Search Result
Results for "
acute leukemias
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-136175
-
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SNDX-5613
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Epigenetic Reader Domain
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Cancer
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Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .
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-
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- HY-P99971
-
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ADC Antibody
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Cancer
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Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen, which present on leukemic myeloblasts of acute myeloid leukemia (AML). Gemtuzumab can be used for synthesis of antibody-drug conjugate (ADC), Gemtuzumab ozogamicin (HY-109539). Gemtuzumab ozogamicin consists of a cytotoxic derivative of Calicheamicin (a cytotoxic antibiotic), and a monoclonal antibody. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia .
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-
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- HY-163328
-
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Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
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Cancer
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DHODH-IN-25 (Compound 25) is an orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 5.4 nM for human DHODH. DHODH-IN-25 can be used for the study of acute myeloid leukemia (AML) .
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-
-
- HY-110071
-
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c-Kit
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Cancer
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APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis .
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-
-
- HY-160174
-
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Bcr-Abl
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Cancer
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BCR-ABL kinase-IN-3 (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research .
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-
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- HY-146002
-
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Isocitrate Dehydrogenase (IDH)
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Cancer
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IDH2R140Q-IN-1 (compound C6) is a potent inhibitor of IDH2 R140Q, with an IC50 of 6.1 nM. IDH2R140Q-IN-1 can be used for the research of acute myeloid leukemia .
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-
-
- HY-135664
-
-
-
- HY-160174A
-
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Bcr-Abl
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Cancer
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BCR-ABL kinase-IN-3 (dihydrocholide) (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research .
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-
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- HY-148036
-
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FLT3
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Cancer
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FLT3-IN-16 is a potent FLT3 inhibitor with an IC50 of 1.1 μM. FLT3-IN-16 can be used for researching acute myeloid leukemia .
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-
-
- HY-163406
-
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Phosphatase
Apoptosis
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Cancer
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PDE1-IN-6 (compound 6c) is a selectivity PDE1 inhibitor with the IC50 of 7.5 nM. PDE1-IN-6 significantly inhibits the proliferation and induced cell apoptosis in Acute myelogenous leukemia cells .
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-
-
- HY-P9963
-
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Anatumomab
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CD19
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Cancer
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Blinatumomab (Anatumomab) is a bispecific monoclonal antibody which can specifically targets the CD19 antigen present on B cells. Blinatumomab can be used for the research of acute lymphoblastic leukemia .
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-
-
- HY-145903
-
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PDGFR
FLT3
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Cancer
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PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
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-
-
- HY-145904
-
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PDGFR
FLT3
|
Cancer
|
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PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
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-
-
- HY-145723
-
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FLT3
FGFR
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Inflammation/Immunology
Cancer
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MAX-40279 is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
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-
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- HY-145723A
-
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FLT3
FGFR
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Inflammation/Immunology
Cancer
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MAX-40279 hydrochloride is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
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- HY-157134
-
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Others
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Cancer
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Y08262 is a potent and selective CBP bromodomain inhibitor. Y08262 selectively inhibits the CBP bromodomain with an IC50 value of 73.1 nM. Y08262 can be used for the research of acute myeloid leukemia (AML) .
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-
-
- HY-145902
-
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PDGFR
FLT3
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Cancer
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PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
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-
-
- HY-145723B
-
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FLT3
FGFR
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Inflammation/Immunology
Cancer
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MAX-40279 hemifumarate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
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-
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- HY-145723C
-
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FLT3
FGFR
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Inflammation/Immunology
Cancer
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MAX-40279 hemiadipate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032) .
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-
-
- HY-N0564
-
-
-
- HY-12344
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UNC2025
2 Publications Verification
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FLT3
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Cancer
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UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
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- HY-123141
-
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Pim
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Cancer
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K00135 is a potent and selective inhibitor of PIM kinases. K00135 inhibits survival and clonogenic growth of acute leukemia cells. K00135 inhibits the phosphorylation of PIM downstream targets .
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- HY-101150
-
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DNA Alkylator/Crosslinker
ADC Cytotoxin
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Cancer
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DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML). DGN462 can be used as a cytotoxic component of antibody-drug conjugates (ADCs) .
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-
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- HY-162386
-
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Others
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Cancer
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UM4118 is a copper ionophore that can initiate a mitochondrial-based noncanonical form of cell death known as cuproptosis. UM4118 exhibits high sensitivity in SF3B1-mutated and adverse risk acute myeloid leukemia (AML), and can be used for AML research .
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- HY-124629
-
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Apoptosis
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Cancer
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DB2313 is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects .
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-
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- HY-141680
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CPS2
1 Publications Verification
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PROTACs
CDK
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Cancer
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CPS2 is a first-in-class, highly potent, selective and irreversible PROTAC CDK2 degrader (IC50= 24 nM). CPS2 can be used for the research of acute myeloid leukemia .
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- HY-109117
-
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ORY-1001
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Histone Demethylase
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Cancer
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Iadademstat (ORY-1001) is a highly potent, orally active and selective LSD1 (KDM1A) inhibitor with antileukemic activity. Iadademstat can be used for relapsed or refractory acute myeloid leukemia research .
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-
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- HY-151634
-
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Syk
STAT
ERK
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Cancer
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Syk-IN-6 is an inhibitor of the lipid-SH2 domain interaction, control the cellular activity of kinases containing SH2 domain. Syk-IN-6 blocks Syk kinase activity, which associated hematopoietic malignancies, including acute myeloid leukemia (AML) .
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-
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- HY-162291
-
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Src
Apoptosis
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Cancer
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Lck-IN-3 (compound 7m) is an LCK inhibitor targeting acute lymphoblastic leukemia (ALL) that inhibits LCK phosphorylation. Lck-IN-3 can induce cell cycle arrest in the G2/M phase, leading to apoptosis in ALL cells .
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- HY-161149
-
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HDAC
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Cancer
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CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells .
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- HY-101266B
-
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DS-3032b; DS-3032 tosylate hydrate
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
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Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis .
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- HY-129592
-
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Apoptosis
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Cancer
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p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
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- HY-112255
-
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Others
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Cancer
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J9 is a small molecule that reverses Dexamethasone (HY-14648) resistance in T-cell acute lymphoblastic leukemia. J9 is lethal to CUTLL1 cells only in the presence of Dexamethasone. J9 inhibits CUTLL1 cell growth with an EC50 of 28 μM in combination with Dexamethasone .
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- HY-149735
-
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Epigenetic Reader Domain
Apoptosis
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Cancer
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BET-IN-20 (compound 10) is an inhibitor of BRD4 BD1 (IC50=1.9 nM) with anticancer activity. BET-IN-20 can promote acute myeloid leukemia (AML) cell apoptosis and arrest the cell cycle in the G0/G1 phase. BET-IN-20 also inhibits c-Myc and CDK6 and enhances PARP cleavage .
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- HY-151560
-
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Dihydroorotate Dehydrogenase
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Cancer
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hDHODH-IN-11 is a potent human dihydroorotate dehydrogenase (hDHODH) inhibitor with an IC50 value of 7.2 nM. hDHODH-IN-11 has low cytotoxicity. hDHODH-IN-11 can be used in research of acute myeloid leukemia (AML) .
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- HY-120395
-
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STAT
Apoptosis
TET Protein
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Inflammation/Immunology
Cancer
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UC-514321, a structural analog of NSC370284 with higher activity, directly targets STAT3/5 and represses TET1 expression, but not TET2 or TET3. UC-514321 has the potential to treat acute myeloid leukemia (AML) both in vitro and in vivo, with low toxicity .
