Search Result
Results for "
AML cells
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-101266
-
|
DS-3032
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
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-129388B
-
|
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Inflammation/Immunology
Cancer
|
|
Pulrodemstat (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. Pulrodemstat benzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
-
- HY-159646
-
-
-
- HY-100548
-
|
|
AMPK
Autophagy
Apoptosis
|
Cancer
|
|
GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation .
|
-
-
- 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-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-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-160415
-
WD6305
2 Publications Verification
|
PROTACs
Apoptosis
METTL3
|
Cancer
|
|
WD6305 is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 has DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 inhibits m 6A modification and proliferation of AML cells, and induces apoptosis. WD6305 has antitumor activity .(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))
|
-
-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine, a chemical probe, 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-Fluorouracil (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-P9983
-
|
SGN-33; HuM-195; GLK-33 Antibody
|
Transmembrane Glycoprotein
Radionuclide-Drug Conjugates (RDCs)
|
Inflammation/Immunology
|
|
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
|
-
-
- HY-161779
-
|
|
Molecular Glues
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models .
|
-
-
- HY-16172
-
DMAPT
2 Publications Verification
Dimethylamino Parthenolide
|
NF-κB
|
Cancer
|
|
DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect .
|
-
-
- HY-15611
-
|
|
CRM1
|
Cancer
|
|
KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts .
|
-
-
- HY-160415A
-
|
|
PROTACs
Apoptosis
METTL3
|
Cancer
|
|
WD6305 TFA is a potent and selective METTL3-METTL14 PROTAC degrader. WD6305 TFA has DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. WD6305 TFA inhibits m 6A modification and proliferation of AML cells, and induces apoptosis. WD6305 TFA has antitumor activity .(Pink: UZH2 (HY-115717); Black: Linker; Blue: VHL ligand (HY-150803))
|
-
-
- HY-P991669
-
|
AML-01
|
Caspase
Apoptosis
|
Cancer
|
|
IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
|
-
-
- HY-B1336
-
|
|
Environmental Pollutants
Antibiotic
Bacterial
Apoptosis
Parasite
|
Infection
Cancer
|
|
Furazolidone is a monoamine oxidase (MAO) inhibitor with antiproliferative, apoptosis-inducing and differentiation-promoting activities. Furazolidone may inhibit leukemia fusion protein-mediated bone marrow transformation by upregulating the stability of the tumor suppressor protein p53. Furazolidone exhibits anti-leukemic activity in acute myeloid leukemia (AML) cell lines and can be used for anti-AML research [2].
|
-
-
- HY-174979
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Dac590 is an orally active and selective obesity-associated protein (FTO) inhibitor with an IC50 of 6.06 nM. Dac590 shows highly selective over ALKBH5 and ALKBH3. Dac590 suppresses oncogenic FTO signaling, induces myeloid differentiation, G1-phase cell cycle arrest, and apoptosis in acute myeloid leukemia (AML) cells. Dac590 inhibits xenograft tumor growth and prolongs survival in acute myeloid leukemia mouse models with no observed toxicity. Dac590 can be used for the research of AML .
|
-
-
- HY-142161
-
ABD957
3 Publications Verification
|
MAGL
|
Cancer
|
|
ABD957 is a potent and selective covalent inhibitor of the ABHD17 family of depalmitoylases, with an IC50 of 0.21 μM for ABHD17B. ABD957 can block N-Ras signaling and the growth of NRAS-mutant AML cells .
|
-
-
- HY-P99390
-
|
MCLA 117
|
CD3
Interleukin Related
IFNAR
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Tepoditamab (MCLA-117) is a full-length human IgG1 bispecific monoclonal antibody that binds to CLEC12A of myeloid cells and CD3 of cytotoxic T cells. Among others, CLEC12A is a myeloid differentiation antigen. Tepoditamab kills AML leukaemia mother cells and AML leukaemia stem cells, induces T cell-mediated proliferative lysis of AML cells. Tepoditamab induces upto 30-fold T-cell expansion. Tepoditamab results in moderate to strong cytokine (IFNγ, IL-6, IL-8, IL-10, and TNFα) and IFNγ release in human whole blood and PBMC, respectively. Tepoditamab can be used in acute myeloid leukaemia (AML) research .
