Search Result
Results for "
Leukemia model
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-148422
-
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Eukaryotic Initiation Factor (eIF)
Apoptosis
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Cancer
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Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .
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- HY-U00442
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CTX1
1 Publications Verification
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MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system .
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- HY-N2108
-
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ADC Cytotoxin
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Cancer
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7-Ethylcamptothecin is one of camptothecin analogues. camptothecin (CPT), a cytotoxic alkaloid isolated from Camptotheca acuminata, is shown to have strong antitumor activity against L1210 leukemia and Walker 256 carcinosarcoma models .
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- HY-136360
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MI-3454
2 Publications Verification
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Epigenetic Reader Domain
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Cancer
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MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .
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- HY-112316
-
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Epigenetic Reader Domain
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Cancer
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BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
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-
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- HY-111209
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S14161
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PI3K
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Cancer
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Pichromene (S14161) is an anticancer agent and weak PI3K inhibitor. Pichromene can effectively inhibit tumor growth in leukemia mouse models and can be used in cancer research .
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-
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- HY-149539
-
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FLT3
RET
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Cancer
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PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
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- HY-114162B
-
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Epigenetic Reader Domain
Apoptosis
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Cancer
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VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
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-
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- HY-N12108
-
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Phosphatase
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Infection
Inflammation/Immunology
Cancer
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Forphenicine is a bacterial metabolite that is found in S. fulvoviridis and an inhibitor of alkaline phosphatase. Forphenicine inhibits the growth of HL-60 leukemia cells at 10 µM. Forphenicine also increases survival in a guinea pig model of experimental autoimmune encephalomyelitis (EAE) .
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-
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- HY-133760
-
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MDM-2/p53
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Cancer
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MI-888 is an orally active MDM2 inhibitor with a Ki of 0.44 nM. MI-888 can inhibit the MDM2-p53 interaction. MI-888 has favorable pharmacokinetic properties and anti-tumor activity .
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- HY-100688
-
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Dihydroorotate Dehydrogenase
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Cancer
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ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models .
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-
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- HY-W016794
-
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Reactive Oxygen Species
Apoptosis
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Cancer
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NSC3852 exhibits anti-proliferative activity against cancer cell MCF-7. NSC3852 promotes the ROS generation, DNA damage, and apoptosis in MCF-7. NSC3852 exhibits anti-tumor against leukemia in mouse model
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- HY-P99272
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BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
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CXCR
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Cancer
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Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
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- HY-B0722
-
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Endogenous Metabolite
Reactive Oxygen Species
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Metabolic Disease
Cancer
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Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
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- HY-129331
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Antibiotic
Bacterial
Fungal
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Infection
Cancer
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Neothramycin A is an antibiotic, which can be isolated from Streptomyces. Neothramycin A exhibits board spectrum antimicrobial activity, inhibits Staphylococcus aureus, Klebsiella pneumoniae, Escherichia coli W677, and Saccharomyces cerevisia with MIC of 25-50 μg/mL. Neothramycin A exhibits antitumor efficacy against leukemia in mouse models .
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- HY-155556
-
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ClpP
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Cancer
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ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
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- HY-148813
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PROTACs
STAT
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Cancer
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AK-2292 is a potent and selective STAT5 PROTAC degrader, with a DC50 of 0.10 μM. AK-2292 induces degradation of STAT5A/B proteins in vitro and in vivo. AK-2292 can induce tumor regression in acute myeloid leukemia and chronic myeloid leukemia xenograft mouse models . AK-2292 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-162658
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HDAC
Apoptosis
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Cancer
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Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models .
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- HY-10082A
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(E)-PAN-811; (E)-NSC# 663249; (E)-OCX191
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DNA/RNA Synthesis
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Cancer
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(E)-3-AP is the E configuration of 3-AP. 3-AP is a potent ribonucleotide reductase inhibitor. 3-AP shows anti-proliferative activity. 3-AP shows anticancer activity in L1210 leukemia model. 3-AP inhibits RR activity and DNA synthesis .
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- HY-112037
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IACS-10759
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Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
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Cancer
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IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research .
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- HY-112316A
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Epigenetic Reader Domain
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Cancer
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(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome .
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- HY-112037A
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IACS-10759 hydrochloride
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Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
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Cancer
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IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research .
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- HY-163803
-
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HDAC
DNA Methyltransferase
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Cancer
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CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models .
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- HY-P1709
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Bacterial
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Infection
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Protactin is a pentapeptide lactone produced by Streptomyces cucumeris strain L703-4 (ATCC 53784) with significant antioxidant properties. Protactin can be converted to actinomycin Zp by ferrocyanide oxidation. Actinomycin Zp exhibits potent antibacterial activity in vitro and has significant antitumor effects against P-388 leukemia in a mouse model .
