enhancing immune cytotoxicity, Trabedersen sodium exhibits significant antiproliferative, antimigratory, and antimetastatic activities, with favorable safety profiles. Trabedersen sodium is widely used in research related to various solid tumors, including anaplastic astrocytoma, glioblastoma, colorectal tumor, and melanoma .
    Trabedersen sodium
  • HY-12564
    Phthalazinone pyrazole

    		Aurora Kinase Apoptosis Mitosis Cancer
    Phthalazinone pyrazole is a potent, selective, and orally active inhibitor of Aurora-A kinase with an IC50 of 0.031 μM. Phthalazinone pyrazole can arrests mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells. Phthalazinone pyrazole suppresses the epithelial-mesenchymal transition (EMT) during the differentiation of hepatocyte-like cells (HLCs) from human embryonic stem cells .
    Phthalazinone pyrazole
  • HY-123045
    PNU-292137

    		CDK Cancer
    PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
    PNU-292137
  • HY-103441
    JNJ28871063 hydrochloride

    		EGFR Cancer
    JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2 .
    JNJ28871063 hydrochloride
  • HY-161916
    Polθ-IN-4

    		DNA/RNA Synthesis Cancer
    Polθ-IN-4 is an orally active prodrug of a DNA polymerase θ (Polθ) inhibitor with Kms of 3.7, 3.7 and 5.2 μM in human, mouse and rat recombinant alkaline phosphatases. Polθ-IN-4 that inhibits Polθ activity by targeting its ATP-dependent helicase domain. Polθ-IN-4 demonstrates significant anti-tumor activity in multiple animal experiments. Polθ-IN-4 can be used for the studies of breast cancer and ovarian cancer .
    Polθ-IN-4
  • HY-13742
    Ropidoxuridine

    IPdR

    		 HSV Cancer
    Ropidoxuridine (IPdR) is a novel orally available, halogenated thymidine analog and is a potential radiosensitizer for use in human tumors.
    Ropidoxuridine

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