Search Result
Results for "
oral carcinoma
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-111458
-
|
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) .
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-
-
- 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 .
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-
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- 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 .
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-
-
- 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 .
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-
-
- 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 .
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-
-
- HY-151461
-
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Others
|
Cancer
|
CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy .
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-
-
- 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]<
|
-
-
- HY-101840A
-
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 .
|
-
-
- HY-101840
-
-
-
- HY-14653
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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 .
|
-
-
- 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 .
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-
-
- 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 .
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-
-
- HY-119272
-
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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 .
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-
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- HY-N0746
-
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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) .
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-
-
- HY-153967
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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 .
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-
-
- HY-13593
-
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 .
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-
-
- 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 .
|
-
-
- 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 .
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-
-
- HY-100492
-
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 .
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-
-
- HY-114338
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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 .
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-
-
- HY-114338A
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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 .
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-
-
- HY-101246
-
|
|
|
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 .
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-
-
- 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) .
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-
-
- HY-125840
-
PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
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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) .
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-
-
- HY-W010593
-
|
Others
|
Cancer
|
Ethylenethiourea is a degradation product of the ethylenebisthiocarbamate group of fungicides. Ethylenethiourea is tumorigenic and teratogenic. Ethylenethiourea is orally active .
|
-
-
- 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].
|
-
-
- 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].
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-
-
- 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 .
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-
-
- 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 .
|
-
-
- 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 .
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-
-
- 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) .
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-
-
- 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) .
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-
-
- HY-16706
-
|
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 .
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-
-
- 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 .
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-
-
- HY-50767
-
Palbociclib
Maximum Cited Publications
134 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 .
|
-
-
- 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 .
|
-
-
- 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 .
|
-
-
- HY-50767C
-
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 .
|
-
-
- HY-50767A
-
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 .
|
-
-
- HY-A0065
-
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 .
|
-
-
- HY-16706A
-
|
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 .
|
-
-
- 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 .
|
-
-
- HY-103018
-
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 .
|
-
-
- 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 .
|
-
-
- HY-119906
-
FW-04-806
|
HSP
Apoptosis
|
Cancer
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo .
|
-
-
- HY-17473
-
Embelin
4 Publications Verification
Embelic acid; Emberine; NSC 91874
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells .
|
-
-
- HY-110088
-
|
MDM-2/p53
|
Cancer
|
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
|
-
-
- HY-147203
-
|
5-HT Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease .
|
-
-
- HY-100491
-
|
FGFR
|
Cancer
|
H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity .
|
-
-
- HY-122214
-
AC-73
3 Publications Verification
|
Autophagy
|
Cancer
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells . AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells .
|
-
- HY-10226
-
R306465
|
Apoptosis
HDAC
|
Cancer
|
JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC) inhibitor, with the IC50 of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21 waf1, cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study .
|
-
- HY-10261
-
BIBW 2992
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261A
-
BIBW 2992MA2
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
p38 MAPK
|
Cancer
|
Afatinib (BIBW 2992) dimaleate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10261D
-
BIBW 2992 oxalate
|
EGFR
Autophagy
Apoptosis
c-Met/HGFR
Akt
|
Cancer
|
Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-10977
-
AV-951; KRN951
|
VEGFR
|
Cancer
|
Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy .
|
-
- HY-10977A
-
AV-951 hydrochloride hydrate; KRN951 hydrochloride hydrate
|
VEGFR
|
Cancer
|
Tivozanib hydrochloride hydrate is the hydrate hydrochloride form of Tivozanib (HY-10977). Tivozanib hydrochloride hydrate is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib hydrochloride hydrate exhibits antitumor efficacy .
|
-
- HY-100008
-
NIK333
|
RAR/RXR
SphK
Autophagy
HCV
|
Infection
Cancer
|
Peretinoin is an oral acyclic retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1 . Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression . Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM .
|
-
- HY-151341
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .
|
-
- HY-10261E
-
(R)-BIBW 2992
|
EGFR
c-Met/HGFR
p38 MAPK
|
Cancer
|
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR wt, EGFR L858R, EGFR L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer .
|
-
- HY-N10009
-
|
NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
|
Inflammation/Immunology
|
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
|
-
- HY-151344
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2) .
|
-
- HY-147504
-
|
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity .
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- HY-10626
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LXR
FXR
ROR
Apoptosis
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Cardiovascular Disease
Metabolic Disease
Cancer
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T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα . T0901317 activates FXR with an EC50 of 5 μM . T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively . T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice .
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- HY-16475
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Hedgehog
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Cancer
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TAK-441 is a highly potent and orally active hedgehog (Hh) signaling inhibitor with an IC50value of 4.4 nM. TAK-441 has strong antitumor activity in solid tumors .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0746
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- HY-N0530
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- HY-N1261
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- HY-N8380
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Structural Classification
Dalbergia hupeana Hance
Source classification
Phenols
Polyphenols
Plants
Fabaceae
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Apoptosis
Autophagy
PI3K
Necroptosis
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(-)-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 .
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- HY-N3665
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- HY-119906
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- HY-17473
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- HY-N10009
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Structural Classification
Brosimopsis oblongifolia
Source classification
Phenols
Polyphenols
Plants
Moraceae
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NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
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Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-13593S
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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].
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- HY-13593S1
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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].
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