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- HY-N2108R
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ADC Cytotoxin
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Cancer
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7-Ethylcamptothecin (Standard) is the analytical standard of 7-Ethylcamptothecin. This product is intended for research and analytical applications. 7-Ethylcamptothecin is one of camptothecin analogues. camptothecin (CPT), a cytotoxic alkaloid isolated from Camptotheca acuminata, is shown to have strong antitumor activity against L1210 leukemia and Walker 256 carcinosarcoma models .
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- HY-160018
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Epigenetic Reader Domain
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Cancer
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BAY-155 is a potent and selective menin-MLL tool inhibitor, with an IC50 of 8 nM. BAY-155 leads to a strong expression down-regulation of the MEIS1 gene and up-regulation of CD11b and MNDA genes. BAY-155 shows anti-proliferative effects in AML/ALL (acute myeloid/lymphoblastic leukemia) models .
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- HY-B0722R
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Endogenous Metabolite
Reactive Oxygen Species
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Metabolic Disease
Cancer
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Histamine (dihydrochloride) (Standard) is the analytical standard of Histamine (dihydrochloride). This product is intended for research and analytical applications. Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
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- HY-170574
-
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Molecular Glues
Ser/Thr Kinase
Apoptosis
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Cancer
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CQ627 is a molecular glue targeting the degradation of RIOK2. It effectively induces the degradation of RIOK2 in the MOLT4 leukemia cell line via the ubiquitin-proteasome system (UPS) by recruiting the E3 ubiquitin ligase RNF126, with a DC50 value of 410 nM. CQ627 dose-dependently induces apoptosis in MOLT4 leukemia cells, blocks their cell cycle in the G2/M phase, and exhibits antiproliferative activities in various cancer cell lines. CQ627 also demonstrates in vivo anticancer activity in a MOLT4 xenograft mouse model .
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- HY-129752
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Antibiotic
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Cancer
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Piperafizine B exhibits slightly cytotoxicity in moser cells, P388 cells and Vincristine (VCR) (HY-N0488)-resistant P388 cells (IC50s is 23.8, 22.6 and 23.7 μg/mL, respectively). Piperafizine B exhibits synergistic effects with Vincristine, enhances the VCR-induced cytotoxicity and ameliorates the leukemia in mouse model .
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- HY-117818
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Antibiotic DC 116
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Antibiotic
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Cancer
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Sapurimycin is an antitumor antibiotic isolated from Streptomyces DO-116 and belongs to the capramycin family. Sapurimycin exhibits potent activity against Gram-positive bacteria and exhibits significant antitumor effects against leukemia P388 and sarcoma 180 in mouse models. In vitro studies have shown that Sapurimycin can induce single-strand breaks in supercoiled plasmid DNA .
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- HY-13905
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HHGV678 mesylate
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Bcr-Abl
c-Kit
PDGFR
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Cancer
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Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .
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- HY-168927
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Apoptosis
Pyroptosis
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Cancer
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Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model .
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- HY-15815
-
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Epigenetic Reader Domain
Apoptosis
CDK
HIV
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Cancer
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Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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- HY-W757743
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ACP-196-d3
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Isotope-Labeled Compounds
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Others
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Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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- HY-13072
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AS-703569; R-763
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Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
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Cancer
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Cenisertib (AS-703569) is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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- HY-169937
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Epigenetic Reader Domain
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Cancer
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(R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
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- HY-164526
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Isocitrate Dehydrogenase (IDH)
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Cancer
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SH1573 is an orally active mIDH2 inhibitor. SH1573 has a strong and selective inhibitory effect on mIDH2 R140Q protein (IC50=4.78 nmol/L), and can effectively reduce the production of the carcinogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum and tumors. SH1573 can be used for the study of acute myeloid leukemia (AML) .
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- HY-17600
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Acalabrutinib
Maximum Cited Publications
24 Publications Verification
ACP-196
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Btk
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Cancer
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Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-18676B
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OSU-T315 analog
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Integrin
Autophagy
Apoptosis
Caspase
PDHK
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Cancer
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ILK-IN-2 (OSU-T315 analog) is an oral PDK2 inhibitor and also an ILK inhibitor, with an IC50 of 0.6 μM. ILK-IN-2 induces cell autophagy and apoptosis, showing anti-tumor activity. ILK-IN-2 directly abolishes AKT activation by preventing AKT from translocating to lipid rafts, triggering Caspase-dependent apoptosis in chronic lymphocytic leukemia (CLL) and extending the lifespan in TCL1 mouse models .
