Search Result
Results for "
NCI
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-156060
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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NCI126224 is a TLR4 signaling inhibitor. NCI126224 suppress LPS (HY-D1056)-induced production of NF-κB, TNF-α, IL-1β, and NO in the nanomolar-low micromolar range. NCI126224 can be used for the research of inflammatory diseases .
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- HY-U00095
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NCI 329680; ZINC01574758
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DNA Alkylator/Crosslinker
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Cancer
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Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.
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- HY-156215
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HCV
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Infection
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NCI-B16 is a small molecule RNA binder and inhibits HCV viral replication .
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- HY-D1161
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NCI 240899
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Fluorescent Dye
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Neurological Disease
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True Blue (NCI 240899) is a fluorescent dye, as neuronal retrograde tracer (excitation wavelength 395-425 nm, barrier filter 450 nm). True Blue can label neuron and has no effects on neuronal survival .
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- HY-U00155
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NSC172112; NSC268497
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DNA Alkylator/Crosslinker
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Cancer
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NCI172112 is a classical bifunctional alkylating agent synthesized in an effort to develop antitumor agents effective against CNS tumors.
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- HY-N0840
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(-)-Bruceantin; NCI165563; NSC165563
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c-Myc
Caspase
Mitochondrial Metabolism
Apoptosis
Parasite
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Infection
Cancer
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Bruceantin ((-)-Bruceantin) is a quassinoid found in B. javanica. Bruceantin activates caspase signaling pathway, causes the mitochondrial dysfunction, inhibits cell proliferation, induces cell differentiation and apoptosis. Bruceantin exhibits anti-leukemia and antiprotozoal activities .
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- HY-157522
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Phosphodiesterase (PDE)
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Cancer
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NCI-14465 is an ectonucleotide pyrophosphatase/phosphodiesterase (ENPP1) inhibitor with an IC 50 of 26.4 μM. NCI-14465 can be used in cancer research .
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- HY-176557
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- HY-123597
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DDUG; NCI C04808
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Autophagy
Checkpoint Kinase (Chk)
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Cancer
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NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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- HY-163000
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EGFR
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Cancer
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EGFR-IN-129 (Compound 10b) is a potent and selective EGFR inhibitor, with an IC50 of 51.2 nM. EGFR-IN-129 exhibits broadest-spectrum antiproliferative activity against the NCI-tumor panel .
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- HY-N14255
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Antibiotic
Bacterial
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Infection
Cancer
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Memnobotrin A is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin A has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
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- HY-N14280
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Antibiotic
Bacterial
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Infection
Cancer
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Memnobotrin B is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin B has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
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- HY-160129
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ML-970; AS-I-145; NSC 716970
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Nucleoside Antimetabolite/Analog
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Cancer
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Centanamycin (ML-970; AS-I-145; NSC 716970) is a novel DNA-binding agent, and shows cytotoxic activity, with an average GI50 of 34 nM in NCI-60 cell line screening .
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- HY-N8900
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Others
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Cancer
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Vernolide-B has cytoxicity (ED50s: 3.78, 5.88, 6.42 μg/mL for KB, NCI-661, and HeLa cells respectively). Vernolide B is sesquiterpene lactone that can be isolated from Vernonia cinerea .
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- HY-N3443
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Others
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Cancer
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Jolkinol A is a natural product that can be found in Euphorbia pubescens. Jolkinol A inhibits cell growth with GI50s of 95.3, 57.3, >100 µM for MCF-7, NCI-460, SF-268 cells, respectively .
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- HY-147728
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-147724
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Microtubule/Tubulin
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Cancer
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Compounds 17O (ic50= 14.0 nm, NCI-H460) and 17p (ic50= 2.9 nm, NCI-H460) and furan groups showed effective cytotoxic activity against various human cancer cell lines at the nanomolar level.
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- HY-125730
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Others
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Cancer
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Kibdelone A is a type of natural compound from the flavonoid family, and it has potential value as an anti-proliferative agent .
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- HY-19797
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p97
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Cancer
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ML241 is a potent, selective and competitive p97 ATPase inhibitor with an IC50 of 0.11 μM. ML241 can be used for the research of cancer .
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- HY-168093
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Ferroptosis
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Cancer
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Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
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- HY-N10307
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Fungal
Bacterial
Endogenous Metabolite
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Infection
Cancer
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Anserinone B is an antifungal and antibacterial benzoquinone. Anserinone B causes radial growth reductions of 50% and 37% against S.fimicola and A. furfuraceus, respectively. Anserinones B also displays moderate cytotoxicity in the NCI’s 60 human tumor cell line panel (GI50=4.4 µg/mL) .
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- HY-173038
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EGFR
ERK
STAT
Apoptosis
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Cancer
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EGFR-IN-151 (Compound 10) inhibits EGFR and its downstream signaling pathways ERK/STAT3. EGFR-IN-151 inhibits the proliferation of a variety lung cancer cells (IC50s for NCI-H1781, HCC827, NCI-H3255 and NCI-H1975 is 11.7, 5.19, 7.32 and 1.53 μM, respectively), inhibits the colony formation and migration of H1975, arrests the cell cycle at G1 phase, and induces apoptosis in H1975 .
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- HY-172426
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Anaplastic lymphoma kinase (ALK)
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Cancer
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Dirozalkib (Compound 4) is the inhibitor for ALK with an IC50 of 0.9 nM. Dirozalkib exhibits anti-proliferative activity in cancer cells NCI-H3122, Karpas-299 and NCI-H2228 with IC50s of 130.4, 0.71 and 15.11 nM, respectively. Dirozalkib exhibits good pharmacokinetics characteristics with an bioavailbility of 30%~50% .
