Search Result
Results for "
tumor cell lines
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N11709
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Others
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Cancer
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Theasaponin E1 is a tea saponin isolated from tea seeds. Theasaponin E1 exhibits potential antitumor activity against human tumor cell lines K562 and HL60. Theasaponin E1 also has quinone reductase (QR)-inducing activity and can act as an anti-tumor agent for cancer prevention .
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- HY-118893
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Antibiotic
Bacterial
Fungal
Molecular Glues
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Infection
Cancer
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Asukamycin, a manumycin-type metabolite, could be isolated from Streptomyces nodosus subsp. asukaensis. Asukamycin is an antibiotic and has antimicrobial activity. Asukamycin inhibits growth of various tumor cell lines .
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- HY-144707
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Apoptosis
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Cancer
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AK-778-XXMU is a potent inhibitor of DNA Binding 2 (ID2) antagonist with a KD of 129 nM. AK-778-XXMU can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and more importantly, slow down the tumor growth .
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- HY-101597
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Apoptosis
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Cancer
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NVX-207, a Betulinic acid-derived anti-cancer compound, shows anti-tumor activity (mean IC50=3.5 μM) against various human and canine cell lines. NVX-207-induced apoptosis is associated with activation of the intrinsic apoptotic pathway via cleavage of caspases -9, -3, -7 and of PARP .
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- HY-101870B
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INCB053914 phosphate
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Pim
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Cancer
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Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
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- HY-101870
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INCB053914
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Pim
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Cancer
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Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines .
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- HY-153272
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Biochemical Assay Reagents
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Cancer
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Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
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- HY-106588
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SKI 2053R
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DNA Alkylator/Crosslinker
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Cancer
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Heptaplatin (SKI 2053R) is a platinum derivative with anticancer activity against various cancer cell lines, including cisplatin-resistant tumor cell lines. SKI-2053R is active in the research of gastric adenocarcinoma and has favorable toxicity profiles .
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- HY-130995
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Antibiotic
ADC Cytotoxin
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Infection
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Agrochelin, an alkaloid cytotoxic antibiotic, is produced by the fermentation of a marine Agrobacterium sp. Agrochelin has cytotoxic activity in tumor cell lines .
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- HY-108491
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SphK
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Cancer
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N,N-Dimethylsphingosine is a potent inhbitor of SphK (sphingosine kinase) as an endogenous metabolite of sphingosine produced in various tissues and tumor cell lines .
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- HY-50909
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KRX-0401; NSC 639966; D21266
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Akt
Autophagy
Apoptosis
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Cancer
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Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
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- HY-100395
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Apoptosis
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Cancer
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F16 is a potent growth inhibitor of the neu-overexpressing cells and also selectively inhibits proliferation of mammary epithelial as well as a variety of mouse mammary tumor and human breast cancer cell lines.
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- HY-125443
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Others
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Cancer
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Lucialdehydes A is a lanostante-type triterpene aldehydes, isolated from the fruiting bodies of Ganoderma lucidum. Lucialdehydes A shows cytotoxic effects on tumor cells, including Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines .
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- HY-14807
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CHR-2797
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Aminopeptidase
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Cancer
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Tosedostat (CHR-2797) is an orally active aminopeptidase inhibitor. CHR-2797 exerts antiproliferative effects against a range of tumor cell lines .
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- HY-130996
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ADC Cytotoxin
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Cancer
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Diacetyl Agrochelin is an acetyl derivative of Agrochelin, which is produced by the fermentation of a marine Agrobacterium sp. Diacetyl Agrochelin has cytotoxic activity in tumor cell lines .
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- HY-119529
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3,8-Quinolinediol
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Others
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Cancer
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Jineol is a cytotoxic alkaloid from the centipede Scolopendra subspinipes. Jineol exhibits modest cytotoxic activity in vitro against the growth of human tumor cell lines .
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- HY-N0984
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Diacetylvilasinin
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Others
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Cancer
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1,3-Diacetylvilasinin (Diacetylvilasinin), a bioactive Triterpenoid from Melia volkensii, shows marginal cytotoxicities against certain human tumor cell lines .
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- HY-128587
-
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SY-1365
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CDK
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Cancer
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Mevociclib (SY-1365) is a potent and first-in-class selective CDK7 inhibitor, with a Ki of 17.4 nM. Mevociclib exhibits anti-proliferative and apoptotic effects in solid tumor cell lines. Mevociclib possesses anti-tumor activity in hematological and multiple aggressive solid tumors .
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- HY-N9339
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(+)-Norglaucine
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Others
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Cancer
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Norglaucine ((+)-Norglaucine), a cytotoxic alkaloid, exhibits cytotoxicity towards the tumor cell lines B16-F10, HepG2, K562 and HL-60 cells .