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- HY-149981
-
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P-glycoprotein
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Cancer
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P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia .
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- HY-149031
-
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Dihydroorotate Dehydrogenase
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Cancer
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DHODH-IN-22 is a potent, selective and orally active dihydroorotate dehydrogenase (DHODH) inhibitor with an IC50 value of 0.3 nM. DHODH-IN-22 can be used for researching acute myelogenous leukemia (AML) .
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-
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- HY-P99014
-
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Apoptosis
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Inflammation/Immunology
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Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML) .
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- HY-109539
-
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Antibody-Drug Conjugates (ADCs)
Apoptosis
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Cancer
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Gemtuzumab ozogamicin is an antibody-drug conjugate (ADC) consisting of a humanized immunoglobulin (IgG4) antibody directed against CD33 that is conjugated to the cytotoxic drug Calicheamicin (HY-19609). Calicheamicin is a cytotoxic antibiotic. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia (AML) .
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- HY-P1613
-
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Cyclo(RGDfV); C(RGDfV)
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Integrin
Apoptosis
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Cancer
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Cyclo(Arg-Gly-Asp-D-Phe-Val) (Cyclo(RGDfV)) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia .
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- HY-153857
-
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FLT3
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Cancer
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PHI-101 is an orally active FLT3 inhibitor that overcomes resistance to multiple drug-resistant mutations. PHI-101 potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. PHI-101 has potential for research in relapsed or refractory acute myeloid leukemia (AML) .
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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-P1613A
-
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Cyclo(RGDfV) TFA; C(RGDfV) TFA
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Integrin
Apoptosis
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Cancer
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Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) (Cyclo(RGDfV) (TFA))is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) can be used for the research of acute myeloid leukemia .
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- HY-D0153
-
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Fluorescent Dye
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Cancer
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Tetramethylrhodamine-5-isothiocyanate is a potent fluorescent dye. Tetramethylrhodamine-5-isothiocyanate can be used for label PG-M3 antibody for rapid diagnosis of acute promyelocytic leukemia (APL). Tetramethylrhodamine-5-isothiocyanate can be used as probe to quantify in vivo the biodistribution of PLGA (poly(lactic-co-glycolic) acid) and PLGA/chitosan nanoparticles .
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-
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- HY-138831
-
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HDAC
Apoptosis
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Cancer
|
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AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research .
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-
-
- HY-134481
-
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FLT3
|
Cancer
|
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FLT3-IN-10 (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 has the potential for the research of FLT3-mutated acute myeloid leukemia (AML) .
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-
-
- HY-121725
-
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STAT
|
Cancer
|
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MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines .
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-
-
- HY-P99285
-
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hBU 12
|
ADC Antibody
CD19
|
Others
|
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Denintuzumab (hBU 12) is a recombinant humanized anti-CD19 monoclonal antibody. Denintuzumab can be used as the antibody moiety (ADC antibody) of antibody-drug conjugates to synthesize ADC, Denintuzumab Mafodotin (SGN-CD19A). Denintuzumab Mafodotin can be used in the research of acute lymphoblastic leukemia .
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-
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- HY-12344A
-
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FLT3
|
Cancer
|
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UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
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- HY-127103
-
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Apoptosis
|
Cancer
|
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FB23-2 is a potent and selective inhibitor of mRNA N 6-methyladenosine (m 6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML) .
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-
- HY-141480
-
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GSK-3
Apoptosis
|
Cancer
|
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GSK-3β inhibitor 3 is a potent, selective, irreversible and covalent inhibitor of Glycogen Synthase Kinase 3β (GSK-3β), with an IC50 of 6.6 μM. GSK-3β inhibitor 3 can be used for the research of acute promyelocytic leukemia .
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- HY-162032
-
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FLT3
|
Cancer
|
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FLT3-IN-25 (compound 17) is a potent inhibitor of FLT3, with IC50s of 1.2 nM, 1.4 nM and 1.1 nM for FLT3-WT, FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-25 plays an important role in acute myeloid leukemia (AML) .
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- HY-153953
-
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Bcl-2 Family
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Cancer
|
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Bcl-2-IN-11 (compound 6) is a potent and selective Bcl-2 activity inhibitor, with an IC50 of 0.9 nM. Bcl-2-IN-11 shows weak inhibition of Bcl-xl (IC50 > 1000 nM). Bcl-2-IN-11 can be used for the research of a variety of cancers caused by abnormal overexpression of Bcl-2 family proteins: especially malignant hematologic diseases of acute lymphoid leukemia, etc. Bcl-2-IN-11 can also avoid toxic side effects caused by Bcl-xl inhibition, such as thrombocytopenia .
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- HY-141797
-
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Histone Methyltransferase
PROTACs
|
Cancer
|
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MS33 is a potent WDR5 degrader, with Kds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia .
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- HY-112852A
-
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Src
Apoptosis
|
Cancer
|
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TL02-59 dihydrochloride is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 dihydrochloride inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 dihydrochloride potently suppresses acute myelogenous leukemia (AML) cell growth .
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- HY-112852
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TL02-59
4 Publications Verification
|
Src
Apoptosis
|
Cancer
|
|
TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth .
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- HY-116830
-
BRD0705
1 Publications Verification
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GSK-3
|
Cancer
|
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BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .
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- HY-146886
-
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FLT3
|
Cancer
|
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FLT3-IN-15 is a highly potent and orally active FLT3 inhibitor with IC50s of 0.87 nM and 0.32 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-15 can be used for researching acute myeloid leukemia .
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- HY-144709
-
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FLT3
|
Cancer
|
|
FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
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- HY-144371
-
-
- HY-129079A
-
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DNA Methyltransferase
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Cancer
|
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TFMB-(S)-2-HG is a potent inhibitor of the 5'-methylcytosine hydroxylase TET2. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML) .
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-
- HY-P99412
-
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OSE-127
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Interleukin Related
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Cancer
|
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Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research .
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- HY-123121
-
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Antibiotic
Apoptosis
Bacterial
NF-κB
|
Infection
Inflammation/Immunology
Cancer
|
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Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia .
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- HY-136291
-
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Drug-Linker Conjugates for ADC
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Cancer
|
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Sulfo-SPDB-DGN462 is a agent-linker conjugate for ADC. Sulfo-SPDB-DGN462 consists a toxin DGN462 (HY-101150) conjugated to the cleavable Sulfo-SPDB linker. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML).
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- HY-106218
-
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5-Fluorocyclocytidine; 5'-Fluorocyclocytidine
|
Nucleoside Antimetabolite/Analog
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Cancer
|
|
Flurocitabine (5-Fluorocyclocytidine) is a fluorinated anlydride analog of cytosine arabinoside, partially hydrolysecl in vivo into two active antitumor substances (arabinosyl-tluorocytosine (ara-FC) and arabinosyl-fluorouracil (ara-FU)). Flurocitabine (5-Fluorocyclocytidine) has antitumor activity during phase I studies in acute leukemia and solid tumors .
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-
- HY-P99264
-
|
Humanized Anti-CD22 Recombinant Antibody
|
ADC Antibody
CD22
|
Cancer
|
|
Inotuzumab (Humanized Anti-CD22 Recombinant Antibody) is a humanized IgG4, κ antibody that targets human CD22. Inotuzumab can be linked to a toxic agent ozogamicin as an antibody-drug conjugate (ADC). Inotuzumab can be used for the research of acute lymphoblastic leukemia and non-Hodgkin lymphoma .