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- HY-171958
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PROTACs
EGFR
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Cancer
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PROTAC EGFR degrader 12 (example 1) is a PROTAC degrader targeting EGFR that can effectively degrade EGFR mutants, but has little effect on EGFR WT. PROTAC EGFR degrader 12 shows IC50s against EGFR L858R-T790M (NCI-H1975 cells), EGFR L858R (NCI-H3255 cells), and EGFR L858R-T790M-L797S (NCI-H1975+CS cells) of all <50 nM .
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- HY-164384
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PI3K
Akt
mTOR
Apoptosis
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Cancer
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DFX117 is a selective, orally active inhibitor for PI3Kα and c-Met tyrosine kinase. DFX117 inhibits PI3K/Akt/mTOR pathway, inhibits the proliferation of NCI-H1975, NCI-H1993, and HCC827 with IC50s 0.02-0.08 µM. DFX117 arrests cell cycle at G0/G1 phase, induces apoptosis in A549 and NCI-H1975. DFX117 exhibits antitumor efficacy in mice .
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- HY-101130
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PNU-74654
Maximum Cited Publications
11 Publications Verification
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Wnt
β-catenin
Apoptosis
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Cancer
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PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell.
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- HY-151394
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Microtubule/Tubulin
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Cancer
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Tubulin polymerization-IN-33 is an inhibitor of [1,2]oxazoloisoindoles tubulin polymerization, exhibits high antiproliferative activity against the NCI panel .
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- HY-N2039
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Others
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Cancer
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20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
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- HY-170764
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YAP
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Cancer
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M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC50 value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC50 value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .
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- HY-162787
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Adenosine Receptor
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Cancer
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Adenosine receptor antagonist 5 (Compound 39) is a selective antagonist for human adenosine A3 receptor (hA3R) with Ki of 12 nM. Adenosine receptor antagonist 5 inhibits IB-MECA (HY-13591)-induced cAMP accumulation in NCI-H1792 cell, inhibits the proliferation of cancer cell LK-2 and NCI-H1792. Adenosine receptor antagonist 5 exhibits a fast metabolic rate in human liver microsomes .
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- HY-169476
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Drug Derivative
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Cancer
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Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, respectively .
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- HY-143296
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SphK
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Cancer
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SphK1-IN-1 (compound 48) is a SphK1 inhibitor with effective antitumor activity. SphK1-IN-1 inhibits SphK1 ATPase with an IC50 value of 4.02 μM. SphK1-IN-1 can be used for the research of cancer .
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- HY-169299
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PARP
Topoisomerase
Apoptosis
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Cancer
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TOPOI/PARP-1-IN-2 (compound 6c) is a dual PARP-1 and topoisomerase 1 (TOPO-1) inhibitor with IC50s of 32.2 nM and 46.2 nM, respectively. TOPOI/PARP-1-IN-2 shows a selectivity for PARP-1 over PARP-2. TOPOI/PARP-1-IN-2 disrupts the cell cycle at the S phase and induces apoptosis in NCI-60 cancer cell lines .
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- HY-N12004
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Others
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Cancer
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19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively .
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- HY-170550
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Ras
ERK
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Cancer
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KRAS G12C inhibitor 69 (Compound K09) is the inhibitor for mutant RAS protein KRASG12C with an IC50 of 4.36 nM. KRAS G12C inhibitor 69 inhibits the ERK phosphorylation in NCI-H358 and MIA-PACA-2 with an IC50 of 12 nM and 7 nM. KRAS G12C inhibitor 69 inhibits the proliferation of cancer cell NCI-H358 and MIA-PACA-2 with IC50 of 3.15 nM and 2.33 nM .
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- HY-173074
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Microtubule/Tubulin
MDM-2/p53
Apoptosis
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Cancer
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Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460 .
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- HY-N12231
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Antibiotic
Bacterial
Lipoxygenase
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Infection
Cancer
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Carbazomycin B is a bacterial metabolite and can be isolated from Streptomyces. Carbazomycin B is an antifungal and antibacterial agent. Carbazomycin B inhibits 5-lipoxygenase (5-LO) activity in extract from RBL-1 cell with the IC50 Of 1.5 µM sup>[2]sup>[3]sup>[4].
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- HY-164033
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Ramnodigin
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Apoptosis
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Cancer
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HOE 689 (Ramnodigin) is an analog of Digitoxin (HY-B1357). HOE 689 exhibits cytotoxicity to lung cancer cells and induces apoptosis in cancer cell NCI-H460 with an IC50 of 52 nM .
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- HY-N10877
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Others
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Cancer
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Chlorajapolide F is a nature product that could be isolated from the aerial part of Chloranthus japonicas. Chlorajapolide F has low cytotoxic activity against NCI-H460 and SMMC-7721 cell lines .
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- HY-148517
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AZD0095
3 Publications Verification
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Monocarboxylate Transporter
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Cancer
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AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
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- HY-100555
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HSP
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Infection
Cancer
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CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
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- HY-139882
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- HY-147726
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
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- HY-173259
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PARP
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Cancer
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PARP7-IN-23 (compound 56) is a potent PARP7 inhibitor with an EC50 of 0.915 nM for pSTAT1 in NCI-H1373 cells. PARP7-IN-23 has the potential for cancer research .