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- HY-W773183
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Betulonic acid methyl ester; Methyl 3-oxolup-20(29)-en-28-oate
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Others
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Cancer
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Methyl betulonate (Betulonic acid methyl ester) is a triterpenoid. Methyl betulonate inhibits cell growth of eight tumor (including resistant) and two normal fibroblast cell lines with the IC50s >50.0 μM .
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- HY-12449
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LY3039478
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Notch
γ-secretase
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Cancer
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Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested .
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- HY-N7611
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Others
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Cancer
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7-Prenyloxyaromadendrin is a flavonoid from Pterocaulon alopecuroides with antitumor activity. 7-Prenyloxyaromadendrin shows good antiproliferative activity in tumor cell lines .
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- HY-132840
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AMG 650
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Microtubule/Tubulin
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Cancer
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Sovilnesib (AMG 650) is a potent, orally active kinesin-like protein KIF18A inhibitor with an IC50 value of 0.071 μM. Sovilnesib can be used for the research of cancer .
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- HY-124084
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Others
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Cancer
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SW203668 is a benzothiazole compound, shows anti-tumor activity against lung cancer cell lines (IC50=0.022-0.116 μM) .
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- HY-11005
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BX-912
4 Publications Verification
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PDK-1
Apoptosis
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Cancer
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BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
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- HY-P99931
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GEN3013
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CD3
CD20
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Cancer
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Epcoritamab (GEN3013) is an bispecific IgG1 antibody redirecting T-cells toward CD3×CD20 + tumor cells. Epcoritamab induces potent T-cell-mediated cytotoxicity towards B-cell NHL cell lines .
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- HY-N10265
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Endogenous Metabolite
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Cancer
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Stephacidin B is a fungal metabolite. Stephacidin B shows in vitro cytotoxicity against a panel of human tumor cell lines. Stephacidin B shows the strongest cytotoxicity against testosterone-dependent prostate LNCaP cancer cells .
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- HY-136824
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Bacterial
Antibiotic
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Infection
Cancer
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Napyradiomycin A1 is one enantioselective compound of napyradiomycins. napyradiomycins are an intriguing family of halogenated natural products with activity against several tumor cell lines as well as some bacterial strains .
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- HY-123143
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MLN576
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Topoisomerase
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Cancer
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XR11576 (MLN576) is an orally active inhibitor of topoisomerase I and II. XR11576 shows cytotoxicity against human and murine tumor cell lines (IC50: 6-47 nM) .
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- HY-79256
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Monomethyl auristatin F methyl ester
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ADC Cytotoxin
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Cancer
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MMAF-Ome, an antitubulin agent, is also an ADC cytotoxin. MMAF-Ome inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4 -) cell lines, respectively.
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- HY-P1632
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Bacterial
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Infection
Cancer
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Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane .
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- HY-N3215
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Others
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Others
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Nagilactone C is a diterpene dilactone compound isolated from Podocarpus neriifolius. Nagilactone C has potent antiproliferative activity against human fibrosarcoma and murine colon carcinoma tumor cell lines .
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- HY-154797
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Others
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Cancer
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N,N-Dimethyldoxorubicin is a Doxorubicin (HY-15142A) analogue. N,N-Dimethyldoxorubicin shows cytotoxicity against a panel of tumor cell lines (IC50s < 0.3 μM) .
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- HY-N6990
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Others
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Cancer
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Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities .
Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines .
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- HY-N6955
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Others
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Cancer
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Eupalinilide B is a guaiane type sesquiterpene lactone that can be found in Eupatorium lindleyanum. Eupalinilide B shows potent cytotoxicity against P-388 and A-549 tumor cell lines .
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- HY-150753
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- HY-121250
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Fatty Acid Synthase (FASN)
Apoptosis
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Cancer
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Fasnall is a selective fatty acid synthase (FASN) inhibitor with an IC50 of 3.71 μM. Fasnall induces apoptosis in HER2 + breast cancer cell lines. Fasnall shows potent anti-tumor activities .
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- HY-145899
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Others
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Cancer
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PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM) .
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- HY-129337
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Antibiotic
Fungal
Apoptosis
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Infection
Cancer
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Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity .
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- HY-N12430
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Others
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Cancer
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Marsdenoside A (compound 7) is a Marsdenoside isolated from Alocasia genus. Marsdenoside A has a weak growth inhibitory effect on two tumor cell lines, MGC-803 and HT-29, with IC50 >50 μg/mL.
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- HY-161096
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ROR
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Cancer
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Antitumor agent-127 (compound 1) is a parent macrocyclic peptide. Antitumor agent-127 displays nanomolar cell-based binding to ROR1 and relatively good internalization in 786-O and MDA-MB-231 tumor cell lines .
