Search Result
Results for "
A375 melanoma
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0150
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Nicotinamide
Maximum Cited Publications
89 Publications Verification
Niacinamide; Nicotinic acid amide
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Environmental Pollutants
Endogenous Metabolite
Sirtuin
HBV
Organoid
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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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-
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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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-
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- HY-B0078
-
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Imidazole Carboxamide
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Nucleoside Antimetabolite/Analog
Apoptosis
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Cancer
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Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC50 of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma .
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-
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- HY-N0351
-
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trans-4-Hydroxycinnamic acid
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Endogenous Metabolite
Bacterial
Apoptosis
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Inflammation/Immunology
Cancer
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p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .
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-
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- HY-15816A
-
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BVD-523 hydrochloride; VRT752271 hydrochloride
|
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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-
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- HY-147268
-
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RAF/KIN_2787
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Raf
p38 MAPK
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Cancer
|
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Exarafenib (RAF/KIN_2787) is an orally-available, selective pan-RAF inhibitor. Exarafenib is effective in RAF-dependent cancers, including all classes of BRAF alterations. Exarafenib suppresses MAPK signaling in RAF-dependent melanoma cell lines. Exarafenib has anticancer activity .
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- HY-122506
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|
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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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-
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- HY-N6843
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-
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- HY-Y1177
-
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Phenyl disulfide
|
PI3K
Akt
mTOR
Ferroptosis
Apoptosis
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
|
Cancer
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|
Diphenyl disulfide (Phenyl disulfide) is an organic disulfide compound. Diphenyl disulfide inhibits the PI3K/AKT/mTOR pathway, and induces ferroptosis (ferroptosis), apoptosis (apoptosis) and autophagy (autophagy) in cancer cells. Diphenyl disulfide downregulates GPX4 expression, inhibits NRF2 phosphorylation, induces lipid peroxidation, promotes xCT ubiquitination, induces proteolytic cleavage of p21 Bax into p18 Bax, and suppresses cell proliferation and viability. Diphenyl disulfide can be used in research related to melanoma and breast cancer .
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-
-
- HY-12538
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-
-
- HY-12842
-
|
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IAP
Survivin
Apoptosis
Caspase
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Inflammation/Immunology
Cancer
|
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UC-112 is a XIAP inhibitor with anticancer activity. UC-112 selectively downregulates and degrades survivin via the ubiquitin-mediated proteasomal degradation pathway. UC-112 reduces XIAP levels in in vivo tumor models. UC-112 activates caspase-3/7 and caspase-9, and induces cancer cell apoptosis. UC-112 is applicable to studies on melanoma, prostate cancer and cancer-related research .
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-
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- HY-118119
-
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PGE synthase
YB-1
Apoptosis
JAK
STAT
TGF-β Receptor
TGF-beta/Smad
PI3K
Akt
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Cancer
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CAY10526 is an inhibitor of Y-box binding protein 1 (YB-1) and microsomal prostaglandin E2 synthase 1 (mPGES1). CAY10526 inhibits the production of PGE2 by suppressing YB-1 and mPGES1. CAY10526 induces cell apoptosis (apoptosis) and inhibits the JAK/STAT, TGF-β/Smad3 and PI3K/AKT signaling pathways. CAY10526 can be used in research related to melanoma, prostate cancer, esophageal adenocarcinoma, T-cell lymphoma, etc .
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- HY-148819A
-
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ADC Payload
Topoisomerase
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Cancer
|
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NH2-bicyclopentane-7-MAD-MDCPT hydrochloride (Formula I) is a topoisomerase I (TOP1) inhibitor. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is applicable to the synthesis of the ADC ABBV-969. NH2-bicyclopentane-7-MAD-MDCPT hydrochloride is used in research on lung adenocarcinoma and melanoma .