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- HY-173262
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PARP
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Cancer
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PARP7-IN-24 (compound 44) is a potent PARP7 inhibitor with an EC50 of 0.375 nM for pSTAT1 in NCI-H1373 cells. PARP7-IN-24 has the potential for cancer research .
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- HY-147208
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YAP
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Cancer
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MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .
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- HY-147703
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Aurora Kinase
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Cancer
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Aurora kinase inhibitor-9 (compound 9d) is a potent AURKA/B dual aurora kinase inhibitor with IC50s of 0.093, 0.09 µM for Aurora A, Aurora B, respectively. Aurora kinase inhibitor-9 shows broad spectrum anti-proliferative activity .
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- HY-161173
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PROTACs
Ras
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Cancer
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PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC50 of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC50 of 5 nM .
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- HY-N7302
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Others
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Cancer
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Anthracophyllone is an aristolane sesquiterpene that can be isolated from the mushroom Anthracophyllum. Anthracophyllone has cytotoxicity against MCF-7, KB, NCI-H187, Vero cells (IC50: 32.97, 18.02, 15.17, 18.06 μM) .
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- HY-147858A
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PROTACs
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Cancer
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PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFRL858R/T790M degrader, with a DC50 of 13 .2 nM.PROTAC EGFR degrader 7 inhibits NCI-H1975 cells proliferation, with an IC50 of 46 .82 nM.PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI-H1975 cell.PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research .
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- HY-157085
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HSP
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Cancer
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BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
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- HY-101567
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Epigenetic Reader Domain
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Cancer
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BMS-986158 is a potent BET inhibitor with IC50s of 6.6 and 5 nM in NCI-H211 small cell lung cancer (SCLC) cells and MDA-MB231 triple negative breast cancer (TNBC) cells, respectively .
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- HY-144337
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DNA Alkylator/Crosslinker
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Cancer
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DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
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- HY-170912
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Topoisomerase
Apoptosis
ROS Kinase
Cytochrome P450
Caspase
Bcl-2 Family
PI3K
Akt
mTOR
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Cancer
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Topo I/II-IN-2 (Compound 3g) is an inhibitor of Topo I and Topo II. Topo I/II-IN-2 inhibits NCI-H446 cells and NCI-H1048 cells with IC50s of 1.30 μM and 1.42 μM, respectively. Topo I/II-IN-2 induces mitochondrial Apoptosis, mitochondrial dysfunction and activity generation. Topo I/II-IN-2 inhibits the PI3K/Akt/mTOR pathway. Topo I/II-IN-2 prevents SCLC (small cell lung cancer) cell proliferation, invasion, and migration in vitro. .
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- HY-115949
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HSP
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Cancer
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Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively .
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- HY-161614
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 44 (Compound 26r) is an inhibitor for tubullin. Tubulin inhibitor 44 exhibits cytotoxicity in cancer cells NCI-H460, BxPC-3 and HT-29, with IC50s of 0.96, 0.66 and 0.61 nM, respectively .
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- HY-W560574
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Xanthine Oxidase
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Cancer
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Xanthine oxidase-IN-14 (Compound 3f) is an inhibitor for xanthine oxidase, with IC50 >100 μM. Xanthine oxidase-IN-14 inhibits proliferations of cancer cells MCF-7, NCI-H460 and SF-268, with IC50 greater than 150 μM .
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- HY-157319
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PI3K
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Cancer
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PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
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- HY-P991462
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CD38
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Cancer
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GBR-1342 is a human bispecific antibody (bsAb) targeting CD38 & CD3. GBR-1342 inhibits the activity of Daudi, RAJI, RPMI8226, IM-9, and NCI-H929 cancer cell lines. GBR-1342 can be used in myeloma research .
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- HY-14389
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Microtubule/Tubulin
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Cancer
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LP-261 is a potent and orally active anti-mitotic agent and shows an inhibition of in vitro tubulin polymerization with an EC50 of 3.2 μM . LP-261 inhibits growth of a human non-small-cell lung tumor (NCI-H522) in vivo and can be used for cancer research .
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- HY-145379
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Parasite
Endogenous Metabolite
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Infection
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Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacterium tuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
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- HY-N2039R
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Reference Standards
Others
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Cancer
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20(R)-Ginsenoside Rg2 (Standard) is the analytical standard of 20(R)-Ginsenoside Rg2. This product is intended for research and analytical applications. 20(R)-Ginsenoside Rg2 shows inhibitory effects on lung cancer NCI-H1650 cells. Anti-cancer activities .
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- HY-173218
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EGFR
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Cancer
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anti-NSCLC agent-1 (compound 8dc) is an inhibitor of tyrosine kinase inhibitors (TKIs) with IC50 values of 0.05 and 0.09 μM in A549 and NCI-H441 cells. anti-NSCLC agent-1 shows anti-NSCLC activities in colony formation, migration, and invasion .
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- HY-117872
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20-O-Acetylsartorypyrone D
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Fungal
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Infection
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Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
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- HY-157888
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SHP2
Phosphatase
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Cancer
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SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC50 value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity .
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- HY-149388
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Microtubule/Tubulin
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Cancer
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Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
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- HY-147858
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PROTACs
EGFR
Apoptosis
|
Cancer
|
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 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-116505
-
|
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JAK
|
Cancer
|
|
JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM) .
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-
- HY-144335
-
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DNA Alkylator/Crosslinker
|
Cancer
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|
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
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-
- HY-153699
-
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SHP2
|
Cancer
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|
SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .
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-
- HY-N10876
-
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Others
|
Others
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8-epi-Chlorajapolide F (compound 1) a sesquiterpene that can be isolated from the aboveground part of the Chloranthus japonicus. 8-epi-Chlorajapolide has few cytotoxic to human cancer cell lines NCI-H460 and SMMC-7721 (IC50s>50 μg/mL) .
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-
- HY-147725
-
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Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization .
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-
- HY-147727
-
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Microtubule/Tubulin
|
Cancer
|
|
Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization .
|
-
- HY-132295
-
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ZN-c3
|
Wee1
|
Cancer
|
|
Azenosertib (ZN-c3) is a selective, orally active inhibitor for Wee1 inhibitor (IC50=3.9 nM). Azenosertib exhibits antitumor activity .
|
-
- HY-124242
-
|
|
Drug Derivative
|
Cancer
|
|
(S)-α-Methylbenzyl ricinoleamide (compound (R,S)-3d) is a fatty acid amide. (S)-α-Methylbenzyl ricinoleamide shows antiproliferative activity, inhibits the growth of human ovarian cancer cells NCI-ADR/RES and glioma cells U251 with GI50s of 1.9 μg/mL and 3.6 μg/mL, respectively .
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-
- HY-N12232
-
|
|
Parasite
Bacterial
|
Infection
Cancer
|
|
Carbazomycin D exhibits antituberculosis and antimalarial activities, that inhibits Plasmodium falciparum with an IC50 > 10 μg/mL, inhibits Mycobacterium tuberculosis with MIC of 25 μg/mL. Carbazomycin D exhibits cytotoxicity in cell MCF-7, KB, NCI-H187 and Vero, with IC50s of 21.3, 33.2, 12.9, and 34.3 μg/mL, respectively .
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-
- HY-157673
-
|
16:1 PE
|
Phosphatase
Apoptosis
|
Cancer
|
|
1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
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-
- HY-W779529
-
|
2'-Acetylneriifolin
|
Na+/K+ ATPase
|
Cancer
|
|
Cerberin is a cardiac glycoside that has been found in C. odollam and has cytotoxic and cardiac modulatory activities. It is cytotoxic to KB and NCI H187 cancer cells (IC50s=1.92 and 1.24 μg/mL).1 Cerberin inhibits Na+/K+-ATPase, increasing intracellular sodium levels and action potential duration in cardiac cells.
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-
- HY-119694
-
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Others
|
Cancer
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|
Rotenolone is an antiproliferative agent. Rotenolone shows antiproliferative activity against the ovarian cancer A2780, breast cancer BT-549, prostate cancer DU 145, NSCLC NCI-H460, and colon cancer HCC-2998 cell lines, with IC50s of 0.95, 1.6, 2.7, 2.0, and 2.9 μM, respectively .
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-
- HY-117440
-
|
|
Kinesin
|
Cancer
|
|
4'-Methoxy-S-trityl-L-cysteinol is an allosteric inhibitor of vertebrate Kinesin Spindle Protein (KSP). 4'-Methoxy-S-trityl-L-cysteinol significantly enhances its inhibitory activity against NCI60 tumor cells by modifying the trityl and cysteine groups. Its EC50 for bipolar spindle formation is 28 μM, showing stronger inhibitory potency than the parent molecule and monastrol.
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-
- HY-146132
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-55 (Compound 8a) is a potent EGFR inhibitor with IC50 values of 70 nM and 3.9 nM against EGFR WT and EGFR L858R/T790M, respectively. EGFR-IN-55 arrests NCI-H1975 cells in G0/G1 phase and shows anticancer activity .
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-
- HY-149265
-
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Reactive Oxygen Species (ROS)
TrxR
Ferroptosis
Apoptosis
|
Cancer
|
|
ROS-generating agent 1 (Compound 2c) covalently modifies the Sec-498 residue of TrxR to generate ROS. ROS-generating agent 1 reduces intracellular TrxR protein level. ROS-generating agent 1 results in ROS-dependent apoptosis and ferroptosis of NCI-H460 cells. ROS-generating agent 1 has anti-cancer activities .
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-
- HY-115950
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively .
|
-
- HY-168180
-
|
|
Wee1
|
Cancer
|
|
WEE1-IN-11 (Compound 13) is a potent CDK2 inhibitor with an IC50 of 2.0 nM. WEE1-IN-11 inhibits NCI–H446, A427, OVCAR3, C33A,and WiDr cells with IC50s of 93.9, 34.5, 86.7, 23.1, and 85 nM, respectively .
|
-
- HY-168013
-
|
|
Ras
|
Cancer
|
|
KRASG12C IN-14 (compound 15) is an inhibitor targeting the KRAS G12C mutation. KRASG12C IN-14 inhibits CYPA-dependent KRAS-BRAF with an IC50 of 0.002 μM. KRASG12C IN-14 inhibits ERK phosphorylation in NCI-H358 cells with an IC50 of 0.002 μM .
|
-
- HY-145312
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13) .
|
-
- HY-W231513
-
|
|
MASTL
Ser/Thr Protease
Aurora Kinase
|
Cancer
|
|
MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
|
-
- HY-W778562
-
|
|
Others
|
Cancer
|
|
10-Deacetyl-13-oxobaccatin III is an taxane that can be isolated from Taxus sumatrana. 10-Deacetyl-13-oxobaccatin III (30 μg/mL) shows cytotoxicity against A498, NCI-H226, A549, PC-3 cells, with inhibition a rate of 29.7%, 49.2%, 43.9%, 65.3% .
|
-
- HY-125010
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Dicycloplatin is a DNA damage inducer. Dicycloplatin induces DNA damage by activating biphosphorylated checkpoint kinase 2 (CHK2), breast cancer 1 (BRCA1) and triphosphorylated p53. Dicycloplatin can induce cell cycle arrest, inhibit proliferation and lead to apoptosis in prostate cancer PC3 cells and lung cancer NCI/H446 cells. Dicycloplatin can be used in cancer researchr .