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-
- HY-149539
-
|
|
FLT3
RET
|
Cancer
|
|
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-10202
-
|
MLN518; CT53518
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML) . Tandutinib has the ability to cross the blood-brain barrier .
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-
- HY-10202A
-
|
MLN518 hydrochloride; CT53518 hydrochloride
|
FLT3
c-Kit
PDGFR
Apoptosis
|
Cancer
|
|
Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML) . Tandutinib hydrochloride has the ability to cross the blood-brain barrier .
|
-
- HY-142690
-
|
|
HDAC
|
Cancer
|
|
HDAC-IN-27 (Compound 11h) is a potent, selective and orally active HDAC Class I inhibitor, with IC50 values ranging from 0.43 nM to 3.01 nM for HDAC1-3. HDAC-IN-27 shows anti-acute myeloid leukemia (AML) activity .
|
-
- HY-13680
-
|
Dian III; N-Methylisoindigotin; Natura-α
|
Apoptosis
|
Cancer
|
|
Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity .
|
-
- HY-P1923
-
|
L-ASNase
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
L-Asparaginase (L-ASNase) is a deamidating enzyme that catalyses the hydrolysis of L-asparagine and L-glutamine, and can be used for the research of acute lymphoblastic leukemia. L-Asparaginase depletes L-asparagine from plasma resulting in inhibition of RNA and DNA synthesis with the subsequent blastic cell apoptosis .
|
-
- HY-144710
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-144711
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-139481
-
|
|
Btk
|
Infection
Cancer
|
|
TL-895 is a potent, orally active, ATP-competitive, and highly selective irreversible BTK inhibitor with an IC50 and a Ki of 1.5 nM and 11.9 nM, respectively . TL-895 is used be for JAKi-relapsed/refractory myelofibrosis, acute myeloid leukemia, COVID-19 and cancer research .
|
-
- HY-144782
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
|
-
- HY-144779
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
|
-
- HY-144782A
-
|
|
HDAC
Autophagy
|
Cancer
|
|
HDAC10-IN-2 hydrochloride (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 hydrochloride modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
|
-
- HY-50671
-
|
RS 33295-198 trihydrochloride; LY-335979 trihydrochloride
|
P-glycoprotein
|
Cancer
|
|
Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research .
|
-
- HY-15255
-
|
RS 33295-198; LY-335979
|
P-glycoprotein
|
Cancer
|
|
Zosuquidar (LY335979) is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research .
|
-
- HY-148530
-
|
|
PROTACs
CDK
|
Cancer
|
|
YX-2-107 is a PROTAC (IC50= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph + ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph +) acute lymphoblastic leukemia (ALL) .
|
-
- HY-146680
-
|
|
FLT3
RET
CDK
MAP4K
|
Cancer
|
|
FLT3/ITD-IN-4 (Compound 16) is a selective FMS-like tyrosine kinase 3 internal tandem duplications (FLT3-ITD) inhibitor with an IC50 of 2.3 nM. FLT3/ITD-IN-4 can be used for acute myeloid leukemia research .
|
-
- HY-111517
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant .
|
-
- HY-12333
-
|
G-749
|
FLT3
Apoptosis
|
Cancer
|
|
Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML) .
|
-
- HY-144675
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-13 (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 induces differentiation of AML (acute myeloid leukemia) cell lines .
|
-
- HY-144675A
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-13 hydrochloride (compound 7e) is an orally active and potent LSD1 inhibitor, with an IC50 of 24.43 nM. LSD1-IN-13 hydrochloride can activate CD86 expression, with an EC50 of 470 nM. LSD1-IN-13 hydrochloride induces differentiation of AML (acute myeloid leukemia) cell lines .
|
-
- HY-120035
-
|
|
Proteasome
Ribosomal S6 Kinase (RSK)
Apoptosis
|
Cancer
|
|
DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation .
|
-
- HY-147574
-
|
|
TAM Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease .
|
-
- HY-118304
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 inhibits FLT3 autophosphorylation. AKN-028 induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 induces apoptosisby activation of caspase 3. AKN-028 can be used in research of acute myeloid leukemia (AML) .
|
-
- HY-118304B
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 acetate inhibits FLT3 autophosphorylation. AKN-028 acetate induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 acetate induces apoptosisby activation of caspase 3. AKN-028 acetate can be used in research of acute myeloid leukemia (AML).
|
-
- HY-145550
-
|
BI894999
|
Epigenetic Reader Domain
|
Cancer
|
|
Amredobresib is a potent inhibitor of BET. Amredobresib inhibits the binding of bromodomains to acetylated lysines on histone H3 and H4 and thus acts as important regulators of gene transcription. Amredobresib is useful for the research of acute myeloid leukemia (AML) and cancer (extracted from patent WO2019145410A1 and WO2021175824A1) .
|
-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
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 .
|
-
- HY-108263B
-
|
(R)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
|
(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML) .
|
-
- HY-149819
-
|
|
HDAC
CDK
|
Cancer
|
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
|
-
- HY-155529
-
|
|
Pim
|
Cancer
|
|
FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .
|
-
- HY-150797
-
|
QA-68-ZU81
|
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
QA-68 (QA-68-ZU81) is a potent bromodomain-containing protein 9 (BRD9) degrader. QA-68 can inhibit cell cycle progression and cell colony formation. QA-68 has antiproliferative activity against acute myeloid leukemia (AML) cell lines . QA-68 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-129239
-
|
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice .
|
-
- HY-108263A
-
|
(S)-CGP52421
|
FLT3
Drug Metabolite
|
Cancer
|
|
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nM for 13 kinases (VEGFR-2, TRK-A, FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML) .
|
-
- HY-136523
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells .
|
-
- HY-145409
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
SR-0813 is a potent and selective ENL/AF9 YEATS domain inhibitor. SR-0813 has IC50 and EC50 values of 25 nM and 205 nM for ENL YEATS domain, respectively. SR-0813 has IC50 and EC50 values of 311 nM and 76 nM (CETSA) for AF9 YEATS domain, respectively. SR-0813 binds MAP3K19 with over 100-fold lower affinity (Kd=3.5 μM) than ENL YEATS (Kd=30 nM). SR-0813 can be used for the research of acute leukemia .
|
-
- HY-139996
-
|
|
PROTACs
Ligands for E3 Ligase
|
Cancer
|
|
Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC containing Pomalidomide, Dovitinib and connected with CRBN. Pomalidomide-C5-Dovitinib shows enhanced antiproliferative effects against FLT3-ITD+ AML cells. Pomalidomide-C5-Dovitinib induces the degradation of the FLT3-ITD and KIT proteins in a ubiquitin-proteasome-dependent manner and completely blocks their downstream signaling pathway. Pomalidomide-C5-Dovitinib has the potential for the research of FLT3-ITD + acute myeloid leukemia .
|
-
- HY-120877
-
|
|
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively . MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells . MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
|
-
- HY-115906
-
|
|
FLT3
MNK
Apoptosis
|
Cancer
|
|
K783-0308 is a potent and selective dual inhibitor of FLT3 and MNK2 with IC50 values of 680 and 406 nM, respectively. K783-0308 inhibits the growth of MOLM-13 (IC50=10.5 µM) and MV-4-11 (IC50=10.4 µM) cells. K783-0308 promotes acute myeloid leukemia (AML) cell apoptosis and cell cycle arrests in the G0/G1 phase .