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- HY-139453
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Others
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Cancer
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LP-184 (compound 6), an acylfulvene analog, inhibits tumor growth. LP-184 has potent anti-cancer activity in the ovarian, colon, prostate and pancreatic cell lines. (patent WO2007019308A2).
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- HY-N7205
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Others
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Cancer
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Glaucocalyxin D is a ent-kauranoid-type diterpenoid that can be isolated from Rabdosia japonica. Glaucocalyxin D shows cytotoxicity against various human tumor cell lines. Glaucocalyxin D can be used for cancer research .
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- HY-N11928
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Others
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Cancer
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Changnanic acid (schisandrin) is a triterpene compound with potential anti-tumor effects. Changnanic acid exhibits moderate cytotoxic activity against human tumor cell lines Bel-7402, MCF-7 and HL-60, with IC50s of 100 μM, 100 μM and 50.51 μM respectively .
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- HY-148827A
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HYBO-165 sodium
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PKA
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Cancer
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GEM231 sodium is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 sodium induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
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- HY-148827
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HYBO-165
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PKA
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Cancer
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GEM231 is an 18mer antisense oligonucleotide targeting the mRNA of the PKA-I (RIα regulatory subunit of cAMP dependent protein kinase type I ). GEM231 induces cell growth arrest, apoptosis, and differentiation in a variety of cancer cell lines in vitro and in tumors in vivo.
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- HY-162148
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EGFR
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Cancer
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HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
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- HY-156112
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Others
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Cancer
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LM2I is a derivative of Spinosyn A (SPA). LM2I is argininosuccinate synthase (ASS1) enzyme activator, and tumor inhibitor that directly interact with ASS1. LM2I has significant antiproliferative activity in seven colorectal cancer cell-lines and xenograft tumors of colorectal cancer. LM2I inhibits colorectal cancer cell growth via the EGFR pathway .
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- HY-N12128
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Others
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Cancer
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Ophiopogonin R (compound 3) is a steroid saponin. Ophiopogonin R was isolated and purified from natural ophiopogonin. Ophiopogonin R was not cytotoxic to five human tumor cell lines (HepG2, HLE, BEL7402, BEL7403 and Hela) .
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- HY-19542
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C6-Cer; N-Hexanoylsphingosine
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C6-ceramide, a ceramide pathway activator, shows activity against a variety of cancer cell lines. C6-ceramide can be used as an adjuvant for chemotherapeutic agents, to enhance anti-tumor effects .
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- HY-146250
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Microtubule/Tubulin
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Cancer
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Antitumor Agent-71 is an antiproliferative activity antitumor agent and against tumor cell lines with IC50 values ranging from 3.98-15.70 μM. Antitumor Agent-71 is an antitumor agent that can inhibit tubulin polymerization.
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- HY-12458
-
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DNA/RNA Synthesis
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Infection
Cancer
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Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml .
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- HY-119198
-
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Apoptosis
Histone Methyltransferase
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Cancer
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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-124617A
-
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Apoptosis
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Inflammation/Immunology
Cancer
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AMXT-1501 tetrahydrochloride is an orally active polyamine transport inhibitor. AMXT1501 blocks tumor growth in immunocompetent mice but not in athymic nude mice lacking T cells . Combination of DFMO and AMXT‐1501 induces caspase‐3 mediated apoptosis in NB cell lines .
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- HY-123298
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Src
Akt
Apoptosis
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Cancer
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Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .
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- HY-N10904
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Others
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Cancer
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Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB) .
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- HY-N12437
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Others
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Cancer
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Marsdenoside B (compound 8) is a Marsdenoside isolated from Alocasia genus. Marsdenoside B inhibits the growth of tumor cell lines MGC-803 and HT-29 with IC50s of 25.6 μg/mL and 32.4 μg/mL, respectively.
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- HY-148413
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ISIS 3521 sodium
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PKC
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Cancer
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Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
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- HY-146819
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Carbonic Anhydrase
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Cancer
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Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
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- HY-115537
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Apoptosis
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Cancer
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NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .
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- HY-18614
-
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Notch
γ-secretase
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Cancer
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LY900009 is a potent and orally active, First-in-class inhibitor of Notch signaling via selective inhibition of the γ-secretase protein (GSI). LY900009 inhibited Notch signalling in tumor cell lines and endothelial cells (IC50 range: 0.005-20 nM). LY900009 can be used for advanced cancer research .
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- HY-N7623
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Others
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Cancer
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Ursonic acid methyl ester is an esterified derivative of Ursolic acid (HY-N0140). Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 µg/ml .
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- HY-N12141
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Apoptosis
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Inflammation/Immunology
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Flaccidoside II inhibits proliferation and induces apoptosis in Malignant peripheral nerve sheath tumors (MPNSTs) cell lines. Flaccidoside II ameliorates collagen-induced arthritis in mice. Flaccidoside II is an active triterpenoid saponin constituent from Anemone flaccida rhizome .