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-
- HY-169310
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
|
-
- HY-159119
-
|
|
Dihydroorotate Dehydrogenase
Ferroptosis
|
Cancer
|
|
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
|
-
- HY-115907
-
|
|
Ras
ERK
Apoptosis
|
Cancer
|
|
K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
|
-
- HY-112616
-
|
|
NAMPT
Drug-Linker Conjugates for ADC
|
Cancer
|
|
NAMPT inhibitor-linker 2 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-4 consists of an NAMPT inhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC50s of <7 pM and 40 pM, respectively.
|
-
- HY-112615
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
NAMPT inhibitor-linker 1 is a agent-linker conjugates for ADC, composed of an NAMPT inhibitor as a payload, and a linker. ADC-3 consists of an NAMPT inhibitor-linker 1 and an anti-c-Kit monoclonal antibody, exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526 cells, with IC50s of <3 pM and 9 pM, respectively.
|
-
- HY-15990
-
|
|
HSP
|
Cancer
|
|
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC50 = 0.15 μM, NCI-N87 IC50 = 0.066 μM). CH5164840 (16) is orally active (t1/2 = 2.64 h) with potent antitumor efficacy .
|
-
- HY-157292
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
2E-3-F16 is a anticancer agent. 2E-3-F16 exhibits tumor cell selectivity between NCI-H446 cancer cells and HBE cells. 2E-3-F16 enhances the sensitivity of A549 cells to Cisplatin (HY-17394) .
|
-
- HY-162540
-
|
|
ATTECs
Discoidin Domain Receptor
|
Cancer
|
|
LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader. LLC355 efficiently degrades DDR1 protein with a DC50 value of 150.8 nM in non-small cell lung cancer NCI-H23 cells. LLC355 induces DDR1 degradation via lysosome-mediated autophagy. LLC355 potently inhibits cancer cell tumorigenicity, migration, and invasion .
|
-
- HY-N4201
-
|
|
EGFR
Src
|
Cancer
|
|
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 .
|
-
- HY-161995
-
|
|
Apoptosis
Necroptosis
FGFR
VEGFR
PDGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
|
-
- HY-155522
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
|
-
- HY-N9475
-
|
|
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Betulonaldehyde is a pentacyclic triterpenoid that can be isolated from Diospyros filipendula. Betulonaldehyde has antiplasmodial activity (IC50: 3.36 µg/mL). Betulonaldehyde has cytotoxic to NCI H187 lung cancer cells and non-cancerous Vero cells (IC50s: 19.23 and 17.09 µg/mL, respectively). Betulonaldehyde inhibits Phorbol 12-myristate 13-acetate (HY-18739) induced inflammation in mice .
|
-
- HY-136704
-
|
|
Glutaminase
|
Cancer
|
|
GLS1 Inhibitor-1 (Compound 27) is an orally active inhibitor for glutaminase 1 (GLS1) with an IC50 of 0.021 μM. GLS1 Inhibitor-1 inhibits the proliferation of PC-3 with an IC50 of 0.3 nM. GLS1 Inhibitor-1 exhibits antitumor efficacy against NCI-H1703 with GI50 of 0.011 μM. GLS1 Inhibitor-1 exhibits moderate pharmacokinetic characteristics .
|
-
- HY-163453
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-19 (Compound 10e) is a potent inhibitor of HER2 and EGFR with IC50 values of 0.87 respectively and 3.5 nM. HER2-IN-19 has potent inhibitory activity against tumor cells, IC50 NCI-N87 = 1.63 nM, IC50 BT474= 15.17 nM, IC50 BaF3-HER2YVMA = 1.49 nM .
|
-
- HY-148278
-
|
|
SOS1
Ras
|
Cancer
|
|
BI-0474 is a potent KRAS G12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models .
|
-
- HY-131339
-
SP-96
1 Publications Verification
|
Aurora Kinase
|
Cancer
|
|
SP-96 is a highly potent, selective and non-ATP-competitive Aurora B (IC50=0.316 nM) inhibitor and shows >2000 fold selectivity against FLT3 and KIT. SP-96 shows selective growth inhibition in NCI60 screening, incluing MDA-MD-468 (GI50=107 nM). SP-96 can be used for the research of triple negative breast cancer (TNBC) .
|
-
- HY-170508
-
|
|
Cytochrome P450
|
Endocrinology
|
|
Aromatase-IN-4 (Compound 6a) is an aromatase (Aromatase) inhibitor. Aromatase-IN-4 exhibits anticancer activity, with GI50 values of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM, and 1.56 μM against the MDAMB-231, MCF-7, A-549, NCI-H23, and A-498 cell lines, respectively . Aromatase-IN-4 effectively blocks aromatase-dependent estrogen production .
|
-
- HY-162577
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. FGFR-IN-14 inhibits FGFR1, FGFR2, FGFR3 and FGFR2 V564F gatekeeper mutant with IC50s of 46, 41, 99, and 62 nM, respectively. FGFR-IN-14 strongly suppresses NCI-H520 lung cancer cells, SNU-16 and KATO III gastric cancer cells proliferation with IC50s of 19, 59, and 73 nM, respectively .