|
-
- HY-151194
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1/2-IN-4, a PCPA derivative, is an inhibitor of lysine-specific demethylase 1 (LSD1) and lysine-specific demethylase 2 (LSD2). LSD1/2-IN-4 inhibits LSD1 and LSD2 with Ki values of 0.11 μM and 130 μM, respectively. LSD1/2-IN-4 can be used for the research of several cancers including T-cell acute lymphoblastic leukemia (TALL) .
|
-
- HY-142696
-
|
|
CDK
Pim
Apoptosis
|
Cancer
|
CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .
|
-
- HY-150025
-
|
|
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
(4aS,8aR)-NPD-001 is a potent and allosteric inhibitor of DNMT3A. (4aS,8aR)-NPD-001 inhibits DNMT3A activity by disrupting protein-protein interactions. (4aS,8aR)-NPD-001 induces apoptosis of acute myeloid leukemia (AML) cell lines. (4aS,8aR)-NPD-001 induces differentiation of distinct AML cell lines including cells with mutated DNMT3A R882 .
|
-
- HY-128888B
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
(S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
|
-
- HY-N2517
-
|
|
mTOR
|
Cancer
|
|
Dihydroevocarpine induces cytotoxicity in acute myeloid leukemia via suppressing the mTORC1/2 activity .
|
-
- HY-162350
-
|
|
Endogenous Metabolite
|
Cancer
|
|
TDI-11055 is an inhibitor of the epigenetic reader protein 11-19 leukemia (ENL) YEATS, which drives the oncogenic transcriptional program of acute myeloid leukemia (AML), the hematopoietic malignancy AML .
|
-
- HY-143434
-
|
|
FLT3
|
Cancer
|
|
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) .
|
-
- HY-139877
-
|
|
Others
|
Cancer
|
|
OXS007417 induces differentiation of acute myeloid leukemia cells (EC50 = 48 nM) in vitro and shows antitumor effects in vivo.
|
-
- HY-132969
-
|
|
Others
|
Cancer
|
|
SBP-3264 is a valuable chemical probe for understanding the roles of STK3 and STK4 in acute myeloid leukemia (AML).
|
-
- HY-N1830
-
|
|
|
|
|
3-Epiwilsonine is an alkaloid from Cephalotaxus wilsoniana, exhibits effect on acute and chronic myeloid leukemia and malignant lymphoma .
|
-
- HY-148422
-
|
|
Eukaryotic Initiation Factor (eIF)
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-14572
-
|
SN 27858
|
DNA Alkylator/Crosslinker
Drug Metabolite
|
Cancer
|
|
PR-104A (SN 27858) is the alcohol metabolite of phosphate proagent PR-104. PR-104A is a hypoxia-selective DNA cross-linking agent/DNA-damaging agent and cytotoxin. Antitumor Activity . PR-104A is metabolized under hypoxia by the 1-electron NADPH:cytochrome P450 oxidoreductase. PR-104A can be used for the research of relapsed/refractory T-lineage acute lymphoblastic leukemia (T-ALL) .
|
-
- HY-13701
-
-
- HY-136522
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice .
|
-
- HY-146749
-
|
|
FLT3
Trk Receptor
Apoptosis
|
Cancer
|
|
FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinase inhibitor with the IC50s of 43.8 nM, 97.2 nM, 92.5 nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD and TrKA, respectively. FLT3/TrKA-IN-1 induces cell cycle arrest at the G0/G1 phase as well as apoptosis and shows antiproliferative activity in vitro. FLT3/TrKA-IN-1 has the potential for the research of Acute myeloid leukemia (AML) .
|
-
- HY-150725
-
|
|
IFNAR
TNF Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
ODN 1585 is a potent inducer of IFN and TNFα production. ODN 1585 is a potent stimulator of NK (natural killer) function. ODN 1585 increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 induces regression of established melanomas in mice. ODN 1585 can confer complete protection against malaria in mice. ODN 1585 can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 can be used as a vaccine adjuvant .
|
-
- HY-15229
-
|
SGI-110 sodium; S-110 sodium
|
DNA Methyltransferase
|
Cancer
|
|
Guadecitabine sodium (SGI-110 sodium) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) .
|
-
- HY-13542
-
|
SGI-110
|
DNA Methyltransferase
|
Cancer
|
|
Guadecitabine (SGI-110) is a second-generation DNA methyltransferases (DNMT) inhibitor for research of acute myeloid leukemia (AML) and myelodysplastic syndromes (MDS) .
|
-
- HY-153714
-
|
BNM-1192; Menin-MLL inhibitor 27
|
Epigenetic Reader Domain
|
Cancer
|
|
BN-104 (BNM-1192) can inhibit the Menin-MLL interaction and can be used in cancer research, such as acute myeloid leukemia .
|
-
- HY-13560
-
AVN-944
4 Publications Verification
VX-944
|
Arenavirus
DNA/RNA Synthesis
Apoptosis
Caspase
Bcl-2 Family
|
Infection
Cancer
|
|
AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research .
|
-
- HY-N8390
-
|
|
Others
|
Cancer
|
|
3-Epidehydropachymic acid, a lanostane triterpenoid, shows totoxicity effect against human acute monocytic leukemia cell line THP-1 (IC50=52.51 μM) .
|
-
- HY-101150A
-
|
|
DNA Alkylator/Crosslinker
ADC Cytotoxin
|
Cancer
|
|
sulfo-DGN462 sodium is degraded to DGN462 in culture medium and plasma. DGN462, a potent DNA-alkylating agent, shows anti-tumor activity, such as acute myeloid leukemia (AML) .
|
-
- HY-126193
-
|
|
NO Synthase
Apoptosis
|
Cancer
|
|
JS-K is a NO donor that reacts with glutathione to generate NO at physiological pH . JS-K inhibits proliferation, induces apoptosis, and disrupts the cell cycle of Jurkat T acute lymphoblastic leukemia cells .
|
-
- HY-16271
-
|
4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
|
-
- HY-U00442
-
CTX1
1 Publications Verification
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
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 .
|
-
- HY-128571
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-4 is a potent and orally effective Fms-like tyrosine receptor kinase 3 (FLT3; IC50=7 nM) inhibitor for treating acute myelogenous leukemia .
|
-
- HY-146809
-
|
|
Galectin
|
Cancer
|
|
Galectin-3 is a β Galactoside specific carbohydrate recognition protein (lectin) has the ability to promote the migration of B cell precursor acute lymphoblastic leukemia (BCP-ALL) cells and withstand drug research.
|
-
- HY-106556
-
|
Rubidazon; Rubidazone
|
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
Zorubicin (Rubidazon) is a derivative of Daunorubicin (HY-13062A). Zorubicin interacts with topoisomerase II and inhibits DNA polymerases. Zorubicin can be used for the research of acute leukemias and sarcomas .
|
-
- HY-128068
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
DHODH-IN-17, a 2-anilino nicotinic acid, is a human DHODH inhibitor (IC50=0.40 μM). DHODH-IN-17 can be used for theresearch of acute myeloid leukemia (AML) .
|
-
- HY-108860
-
|
PEG-L-asparaginase; Pegasparaginase
|
Others
|
Cancer
|
|
Oncaspar (PEG-L-asparaginase; Pegasparaginase), a pegylated form of native Escherichia coli-derived L-asparaginase, breaks down the amino acid asparagine that are circulating in the bloodstream. Oncaspar plays an important role in acute lymphoblastic leukemia (ALL) .
|
-
- HY-112041
-
|
PTC596
|
Apoptosis
|
Cancer
|
|
Unesbulin (PTC596) is an orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor. Unesbulin downregulates MCL-1 and induces p53-independent mitochondrial apoptosis in acute myeloid leukemia (AML) cells. Unesbulin has anti-leukemic activity .