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- HY-16261
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INNO-206; DOXO-EMCH
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Topoisomerase
ADC Cytotoxin
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Cancer
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Aldoxorubicin (INNO-206) is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-N6679
-
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Antibiotic
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Cancer
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(R)-10,11-Dehydrocurvularin is a secondary metabolite isolated from Curvularia sp.. (R)-10,11-Dehydrocurvularin displays concentration-dependent cytotoxicity towards human tumor cell lines with a mean IC50 value of 1.25 µM .
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- HY-125664
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Antibiotic
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Cancer
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Lucialdehyde B is a tetracyclic triterpene isolated from the substrates of Ganoderma lucidum with antiviral and cytotoxic activities. Lucialdehyde B has cytotoxic effects against Lewis lung cancer (LLC), T-47D, Sarcoma 180 and Meth-A tumor cell lines .
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- HY-149375
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 37 (Compound 12) is a Tubulin inhibitor that can effectively inhibit Tubulin aggregation (IC50=1.3 µM). Tubulin inhibitor 37 exhibits antiproliferative activity against human tumor cell lines and has potential for studying cancer .
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- HY-16261C
-
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INNO-206 hydrochloride; DOXO-EMCH hydrochloride
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Topoisomerase
ADC Cytotoxin
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Cancer
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Aldoxorubicin (INNO-206) hydrochloride is an albumin-binding proagent of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin hydrochloride (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
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- HY-115735
-
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SphK
Apoptosis
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Cancer
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SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines .
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- HY-146366
-
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
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- HY-145406
-
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Adenosine Receptor
HDAC
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Inflammation/Immunology
Cancer
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IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
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- HY-101667
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LTURM34
4 Publications Verification
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DNA-PK
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Cancer
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LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines .
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- HY-122829
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PROTACs
Bcl-2 Family
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Cancer
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BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research .
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- HY-109583
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4-Oxo-4-HPR
|
Apoptosis
Reactive Oxygen Species
Drug Metabolite
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Cancer
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4-Oxofenretinide (4-Oxo-4-HPR) is a metabolite of Fenretinide (HY-15373). 4-Oxofenretinide induces cell growth inhibition in ovarian, breast, and neuroblastoma tumor cell lines. 4-Oxofenretinide causes a marked accumulation of cells in G2-M. 4-Oxofenretinide induces cancer cell apoptosis through caspase-9 .
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- HY-15970
-
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KPT-335
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CRM1
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Cancer
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Verdinexor(KPT-335) is a novel, orally bioavailable selective inhibitor of nuclear export (SINE), inhibits nuclear export protein Exportin 1(XPO1/CRM1) against canine tumor cell lines; also reduce influenza virus replication in vitro and in vivo.
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- HY-162105
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Cytochrome P450
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Endocrinology
Cancer
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Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. Through suppressing the conversion of androstenedione to oestrogen caused by aromatase, Aromatase-IN-3 exerts an appreciable tumor growth inhibitory activities against breast cancer cell lines, suggesting its usage for ER+ cancer research .
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- HY-N12607
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Others
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Cancer
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Garcilatelic acid (Compound 5) is a compound that can be isolated from Garcinia lateriflora. Garcilatelic acid has antiproliferative activity against tumor cell lines (A549, MDA-MB-231, MCF-7, KB and KB-VIN), with IC50 values of 0.5-1.3 μM .
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- HY-155073
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin inhibitor 35 (compound 6b) is a dual inhibitor of topoisomerase I (IC50=~50 μM) and tubulin polymerization (IC50=5.69 μM). Tubulin inhibitor 35 inhibits migration and invasion of MGC-803 and RKO cell lines，and induces apoptosis via arresting cell cycle at G2/M phase. Tubulin inhibitor 35 exhibis potent efficacy in gastrointestinal tumor inhibiton (inhibits MGC-803 (IC50=0.09 μM) and RKO (IC50=0.2 μM) cell lines) .
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- HY-15096
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FJ-776
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Fluorescent Dye
HSP
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Cancer
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MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
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- HY-N4201
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EGFR
Src
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Cancer
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Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermum erythrorhizon, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells .
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- HY-120275
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Bcl-2 Family
Apoptosis
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Cancer
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CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
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- HY-146316
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Topoisomerase
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Cancer
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Topoisomerase II inhibitor 6 (Compound 5), a tryptanthrin derivative, is a potent and selective inhibitor of topoisomerase II. Topoisomerase II inhibitor 6 exhibits antiproliferative activity on different tumor cell lines. Topoisomerase II inhibitor 6 blocks the cell cycle of CCRF-CEM in the G2 phase and induces DNA DSB. Topoisomerase II inhibitor 6 has the potential for the research of cancer diseases .