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- HY-143286
-
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PROTACs
FLT3
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Cancer
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PF15 is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 is a high selective FLT3-ITD degrader, with a DC50 of 76.7 nM. PF15 significantly inhibits the proliferation of FLT3-ITD-positive cells, can down-regulate the phosphorylation of FLT3 and STAT5. PF15 also inhibits tumor growth in mouse models and can be used in study of leukemia .
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- HY-P99623
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MGD006; S80880
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CD3
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Cancer
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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- HY-137307
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(22S)-Hydroxycholesterol
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LXR
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Inflammation/Immunology
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Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models .
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- HY-107592
-
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IKK
STAT
Apoptosis
|
Inflammation/Immunology
Cancer
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ACHP (compound 4j) is a selective and orally active IκB kinase inhibitor with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. ACHP can effectively inhibit the STAT3 signaling pathway and induce cancer cell cycle arrest and apoptosis. ACHP shows anti-inflammatory activity in a mouse ear edema model. ACHP can be used in anti-inflammatory and anti-cancer (such as multiple myeloma and leukemia) studies .
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- HY-13072B
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AS-703569 benzoate; R-763 benzoate
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Aurora Kinase
Bcr-Abl
Akt
STAT
FLT3
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Cancer
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Cenisertib (AS-703569) benzoate is an ATP-competitive multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. Cenisertib benzoate induces major growth-inhibitory effects by blocking the activity of several different molecular targets in neoplastic mast cells (MC). Cenisertib benzoate inhibits tumor growth in xenograft models of pancreatic, breast, colon, ovarian, and lung tumors and leukemia .
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- HY-143286A
-
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PROTACs
FLT3
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Cancer
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PF15 TFA is a PROTAC connected by ligands for FLT3 kinase and CRBN. PF15 TFA is a high selective FLT3-ITD degrader,with a DC50 of 76.7 nM. PF15 TFA significantly inhibits the proliferation of FLT3-ITD-positive cells,can down-regulate the phosphorylation of FLT3 and STAT5. PF15 TFA also inhibits tumor growth in mouse models and can be used in study of leukemia .
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- HY-17600R
-
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Btk
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Cancer
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Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-W014109
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(E)-5-(2-Bromovinyl)uracil; BVU
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Others
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Infection
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(E)-5-(2-Bromovinyl)uracil (BVU) is a pyrimidine base and an inactive metabolite of the antiviral agents sorivudine and (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) that may be regenerated to BVDU in vivo. BVU irreversibly inactivates dihydropyrimidine dehydrogenase (DPD) in an NADPH-dependent manner. It enhances the efficacy of the chemotherapeutic agent and DPD substrate 5-fluorouracil (HY-90006) in a P388 murine leukemia model when administered at a dose of 200 μmol/kg, increasing survival time.
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- HY-164689
-
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Proteasome
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Cancer
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Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
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- HY-168493
-
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FLT3
VEGFR
HDAC
STAT
PERK
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Cancer
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FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia .
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- HY-P10415
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hSA(408–423) peptide
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CXCR
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Infection
Inflammation/Immunology
Cancer
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EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
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- HY-158783
-
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Ceramidase
Bcl-2 Family
LPL Receptor
Apoptosis
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Neurological Disease
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SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
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- HY-128724
-
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p97
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Cancer
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CB-5339 is an oral activity potent p97 inhibitor with an IC50 <30 nM. CB-5339 can be used for leukemia research . CB-5339 extracted from WO2015109285A1 compound FF07.
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- HY-159803
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6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin
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Endogenous Metabolite
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Cancer
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IST-622 (6-O-(3-Ethoxypropionyl)-3',4'-O-exo-benzylidenechartreusin) is an anti-tumor agent with significant growth inhibitory activity. IST-622 exhibits significant anti-tumor effects against a variety of mouse tumors such as P388 and L1210 leukemias, B16 melanoma, Lewis lung carcinoma, Colon 26 and Colon 38 adenocarcinomas, and M5076 reticulum cell sarcoma. IST-622 was orally administered and the results showed efficacy in different tumor types. In addition, IST-622 provided significant inhibitory effects against two human tumor xenograft models: large cell lung carcinoma (Lu-116) and gastric adenocarcinoma (St-4). IST-622 also exhibited significant growth inhibitory activity against P388 leukemia in vitro, with a half inhibitory concentration (IC50) more than 20 times lower than CT .
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- HY-137936
-
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Antibiotic
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Infection
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Terrecyclic acid is a sesquiterpene originally isolated from A. terreus with antibiotic and anticancer activity. It is active against S. aureus, B. subtilis, and M. roseus (MICs=25, 50, and 25 μg/mL, respectively). Terrecyclic acid induces a heat shock response, increases levels of reactive oxygen species (ROS), and inhibits NF-κB activity and cell growth in 3T3-Y9-B12 cells.2 In vivo, terrecyclic acid (0.1, 1, and 10 mg/ml) reduces the number of ascitic fluid tumor cells in a mouse model of P388 murine leukemia.