|
-
- HY-101025
-
|
|
|
|
|
Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML) .
|
-
- HY-14519S
-
|
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
|
-
- HY-162088
-
-
- HY-101266
-
|
DS-3032
|
|
|
|
Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis .
|
-
- HY-150586
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
PTG-0861 is a selective histone deacetylase 6 (HDAC6) inhibitor with the IC50 value of 5.92 nM. PTG-0861 induces apoptosis and can be used in the study of acute myeloid leukemia, multiple myeloma and other hematological cancers .
|
-
- HY-18948
-
GSK321
1 Publications Verification
|
|
|
|
GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia .
|
-
- HY-148602
-
|
|
Others
|
Cancer
|
|
KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively .
|
-
- HY-16782
-
|
ARRY-614
|
p38 MAPK
Autophagy
|
Cancer
|
|
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
|
-
- HY-112316
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
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).
|
-
- HY-N0071
-
|
Isoguanosine
|
FLT3
HDAC
|
Cancer
|
|
Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the research of AML .
|
-
- HY-100688
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
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 .
|
-
- HY-111249
-
|
|
FLT3
|
Cancer
|
|
TTT 3002 is a potent and orally active FLT3 inhibitor. TTT 3002 potently inhibits FLT3 phosphorylation by activating mutations at residue D835, with an IC50 of 0.2 nM. TTT 3002 can be used for AML (acute myeloid leukemia) research .
|
-
- HY-19541A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
|
-
- HY-14519
-
|
Amethopterin; CL14377; WR19039
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .
|
-
- HY-14519D
-
|
Amethopterin monohydrate; CL14377 monohydrate; WR19039 monohydrate
|
Antifolate
DNA/RNA Synthesis
ADC Cytotoxin
Apoptosis
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Methotrexate (Amethopterin) monohydrate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate monohydrate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .
|
-
- HY-13297
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .
|
-
- HY-139535
-
|
CG-806
|
FLT3
Btk
Apoptosis
|
Cancer
|
|
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .
|
-
- HY-153939S
-
|
RG7388-d3-1
|
Isotope-Labeled Compounds
|
Cancer
|
|
Idasanutlin-d3-1 (RG7388-d3-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of MDM2/p53. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .
|
-
- HY-155188
-
|
|
Bcl-2 Family
|
Neurological Disease
|
|
NWP-0476 is BCL-2/BCL-xL inhibitor. NWP-0476 has a modified structure with fine-tuned BCL-xL activity. NWP-0476 can be used for relapsed T-acute lymphoblastic leukemia (T-ALL) research .
|
-
- HY-103275
-
|
NSC 680410
|
Bcr-Abl
Apoptosis
|
Cancer
|
|
Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210 bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells .
|
-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
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 .
|
-
- HY-14519A
-
|
Amethopterin disodium; CL14377 disodium; WR19039 disodium
|
|
|
|
Methotrexate (Amethopterin) disodium, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate disodium, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .
|
-
- HY-161123
-
|
|
WDR5
|
Cancer
|
|
WDR5-IN-8 is a WDR5 inhibitor with IC50 value of 15.5 nM. WDR5-IN-8 shows good anti-proliferative activity in two human acute leukemia cell lines. WDR5-IN-8 has antitumor activity .
|
-
- HY-144835
-
|
|
Oxidative Phosphorylation
Epigenetic Reader Domain
|
Cancer
|
|
FHD-286 is a selective, oral inhibitor of SMARCA4/SMARCA2 ATPase (BRG1 and BRM) inhibitor. FHD-286 has the potential for the research of BAF (BRG1/BRM-associated factor)-related disorders such as acute myeloid leukemia .
|
-
- HY-155556
-
|
|
ClpP
Biochemical Assay Reagents
|
Cancer
|
|
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 .
|
-
- HY-N2492
-
|
Methyl trans-p-coumarate
|
Bacterial
Apoptosis
|
Infection
Cancer
|
|
(E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
|
-
- HY-129079
-
|
|
Others
|
Cancer
|
|
TFMB-(R)-2-HG, a cell membrane-permeable version of (R)-2-HG, is a carcinogenic factor in Acute myeloid leukemia (AML).
TFMB-(R)-2-HG impairs SCF ER-Hoxb8 cells differentiation in response to estrogen withdrawal .
|
-
- HY-124573
-
|
TH-3424
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
OBI-3424 (TH-3424) is a proagent that is selectively converted by AKR1C3 (aldo-keto reductase 1C3) to a potent DNA-alkylating agent. OBI-3424 can be used for hepatocellular carcinoma, castrate-resistant prostate cancer, and acute lymphoblastic leukemia (ALL) research .
|
-
- HY-155153
-
|
|
Apoptosis
CDK
|
Others
|
|
CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research .
|
-
- HY-112037
-
|
IACS-10759
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-112316A
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
(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 .
|
-
- HY-16018A
-
|
ABT-348 hydrochloride
|
Aurora Kinase
PDGFR
VEGFR
|
Cancer
|
|
Ilorasertib (ABT-348) hydrochloride is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib hydrochloride also is a potent VEGF, PDGF inhibitor. Ilorasertib hydrochloride has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-16018
-
|
ABT-348
|
Aurora Kinase
VEGFR
PDGFR
|
Cancer
|
|
Ilorasertib (ABT-348) is a potent, orally active and ATP-competitive aurora inhibitor with IC50s of116, 5, 1 nM for aurora A, aurora B, aurora C, respectively. Ilorasertib also is a potent VEGF, PDGF inhibitor. Ilorasertib has the potential for the research of acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) .
|
-
- HY-112037A
-
|
IACS-10759 hydrochloride
|
Oxidative Phosphorylation
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-132189
-
|
R101933
|
P-glycoprotein
|
Cancer
|
|
Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters . Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) . Laniquidar has limited oral bioavailability .
|
-
- HY-163160
-
|
|
Apoptosis
Epigenetic Reader Domain
|
Cancer
|
|
Bet-in-23 (Compound 23) is a BD2-selective BET inhibitor with an IC50 of 2.9 nM. BET-IN-23 has anticancer activity and can significantly inhibit the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 arrest and apoptosis in vitro .
|
-
- HY-162250
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .
|
-
- HY-14519S1
-
|
|
Isotope-Labeled Compounds
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Methotrexate-d3 diammonium is the deuterium labeled Methotrexate diammonium. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .
|
-
- HY-148026
-
|
BGB 11417
|
Bcl-2 Family
|
Cancer
|
|
Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines .
|
-
- HY-117596
-
UNC569
1 Publications Verification
|
TAM Receptor
|
Cancer
|
|
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
|
-
- HY-160018
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
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 .
|
-
- HY-151902
-
|
|
PROTACs
JAK
|
Cancer
|
|
SJ988497 is a PROTAC JAK2 degrader. SJ988497 potently inhibits CRLF2-rearranged (CRLF2r) cell proliferation and degrades the CRBN neosubstrate GSPT1. SJ988497 consists of a Ruxolitinib (HY-50856) derivative, linker, and CRBN ligand Pomalidomide. SJ988497 can be used in the research of acute lymphoblastic leukemia (ALL) .
|
-
- HY-132231
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
FD223 is a potent and selective phosphoinositide 3-kinase delta (PI3Kδ) inhibitor. FD223 displays high potency (IC50=1 nM) and good selectivity over other isoforms (IC50s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .
|
-
- HY-151366
-
|
|
HDAC
Epigenetic Reader Domain
|
Cancer
|
|
HDAC8/BRPF1-IN-1 (Compound 23a) is a dual inhibitor of HDAC8 and BRPF1 with an IC50 of 443 nM against human HDAC8 and a Kd of 67 nM against human BRPF1. HDAC8/BRPF1-IN-1 shows low in vitro activity against HDAC1 and 6 .
|
-
- HY-110075
-
|
|
Others
|
Cardiovascular Disease
|
|
Dexrazoxane monohydrochloride is the hydrochloride of Dexrazoxane (HY-B0581). Dexrazoxane prevents or reduces cardiac injury .
|
-
- HY-129388A
-
|
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-149595
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line .
|
-
- HY-16291
-
|
LOR-253; LT-253
|
c-Myc
KLF
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor . APTO-253 has antiarthritic activity .
|
-
- HY-114226
-
|
FT-2102
|
Isocitrate Dehydrogenase (IDH)
|
Inflammation/Immunology
Cancer
|
|
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
|
-
- HY-129388B
-
|
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-106634
-
|
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
|
HIV
Apoptosis
|
Infection
Cancer
|
|
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
|
-
- HY-116830A
-
|
|
GSK-3
|
Cancer
|
|
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
|
-
- HY-13518
-
|
Astringenin; trans-Piceatannol
|
Syk
Autophagy
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Piceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI) . Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties . Piceatannol induces apoptosis in DLBCL cell lines . Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells .
|
-
- HY-116830B
-
|
(R)-BRD0705
|
GSK-3
|
Cancer
|
|
BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
|
-
- HY-148522
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-18 is a potent and selective FLT3 inhibitor with an IC50 value of 0.003 μM. FLT3-IN-18 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-18 inhibits FLT3 and STAT5 phosphorylation. FLT3-IN-18 has the potential for the research of acute myeloid leukemia (AML) .
|
-
- HY-12445
-
|
CDKI-73; LS-007
|
CDK
Apoptosis
|
Inflammation/Immunology
Cancer
|
Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion .
|
-
- HY-129388
-
|
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-16379A
-
|
SB1518 hydrochloride
|
JAK
FLT3
|
Cancer
|
|
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
|
-
- HY-151404
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) proagent with antitumor activity .
|
-
- HY-50907
-
ABT-737
Maximum Cited Publications
36 Publications Verification
|
Bcl-2 Family
Apoptosis
Autophagy
Mitophagy
|
Cancer
|
|
ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
- HY-115446A
-
|
Cereblon ligand 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 32 hydrochloride
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Lenalidomide-C4-NH2 hydrochloride is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTAC (Compound 24), which has IC50s of 0.98 nM and 13.7 nM in inhibition of RS4;11 and MOLM-13 acute leukemia cell lines growth, respectively .
|
-
- HY-134978A
-
|
|
SHMT
|
Cancer
|
|
(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with 13C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519) . (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
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) .
|
-
- HY-149474
-
|
|
FLT3
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC50: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC50: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-18949
-
|
|
|
|
|
JI6 is a potent, selective and orally active FLT3 inhibitor, with IC50s of ∼40, 8, and 4 nM for FLT3-WT, FLT3-D835Y, and FLT3-D835H, respectively. JI6 also inhibits JAK3 and c-Kit, with IC50s of ∼250 and ∼500 nM, respectively. JI6 can be used for the research of acute myeloid leukemia .
|
-
- HY-153200
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2/XIAP-IN-2 is a dual inhibitor of murine double minute 2 (MDM2) and X-linked inhibitor of apoptosis protein (XIAP). MDM2/XIAP-IN-2 degrades MDM2, and inhibits XIAP mRNA translation to inhibits cancer cells. Particularly, MDM2/XIAP-IN-2 inhibits acute lymphoblastic leukemia cell line EU-1 with an IC50 value of 0.3 μM .
|
-
- HY-16379B
-
|
SB1518 citrate
|
JAK
FLT3
|
Cancer
|
|
Pacritinib (SB1518) citrate is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib citrate also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
|
-
- HY-16445A
-
-
- HY-16445B
-
-
- HY-143584
-
|
|
CDK
|
Cancer
|
|
AZ5576 is a potent and highly selective CDK9 inhibitor (IC50: <5 nM). AZ5576 can be used for hematological Malignancy research .
|
-
- HY-147611
-
|
|
c-Fms
|
Cancer
|
|
CSF1R-IN-10 (Compound 48) is a CSF-1R inhibitor with an IC50 of 0.005 μM .
|
-
- HY-147609
-
|
|
c-Fms
|
Cancer
|
|
CSF1R-IN-8 (Compound 22) is a CSF-1R inhibitor with an IC50 of 0.012 μM .
|
-
- HY-147610
-
|
|
c-Fms
|
Cancer
|
|
CSF1R-IN-9 (Compound 46) is a CSF-1R inhibitor with an IC50 of 0.028 μM .
|
-
- HY-153698
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
CC-3060 is a Cereblon modulator that promotes ZBTB16 degradation. CC-3060 degrades ZBTB16 with a DC50 of 0.47 nM in HT-1080 cells. CC-3060 targets ZBTB16 for degradation by primarily engaging distinct structural degrons on different zinc finger domains .
|
-
- HY-163068
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-24 (compound 24) is a potent and selective inhibitor of FLT3 kinase with an IC50 of 7.94 nM. FLT3-IN-24 has cell antiproliferative effects .
|
-
- HY-143238
-
|
|
Histone Demethylase
|
Cancer
|
|
FY-56 is a highly potent and selective LSD1/KDM1A inhibitor (IC50=42 nM) and exhibits high selectivity over MAO-A/B. FY-56 induces differentiation of MOLM-13 and MV4-11 cell and has the potential for AML research .
|
-
- HY-12892
-
|
|
|
|
|
SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines .
|
-
- HY-143317
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-161323
-
|
|
FLT3
Bcr-Abl
Apoptosis
|
Cancer
|
|
FLT3-ITD/D835Y-IN-1 (Compound 1) is a FLT3-ITD and BCR-ABL inhibitor. FLT3-ITD/D835Y-IN-1 mediates proapoptosis by inhibiting the FLT3 and BCR-ABL pathways, as well as other possible targets. FLT3-ITD/D835Y-IN-1 can be used in the study of acute myeloid leukemia (AML) .
|
-
- HY-50907S
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
- HY-124500
-
|
|
STAT
Apoptosis
|
Cancer
|
|
AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .
|
-
- HY-143895
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-12 is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 1.48 nM and 2.87 nM for FLT3-WT and FLT3-D835Y, respectively. FLT3-IN-12 possesses high selectivity over c-KIT (>1000-fold). FLT3-IN-12 has an excellent anti-AML (acute myeloid leukemia) activity (MV4-11, IC50 of 0.75 nM) .
|
-
- HY-13001
-
|
AC220
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
Autophagy
|
Cancer
|
|
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
|
-
- HY-15187
-
|
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-13735A
-
|
Mepacrine dihydrochloride; SN-390 dihydrochloride
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Infection
Cancer
|
|
Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis .
|
-
- HY-15187B
-
|
ARRY-520 TFA
|
Kinesin
|
Cancer
|
|
Filanesib TFA (ARRY-520 TFA) is a selective kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib TFA induces cell death by apoptosis in vitro. Filanesib TFA has potent anti-proliferative activity .
|
-
- HY-13735B
-
|
Mepacrine hydrochloride hydrate; SN-390 hydrochloride hydrate
|
Parasite
Apoptosis
Autophagy
Mitophagy
|
Infection
Cancer
|
|
Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis .
|
-
- HY-141796
-
|
|
Histone Methyltransferase
PROTACs
|
Cancer
|
|
MS67 is a potent and selective WD40 repeat domain protein 5 (WDR5) degrader with a Kd of 63 nM. MS67 is inactive against other protein methyltransferases, kinases, GPCRs, ion channels, and transporters. MS67 shows potent acticancer effects .
|
-
- HY-119769
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XX-650-23 is a potent CREB inhibitor. XX-650-23inhibits CREB function through disruption of CBP-CREB interaction. XX-650-23 can be used for AML research .
|
-
- HY-149522
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
BCL6-IN-10 (Compound WK499) is a BCL6 inhibitor. BCL6-IN-10 interrupts the binding of BCL6 to SMRT protein. BCL6-IN-10 induces cell apoptosis, cell cycle arrest and DNA damage. BCL6-IN-10 inhibits AML cell proliferation (IC50s: 0.91, 1.63, 1.026, 7.42, 0.87, 0.85μM for OCl-AML3, THP1, MOLM13, HL60, KG1, NB4 cell respectively) .
|
-
- HY-15187C
-
|
ARRY-520 hydrochloride
|
Kinesin
Apoptosis
|
Neurological Disease
|
|
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
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 .
|
-
- HY-143894
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM) .
|
-
- HY-134557
-
|
|
GSK-3
|
Cancer
|
|
GS87 is a highly specific and potent GSK3 inhibitor with IC50s of 415nM and 521nM for GSK3α and GSK3β, respectively. GS87 induces differentiation of acute myeloid leukemia (AML) cell lines by effectively activating GSK3-dependent signaling components including MAPK signaling. GS87 modulates key GSK3 target proteins involved in cell proliferation and differentiation more effectively than Lithium and SB415285 (SB). GS87 has the potential for acting as a differentiation agent for non-promyelocytic AML research .
|
-
- HY-162367
-
|
|
FLT3
Checkpoint Kinase (Chk)
|
Cancer
|
|
FLT3/CHK1-IN-2 (Compound 30) is a dual inhibitor of FLT3 and CHK1, with IC50s of 25.63, 16.39, 22.80 nM for CHK1, FLT3-WT, and FLT-D835Y respectively. FLT3/CHK1-IN-2 has favorable oral PK properties and kinase selectivity. FLT3/CHK1-IN-2 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-136499
-
|
|
Others
|
Cancer
|
|
DI-82 is a potent deoxycytidine kinase (dCK) inhibitor with an IC50 app of 27.8 nM and Ki app of 9.2 nM. DI-82 has antitumor activity .
|
-
- HY-115463
-
EB-3D
1 Publications Verification
|
AMPK
Apoptosis
|
Cancer
|
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity .
|
-
- HY-145015
-
|
HM43239
|
FLT3
Apoptosis
|
Cancer
|
|
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-153112
-
-
- HY-145015A
-
|
HM43239 hydrate
|
FLT3
Apoptosis
|
Cancer
|
|
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-156158
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH2 R140Q-IN-2 (compound 36) is an an orally active IDH2 R140Q inhibitor (IC50: 29 nM). IDH2 R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2 R140Q (IC50: 10 nM). IDH2 R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2 R140Q-IN-2 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-120508
-
|
AN-9; Pivalyloxymethyl butyrate
|
HDAC
Bcr-Abl
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties .
|
-
- HY-135231
-
NL-1
1 Publications Verification
|
Mitochondrial Metabolism
Autophagy
|
Cancer
|
|
NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway .
|
-
- HY-N10264
-
|
(+)-Avrainvillamide; CJ-17,665
|
Antibiotic
|
Infection
Cancer
|
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
- HY-155361
-
|
|
PROTACs
|
Cancer
|
|
PROTAC BRD9 Degrader-7 is an orally active and selective degrader of BRD9 with a DC50 of 1.02 nM. PROTAC BRD9 Degrader-7 has superior oral activity with a Cmax of 3436.95 ng/mL .
|
-
- HY-157213
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
LWY713 is a FLT3 degrader (DC50=0.64 nM) that selectively induces FLT3 degradation in a cereblon- and proteasome-dependent manner. LWY713 inhibits cell proliferation and induces G0/G1 arrest and apoptosis in MV4-11 cells. LWY713 exhibits potent in vivo antitumor activity in an MV4-11 xenograft model .
|
-
- HY-16786
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
AI-10-49 is an inhibitor of leukemic oncoprotein CBFβ-SMHHC. AI-10-49 inhibits the binding of CBFβ-SMMHCto the RUNX1 Runt domain with IC50 value of 0.26 μM. AI-10-49 can be used for the research of leukemia .
|
-
- HY-137471
-
|
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation .
|
-
- HY-144777
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
|
-
- HY-148683
-
|
|
Arp2/3 Complex
|
Cancer
|
|
EG-011 is the first-in-class and potent Wiskott-Aldrich syndrome protein (WASP) activator. EG-011 activates the auto-inhibited form of WASP with strong actin polymerization. EG-011 has selective anti-tumor activity in lymphomas .
|
-
- HY-131061
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .
|
-
- HY-16700
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
|
-
- HY-139514
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
RB-3, a polycomb repressive complex 1 (PRC1) inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM .
|
-
- HY-144433
-
|
|
DNA Methyltransferase
|
Infection
|
|
DNMT3A-IN-1 is a potent and selective DNMT3A inhibitor. DNMT3A-IN-1 shows inhibitor activities against DNMT3A with kI values range from 9.16-18.85 μM (AdoMet) and 11.37-23.34 μM (poly dI-dC) .
|
-
- HY-151411
-
|
|
Others
|
Cancer
|
|
RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model .
|
-
- HY-16700G
-
|
|
ADC Cytotoxin
Topoisomerase
|
Cancer
|
|
PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
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 .
|
-
- HY-144673
-
-
- HY-150109
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
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 .
|
-
- HY-114358
-
|
ONO-7475
|
TAM Receptor
Trk Receptor
|
Cancer
|
|
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
|
-
- HY-136446
-
|
|
Others
|
Cardiovascular Disease
Cancer
|
|
MYLS22 is a selective optic atrophy 1OPA1 inhibitor. MYLS22 reduces tumor vascularization and associated lymphatic angiogenesis by inhibiting OPA1, thereby limiting tumor growth and metastasis and effectively normalizing tumor vascular morphology. MYLS22 has anticancer activity .
|
-
- HY-151190
-
|
S1024
|
Histone Demethylase
|
Cancer
|
|
cis-4-Br-2,5-F2-PCPA (S1024) is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 94 nM instead of 8.4 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and by increasing the level of dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells .
|
-
- HY-151192
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 (LSD1), with a Ki value of 11 nM instead of 7 μM for LSD2. There is aberrant expression of LSD1 in cancer stem cells, LSD1/2-IN-1 inhibits LSD1 cell proliferation .
|
-
- HY-120758
-
|
|
Pim
FLT3
Apoptosis
|
Cancer
|
SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively .
|
-
- HY-145898
-
|
14-D-Valine-TPL
|
c-Myc
Molecular Glues
|
Cancer
|
|
WBC100 (14-D-Valine-TPL) is a potent, selective, and orally active c-Myc molecule glue degrader. WBC100 is a c-Myc degrader and targets ubiquitin E3 ligase CHIP mediated 26S proteasome pathway. WBC100 is used for c-Myc overexpressing tumors research .