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- HY-P99361
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PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
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TNF Receptor
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Cancer
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Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
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- HY-N6061
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Others
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Cancer
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Ophiopogonin C, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin C shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 19.76 μM and 15.51 μM, respectively .
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- HY-137605
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Others
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Cancer
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WSF1-IN-1 (compound 136), an orally active WSF1 inhibitor, can be used in the study for WSF1 (Wolfram syndrome) related tumors, with IC50 values of 0.33 μM and >27 μM in HepG2 parental and HepG2 WFS1 KO cell lines, respectively .
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- HY-120574
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ADC Cytotoxin
Topoisomerase
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Cancer
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TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile .
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- HY-163062
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Microtubule/Tubulin
Apoptosis
Complement System
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Cancer
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Tubulin/NRP1-IN-1 (compound TN-2) is a dual inhibitor of Tubulin and NRP1 with IC50s of 0.71 and 0.85 μM, respectively. Tubulin/NRP1-IN-1 significantly inhibits the viability of prostate tumor cell lines and induces apoptosis .
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- HY-146454
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Others
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Cancer
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Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
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- HY-161324
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Microtubule/Tubulin
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Cancer
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Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
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- HY-158105
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PROTACs
BCL6
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Cancer
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ARV-393 is an orally active PROTAC that utilizes the ubiquitin-proteasome system to target the degradation of BCL6. ARV-393 consists of ligand conjugates targeting BCL6 and the E3 ligase cereblon, respectively. ARV-393 has DC50 and GI50 values of <1 nM in multiple cell lines of diffuse large B-cell lymphoma (DLBCL) and Burkitt lymphoma (BL). ARV-393 also demonstrated considerable tumor suppressor activity in tumor xenograft models. ARV-393 is being studied to inhibit non-Hodgkin lymphoma.
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- HY-N10354
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Apoptosis
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Cancer
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27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
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- HY-N2584A
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HSV
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Infection
Cancer
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Isoxanthohumol is a prenylflavonoid from hops and beer. Isoxanthohumol exhibits an antiproliferative activity against several human cancer cell lines. Isoxanthohumol inhibits the development of lung metastatic foci in tumor-challenged animals. Isoxanthohumol shows an antiviral activity towards herpes viruses (HSV1 and HSV2) and bovine viral diarrhea virus (BVDV) .
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- HY-146462
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Apoptosis
ROS Kinase
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Cancer
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Anticancer agent 59 (compound 11) has inhibitory activity against kinds of cancer cell lines, especially in A549 with IC50 of 0.2 μM. Anticancer agent 59 induces apoptosis and an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 59 significantly decreases mitochondrial membrane potential. Anticancer agent 59 can suppress tumor growth in A549 mouse xenograft model .
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- HY-163435
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Apoptosis
Caspase
PARP
Bcl-2 Family
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Cancer
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Anticancer agent 201 (Compound 2f) has IC50 values in the low micromolar range for multiple tumor cell lines. Anticancer agent 201 is highly cytotoxic to CCRF-CEM cells in vitro, inducing apotosis by activating caspase-3 in the intrinsic mitochondrial pathway and lysis of PARP, as well as reducing the expression of Bcl-2 and Bcl-XL proteins. Anticancer agent 201 can be used in cancer research .
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- HY-15205
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Ganetespib
Maximum Cited Publications
30 Publications Verification
STA-9090
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HSP
Apoptosis
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Cancer
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Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
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- HY-128910
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Drug-Linker Conjugates for ADC
Microtubule/Tubulin
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Cancer
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MC-VC(S)-PABQ-Tubulysin M is a synthetic ADC drug-linker conjugate composed of the tubulin polymerization inhibitor Tubulysin M (an ADC Cytotoxin) (HY-N7053) and MC-VC(S)- PABQ (an ADC linker) is connected. MC-VC(S)-PABQ-Tubulysin M is effective against multidrug-resistant lymphoma cell lines and tumors .
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- HY-146565
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DNA-PK
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Cancer
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DNA-PK-IN-8 is a highly potent, selective and orally active DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of 0.8 nM. DNA-PK-IN-8 exhibits synergistic antiproliferative activity against a series of cancer cell lines and significantly suppresses HL-60 tumor growth, when using in combination with Doxorubicin .
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- HY-101849
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GLUT
TNF Receptor
Apoptosis
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Cardiovascular Disease
Cancer
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Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
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- HY-146452
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Apoptosis
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Cancer
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Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
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- HY-105416
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UCN-1028C
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Antibiotic
PKC
Apoptosis
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Infection
Cancer
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Calphostin C is a potent and specific inhibitor of protein kinase C. Calphostin C is an antitumor antibiotic. Calphostin C has 1000 times more inhibitory to protein kinase C with an IC50 of 0.05 μM than other protein kinases. Calphostin C induces apoptosis in some tumor cell lines. Calphostin C has potent cytotoxic activity and antitumor activity .