|
-
-
- HY-158341
-
|
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
|
IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM for PHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity .
|
-
-
- HY-173320
-
|
|
Hsp-targeting Chimeras
Wee1
HSP
|
Cancer
|
|
HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
|
-
-
- HY-153604
-
MC4171
2 Publications Verification
|
Histone Acetyltransferase
|
Cancer
|
|
MC4171 (compound 34) is a selective KAT8 inhibitor (IC50=8.1 µM). MC4171 has been shown to exhibit moderate micromolar antiproliferative activity in different cancer cell lines, including NSCLC and AML, with potential for studying cancer .
|
-
-
- HY-120084
-
BTX161
1 Publications Verification
|
Casein Kinase
|
Cancer
|
|
BTX161, a thalidomide analog, is an effective CKIα degrader. BTX161 mediates human AML cell CKIα degradation more effectively than lenalidomide and activates the DNA damage response (DDR) and p53, while stabilizing p53 antagonist MDM2.
|
-
-
- HY-P99916
-
|
AMG-427
|
FLT3
CD3
TNF Receptor
|
Inflammation/Immunology
Cancer
|
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
|
-
-
- HY-129099A
-
|
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .
|
-
-
- 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-175802
-
|
HYBI-084
|
WDR5
Potassium Channel
|
Inflammation/Immunology
Cancer
|
|
HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 + cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM .
|
-
-
- HY-16981
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells .
|
-
-
- HY-150725C
-
|
|
TNF Receptor
IFNAR
|
Infection
Inflammation/Immunology
Cancer
|
|
ODN 1585 sodium is a potent inducer of IFN and TNFα production. ODN 1585 sodium is a potent stimulator of NK (natural killer) function. ODN 1585 sodium increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 sodium induces regression of established melanomas in mice. ODN 1585 sodium can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 sodium can be used as a vaccine adjuvant .
|
-
-
- HY-175783
-
|
|
Apoptosis
|
Cancer
|
|
MM927 is a potent NVL inhibitor, with an IC50 of 0.053 μM. MM927 blocks 60S ribosomal subunit biogenesis in the nucleolus. MM927 induces half-mer polysomes, cell cycle arrest at G1/S and G2/M and apoptosis in cells. MM927 demonstrates antitumor efficacy in MOLM-13 AML and HCT116 CRC xenograft models. MM927 can be used for the study of cancers such as acute myeloid leukemia (AML) and colorectal cancer (CRC) .
|
-
-
- HY-173444
-
|
|
HDAC
Transferrin Receptor
Apoptosis
Ferroptosis
|
Cancer
|
|
HDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC50: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC50: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research .
|
-
-
- HY-178500
-
|
|
Deubiquitinase
Apoptosis
STAT
JAK
Akt
PI3K
|
Cancer
|
|
WCY-8-67 is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways in vitro. WCY-8-67 inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 can be used for the study of acute myeloid leukemia .
|
-
-
- HY-142696A
-
|
|
CDK
Pim
Apoptosis
|
Cancer
|
CDK6/PIM1-IN-1 (Compound 51) hydrochloride is an orally active and potent dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 hydrochloride inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 hydrochloride 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-129388A
-
|
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Inflammation/Immunology
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, MAO-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
-
- HY-P991517
-
|
|
Transmembrane Glycoprotein
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Cancer
|
|
BI-836858 is a fully human anti-CD33 monoclonal antibody. BI-836858 reduces CD33+ cells via antibody-dependent cellular cytotoxicity (ADCC), blocks downstream signaling of S100A9/CD33, decreases the secretion of immunosuppressive cytokines and reactive oxygen species-induced genomic instability, and restores bone marrow hematopoietic function. BI-836858 is applicable to the research of myelodysplastic syndrome (MDS) and AML .
|
-
-
- HY-115590
-
|
|
Pim
Caspase
Apoptosis
Necroptosis
PARP
NF-κB
|
Cancer
|
|
JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM). JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC). JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC) .