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-
-
- HY-156418
-
|
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DNA/RNA Synthesis
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
|
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KY386 is a DHX33 helicase inhibitor with an IC50 of 0.019 μM. KY386 inhibits the cell viability of various cancer cells. KY386 induces ferroptosis in cancer cells, and induces apoptosis in some cancer cell lines. KY386 increases the intracellular levels of ROS, LPO and Fe 2+, and decreases the level of GSH in cancer cells . KY386 inhibits the growth of gastric cancer and colon cancer xenografts in nude mice. KY386 is applicable to the related research on liver cancer, lung cancer, pancreatic cancer, colorectal cancer, gastric cancer, breast cancer, leukemia, renal cancer, prostate cancer, esophageal cancer, cervical cancer, brain cancer (glioblastoma) and melanoma .
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- HY-137487
-
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PROTACs
Raf
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Cancer
|
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PROTAC BRAF-V600E degrader-1 (compound 23) is a potent PROTAC BRAF-V600E degrader whlie no degradation activity against BRAF-WT. PROTAC BRAF-V600E degrader-1 exhibits Kd values of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS) and inhibits the growth of melanoma cells . (In the molecular structure, target protein ligand: BI-882370 (HY-107779), red part; E3 ubiquitin enzyme ligand: Pomalidomide (HY-10984), blue part; PROTAC linker: G007-LK (HY-12438), black part.
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- HY-N0351R
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trans-4-Hydroxycinnamic acid (Standard)
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Reference Standards
Endogenous Metabolite
Bacterial
Apoptosis
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Inflammation/Immunology
Cancer
|
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p-Coumaric acid (Standard) is the analytical standard of p-Coumaric acid. This product is intended for research and analytical applications. p-Coumaric acid (trans-4-Hydroxycinnamic acid) is an isomer of cinnamic acid with oral activity. p-Coumaric acid inhibits cell proliferation and promotes apoptosis. p-Coumaric acid has antibacterial, anti-inflammatory, antioxidant and anti-tumor activities .
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- HY-112062
-
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DNA/RNA Synthesis
Apoptosis
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Cancer
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POL1-IN-1 is a class of RNA polymerase I inhibitors with broad-spectrum antiproliferative activity against tumor cells, while selectively inhibiting RNA polymerase I transcription. By blocking RNA polymerase I-mediated rRNA synthesis, POL1-IN-1 impairs ribosome biogenesis, thereby inhibiting tumor cell proliferation and inducing apoptosis. POL1-IN-1 can be used for the research of malignant tumors .
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- HY-175370
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PROTACs
RIP kinase
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Cancer
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PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma. (Pink: RIPK1-ligand-2: HY-175371, Blue: (S,R,S)-AHPC-Me: HY-112078, Pink + Black: RIPK1 ligand-Linker Conjugate-1: HY-175374, Black: Bispiperidin-piperazin-acetater: HY-175373) .
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- HY-117996
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CRM1
Apoptosis
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Cancer
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KPT-251 is an orally active chromosome region maintenance 1 protein (CRM1) inhibitor. KPT-251 induces cancer cell apoptosis and shows antileukemic activity .
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-
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- HY-12847
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Raf
Src
Apoptosis
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Cancer
|
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CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .
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- HY-161108
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PROTACs
Checkpoint Kinase (Chk)
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Cancer
|
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PROTAC Chk1 degrader-1 is a Chk1-targeting PROTAC.PROTAC Chk1 degrader-1 recruits the Cereblon E3 ligase to induce ubiquitination and proteasomal degradation of Chk1.PROTAC Chk1 degrader-1 exhibits Chk1 degradation activity in malignant melanoma cells without showing a hook effect.PROTAC Chk1 degrader-1 can be used for the research of malignant melanoma .