|
-
- HY-160218
-
|
|
MAP4K
|
Cancer
|
|
HPK1-IN-42 (compound 185) ia a HPK1 inhibitor with the IC50 50 of 0.24 nM .
|
-
- HY-N2127
-
-
- HY-133136
-
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D0153
-
|
|
Fluorescent Dyes/Probes
|
|
Tetramethylrhodamine-5-isothiocyanate is a potent fluorescent dye. Tetramethylrhodamine-5-isothiocyanate can be used for label PG-M3 antibody for rapid diagnosis of acute promyelocytic leukemia (APL). Tetramethylrhodamine-5-isothiocyanate can be used as probe to quantify in vivo the biodistribution of PLGA (poly(lactic-co-glycolic) acid) and PLGA/chitosan nanoparticles .
|
-
- HY-16700G
-
|
|
Fluorescent Dye
|
|
PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
|
| Cat. No. |
Product Name |
Type |
-
- HY-E70016
-
|
TdT
|
Biochemical Assay Reagents
|
|
Terminal deoxyribonucleotidyltransferase (TdT) catalyses the condensation of deoxyribonucleotide triphosphates onto the 3' hydroxyl ends of DNA strands and adds N-regions to gene segment junctions during V(D)J recombination. Terminal deoxyribonucleotidyltransferase is expressed in immature, pre-B, pre-T lymphoid cells, and acute lymphoblastic leukemia/lymphoma cells .
|
-
- HY-16700G
-
|
|
Biochemical Assay Reagents
|
|
PNU-159682 GMP is a GMP grade PNU-159682 (HY-16700). PNU-159682, a metabolite of the anthracycline Nemorubicin, is a highly potent DNA topoisomerase II inhibitor with excellent cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 can be used in EDV-nanocell technology to overcome agent resistance.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1613A
-
|
Cyclo(RGDfV) TFA; C(RGDfV) TFA
|
Integrin
Apoptosis
|
Cancer
|
|
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) (Cyclo(RGDfV) (TFA))is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) can be used for the research of acute myeloid leukemia .
|
-
- HY-P3508
-
|
|
Peptides
|
Cancer
|
|
PNC-27 is an anticancer peptide, containing an HDM-2-binding domain. PNC-27 shows anti-tumor activity and can be used in acute myeloid leukemia research .
|
-
- HY-P1613
-
|
Cyclo(RGDfV); C(RGDfV)
|
Integrin
Apoptosis
|
Cancer
|
|
Cyclo(Arg-Gly-Asp-D-Phe-Val) (Cyclo(RGDfV)) is an integrin αvβ3 inhibitor. Cyclo(Arg-Gly-Asp-D-Phe-Val) has antitumor activity. Cyclo(Arg-Gly-Asp-D-Phe-Val) can be used for the research of acute myeloid leukemia .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99971
-
|
|
ADC Antibody
|
Cancer
|
|
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen, which present on leukemic myeloblasts of acute myeloid leukemia (AML). Gemtuzumab can be used for synthesis of antibody-drug conjugate (ADC), Gemtuzumab ozogamicin (HY-109539). Gemtuzumab ozogamicin consists of a cytotoxic derivative of Calicheamicin (a cytotoxic antibiotic), and a monoclonal antibody. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia .
|
-
- HY-P9963
-
|
Anatumomab
|
CD19
|
Cancer
|
|
Blinatumomab (Anatumomab) is a bispecific monoclonal antibody which can specifically targets the CD19 antigen present on B cells. Blinatumomab can be used for the research of acute lymphoblastic leukemia .
|
-
- HY-P99014
-
|
|
Apoptosis
|
Inflammation/Immunology
|
|
Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML) .
|
-
- HY-P99285
-
|
hBU 12
|
ADC Antibody
CD19
|
Others
|
|
Denintuzumab (hBU 12) is a recombinant humanized anti-CD19 monoclonal antibody. Denintuzumab can be used as the antibody moiety (ADC antibody) of antibody-drug conjugates to synthesize ADC, Denintuzumab Mafodotin (SGN-CD19A). Denintuzumab Mafodotin can be used in the research of acute lymphoblastic leukemia .
|
-
- HY-P99958
-
|
AMV-564; TandAb T564
|
Inhibitory Antibodies
|
Cancer
|
|
Vixtimotamab (AMV-564; TandAb T564) is a bispecific tetravalent tandem diabody (TandAb) that targets human CD33 and human CD3 antigens. Vixtimotamab can be used for the research of acute myeloid leukemia (AML) .
|
-
- HY-P99412
-
|
OSE-127
|
Interleukin Related
|
Cancer
|
|
Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research .
|
-
- HY-P99264
-
|
Humanized Anti-CD22 Recombinant Antibody
|
ADC Antibody
CD22
|
Cancer
|
|
Inotuzumab (Humanized Anti-CD22 Recombinant Antibody) is a humanized IgG4, κ antibody that targets human CD22. Inotuzumab can be linked to a toxic agent ozogamicin as an antibody-drug conjugate (ADC). Inotuzumab can be used for the research of acute lymphoblastic leukemia and non-Hodgkin lymphoma .
|
-
- HY-P99272
-
|
BMS 936564; MDX 1338; Anti-Human CXCR4 Recombinant Antibody
|
CXCR
|
Cancer
|
|
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 .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
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) .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
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 .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N0564
-
-
-
- HY-13680
-
-
-
- HY-N2517
-
-
-
- HY-123121
-
-
-
- HY-N8390
-
-
-
- HY-N0071
-
-
-
- HY-N2492
-
-
-
- HY-13518
-
-
-
- HY-N10264
-
|
(+)-Avrainvillamide; CJ-17,665
|
Infection
Alkaloids
Structural Classification
Microorganisms
Pyrrole Alkaloids
Classification of Application Fields
Source classification
Disease Research Fields
Indole Alkaloids
|
Antibiotic
|
|
Avrainvillamide ((+)-Avrainvillamide) is a naturally occurring alkaloid with antiproliferative effects, binds to the nuclear chaperone nucleophosmin, a proposed oncogenic protein that is overexpressed in many different human tumors. Avrainvillamide affects cell biology both by directly binding NPM1 and Crm1 as well as by inhibiting the association of these proteins with certain native cellular partners. Avrainvillamide, an antibiotic, inhibits growth of multi-agent resistant Staphylococcus aureus, Streptococcus pyogenes, and Enterococcus faecalis, with MICs of 12.5, 12.5 and 25 μg/ml, respectively .
|
-
-
- HY-N2127
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14519S
-
|
|
|
Methotrexate-d3 (Amethopterin-d3) is the deuterium labeled Methotrexate. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia)[1][2][3].
|
-
-
- HY-153939S
-
|
|
|
Idasanutlin-d3-1 (RG7388-d3-1) is the deuterium labeled Idasanutlin. Idasanutlin is a potent antagonist of MDM2/p53. Idasanutlin inhibits relapsed or refractory acute myeloid leukemia .
|
-
-
- HY-14519S1
-
|
|
|
Methotrexate-d3 diammonium is the deuterium labeled Methotrexate diammonium. Methotrexate (Amethopterin), an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis. Methotrexate, also an immunosuppressant and antineoplastic agent, is used for the research of rheumatoid arthritis and a number of different cancers (such as acute lymphoblastic leukemia) .
|
-
-
- HY-50907S
-
|
|
|
ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-161080
-
|
|
|
Alkynes
|
|
4'-Ethynyl-2'-deoxycytidine is an anticancer nucleoside. 4'-Ethynyl-2'-deoxycytidine can used in study acute lymphoblastic leukemia and diffuse large B-cell lymphoma .
|
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