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- HY-100128
-
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Microtubule/Tubulin
ADC Cytotoxin
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Cancer
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DM1-SMe is an unconjugated form of the Maytansinoid in IMGN901. DM1-SMe is about 3-10-fold more potent than the parent agent Maytansine, with IC50s ranging from 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines .
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- HY-120599
-
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VERU-111; ABI-231
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Microtubule/Tubulin
Apoptosis
HPV
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Cancer
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VERU-111 (ABI-231) is a potent and orally active α and β tubulin inhibitor, which displays strong antiproliferative activity, with an average IC50 of 5.2 nM against panels of melanoma and prostate cancer cell lines. VERU-111 (ABI-231) suppresses tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7, and has potential for the treatment of prostate cancer .
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- HY-154949
-
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WDR5
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Cancer
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WDR5-IN-6 is a WDR5 inhibitor, targeting to WBM site. WDR5-IN-6 inhibits cell proliferation of neuroblastoma cell lines with potent anti-tumor activity. WDR5-IN-6 shows high synergy with OICR-9429 (HY-16993), a WDR5 inhibitor targeting to WIN site. WDR5-IN-6 can be used for reasearch in neuroblastoma .
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- HY-13208
-
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AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
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IAP
Apoptosis
|
Cancer
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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 .
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- HY-15794
-
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Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
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G-quadruplex
|
Cancer
|
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Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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- HY-101448
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WAY-171318
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|
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TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood . TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines .
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- HY-151286
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STAT
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Cancer
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Antitumor agent-73 is a Diosgenin (HY-N0177) derivative, which inhibits STAT3 signaling and activates Pdia3/ERp57 exogenously. Antitumor agent-73 shows potent anti-tumor activity against various cancer cell lines, 7.9-341.7-fold stronger than Diosgenin .
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- HY-160597
-
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ADC Cytotoxin
Topoisomerase
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Cancer
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Exatecan-amide-bicyclo[1.1.1]pentan-1-ol (Compound 79) is an exatecan (HY-13631) derivative that can be used as a payload in drug conjugates. Exatecan-amide-bicyclo[1.1.1]pentan-1-ol has significant inhibitory activity against a variety of tumor cell lines .
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![Exatecan-amide-bicyclo[1.1.1]pentan-1-ol](//file.medchemexpress.com/product_pic/hy-160597.gif)
- HY-160066
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Others
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Cancer
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SYL3C aptamer sodium is a DNA aptamer that targets the epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets multiple human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III is 38 nM and 67 nM, respectively. SYL3C aptamer sodium provides stability, high binding affinity, and selectivity for targeted cancer therapy, cancer cell imaging, and circulating tumor cell detection .
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- HY-162264
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Microtubule/Tubulin
Proton Pump
Apoptosis
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Inflammation/Immunology
Cancer
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Tubulin polymerization/V-ATPase-IN-1 (compound F10) is a Tubulin polymerization/V-ATPase inhibitor. Tubulin polymerization/V-ATPase-IN-1 shows robust antiproliferation activity against four human cancer cell lines, and exerts antiproliferative activity by inhibiting tubulin and V-ATPase. Tubulin polymerization/V-ATPase-IN-1 induces immunogenic cell death in addition to apoptosis, and inhibits tumor growth in an RM-1 homograft model with enhanced T lymphocyte infiltration .
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- HY-19671
-
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SR-45023A; SR 9223i; SK&F-99085
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Apoptosis
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Cancer
|
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Apomine (SR-45023A) is an antineoplastic agent that inhibits the mevalonate/isoprenoid pathway in cholesterol synthesis. It can accelerate the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR). Apomine can also inhibit the growth of various types of cancer cells, including lung cancer, colon cancer, breast cancer, and skin cancer. In addition, Apomine is able to induce apoptosis in tumor cell lines derived from leukemia, colon cancer, liver cancer, ovarian cancer, and breast cancer .
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- HY-N3504
-
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Sirtuin
|
Cancer
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Ophiopogonin D', isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D' shows cytotoxic activity against two human tumor cell lines MG-63 and SNU387 with IC50s of 3.09 μM and 3.63 μM, respectively . Ophiopogonin D' activates SIRT1 in a dose-dependent manner .
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- HY-18979
-
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Lactimidomycin is a glutarimide-containing compound isolated from Streptomyces. Lactimidomycin is a potent inhibitor of eukaryotic translation elongation. Lactimidomycin has a potent antiproliferative effect on tumor cell lines and selectively inhibit protein translation. Lactimidomycin inhibits protein synthesis with an IC50 value of 37.82 nM. Lactimidomycin is also a potent and non-toxic inhibitor of dengue virus 2 and other RNA viruses. Anticancer and antiviral activities .