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- HY-15816R
-
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BVD-523 (Standard); VRT752271 (Standard)
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ERK
Reference Standards
|
Cancer
|
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Ulixertinib (Standard) is the analytical standard of Ulixertinib. This product is intended for research and analytical applications. 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-107767
-
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DC 81
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Antibiotic
Apoptosis
DNA/RNA Synthesis
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Cancer
|
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Antibiotic DC 81 (DC 81), an antitumor antibiotic produced by Streptomyces species, is a PBD (pyrrolo[2,1-c][1,4]benzodiazepine). Antibiotic DC 81 is potent inhibitor of nucleic acid synthesis. Antibiotic DC 81 can recognize and bind to specific sequences of DNA and form a labile covalent adduct .
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- HY-179505
-
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YAP
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Cancer
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OPN-9652 is a potent, orally active, and covalent TEAD inhibitor (MSTO-211H TEAD IC50 = 0.005 µM) targeting the central palmitate binding pocket of TEADs. OPN-9652 reduces TEAD-dependent reporter activity and expression of TEAD targets (CTGF and CYR61). OPN-9652 resensitizes drug-tolerant SOX10 KO cells to BRAFi + MAPKi. OPN-9652 delays the onset of tumor resistance to BRAFi + MEKi from minimal residual disease (MRD) in a BRAF mutant A375 xenograft mouse model. OPN-9652 can be used for melanoma research .
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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-16461
-
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(-)-Solenopsin A
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Akt
Ribosomal S6 Kinase (RSK)
PI3K
PDK-1
FOXO
Mitophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
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Cardiovascular Disease
|
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Solenopsin ((-)-Solenopsin A) is an ATP-competitive and selective Akt-1 inhibitor with an IC50 of 5-10 μM, and also acts as an RSK1 inhibitor. Solenopsin inhibits the activities of PDK1 in lipid rafts, downregulates PI3K, blocks PI3K-dependent generation of 3-phosphoinositides, and suppresses the phosphorylation of FOXO1a. Solenopsin induces Mitophagy and ROS production, reduces mitochondrial oxygen consumption, and exhibits antiproliferative and antiangiogenic activities. Solenopsin can be used in research related to hyperproliferative skin diseases and malignant diseases .
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- HY-179717
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PROTACs
Microphthalmia Associated Transcription Factor (MITF)
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Cancer
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WZS0347 is a MITF PROTAC degrader. WZS0347 effectively reduces the MITF protein levels in several melanoma cell lines, including B16F10, A375, and GAK. WZS0347 significantly inhibits the proliferation, migration, and invasion of melanoma cells. WZS0347 can be used for research on melanoma (Pink: MITF ligand: (HY-179718); Blue: CRBN ligand: (HY-131717); Black: linker: (HY-22391)) .
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- HY-175496
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Ceramidase
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Inflammation/Immunology
|
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Acid Ceramidase-IN-3 is a acid ceramidase (aCDase) inhibitor. Acid Ceramidase-IN-3 inhibits the enzymatic activity of aCDase with a pIC 50 of 8.5 in enzymatic assays and 6.8 in A375 melanoma cellular assays. Acid Ceramidase-IN-3 promotes HSC inactivation, as measured by a dose-dependent
reduction in COL1A1 and ACTA2. Acid Ceramidase-IN-3 inhibits aCDase activity in HSCs, promotes HSC inactivation and suppresses YAP/TAZ nuclear localization. Acid Ceramidase-IN-3 increases Dynein/Kinesin (NDE1, NDEL1.
KIF3B, KIF15) while decreases several proteins involved with signaling pathway (SARM1, RGAP1,
PDGF-D,PDGFR-B). Acid Ceramidase-IN-3 can be used for the study of fibrotic diseases .
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- HY-177914
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MEK
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Cancer
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MEK-IN-7 (compound WX086) is potent, orally active and selective MEK inhibitor (MEK1 IC50 = 29.62 nM). MEK-IN-7 inhibits HT29 and A375 cell proliferation with IC50s of 0.62 and 0.40 nM. MEK-IN-7 inhibits tumor growth in a HL-29 xenograft mouse model. MEK-IN-7 can be used for melanoma and colon cancer research .
