Search Result
Results for "
A375 cells
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N10335
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FAK
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Inflammation/Immunology
Cancer
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Harringtonolide is a potent RACK1 inhibitor (IC50=39.66 μM in A375 cells). Harringtonolide inhibits the epithelial-mesenchymal transition (EMT) process and cell proliferation by affecting the interaction between FAK and RACK1. Harringtonolide has plant growth inhibitory, antiviral, anti-inflammatory, and antiproliferation activities .
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- HY-153469
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ADC Cytotoxin
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Cancer
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Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
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- HY-16667
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Early 2 Factor (E2F)
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Cancer
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HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells.
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- HY-120607
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Parasite
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Infection
Cancer
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Chevalone C, a meroterpenoid fungal metabolite, shows antimalarial activity with IC50 value of 25.00 μg/mL. Chevalone C has anti-proliferative activity on colon HCT116, liver HepG2 and melanoma A375 cancer cell lines .
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- HY-153864
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PROTACs
MEK
ERK
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Cancer
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PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
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- HY-162900
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HSP
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Cancer
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HSP90-IN-32 is a Hsp90 C-terminal inhibitor that displays anti-proliferative activities against SKMel173, SKMel103, SKMel19 and A375 cells with IC50 values of 1.01 μM, 0.782 μM, 0.607 μM and 1.413 μM , respectively. HSP90-IN-32 is promising for research of anti-cancer agents .
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- HY-144271
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Raf
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Cancer
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RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively .
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- HY-153445A
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MEK
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Cancer
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MEK-IN-6 hydrate (compound 69) is a MEK inhibitor. MEK-IN-6 hydrate has an IC50 of 2 nM for A375 cells .
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- HY-144269
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Raf
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Cancer
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SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
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- HY-161882
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PROTACs
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Cancer
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PROTAC SMARCA2 degrader-8 (compound 1) is a potent SMARCA2 degrader with a DC50 of 28nM in A375 cells .
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- HY-122506
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STAT
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Cancer
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Salviolone is a natural diterpenoid derivative that can against melanoma cells. Salviolone exhibits a pleiotropic effect against melanoma by hampering cell cycle progression, STAT3 signaling, and malignant phenotype of A375 melanoma cells .
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- HY-N3838
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Others
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Cancer
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Epitulipinolide diepoxide (compound 9) is a natural compound isolated from the herbs of Liriodendron chinense (Hemsl.) Sarg. Epitulipinolide diepoxide displays cytoxicity in A375 cells, with the IC50 of 52.03 μM .
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- HY-171186
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Drug Derivative
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Cancer
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EAPB0202 is an imidazolium and quinoxaline derivative. EAPB0202 shows significant cytotoxicity to A375 human melanoma cell line with an IC50 of 2.35 μM. EAPB0202 can be used in the study of cancer .
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- HY-128224
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Others
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Cancer
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Antiproliferative agent-13 (compound 16c) shows an antiproliferative activity against human A375 cells with an IC50 value of 32.7 nM. Antiproliferative agent-13 can be used for the research of cancer .
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- HY-169298
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Ferroptosis
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Cancer
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Ferroptosis-IN-15 (compound 12) is a potent inhibitor of ferroptosis, with the EC50s of 0.76 and 0.67 μM in A375 cells and 786-O cells, respectively.Ferroptosis-IN-15 is a potential iron chelator and radical trapping antioxidant .
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- HY-13323
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DNA/RNA Synthesis
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Cancer
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CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
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- HY-12842
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IAP
Apoptosis
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Cancer
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UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
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- HY-153445
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ERK
MEK
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Cancer
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MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer .
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- HY-13323A
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DNA/RNA Synthesis
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Cancer
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CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
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- HY-147734
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Calcium Channel
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Cancer
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Calpain Inhibitor-2 (compound 5) is a peptide inhibitor of μ-calpain (Ki=9 nM). Calpain Inhibitor-2 exhibits antiproliferative activity against melanoma cell lines (A-375 and B-16F1) and PC-3 prostate cancer cells in vitro .
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- HY-N0201
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TNF Receptor
Toll-like Receptor (TLR)
JAK
STAT
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Cancer
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Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
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- HY-147788
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Dihydroorotate Dehydrogenase
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Cancer
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hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .
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- HY-N7484
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Fungal
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Cancer
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(−)-Voacangarine is an indole alkaloid, which exhibits cytotoxic effects against cancer cells HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 of 5~20 mg/mL. (−)-Voacangarine inhibits the cultivation of Saccharomyces cerevisiae wildtype and repair-deficient mutants .