|
-
-
- HY-163707
-
|
|
Apoptosis
|
Cancer
|
|
UR778Br targets the GTPase-activating protein-related domain (GRD domain) of IQGAP1 proteins. UR778Br inhibits the proliferation of human acute myeloid leukemia (AML), arrests the cell cycle at the G2/M phase, and induces apoptosis. UR778Br inhibits colony formation of primary and AML cells, without significant impacts on normal bone marrow cells .
|
-
-
- HY-179094
-
|
|
PROTACs
IRAK
NF-κB
Enolase
|
Inflammation/Immunology
Cancer
|
|
PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML) .
|
-
-
- HY-122623A
-
|
|
Apoptosis
|
Cancer
|
|
DB818 dihydrochloride is the dihydrochloride salt form of DB818 (HY-122623). DB818 dihydrochloride is an inhibitor for Homeobox A9 (HOXA9). DB818 dihydrochloride reduces the formation of HOXA9-DNA complexes, inhibits the growth and induces apoptosis in AML cell lines OCI/AML3, MV4-11, and THP-1 .
|
-
-
- HY-16172A
-
|
(S)-Dimethylamino Parthenolide
|
NF-κB
|
Cancer
|
|
(S)-DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect .
|
-
-
- HY-177467
-
|
|
Apoptosis
FLT3
|
Cancer
|
|
P0064 is a selective inhibitor targeting the PR domain of PRDM16. P0064 selectively reduces proliferation and survival of FLT3-ITD+ leukemia cells and induces cell apoptosis. P0064 is promising for research of acute myeloid leukemia (AML) .
|
-
-
- 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-129099
-
|
|
PKC
Estrogen Receptor/ERR
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation .
|
-
-
- HY-P991665
-
|
OBT357NF; OBT357
|
Transmembrane Glycoprotein
|
Cancer
|
|
MEN1112 (OBT357NF) is a selective humanized monoclonal antibody targeting the Bst1/CD157 antigen (EC50=1 nM). MEN1112 exerts potent antitumor activity against acute myeloid leukemia (AML) cells. MEN1112 is promising for research of hematological malignancies such as AML .
|
-
-
- 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-101266B
-
|
DS-3032b; DS-3032 tosylate hydrate
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
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 .
|
-
-
- HY-175040
-
|
|
PROTACs
Molecular Glues
FLT3
IKZF Family
|
Cancer
|
|
PROTAC FLT-3 degrader 5 is a FLT3 PROTAC degrader (DC50 = 1.2 nM). PROTAC FLT-3 degrader 5 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT-3 degrader 5 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide: (HY-14658); Black: linker; Thalidomide + linker: (HY-W1123823)) .
|
-
-
- HY-178500A
-
|
|
Deubiquitinase
Apoptosis
STAT
JAK
Akt
PI3K
|
Cancer
|
|
WCY-8-67 TFA is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 TFA induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways. WCY-8-67 TFA inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 TFA demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 TFA can be used for the study of acute myeloid leukemia .
|
-
-
- HY-111275
-
|
|
JAK
STAT
Apoptosis
Caspase
PARP
|
Cancer
|
|
WP-1034 is a JAK-STAT inhibitor with proapoptotic and antileukemic activity in acute myeloid leukemia (AML). WP-1034 blocks activation of Stat 3 and 5. WP-1034 induces cell cycle arrest and triggers apoptosis. WP-1034 can be used for AML research .
|
-
-
- HY-179267
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
c-Myc
RAR/RXR
Apoptosis
|
Cancer
|
|
FTO-IN-16 (Compound 8a-1), a FTO-IN-15 (HY-179266) prodrug, is a potent FTO inhibitor. FTO-IN-16 suppresses acute myeloid leukemia (AML) cell viability, increases m 6A levels, downregulates c-Myc and CEBPA, and upregulates ASB2 and RARA. FTO-IN-16 induces apoptosis. FTO-IN-16 demonstrates strong in vivo efficacy in AML mouse xenografts. FTO-IN-16 can be used for the research of AML .
|
-
- HY-177750
-
|
|
Molecular Glues
Apoptosis
|
Cancer
|
|
TD-522 is a potent and selective molecular glue GSPT1 degrader, with a DC50 of 0.269 nM. TD-522 exhibits strong anti-proliferative effects and induces apoptosis in acute myeloid leukemia (AML) and diffuse large B-cell lymphoma (DLBCL) cells. TD-522 suppresses tumor growth in a TMD-8 xenograft model. TD-522 can be used for AML and DLBCL research .