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- HY-P990027
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ADC Antibody
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Cancer
|
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Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
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- HY-15160
-
TAK-960
2 Publications Verification
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Polo-like Kinase (PLK)
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Cancer
|
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TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
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- HY-15160B
-
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Polo-like Kinase (PLK)
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Cancer
|
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TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
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- HY-15160A
-
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Polo-like Kinase (PLK)
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Cancer
|
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TAK-960 hydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 hydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 hydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
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- HY-N12198
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Others
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Cancer
|
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Mollicellin H is a secondary metabolite of the fungus C. brasiliense and has a wide range of biological activities, including immunomodulation, cytotoxicity and anti-tumor effects. The growth inhibitory effects (GI50s) of Mollicellin H on human breast cancer (Bre04), human lung (Lu04) and human neuroma (N04) cell lines are 5.1 μg/mL, 6.5 μg/mL and 2.5 μg/mL respectively .
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- HY-146461
-
|
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Apoptosis
Caspase
ROS Kinase
|
Cancer
|
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Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca 2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model .
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-
- HY-146307
-
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TrxR
|
Cancer
|
|
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins .
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-
- HY-146260
-
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PI3K
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Cancer
|
|
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity .
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- HY-147165
-
|
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YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-147165A
-
|
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YAP
|
Cancer
|
|
VT02956 is a LATS inhibitor (IC50: 0.76 nM for LATS1, 0.52 nM for LATS2). VT02956 targets the Hippo pathway. VT02956 inhibits ESR1 expression and growth of ER+ breast cancer cell lines and patient-derived tumor organoids . VT02956 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-100022
-
|
eFT508
|
MNK
PD-1/PD-L1
|
Cancer
|
|
Tomivosertib (eFT508) is a potent, highly selective, and orally active MNK1 and MNK2 inhibitor, with IC50s of 1-2 nM against both isoforms. Tomivosertib (eFT508) treatment leads to a dose-dependent reduction in eIF4E phosphorylation at serine 209 (IC50=2-16 nM) in tumor cell lines . Tomivosertib (eFT508) also dramatically downregulates PD-L1 protein abundance .
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-
- HY-103712A
-
|
CT7001 hydrochloride; ICEC0942 hydrochloride
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib hydrochloride (CT7001 hydrochloride) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride has anti-tumor effects .
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-
- HY-15160C
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
TAK-960 monohydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 monohydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 monohydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
|
-
- HY-103712B
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-103712
-
|
CT7001; ICEC0942
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib has anti-tumor effects .
|
-
- HY-103712C
-
|
CT7001 hydrochloride hydrate; ICEC0942 hydrochloride hydrate
|
CDK
Apoptosis
|
Cancer
|
|
Samuraciclib (CT7001) hydrochloride hydrate is a potent, selective, ATP-competitive and orally active CDK7 inhibitor, with an IC50 of 41 nM. Samuraciclib hydrochloride hydrate displays 45-, 15-, 230- and 30-fold selectivity over CDK1, CDK2 (IC50 of 578 nM), CDK5 and CDK9, respectively. Samuraciclib hydrochloride hydrate inhibits the growth of breast cancer cell lines with GI50 values between 0.2-0.3 µM. Samuraciclib hydrochloride hydrate has anti-tumor effects .
|
-
- HY-15794G
-
|
Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
|
G-quadruplex
|
Cancer
|
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Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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- HY-147682
-
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NF-κB
Apoptosis
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Cancer
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NF-κB-IN-5 (compound 4d) is an orally active and potent NF-κB inhibitor by interacting directly with NF-κB. NF-κB-IN-5 shows antitumor activity against human cancer cell lines (HCT116, U87-MG, HepG2, BGC823, PC9), with IC50 values of 5.35, 2.81, 2.83, 2.02 and 3.90 μM, respectively. NF-κB-IN-5 induces apoptosis in U87-MG tumor cell and cell cycle arrest in G0/G1 phase .
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- HY-100195
-
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SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents .
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- HY-123981
-
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Phosphatase
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Cancer
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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 .
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- HY-118119
-
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PGE synthase
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Cancer
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CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
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- HY-139659
-
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PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
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Cancer
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ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-143317
-
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Epigenetic Reader Domain
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Cancer
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XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
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- HY-157125
-
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PI3K
Apoptosis
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Cancer
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PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
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-
- HY-19896
-
COTI-2
2 Publications Verification
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MDM-2/p53
Apoptosis
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Cancer
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COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
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-
- HY-144692
-
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MEK
PI3K
PERK
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Cancer
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MEK/PI3K-IN-1 (compound 6r) is a potent MEK/PI3K inhibitor, with IC50 values of 124 nM (MEK1), 130 nM (PI3Kα), and 236 nM (PI3Kδ), respectively. MEK/PI3K-IN-1 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-1 shows anti-proliferative activity against tumor cell lines .