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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-15816A
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BVD-523 hydrochloride; VRT752271 hydrochloride
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ERK
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Cancer
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Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-13323R
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DNA/RNA Synthesis
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Cancer
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CX-5461 (Standard) is the analytical standard of CX-5461. This product is intended for research and analytical applications. CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively .
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- HY-15816
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BVD-523; VRT752271
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ERK
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Cancer
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Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
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- HY-N12834
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Others
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Inflammation/Immunology
Cancer
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Ecdysoside B (compound 6b) is a pregnanoside compound isolated from the plant Ecdysanthera rosea. Ecdysoside B and its derivatives and isomers shows anticancer, immunosuppressive and anti-inflammatory activities. Ecdysoside B shows cytotoxicity to a variety of human tumor cell lines, including PANC-1 (human pancreatic cancer cells), A375 (human melanoma cells) and U87 (brain glioma U87 cells). Ecdysoside B can be used for research in the areas of cancer, immunomodulation and anti-inflammato .
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- HY-N0201R
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TNF Receptor
Toll-like Receptor (TLR)
JAK
STAT
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Cancer
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Atractylenolide I (Standard) is the analytical standard of Atractylenolide I. This product is intended for research and analytical applications. Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
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- HY-158027
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Raf
VEGFR
FGFR
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Cancer
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B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer .
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- HY-N13739
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Tyrosinase
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Cancer
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Taraxinic acid can be found in the roots of Taraxacum flavostylum and Taraxacum lucidum. It is a Tyrosinase inhibitor that dose-dependently inhibits Tyrosinase activity, showing approximately 54.5% inhibition at a concentration of 50 μg/mL. Taraxinic acid has an IC50 of 83.2 μM against melanoma cells A375 and HTB140, and an IC50 of 60.4 μM against melanoma cells WM793, with activity being both dose- and time-dependent. Taraxinic acid holds promise for research in the field of anticancer therapy .
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- HY-169086
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PROTACs
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Cancer
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KL-465 is a PROTAC degrader for MAGE-A3, that degrades MAGE-A3 with a DC50 of 2 μM in HeLa cell. KL-465 inhibits viability of MAGE-A3 positive cancer cell HCT116, A375 and HeLa. (Blue: Ligand for E3 ligase (HY-151227); Black: Linker (HY-W679862); Pink: Ligand for target protein (HY-169087))
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- HY-P1726A
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Melanocortin Receptor
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Cancer
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MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
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- HY-164474
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MEK
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Cancer
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DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
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- HY-153341
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PROTACs
Raf
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Cancer
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CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ™) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. CFT1946 can be used in tumor research .
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- HY-169409
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VEGFR
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Cancer
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VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property .
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- HY-161628
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Topoisomerase
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Cancer
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Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
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- HY-153738
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ERK
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Cancer
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ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
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- HY-138098
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Endogenous Metabolite
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Cancer
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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 .
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- HY-121255
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(R)-Cryptopleurine; NSC 19912
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TMV
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Cancer
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(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
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- HY-117991
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VEGFR
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Cancer
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DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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- HY-164781
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-
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- HY-149005
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Histone Methyltransferase
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Cancer
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PRMT5-IN-19 (Compound 41) is an selective orally active non-nucleoside PRMT5 inhibitor with IC50 values of 23.9 nM (radioactive biochemical assay) and 47 nM (AlphaLISA assay). PRMT5-IN-19 can occupy the SAM-binding pocket in PRMT5 and block methyltransferase activity, which displays good selectivity over other PRMTs and PKMTs. PRMT5-IN-19 inhibits cell proliferation by inducing cell apoptosis, and can be used for cancer-related research .
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- HY-163356
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Microtubule/Tubulin
Apoptosis
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Cancer
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Tubulin polymerization-IN-60 (BF3) is a tubulin polymerization inhibitor with anticancer activity. Tubulin polymerization-IN-60 (BF3) belongs to the colchicine binding site inhibitors (CBSIs) and disturbs cell cycle progression leading to G2/M arrest and apoptosis .
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- HY-163595
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Ras
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Cancer
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Pan-RAS-IN-4 (compound 2) is a potent inhibitor of RAS, with the IC50 of < 100 nM for KRAS G12D. Pan-RAS-IN-4 plays an important rile in cancer research .
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- HY-126214S
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DNA/RNA Synthesis
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Cancer
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JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .
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- HY-163858
-
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Haspin Kinase
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Cancer
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Haspin-IN-4 (Compound 60) is a selective inhibitor of Haspin with an IC50 value of 0.01 nM. Haspin-IN-4 possesses anticancer activity and can be used in cancer research .