|
-
- 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-18952A
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3 .
|
-
- HY-174911
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-33 (Compound 7r) is a FLT3 inhibitor with an IC50 of 7.82 nM. FLT3-IN-33 has superior anticancer activities against acute myeloid leukemia (AML) cells, such as MV4-11 and MOLM-13 cells. FLT3-IN-33 significantly induces cell apoptosis and inhibits phosphorylation of FLT3 pathways. FLT3-IN-33 can be used for AML and other cancers research .
|
-
- HY-129388C
-
|
CC-90011 hydrochloride; LSD1-IN-7 hydrochloride
|
Histone Demethylase
|
Inflammation/Immunology
Cancer
|
|
Pulrodemstat (CC-90011) hydrochloride is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 value of 0.25 nM. Pulrodemstat hydrochloride is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat hydrochloride induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- 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-P990905
-
|
SAR-443579
|
Interleukin Related
|
Cancer
|
|
Bexatamig (SAR-443579) is a trifunctional natural killer cell engager targeting IL-3R α/CD123, NKp46/NCR1/CD335 and Fc gamma RIIIA/CD16a. Bexatamig forms a cytolytic synapse between natural killer cells and CD123-positive tumor cells. By activating natural killer cells to induce tumor cell death, Bexatamig effectively reduces the burden of CD123-positive acute myeloid leukemia (AML) blasts. Bexatamig has been granted FDA Fast Track designation, and is primarily investigated for relapsed or refractory acute myeloid leukemia, B-cell acute lymphoblastic leukemia, and high-risk myelodysplastic syndromes .
|
-
- HY-162265
-
|
|
Apoptosis
|
Cancer
|
|
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells, that can be used for the research of AML .
|
-
- HY-117690A
-
-
- HY-P11076
-
|
|
Complement System
|
Cancer
|
|
CP-EPS8-NLS is a peptide with anti-AML property. CP-EPS8-NLS interferes with EPS8-associated signaling and exerts anti-AML activity in various AML cell types. CP-EPS8-NLS has potent antitumor activity in xenograft tumor models. CP-EPS8-NLS downregulates EPS8 expression and its downstream pathway .
|
-
- HY-175274
-
|
|
FLT3
|
Cancer
|
|
MolPort-002-705-878 is a highly selective FMS-like tyrosine kinase 3 (FLT3) inhibitor with a binding affinity of −11.33 kcal/mol. MolPort-002-705-878 inhibits the proliferation of FLT3-mutated acute myeloid leukemia (AML) cells. MolPort-002-705-878 is promising for research of FLT3-mutated AML .
|
-
- HY-178996
-
|
|
FLT3
Apoptosis
Akt
ERK
PI3K
STAT
Mitochondrial Metabolism
|
Cancer
|
|
FLT3-IN-36 is a potent FLT3 inhibitor. FLT3-IN-36 exhibits antitumor activity against FLT3-mutated acute myeloid leukemia (AML) cells. FLT3-IN-36 induces cell cycle arrest, reduces mitochondrial membrane potential, and induces apoptosis, downregulating FLT3 and downstream protein expression (including AKT, ERK, PI3K, and STAT5). FLT3-IN-36 can be used for AML research .
|
-
- HY-138831
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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-174827
-
|
|
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
POLRMT-IN-2 is a potent POLRMT inhibitor. POLRMT-IN-2 exhibits strong antiproliferative activity in MOLM-13 cells, with an IC50 of 1.01 μM. POLRMT-IN-2 disrupts mitochondrial function and induces apoptosis in MOLM-13cells. POLRMT-IN-2 can be used for the study of acute myeloid leukemia(AML) .
|
-
- HY-157481
-
|
|
HDAC
|
Cancer
|
|
HDAC1-IN-6 (compound 1) is an inhibitor of HDAC1 and 11, with an IC50 of 1.9 μM and 1.6 μM, respectively. HDAC1-IN-6 induces differentiation in AML cells .