|
-
- HY-172970
-
|
|
CDK
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
HQY1428 is an orally active CDK12 inhibitor. HQY1428 inhibits DNA replication, causes G2/M arrest in SKOV3 cells, induces DNA double-strand breaks and apoptosis. HQY1428 has anti-tumor activity in the SKOV3 xenograft mouse model. HQY1428 combined with the HER2 inhibitor Lapatinib (HY-50898) in the NCI-N87 xenograft mouse model produces a synergistic therapeutic effect .
|
-
- HY-170343
-
|
|
PROTACs
SWI/SNF Complex
|
Cancer
|
|
PROTAC SMARCA2 degrader-32 (Compound 27) is the degrader for SMARCA2 with a DC50 of 1.3 nM. PROTAC SMARCA2 degrader-32 inhibits the proliferation of lung cancer cell NCI-H838 with a GI50 of 34 nM . (Pink: ligand for target protein SMARCA2 ligand-11 (HY-170349); Black: linker (HY-W895794); Blue: ligand for E3 ligase VHL (HY-170348))
|
-
- HY-12892
-
SKI-178
1 Publications Verification
|
SphK
Apoptosis
|
Cancer
|
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines .
|
-
- HY-168577
-
|
|
Ras
EGFR
|
Cancer
|
|
KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM .
|
-
- HY-155391
-
|
|
Carbonic Anhydrase
P-glycoprotein
Wnt
β-catenin
|
Cancer
|
|
hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity. hCA/Wnt/β-catenin-IN-1 also inhibits Wnt/β-catenin signaling pathway. hCA/Wnt/β-catenin-IN-1 inhibits cancer cell viability, including the NCI/ADR-RES DOX-resistant cell line .
|
-
- HY-N10503
-
|
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
Cancer
|
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
- HY-N8470
-
|
NSC 204855; U 40615
|
Bacterial
|
Infection
|
|
Steffimycin B is an anthracycline bacterial metabolite originally isolated from Streptomyces. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine.2 Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells (IC50s=3.5, 6.75, 3.28, and 10.5 μM, respectively). It is active against M. tuberculosis (MIC=5.2 nM), B. cereus (MIC=1.56 μg/mL), and P. falciparum (IC50=2.19 μM).
|
-
- HY-170995
-
|
|
PROTACs
ROR
Apoptosis
|
Cancer
|
|
PROTAC ROR1 degrader-1 (Compound 11d) is a PROTAC degrader for pseudokinase ROR1 that degrades ROR1 in NSCLC cells with a DC50s of 40-80 nM. PROTAC ROR1 degrader-1 causes the cleavage of PARP and induces apoptosis in NCI-H23 . (Pink: ligand for target protein ROR1 ligand-1 (HY-170996); Black: linker (HY-W014787); Blue: ligand for VHL E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- HY-N10564
-
|
|
P-glycoprotein
|
Cancer
|
|
8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX .
|
-
- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
|
-
- HY-173488
-
|
|
NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
|
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
|
-
- HY-N10621
-
|
|
Others
|
Cancer
|
|
3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM .
|
-
- HY-129900
-
|
|
Bacterial
Fungal
|
Infection
|
|
(-)-Luteoskyrin has a wide range of antibacterial activity, such as against malaria (with an IC50 of 0.51 μg/mL), tuberculosis (MIC of 6.25 μg/mL), and it also shows antibacterial effects (with MIC for Gram-positive bacteria ranging from 0.39 to 1.56 μg/mL, and for Gram-negative bacteria from 3.13 to 12.50 μg/mL), as well as antifungal activity (with MIC against plant pathogens ranging from 3.13 to 50μg/mL). (-)-Luteoskyrin exhibits cytotoxicity against NCI-H187 cells, with an IC50 range of 0.16–17.99 μg/mL .
|
-
- HY-138098
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
|
-
- HY-172113
-
|
|
PROTACs
YAP
c-Myc
|
Cancer
|
|
H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC50 of 3 nM, and exhibits good affinity to TEAD2, TEAD3, and TEAD4 with Ki of 2.0, 3.6 and 1.6 nM. H122 downregulates the expression of Myc. H122 inhibits the cell growth of MSTO-211H and NCI-H226 with IC50 of 21.3 nM and 0.6 nM, and exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-151525); Black: linker (HY-W573128); Blue: ligand for E3 ligase Cereblon (HY-W087383))
|
-
- HY-170403
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .
|
-
- HY-153713
-
|
|
PROTACs
c-Myc
Apoptosis
|
Cancer
|
|
MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research . MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
|
-
- HY-158342
-
|
|
PROTACs
YAP
|
Cancer
|
|
PROTAC TEAD degrader-1 (Compound 27) is a PROTAC degrader for transcriptional enhanced associate domain (TEAD). PROTAC TEAD degrader-1 selectively degrades the Flag TEAD2 in a ubiquitin proteasome-dependent manner, with a DC50 of 54.1 nM in 293T cells, inhibits proliferation of NF2-deficient NCI-H226 with an IC50 of 0.21 μM, and regulates expressions of yes associated protein (YAP) target genes. (Pink: TEAD ligand (HY-158400); Black: linker (HY-W008474); Blue: E3 ligase ligand (HY-W087383))
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-
- HY-173619
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-160 (Compound R12) is an EGFR inhibitor (IC50 values are 1.62, 0.49 and 0.98 μM for EGFR WT, EGFR T790M and EGFR L858R/T790M/C797S, respectively). EGFR-IN-160 induces G2/M and S phase arrest and apoptosis in NCI-H522 cells, and has anticancer activity. EGFR-IN-160 has antioxidant effects against DPPH (IC50: 12.11 µM) and H2O2 (IC50: 8.89 µM) .