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- HY-144693
-
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MEK
PI3K
PERK
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Cancer
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MEK/PI3K-IN-2 (compound 6s) is a potent MEK/PI3K inhibitor, with IC50 values of 352 nM (MEK1), 107 nM (PI3Kα), and 137 nM (PI3Kδ), respectively. MEK/PI3K-IN-2 suppresses pAKT and pERK1/2 levels. MEK/PI3K-IN-2 shows anti-proliferative activity against tumor cell lines .
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-
- HY-112296
-
T025
2 Publications Verification
|
CDK
Apoptosis
DYRK
|
Cancer
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|
T025 is an orally active and highly potent inhibitor of Cdc2-like kinase (CLKs), with Kd values of 4.8, 0.096, 6.5, 0.61, 0.074, 1.5 and 32 nM for CLK1, CLK2, CLK3, CLK4, DYRK1A, DYRK1B and DYRK2, respectively. T025 induces caspase-3/7-mediated cell apoptosis. T025 reduces CLK-dependent phosphorylation. T025 exerts anti-proliferative activities in both hematological and solid cancer cell lines (IC50 values: 30-300 nM). T025 has an anti-tumor efficiency, mainly for MYC-driven disease research .
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-
- HY-155066
-
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PI3K
mTOR
|
Cancer
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|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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-
- HY-156158
-
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Isocitrate Dehydrogenase (IDH)
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Cancer
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IDH2 R140Q-IN-2 (compound 36) is an an orally active IDH2 R140Q inhibitor (IC50: 29 nM). IDH2 R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2 R140Q (IC50: 10 nM). IDH2 R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2 R140Q-IN-2 can be used for research of acute myeloid leukemia (AML) .
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- HY-163434
-
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EGFR
Histone Methyltransferase
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Cancer
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PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
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-
| Cat. No. |
Product Name |
Type |
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- HY-15096
-
|
FJ-776
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Dyes
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MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
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-
- HY-15794G
-
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Methoxymorpholinyl doxorubicin (GMP); FCE 23762 (GMP); PNU 152243 (GMP)
|
Fluorescent Dye
|
|
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
|
| Cat. No. |
Product Name |
Type |
-
- HY-15794G
-
|
Methoxymorpholinyl doxorubicin (GMP); FCE 23762 (GMP); PNU 152243 (GMP)
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Biochemical Assay Reagents
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|
Nemorubicin (Methoxymorpholinyl doxorubicin) GMP is a GMP-class Nemorubicin (HY-15794). Nemorubicin is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1632
-
|
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Bacterial
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Infection
Cancer
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Tachyplesin I is a β-hairpin antimicrobial peptide that contains 17 amino acid residues. Tachyplesin I exhibits cytotoxic properties against various human tumor cell lines acting primarily by impairing the integrity of the outer cell membrane .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99931
-
|
GEN3013
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CD3
CD20
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Cancer
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Epcoritamab (GEN3013) is an bispecific IgG1 antibody redirecting T-cells toward CD3×CD20 + tumor cells. Epcoritamab induces potent T-cell-mediated cytotoxicity towards B-cell NHL cell lines .
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-
- HY-P99361
-
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PDL192; ABT-361; Anti-TNFRSF12A/TWEAKR/CD266 Reference Antibody (enavatuzumab)
|
TNF Receptor
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Cancer
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Enavatuzumab (PDL192; ABT-361) is a humanized IgG1 monoclonal antibody targeting the receptor of TNF-like weak inducer of apoptosis (TWEAK). TWEAK (Fn14; TNFRSF12A), the natural ligand of the TWEAK receptor (TweakR), stimulates multiple cellular responses. Enavatuzumab induces tumor growth inhibition through direct TweakR signaling and antibody dependent cell-mediated cytotoxicity (ADCC). Enavatuzumab can actively recruits and activates myeloid effectors to kill tumor cells. Enavatuzumab inhibits the growth of various human TweakR-positive cancer cell lines and xenografts in vitro and in vivo .
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-
- HY-P99413
-
|
ASP1650
|
Inhibitory Antibodies
|
Cancer
|
|
IMAB027 (ASP1650) is a specific anti-CLDN6 mAb, while CLDN6 (Claudin 6) is a tight junction membrane protein, aberrantly expressed in various human cancer types, ovarian cancers particularly. IMAB 027 shows anti-tumor activity, and induces apoptosis in CLDN6 + ovarian and testicular cancer cell lines .
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-
- HY-P990027
-
|
|
ADC Antibody
|
Cancer
|
|
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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