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oral carcinoma

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71

Inhibitors & Agonists

10

Natural
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2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-101246

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
    RPI-1
  • HY-106735

    Ro 13-6298; Arotinoid ethyl ester

    RAR/RXR Inflammation/Immunology Cancer
    Arotinoid (RO 13-6298) is a retinoid, and acts as an orally active and highly potent agonist of retinoic acid receptors (RARs) with antipsoriatic effects. Arotinoid has antipapiltoma activity with an ED50 of 0.05 mg/kg. Arotinoid can be used for the research of skin carcinomas .
    Arotinoid
  • HY-10320G

    BIRB 796 (GMP)

    p38 MAPK Cancer
    Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC50s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor efficacy against oral epidermoid carcinoma and cervical cancer. Doramapimod also exhibits anti-inflammatory activity .
    Doramapimod (GMP)
  • HY-155785

    Apoptosis Autophagy Reactive Oxygen Species JAK Cancer
    MTP is a PKM2 inhibitor. MTP induces cancer cell apoptosis by modulating caspase-3 activation. MTP induces autophagy and increases ROS generation. MTP also inhibits JAK2 signaling. MTP can be used for research of oral squamous cell carcinoma .
    MTP
  • HY-144254

    PI3K Akt Apoptosis Cancer
    PI3Kδ-IN-10 is a highly potent and orally active PI3Kδ inhibitor with IC50 of 2 nM. PI3Kδ-IN-10 robustly suppresses the downstream AKT pathway to induce subsequent apoptosis in hepatocellular carcinoma models .
    PI3Kδ-IN-10
  • HY-N12960

    Apoptosis Bcl-2 Family Caspase COX MMP STAT Cancer
    Artobiloxanthone (Compound AA3) exhibits antitumor activity, particularly against oral squamous cell carcinoma (OSCC). Artobiloxanthone inhibits Akt/mTOR pathway and STAT3 pathway, inhibits proliferation of SAS and T.Tn (with IC50 of 11 and 22 μM), and inhibits the cancer cell migration. Artobiloxanthone arrests cell cycle at S phase, and induces apoptosis in OSCC cells through activation of caspase 3/9 .
    Artobiloxanthone
  • HY-106364

    Bleomycin PEP; Pepleomycin

    Antibiotic Cancer
    Peplomycin (Bleomycin PEP; Pepleomycin) is an antibiotic analogue of Bleomycin (HY-108345), with high antitumor effect and less pulmonary toxicity. Peplomycin induce apoptosis in oral squamous carcinoma cell line SSCKN cells and pulmonary fibrosis in rats .
    Peplomycin
  • HY-111458
    GSK2643943A
    5 Publications Verification

    Deubiquitinase Cancer
    GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
    GSK2643943A
  • HY-101266A

    DS-3032 tosylate

    MDM-2/p53 Cancer
    Milademetan tosylate is the tosylate salt form of Milademetan (HY-101266). Milademetan tosylate is an orally active inhibitor for MDM2. Milademetan tosylate arrests the cell cycle at G1 pahse, induces the apoptosis Milademetan tosylate restores the p53 activity by targeting the p53-MDM2 interaction, and exhibits anticancer activity against Merkel cell carcinoma (MCC) .
    Milademetan tosylate
  • HY-151461

    Others Cancer
    CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy .
    CHNQD-01255
  • HY-N1261

    Others Cancer
    Scutebarbatine B shows significant cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, with IC50 values in the range 3.5-8.1 mM [1]<
    Scutebarbatine B
  • HY-101840A
    EIPA hydrochloride
    40+ Cited Publications

    L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride

    TRP Channel Autophagy COX Prostaglandin Receptor Na+/H+ Exchanger (NHE) Inflammation/Immunology Cancer
    EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma .
    EIPA hydrochloride
  • HY-101840
    EIPA
    40+ Cited Publications

    L593754; MH 12-43; Ethylisopropylamiloride

    TRP Channel Prostaglandin Receptor Autophagy COX Na+/H+ Exchanger (NHE) Inflammation/Immunology Cancer
    EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma .
    EIPA
  • HY-14653

    TAC-101; Am 555S

    RAR/RXR Apoptosis Cancer
    Amsilarotene (TAC-101; Am 555S), an orally active synthetic retinoid, has selective affinity for retinoic acid receptor α (RAR-α) binding with Ki of 2.4, 400 nM for RAR-α and RAR-β. Amsilarotene induces the apoptotic of human gastric cancer, hepatocellular carcinoma and ovarian carcinoma cells. Amsilarotene can be used for the research of cancer .
    Amsilarotene
  • HY-N8380