|
-
- HY-171754
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
LM-305 is an anti-G protein-coupled receptor class 5 member D (GPRC5D) antibody-drug conjugate (ADC). LM-305 consists of Anti-GPRC5D Antibody (HY-P991197) and VcMMAE (HY-15575). LM-305 exhibits potent cytotoxicity against multiple myeloma cells (NCI-H929 and MM.1R) with IC50 values ranging from 0.1 to 0.3 nM. LM-305 can be used in the study of GPRC5D-related relapsed and refractory multiple myeloma (RRMM) .
|
-
- HY-147697
-
|
|
Histone Demethylase
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC50 of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity .
|
-
- HY-168012
-
|
|
Ras
Phosphatase
|
Cancer
|
|
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
|
-
- HY-155816
-
|
|
PROTACs
|
Cancer
|
|
PROTAC NSD3 degrader-1 (compound 56) is a PROTAC targeting to Nuclear receptor binding SET domain protein NSD3. PROTAC NSD3 degrader-1 specifically induces NSD3 degradation with DC50 values of 1.43 and 0.94 μM in lung cancer cells NCI-H1703 and A549, respectively. PROTAC NSD3 degrader-1 suppresses the methylation of H3K36, induces apoptosis, and causes cell-cycle arrest. PROTAC NSD3 degrader-1 also downregulates the expression of NSD3-associated genes such as CDC25A, ALDH1A1, and IGFBP.
|
-
- HY-169921
-
|
|
c-Myc
Apoptosis
|
Cancer
|
|
c-Myc inhibitor 15 (Compound A5) is a selective c-Myc inhibitor that exerts anticancer effects by disrupting the interaction between c-Myc and Max, leading to the degradation of c-Myc protein and the induction of apoptosis. Its IC50 values are 4.08 μM and 7.86 μM in A549 and NCI-H1299 lung cancer cell lines, respectively, demonstrating strong cytotoxic activity. In a syngeneic tumor model, c-Myc inhibitor 15 exhibited outstanding antitumor efficacy, achieving a tumor growth inhibition rate of 76.4% and significantly reducing c-Myc protein expression levels. c-Myc inhibitor 15 holds promise for research related to c-Myc-driven lung cancers .
|
-
- HY-173250
-
|
|
PROTACs
Ras
Apoptosis
|
Cancer
|
|
YN14-H is a PROTAC degrader targeting KRAS G12C. YN14-H inhibits cell growth in NCI-H358 and MIA PaCa-2 cells (IC50 values of 0.042, 0.021 μM, DC50 values of 28.9, 18.1 nM, respectively). YN14-H significantly induces apoptosis and inhibits migration. YN14-H demonstrates favorable pharmacokinetic properties and excellent antitumor activity in vivo. (Structure Note: Pink: target protein ligand (HY-173252); Blue: E3 ligase ligand (HY-125905); Black: linker (HY-Y0840); E3 ligase ligand + linker (HY-173253) .
|
-
- HY-157432
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
|
-
- HY-170978
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-11 (Compound C3) is an orally active PROTAC degrader for CDK9 with DC50 of 1.09 nM. PROTAC CDK9 degrader-11 exhibits cytotoxicity in multi small cell lung cancer cell with IC50 of nanomolar levels. PROTAC CDK9 degrader-11 arrests cell cycle at G0/G1 phase, inhibits the cell invasion in DMS114 and DMS53 cell. PROTAC CDK9 degrader-11 exhibits antitumor efficacy in NCI-H446 xenograft mouse models .(Pink: ligand for target protein CDK9 ligand 3 (HY-170979); Black: linker; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 56 (HY-W247437))
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-
- HY-N2609
-
|
|
COX
CCR
NF-κB
|
Inflammation/Immunology
Endocrinology
|
|
7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid, which can be isolated from Glycyrrhiza uralensis. 7,4'-Dihydroxyflavone is eotaxin/CCL11 inhibitor and CBR1 inhibitor (IC50=0.28 μM). 7,4'-Dihydroxyflavone has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production . 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM .
|
-
- HY-168597
-
|
|
FGFR
Apoptosis
VEGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-3 (Compound 8m) is a dual inhibitor of FGFR1/VEGFR2. FGFR1/VEGFR2-IN-3 exhibits anti-proliferative and anti-migratory activities against cancer cells, and is capable of inducing cell apoptosis .
|
-
- HY-164392
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D1161
-
|
NCI 240899
|
Fluorescent Dyes/Probes
|
|
True Blue (NCI 240899) is a fluorescent dye, as neuronal retrograde tracer (excitation wavelength 395-425 nm, barrier filter 450 nm). True Blue can label neuron and has no effects on neuronal survival .