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- HY-155066
-
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PI3K
mTOR
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Cancer
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FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
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- HY-N1181
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-
- HY-161615
-
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Apoptosis
PROTACs
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Cancer
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PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
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- HY-150772
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Microtubule/Tubulin
HDAC
Apoptosis
Mitochondrial Metabolism
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Cancer
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Tubulin/HDAC-IN-1 is a dual tubulin and HDAC-IN-1 inhibitor through CH/π interaction with tubulin and hydrogen bond interaction with HDAC8. Tubulin/HDAC-IN-1 inhibits tubulin polymerization and selectively inhibits HDAC8 (IC50: 150 nM). Tubulin/HDAC-IN-1 has cytotoxicity against various human cancer cells, also arrests cell cycle in the G2/M phase and induces cell apoptosis. Tubulin/HDAC-IN-1 can be used in the research of hematologic and solid tumors such as neuroblastoma, leukemia .
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- HY-150109
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HDAC
Apoptosis
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Cancer
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Purinostat mesylate is a selective inhibitor of HDAC. Purinostat mesylate inhibits class I and class IIb HDACs with IC50s from 0.81 to 11.5 nM. Purinostat mesylate induces apoptosis and affects cell cycle of LAMA84 and 188 BL-2 cells, and shows potently anti-leukemia effects in vivo. Purinostat mesylate can be used for the research of lymphoblastic leukemia .
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- HY-P99395
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JNJ 56022473; CSL 362
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Interleukin Related
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Cancer
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Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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- HY-N4107
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TGF-beta/Smad
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Infection
Inflammation/Immunology
Cancer
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Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
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- HY-N4107R
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TGF-beta/Smad
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Infection
Inflammation/Immunology
Cancer
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Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10415
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hSA(408–423) peptide
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CXCR
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Infection
Inflammation/Immunology
Cancer
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EPI-X4 (hSA408–423 peptide) is an antagonist for C-X-C motif chemokine receptor 4 (CXCR4) with IC50 of 8.6 μM. EPI-X4 blocks the CXCL12-mediated signaling, inhibits chemokine-mediated migration and invasion of leukemia cell. EPI-X4 exhibits anti-inflammatory activity in mouse model. EPI-X4 exhibits antiviral activity against CXCR4-tropic HIV with IC50 of 8.6 μM .
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- HY-P1709
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Bacterial
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Infection
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Protactin is a pentapeptide lactone produced by Streptomyces cucumeris strain L703-4 (ATCC 53784) with significant antioxidant properties. Protactin can be converted to actinomycin Zp by ferrocyanide oxidation. Actinomycin Zp exhibits potent antibacterial activity in vitro and has significant antitumor effects against P-388 leukemia in a mouse model .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99272
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BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
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CXCR
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Cancer
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Ulocuplumab (Anti-Human CXCR4 Recombinant Antibody/BMS-936564/MDX1338) is a fully human IgG4 anti-CXCR4 antibody. Ulocuplumab induces apoptosis and inhibits CXCL12 mediated CXCR4 activation-migration of chronic lymphocytic leukemia (CLL). Ulocuplumab exhibits antitumor activity in established tumors including acute myeloid leukemia (AML), non-Hodgkin lymphoma (NHL), and multiple myeloma xenograft models .
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- HY-P99623
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MGD006; S80880
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CD3
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Cancer
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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- HY-P99395
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JNJ 56022473; CSL 362
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Interleukin Related
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Cancer
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Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-W757743
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Acalabrutinib-d3 (ACP-196-d3) is the deuterated form of Acalabrutinib (HY-17600). Acalabrutinib (ACP-196) is an orally active, irreversible, highly selective second-generation BTK inhibitor. Acalabrutinib covalently binds to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib shows strong targeting and efficacy in mouse models of chronic lymphocytic leukemia (CLL).
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Cat. No. |
Product Name |
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Classification |
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- HY-158822A
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CpG ODNs
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IMT504 sodium, a non-CpG 24-mer oligodeoxynucleotide, is an immunomodulatory oligonucleotide currently being investigated as a rabies vaccine. IMT504 sodium has been previously proven to be effective in animal models of vaccine potency, chronic lymphocytic leukemia, tissue regeneration, and sepsis.
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- HY-158822
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CpG ODNs
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IMT504, a non-CpG 24-mer oligodeoxynucleotide, is an immunomodulatory oligonucleotide currently being investigated as a rabies vaccine. IMT504 has been previously proven to be effective in animal models of vaccine potency, chronic lymphocytic leukemia, tissue regeneration, and sepsis.
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