    Apoptosis Autophagy PI3K Necroptosis Cardiovascular Disease Inflammation/Immunology Cancer
    (-)-Latifolin, a flavonoid, induces apoptotic cell death by targeting PI3K/AKT/mTOR/p70S6K signaling. (-)-Latifolin significantly inhibits the cell proliferation of oral squamous cell carcinoma (OSCC), and causes the anti-metastatic activities by effectively blocking cell migration, invasion, and adhesion via the inactivation of FAK/Src. (-)-Latifolin suppresses autophagic-related proteins and autophagosome formation. (-)-Latifolin inhibits necroptosis by dephosphorylating necroptosis-regulatory proteins (RIP1, RIP3, and MLKL). (-)-Latifolin has beneficial effects on anti-aging, anti-carcinogenic, anti-inflammatory, and cardio-protective activities .
    (-)-Latifolin
  • HY-108527

    RAR/RXR Cancer
    CD1530 is a selective RARγ agonist with an Kd of 150 nM . CD1530 has been used in combination with bexarotene to inhibit oral carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide in a mouse model of human oral-cavity and esophageal squamous-cell carcinoma .
    CD1530
  • HY-N12760

    Others Cancer
    Lobophorin CR-2 is a lobophorin congener which induces UPR-associated gene expression, inhibits oral squamous cell carcinoma cell growth, and causes UPR-dependent cell death in MEF cells .
    Lobophorin CR-2
  • HY-119272

    ERK Caspase Cancer
    EF24 is a curcumin analogue with greater anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 treatment increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK .
    EF24
  • HY-N0746
    Oxysophocarpine
    4 Publications Verification

    Others Cancer
    Oxysophocarpine is an alkaloid extracted from Sophora alopecuroides. Oxysophocarpine has neuroprotective and anti-nociceptive effects on the central and peripheral nervous systems . Oxysophocarpine inhibits the growth and metastasis of  oral squamous cell carcinoma (OSCC) .
    Oxysophocarpine
  • HY-153967
    BLU0588
    1 Publications Verification

    PKA Cancer
    BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .
    BLU0588
  • HY-13593
    Chlorambucil
    4 Publications Verification

    CB-1348; WR-139013

    DNA Alkylator/Crosslinker Cancer
    Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease .
    Chlorambucil
  • HY-103706

    Autophagy Apoptosis Cancer
    ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis .
    ROC-325
  • HY-N0530

    Dryocrassin

    Apoptosis Influenza Virus Cancer
    Dryocrassin ABBA (Dryocrassin) is an orally active phloroglucinol derivative that can be extracted from Phyllopteris officinalis. Dryocrassin ABBA has antitumor and antiviral activity. Dryocrassin ABBA induced apoptosis of human hepatocellular carcinoma cells through mitochondrial pathway mediated by Caspase .
    Dryocrassin ABBA
  • HY-100492
    Fisogatinib
    1 Publications Verification

    BLU-554

    FGFR Cancer
    Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling .
    Fisogatinib
  • HY-114338

    SHR-6390

    CDK Cancer
    Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
    Dalpiciclib
  • HY-114338A

    SHR-6390 hydrochloride

    CDK Cancer
    Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
    Dalpiciclib hydrochloride
  • HY-163569

    FGFR Cancer
    FGFR4-IN-20 (comp 11) is an orally active and selective FGFR4 inhibitor with IC50s of 19 and 36 nM against Huh7 cells and FGFR4 enzyme. FGFR4-IN-20 can be used for hepatocellular carcinoma research .
    FGFR4-IN-20
  • HY-N3665

    Tyrosinase Cancer
    Cyclocommunol is a prenylflavonoid with antityrosinase and antiplatelet activitie, can be solated from breadfruit. Cyclocommunol exerts anti-tumor activity and inhibits the growth of human hepatoma and gastric cancer cells with IC50 values between 16 and 80 µM. Cyclocommunol shows proapoptotic effect on oral squamous cell carcinoma (OSCC) .
    Cyclocommunol
  • HY-W010593

    Others Cancer
    Ethylenethiourea is a degradation product of the ethylenebisthiocarbamate group of fungicides. Ethylenethiourea is tumorigenic and teratogenic. Ethylenethiourea is orally active .
    Ethylenethiourea
  • HY-125840
    Belzutifan
    3 Publications Verification

    PT2977; MK-6482

    HIF/HIF Prolyl-Hydroxylase Cancer
    Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
    Belzutifan
  • HY-13593S

    CB-1348-d8; WR-139013-d8

    Isotope-Labeled Compounds DNA Alkylator/Crosslinker Cancer
    Chlorambucil-d8 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].
    Chlorambucil-d8
  • HY-13593S1

    CB-1348-d8-1; WR-139013-d8-1

    Isotope-Labeled Compounds DNA Alkylator/Crosslinker Cancer
    Chlorambucil-d8-1 is the deuterium labeled Chlorambucil. Chlorambucil (CB-1348), an orally active antineoplastic agent, is a bifunctional alkylating agent belonging to the nitrogen mustard group. Chlorambucil can be used for the research of lymphocytic leukemia, ovarian and breast carcinomas, and Hodgkin’s disease[1][2][3][4].
    Chlorambucil-d8-1
  • HY-145835