|
| Cat. No. |
Product Name |
Type |
-
- HY-157673
-
|
16:1 PE
|
Drug Delivery
|
|
1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2055
-
|
|
Peptides
|
Endocrinology
|
|
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P990506
-
|
NCI m971
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
|
Anti-Siglec-2/CD22 Antibody (NCI m971) is a humanized antibody expressed in CHO cells that targets Siglec-2/CD22. Anti-Siglec-2/CD22 Antibody (NCI m971) features a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 146.64 kDa. The isotype control for Anti-Siglec-2/CD22 Antibody (NCI m971) can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
|
-
- HY-P990507
-
|
NCI m972
|
Inhibitory Antibodies
|
Inflammation/Immunology
|
|
The Anti-Siglec-2/CD22 Antibody (NCI m972) is a humanized antibody expressed in CHO, targeting Siglec-2/CD22. The Anti-Siglec-2/CD22 Antibody (NCI m972) has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 144.3 kDa. The isotype control for Anti-Siglec-2/CD22 Antibody (NCI m972) can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
|
-
- HY-P991462
-
|
|
CD38
|
Cancer
|
|
GBR-1342 is a human bispecific antibody (bsAb) targeting CD38 & CD3. GBR-1342 inhibits the activity of Daudi, RAJI, RPMI8226, IM-9, and NCI-H929 cancer cell lines. GBR-1342 can be used in myeloma research .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0840
-
-
-
- HY-N2039
-
-
-
- HY-N14255
-
-
-
- HY-N14280
-
-
-
- HY-N8900
-
-
-
- HY-N3443
-
-
-
- HY-125730
-
-
-
- HY-N10307
-
-
-
- HY-N12004
-
-
-
- HY-N12231
-
-
-
- HY-N10877
-
-
-
- HY-N7302
-
-
-
- HY-145379
-
-
-
- HY-N2039R
-
-
-
- HY-117872
-
-
-
- HY-N10876
-
-
-
- HY-N12232
-
-
-
- HY-W778562
-
-
-
- HY-N4201
-
-
-
- HY-N9475
-
-
-
- HY-N10503
-
|
|
Structural Classification
Flavonoids
Flavones
Plants
Moraceae
|
Tyrosinase
Ras
Raf
MAPKAPK2 (MK2)
Apoptosis
|
|
Norartocarpetin is a tyrosinase inhibitor. Norartocarpetin has strong tyrosinase inhibitory activity with an IC50 value of 0.47 μM. Norartocarpetin as an antibrowning agent can be used for the research of food systems. Norartocarpetin also has a significant anticancer activity in lung carcinoma cells (NCI-H460) with an IC50 value of 22 μM. Norartocarpetin has antiproliferative effects are mediated via targeting Ras/Raf/MAPK signalling pathway, mitochondrial mediated apoptosis, S-phase cell cycle arrest and suppression of cell migration and invasion in human lung carcinoma cells .
|
-
-
- HY-N10564
-
-
-
- HY-N10621
-
|
|
Structural Classification
Combretaceae
Phenols
Polyphenols
Plants
Quisqualis indica Linn.
|
Others
|
|
3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM .
|
-
-
- HY-138098
-
-
-
- HY-N2609
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Leguminosae
Source classification
Phenols
Polyphenols
Plants
Glycyrrhiza uralensis Fisch.
Disease Research Fields
Endocrinology
|
COX
CCR
NF-κB
|
|
7,4'-Dihydroxyflavone (7,4'-DHF) is a flavonoid, which can be isolated from Glycyrrhiza uralensis. 7,4'-Dihydroxyflavone is eotaxin/CCL11 inhibitor and CBR1 inhibitor (IC50=0.28 μM). 7,4'-Dihydroxyflavone has the ability to consistently suppress eotaxin production and prevent dexamethasone (Dex)‐paradoxical adverse effects on eotaxin production . 7,4'-Dihydroxyflavone (7,4'-DHF) inhibits MUC5AC gene expression, mucus production and secretion via regulation of NF-κB, STAT6 and HDAC2.7,4'-Dihydroxyflavone (7,4'-DHF) decreases phorbol 12-myristate 13-acetate (PMA) stimulated NCI-H292 human airway epithelial cell MUC5AC gene expression and mucus production with IC50 value of 1.4 µM .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-147858
-
|
|
|
Alkynes
|
|
PROTAC EGFR degrader 7 (compound 13b) is a potent and selective CRBN-recruiting PROTAC EGFR L858R/T790M degrader, with a DC50 of 13.2 nM. PROTAC EGFR degrader 7 inhibits NCI–H1975 cells proliferation, with an IC50 of 46.82 nM. PROTAC EGFR degrader 7 significantly induces apoptosis and G2/M phase arrest in NCI–H1975 cell. PROTAC EGFR degrader 7 shows antitumor activity, and can be used for non-small cell lung cancer (NSCLC) research . PROTAC EGFR degrader 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-168093
-
|
|
|
Alkynes
|
|
Cetzole (Compound 1) is a ferroptosis inducer that induces cell death through ROS accumulation. The CC50 values of Cetzole for NCI-H522, NCI-H522 GFP-SCL7A11 #8, NCI-H522 RV-GFP, HT-1080, NARF2, and MDA-MB-231 are 2.56, 10.31, 2.71, 3.07, 14.9, and 6.28 μM, respectively. Cetzole holds potential for research in the field of cancer .
|
-
- HY-159119
-
|
|
|
Alkynes
|
|
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-157673
-
|
16:1 PE
|
|
Phospholipids
|
|
1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine (16:1 PE) is a phosphatidylethanolamine that can enhance PP2A and PTP1B activities in malignant pleural mesothelioma cells. 1,2-Dipalmitoleoyl-sn-glycero-3-phosphoethanolamine induces apoptosis of NCI-H28 malignant pleural mesothelioma cells .
|
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