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- HY-164039
-
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Others
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Cancer
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Talorasib (compound 1-2) has antitumor activity .
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- HY-B0150A
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Niacinamide Hydrochloride; Nicotinic acid amide Hydrochloride
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Sirtuin
Endogenous Metabolite
HBV
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Infection
Cancer
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Nicotinamide Hydrochloride is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide Hydrochloride also inhibits SIRT1. Nicotinamide Hydrochloride increases cellular NAD+, ATP, ROS levels. Nicotinamide Hydrochloride inhibits tumor growth and improves survival. Nicotinamide Hydrochloride also has anti-HBV activity .
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- HY-B0150
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Nicotinamide
Maximum Cited Publications
55 Publications Verification
Niacinamide; Nicotinic acid amide
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Organoid
Endogenous Metabolite
Sirtuin
HBV
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Cancer
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Nicotinamide is a form of vitamin B3 or niacin. Nicotinamide Hydrochloride inhibits SIRT2 activity (IC50: 2 μM). Nicotinamide also inhibits SIRT1. Nicotinamide increases cellular NAD+, ATP, ROS levels. Nicotinamide inhibits tumor growth and improves survival. Nicotinamide also has anti-HBV activity .
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- HY-N0202
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Asterolide
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ERK
Apoptosis
p38 MAPK
Akt
Src
STAT
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
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Atractylenolide II (Asterolide) is a sesquiterpenoid compound. Atractylenolide II can induce G1 phase cell cycle arrest and apoptosis in B16 melanoma cells. Atractylenolide II is an orally effective anticancer agent that can exert anti-melanoma effects by inhibiting the STAT3 signaling pathway. In addition, Atractylenolide II has been shown to ameliorate myocardial fibrosis, oxidative stress, and neuroprotective activity .
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- HY-148174
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DGK
|
Cancer
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JNJ-3790339, a Ritanserin (HY-10791) analog, is a potent and selective diacylglycerol kinase (DGKα) inhibitor with an IC50 of 9.6 μM. JNJ-3790339 has induction of toxicity in malignant cells, and improves ability to upregulate T cell activation .
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- HY-P99115
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ASC 22; KN 035
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PD-1/PD-L1
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Cancer
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Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC50 value of 5.25?nM. Envafolimab has the potential for the research of solid tumors .
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- HY-147356
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DNA/RNA Synthesis
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Cancer
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ERCC1-XPF-IN-2 is a potent ERCC1-XPF endonuclease inhibitor with an IC50 value of 0.6 µM. ERCC1-XPF-IN-2 shows activity in nucleotide excision repair, cisplatin enhancement and γH2AX assays .
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- HY-148713
-
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Apoptosis
|
Cancer
|
Anti-CSCs agent-1 is a potent anti-CSCs agent. Anti-CSCs agent-1 inhibits cell growth and cell migration. Anti-CSCs agent-1 induces Apoptosis. Anti-CSCs agent-1 inhibits the viability of CSCs. Anti-CSCs agent-1 enhances the production of ROS in CSCs. Anti-CSCs agent-1 shows antitumor activity .
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- HY-145702
-
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MEK
ERK
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Cancer
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
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- HY-157979
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Aquaporin
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Cancer
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AQP3-IN-1 (compounds 3) is an AQP3 inhibitor with a IC50 value of 8.91 μM. AQP3-IN-1 inhibits cell proliferation of melanoma cells .
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- HY-146276
-
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HDAC
CDK
Apoptosis
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Cancer
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CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1726A
-
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Melanocortin Receptor
|
Cancer
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MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses the induced hyperalgesia in female mice, with no effect in male mice.
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99115
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ASC 22; KN 035
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PD-1/PD-L1
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Cancer
|
Envafolimab (ASC 22; KN 035) is a recombinant protein of a humanized single-domain anti- PD-L1 antibody. Envafolimab is created by a fusion of the of anti-PD-L1 domain with Fc fragment of human IgG1 antibody. Envafolimab blocks interaction between PD-L1 and PD-1 with an IC50 value of 5.25?nM. Envafolimab has the potential for the research of solid tumors .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-126214S
-
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JH-RE-06-d6 is deuterium labele JH-RE-06. JH-RE-06, a potent REV1-REV7 interface inhibitor (IC50=0.78 μM; Ki=0.42 μM), targets REV1 that interacts with the REV7 subunit of POLζ. JH-RE-06 disrupts mutagenic translesion synthesis (TLS) by preventing recruitment of mutagenic POLζ. JH-RE-06 improves chemotherapy .
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