    PERK Cancer
    PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
    PERK-IN-5
  • HY-144614

    DYRK Apoptosis Neurological Disease Cancer
    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
    JH-XVII-10
  • HY-119198

    Apoptosis Histone Methyltransferase Cancer
    NSC745885 an effective anti-tumor agent, shows selective toxicity against multiple cancer cell lines but not normal cells. NSC745885 is an effective down-regulator of EZH2 via proteasome-mediated degradation. NSC745885 provides possibilities for the study of advanced bladder and oral squamous cell carcinoma (OSCC) cancers .
    NSC745885
  • HY-111226
    GSK5182
    2 Publications Verification

    Estrogen Receptor/ERR Reactive Oxygen Species Cardiovascular Disease Cancer
    GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC) .
    GSK5182
  • HY-150072

    PKA Cancer
    DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC) .
    DS89002333
  • HY-158762

    SHP2 Cancer
    TK-642 is a highly active, selective, orally activity SHP2 inhibitor based on pyrazole and pyrazine (IC50=2.7 nmol/L). TK-642 can effectively inhibit the proliferation of esophageal carcinoma cells and induce cell apoptosis. TK-642 can be used in the study of esophageal cancer .
    TK-642
  • HY-16706
    Remodelin
    5+ Cited Publications

    Histone Acetyltransferase Cancer
    Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
    Remodelin
  • HY-W008634

    Toll-like Receptor (TLR) Cancer
    Bropirimine is a synthetic agonist for toll-like receptor 7 (TLR7). Bropirimine inhibits differentiation of osteoclast precursor cells into osteoclasts via TLR7-mediated production of IFN-β. Bropirimine is an orally active immunomodulator that has demonstrated anticancer activity in transitional cell carcinoma in situ (CIS) in both the bladder and upper urinary tract .
    Bropirimine
  • HY-50767
    Palbociclib
    Maximum Cited Publications
    140 Publications Verification

    PD 0332991

    CDK Cancer
    Palbociclib (PD 0332991) is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
    Palbociclib
  • HY-111226A

    Estrogen Receptor/ERR Reactive Oxygen Species Cardiovascular Disease Cancer
    (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM . GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma .
    (E/Z)-GSK5182
  • HY-50767B

    PD-0332991 dihydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) dihydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib dihydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
    Palbociclib dihydrochloride
  • HY-50767C
    Palbociclib hydrochloride
    120+ Cited Publications

    PD-0332991 hydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) hydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib hydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib hydrochloride can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
    Palbociclib hydrochloride
  • HY-50767A
    Palbociclib monohydrochloride
    Maximum Cited Publications
    140 Publications Verification

    PD 0332991 monohydrochloride

    CDK Cancer
    Palbociclib (PD 0332991) monohydrochloride is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib monohydrochloride has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
    Palbociclib monohydrochloride
  • HY-A0065
    Palbociclib isethionate
    Maximum Cited Publications
    140 Publications Verification

    PD 0332991 isethionate

    CDK Cancer
    Palbociclib (PD 0332991) isethionate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib isethionate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells, which can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
    Palbociclib isethionate
  • HY-16706A
    Remodelin hydrobromide
    5+ Cited Publications

    Histone Acetyltransferase Cancer
    Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
    Remodelin hydrobromide
  • HY-50767D

    PD 0332991 orotate

    CDK Cancer
    Palbociclib (PD 0332991) orotate is an orally active selective CDK4 and CDK6 inhibitor with IC50 values of 11 and 16 nM, respectively. Palbociclib orotate has potent anti-proliferative activity and induces cell cycle arrest in cancer cells. Palbociclib orotate can be used in the research of HR-positive and HER2-negative breast cancer and hepatocellular carcinoma .
    Palbociclib orotate
  • HY-103018
    Gusacitinib
    1 Publications Verification

    ASN-002

    JAK Syk Inflammation/Immunology Cancer
    Gusacitinib (ASN-002) is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
    Gusacitinib
  • HY-103018A

    ASN-002 hydrochloride

    JAK Syk Inflammation/Immunology Cancer
    Gusacitinib (ASN-002) hydrochloride is an orally active dual SYK/JAK kinase inhibitor with IC50 values of 5, 46, 4, 11 and 8 nM for SYK, JAK1, JAK2, JAK3 and TYK2, respectively. Gusacitinib hydrochloride rapidly and significantly suppressed key inflammatory pathways implicated in atopic dermatitis pathogenesis. Gusacitinib hydrochloride can be used in the research of chronic hand eczema and cancers such as basal cell carcinoma .
    Gusacitinib hydrochloride

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