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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-153735
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PROTACs
ERK
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Cancer
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ERK-CLIPTAC is a ERK CLIPTAC (click chemistry-synthesized proteolysis-targeting chimera) degrader. ERK-CLIPTAC forms intracellularly via click chemistry from ERK1/2-IN-14 (HY-175578) and Tz-thalidomide (HY-101460). The formed ERK-CLIPTAC recruits the E3 ubiquitin ligase CRBN to ERK1/2, thereby inducing ubiquitination and subsequent degradation of ERK1/2. Due to its lack of cell permeability, ERK-CLIPTAC cannot induce ERK1/2 degradation in cells. ERK-CLIPTAC can be used in research related to melanoma and colorectal cancer .
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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 RAF inhibitor. RAF-IN-1 suppresses RAF enzymatic activity and reduces cancer cell proliferation. RAF-IN-1 can be used for cancer research .
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- HY-120281
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MEK
PI3K
Akt
Apoptosis
Caspase
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Cancer
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ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research .
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- HY-B0078R
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Imidazole Carboxamide (Standard)
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Apoptosis
Nucleoside Antimetabolite/Analog
Reference Standards
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Cancer
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Dacarbazine (Standard) is the analytical standard of Dacarbazine. This product is intended for research and analytical applications. Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC50 of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma .
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- HY-157800
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TRX-E-009-1
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Microtubule/Tubulin
Apoptosis
PARP
Caspase
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Cancer
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Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity .
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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-179012
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APC
CDK
Raf
Akt
HSP
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Cancer
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CDC20/HSP90-IN-1 (Compound 2b) is a Cdc20/Hsp90 inhibitor with a Kd of 16.2 μM for Cdc20 and a Kd of 0.241 μM for Hsp90α. CDC20/HSP90-IN-1 exerts potent antitumor activity through reducing p53-mediated Cdc20, upregulating Bim, downregulating Cyclin B1 expression, and disturbing B-Raf and AKT pathways via destroying Hsp90 chaperone function. CDC20/HSP90-IN-1 overcomes Vemurafenib (HY-12057)-induced resistant melanoma .
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- HY-178336
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VD/VDR
HDAC
Microtubule/Tubulin
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Inflammation/Immunology
Cancer
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AC-340 is a potent hybrid VDR agonist/HDAC inhibitor. AC-340 superinduces VDR target genes (e.g., CYP24A1) and inhibits HDAC6 (IC50 = 0.37 μM) with ~10-fold selectivity over HDAC2. AC-340 induces VDR hyperagonism by causing widespread protein hyperacetylation (e.g., tubulin and H3K9/K27), which leads to elevated H3K27 acetylation on VDR target genes. AC-340 can be used for melanoma cancer research .
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- HY-175828
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DNA/RNA Synthesis
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Cancer
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DHPS-IN-2 is an allosteric deoxyhypusine synthase (DHPS) inhibitor with an IC50 of 70 nM and a Kd of 26.4 μM. DHPS-IN-2 significantly suppresses melanoma cell migration and invasiveness in vitro and exhibits potent anti-tumor efficacy in an A375 cell zebrafish xenograft model. DHPS-IN-2 can be used for the study of melanoma .
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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-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-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-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-174274
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ERK
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Cancer
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ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAF V600E mutant cells (IC50=250 nM in A375 cells). ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma .
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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-117707
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Raf
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Cancer
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EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
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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-178382
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Raf
Bcr-Abl
P-glycoprotein
PERK
Apoptosis
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Cancer
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BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma .
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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-120454
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MEK
Potassium Channel
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Cancer
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G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
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- HY-173558
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PD-1/PD-L1
HDAC
Apoptosis
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Cancer
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PD-L1/HDAC3-IN-1 (PH3) is a dual PD-L1/HDAC3 Inhibitor with IC50 values of 89.4 nM and 107 nM for PD-1/PD-L1 and HDAC3, respectively. PD-L1/HDAC3-IN-1 induces cell apoptosis and arrests cell cycle at G0/G1 phase. PD-L1/HDAC3-IN-1 shows anticancer activity both in vivo and in vitro .
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- HY-158023
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- HY-180329
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Ligands for E3 Ligase
ERK
Raf
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CG 858-Neg (compound 13) is a negative control for Thalidomide (HY-14658)-derived PROTAC degraders, targeting BRAF and BRAF V600E with Ki values of 9.5 nM and 14.4 nM, respectively. CG 858-Neg inhibits downstream ERK phosphorylation and suppresses BRAF V600E-driven melanoma (e.g., A375 cells, IC50=492 nM) and colorectal cancer (e.g., HT-29 cells, IC50=459 nM) cells. CG 858-Neg can be used in research related to melanoma and colorectal cancer .
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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-118912
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Orphan Nuclear Receptor
MDM-2/p53
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Inflammation/Immunology
Cancer
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BMH-9 (Compound Z54) is a modulator for nuclear receptor subfamily 2, group F, member 6 (NR2F6) (also known as nuclear orphan receptor Ear2) . BMH-9 is an activator for p53 signaling pathway through interaction with DNA. BMH-9 inhibits proliferation of human cancer cells, exhibits antitumor efficacy in NOD-SCID mouse models .
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- HY-182538
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MEK
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Cancer
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G-963 is an allosteric inhibitor of mitogen-activated protein kinase kinase (MEK) with a MEK1 IC50 of 0.012 μM. G-963 interacts with Ser212 of MEK and exhibits potent antiproliferative activity against HCT116 colon cancer cells (EC50 = 0.120 μM) and A375 melanoma cells (EC50 = 0.025 μM). G-963 can be used for the research of colon cancer, melanoma .
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- HY-123859
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Casein Kinase
FLT3
CDK
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Neurological Disease
Inflammation/Immunology
Cancer
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SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .
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- HY-D3141
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Cancer
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DR probe is a "dual-key-and-lock" fluorescent probe designed based on the Resorufin (HY-123533) scaffold (Ex/Em = 647 nm/663-738 nm). DR probe can be sequentially activated by hydrogen peroxide to form the intermediate SR, which acts as a tyrosinase substrate to trigger a fluorescence turn-on signal. DR probe can distinguish normal melanocytes from melanoma cells. DR probe supports cell imaging and can be applied to mouse melanoma models to achieve melanoma diagnosis with higher accuracy and lower false-positive rates. DR probe is applicable to relevant research on melanoma .
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- HY-B0150G
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Niacinamide; Nicotinic acid amide
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Endogenous Metabolite
Sirtuin
HBV
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Infection
Cancer
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Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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-P992392
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Transmembrane Glycoprotein
Akt
mTOR
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Cancer
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JM1-24-3 is an anti-MUC18 mouse monoclonal antibody with a Kd value of 1.60e-9 M. JM1-24-3 reduces the phosphorylation levels of p-AKT (Ser473) and p-mTOR (Ser2448) in a time-dependent manner. JM1-24-3 exhibits anticancer activity against melanoma. JM1-24-3 can be used in studies related to metastatic melanoma .
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- HY-181726
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PERK
P-glycoprotein
Apoptosis
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Cancer
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BRAFV600E/ABL2-IN-2 is a dual BRAFV 600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV 600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma .
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- HY-181545A
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NO Synthase
IFNAR
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Cancer
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nNOS-IN-2 trihydrochloride is a blood-brain barrier-permeable nitric oxide synthase (nNOS) inhibitor. nNOS-IN-2 trihydrochloride exhibits Ki values of 1.7 nM and 2.3 nM against human and rat nNOS, respectively, and shows high selectivity for human eNOS and iNOS. nNOS-IN-2 trihydrochloride also effectively reduces PD-L1 expression in human melanoma cells under both basal conditions and IFN-γ exposure. nNOS-IN-2 trihydrochloride can be used for the study of melanoma and related signaling pathways .
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- HY-D3140
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Fluorescent Dye
Tyrosinase
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Cancer
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MB-m-borate is a double-locked near-infrared fluorescence-activated probe (Ex/Em ≈ 647 nm/684 nm). MB-m-borate undergoes cascade activation by hydrogen peroxide and tyrosinase to release the fluorophore methylene blue, thereby generating a fluorescence activation response. MB-m-borate enables precise detection of melanoma in melanoma cells and mouse models. MB-m-borate can be used for melanoma research .
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- HY-182899
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PERK
Ras
COX
PD-1/PD-L1
Apoptosis
DNA/RNA Synthesis
Mitochondrial Metabolism
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Cancer
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DPAP is a p-ERK1/2 inhibitor with an IC50 of 7.85 μM against p-ERK1/2. DPAP inhibits the expression of p-MEK1/2 and disrupts the Ras-ERK signaling pathway. DPAP inhibits the expression of COX-2 in nerve cells. DPAP damages DNA and mitochondria, induces Apoptosis via the mitochondrial pathway, and upregulates PD-L1. DPAP inhibits melanoma metastasis and angiogenesis, and inactivates spinal microglia and astrocytes. DPAP exhibits anti-melanoma activity and can be combined with anti-PD-1 monoclonal antibodies to modify anti-tumor effects. DPAP is applicable for the research of melanoma .
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- HY-181131
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CDK
Apoptosis
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Cancer
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Anticancer agent 300 (compound P14) is a CCND1, CDK4, CDK6, and CCNE1 modulator, with anti-proliferative, cell-cycle modulatory, senescence-inducing, and apoptosis-inducing activity. Anticancer agent 300 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma .
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- HY-183806
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Others
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Cancer
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ANTXR1-IN-1 is a ANTXR1 inhibitor with a Ka of 2.88 μM for hANTXR1, and exhibits anti-tumor cell activity. ANTXR1-IN-1 undergoes acylation with Ser229 of ANTXR1, thereby inhibiting tumor cell proliferation. ANTXR1-IN-1 induces G2/M phase arrest and apoptosis in tumor cells. ANTXR1-IN-1 can be used for research on melanoma, non-small cell lung cancer, hepatocellular carcinoma, and colorectal cancer .
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- HY-18658B
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NVP-HDM201 succinate; HDM201 succinate
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MDM-2/p53
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Cancer
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Siremadlin (NVP-HDM201) succinate is an MDM2 inhibitor and cell cycle regulator. Siremadlin succinate blocks the p53-binding pocket of MDM2, inhibits MDM2-mediated ubiquitination and degradation of p53, thereby activating the p53 pathway in p53 wild-type cells. Siremadlin succinate can be used in the research of cutaneous melanoma .
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- HY-181130
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CDK
Apoptosis
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Cancer
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Anticancer agent 299 (compound P12) is a cell-cycle inhibitor, senescence inducer, apoptosis inducer, and antiproliferative agent. Anticancer agent 299 exhibits selective activity against cancer cells with minimal effects on non-tumoral chondrocyte cells at relevant concentrations. Anticancer agent 299 can be used for the research of ER+/HER2− breast cancer and BRAF-mutant melanoma .
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- HY-182780
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Drug Derivative
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Cancer
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LSPN925 is an anticancer agent. LSPN925 exhibits cytotoxic and antiproliferative activities against tumor cells. LSPN925 has predicted oral bioavailability, low risks of hepatotoxicity and acute toxicity, and no risk of cardiotoxicity. LSPN925 can be used for the research of ovarian cancer, melanoma and breast cancer .
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- HY-P991896
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AT14-012
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Transmembrane Glycoprotein
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Inflammation/Immunology
Cancer
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AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
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- HY-180419
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ERK
Apoptosis
c-Myc
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Inflammation/Immunology
Cancer
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SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup .
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- HY-181529
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VDAC
PERK
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Cancer
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NCATS-SM0225 is an endoplasmic reticulum-associated degradation (ERAD) inhibitor and a direct binder of VDAC1, VDAC2 and VDAC3. NCATS-SM0225 exhibits an IC50of 1.02 μM for ERAD and a Kd of 3.13 μM for human VDAC1 binding. NCATS-SM0225 disrupts cellular calcium homeostasis, enhances VDAC1-IP3R coupling and activating PERK. NCATS-SM0225 selectively kills cancer cells, exhibits tumor growth inhibitory effects in melanoma xenograft models. NCATS-SM0225 can be used for research on multiple cancers including melanoma, as well as the molecular mechanisms of ERAD and calcium homeostasis regulation .
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| Cat. No. |
Product Name |
Type |
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- HY-D3141
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Fluorescent Dyes
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DR probe is a "dual-key-and-lock" fluorescent probe designed based on the Resorufin (HY-123533) scaffold (Ex/Em = 647 nm/663-738 nm). DR probe can be sequentially activated by hydrogen peroxide to form the intermediate SR, which acts as a tyrosinase substrate to trigger a fluorescence turn-on signal. DR probe can distinguish normal melanocytes from melanoma cells. DR probe supports cell imaging and can be applied to mouse melanoma models to achieve melanoma diagnosis with higher accuracy and lower false-positive rates. DR probe is applicable to relevant research on melanoma .
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- HY-B0150G
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Niacinamide; Nicotinic acid amide
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Fluorescent Dyes
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Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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-D3140
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Fluorescent Dyes
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MB-m-borate is a double-locked near-infrared fluorescence-activated probe (Ex/Em ≈ 647 nm/684 nm). MB-m-borate undergoes cascade activation by hydrogen peroxide and tyrosinase to release the fluorophore methylene blue, thereby generating a fluorescence activation response. MB-m-borate enables precise detection of melanoma in melanoma cells and mouse models. MB-m-borate can be used for melanoma research .
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| Cat. No. |
Product Name |
Type |
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- HY-B0150G
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Niacinamide; Nicotinic acid amide
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Biochemical Assay Reagents
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Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P992392
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Transmembrane Glycoprotein
Akt
mTOR
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Cancer
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JM1-24-3 is an anti-MUC18 mouse monoclonal antibody with a Kd value of 1.60e-9 M. JM1-24-3 reduces the phosphorylation levels of p-AKT (Ser473) and p-mTOR (Ser2448) in a time-dependent manner. JM1-24-3 exhibits anticancer activity against melanoma. JM1-24-3 can be used in studies related to metastatic melanoma .
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(5)
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- HY-P991896
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AT14-012
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Transmembrane Glycoprotein
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Inflammation/Immunology
Cancer
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AT1412 is a CD9-binding antibody. AT1412 binds to the tetraspanin protein CD9 and modulates CD9 function by enhancing T cell adhesion to endothelial cells (HUVECs) and transendothelial migration. AT1412 binds to B-ALL cell lines but not to T-ALL. AT1412 induces antibody-dependent cellular cytotoxicity in B-ALL cell lines. AT1412 binds to melanoma cells, B-ALL, gastric cancer, colorectal cancer, and pancreatic cancer cells [1] .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0150G
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Niacinamide; Nicotinic acid amide
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Endogenous Metabolite
Sirtuin
HBV
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Infection
Cancer
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Nicotinamide (GMP) (Niacinamide (GMP)) is the GMP level of Nicotinamide (HY-B0150). GMP guidelines are used to produce Nicotinamide (GMP). GMP small molecules works appropriately as an auxiliary reagent for cell research manufacture. 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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