|
-
- HY-P991294
-
|
|
ADC Antibody
|
Cancer
|
|
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .
|
-
- HY-129388
-
|
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Inflammation/Immunology
Cancer
|
|
Pulrodemstat (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. Pulrodemstat Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MAO-A, and MAO-B. Pulrodemstat Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-129099AR
-
|
|
Reference Standards
PKC
Estrogen Receptor/ERR
Drug Metabolite
Endogenous Metabolite
|
Cancer
|
|
N-Desmethyltamoxifen (hydrochloride) (Standard) is the analytical standard of N-Desmethyltamoxifen (hydrochloride). This product is intended for research and analytical applications. N-Desmethyltamoxifen hydrochloride is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen hydrochloride is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation[1][2][3].
|
-
- 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-110071
-
|
|
c-Kit
|
Cancer
|
|
APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis .
|
-
- HY-B1336R
-
|
|
Reference Standards
Bacterial
Apoptosis
Antibiotic
Parasite
|
Infection
Cancer
|
|
Furazolidone (Standard) is the analytical standard of Furazolidone. This product is intended for research and analytical applications. Furazolidone is a nitrofuran derivative with antiprotozoal and antibacterial activity. It inhibits AML1-ETO transformed cells with an IC50 of 12.7 μM.
|
-
- HY-172153
-
|
|
CDK
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that exerts anticancer activity by binding to CDK2, thereby inhibiting the cell cycle, inducing cytotoxicity, promoting ROS production, and triggering Apoptosis. CDK2-IN-41 exhibits an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. It holds potential for research in AML-related cancer therapy .
|
-
- HY-111180
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
ML-262 is an inhibitor of hepatic lipid droplet formation (IC50=6.4 nM in murine AML-12 cells), which is associated with non-alcoholic fatty liver disease.1 ML-262 does not induce cytotoxicity (up to 33 μM) or inhibit fatty acid uptake (up to 50 μM).
|
-
- HY-P991425
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
AT-1413 is a human monoclonal antibody (mAb) targeting CD43. AT-1413 induces antibody-dependent cell-mediated cytotoxicity (ADCC) in melanoma cell lines and acute myeloid leukemia (AML) cells. AT-1413 has antitumor activity in AML mouse models. AT-1413 can be used in Acute myeloid leukaemia, Breast cancer, Malignant melanoma and Myelodysplastic syndromes research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
- HY-177821
-
|
|
c-Kit
|
Cancer
|
|
CD117/c-Kit aptamer sodium is a single-strand DNA aptamer specific for the biomarker CD117, which is highly expressed on acute myeloid leukemia (AML) cells.
|
-
- 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-175473
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
HI042 is a FMS-like Tyrosine Kinase 3 (FLT3) inhibitor. HI042 shows IC50 values of 0.62 μM for MOLM-13, 0.33 μM for MV4-11, and 0.89 μM for OCI-AML3 cells. HI042 selectively reduces the viability of FLT3-internal tandem duplication
(FLT3-|TD) mutations-positive cell lines, induces apoptosis, disrupts cell cycle progression, and diminishes the clonogenic potential. HI042 can be used for the research of acute myeloid leukemia (AML) .
|
-
- HY-172457
-
|
|
MNK
|
Cancer
|
|
NUCC-0200808 (Compound 12g) is an inhibitor of MNK1 with an IC50 of 42 nM. NUCC-0200808 reduces eIF4E phosphorylation and cell viability in AML cells, and induces apoptosis. NUCC-0200808 holds promise for research in the field of leukemia .
|
-
- HY-E70724
-
|
|
FLT3
|
Cancer
|
|
FLT3 (FMS-like tyrosine kinase 3, CD135) is a type 3 receptor tyrosine kinase that plays important roles in cell survival, proliferation, and differentiation during normal hematopoiesis. FLT3 is one of the most frequently mutated genes in acute myeloid leukemia (AML). FLT3 ITD is a internal tandem duplication (ITD) mutation of FLT3 that may be present in AML cells. FLT3 ITD Recombinant Human Active Protein Kinase is a recombinant FLT3 ITD protein that can be used to study FLT3 ITD-related functions .
|
-
- HY-117947
-
|
|
Histone Methyltransferase
|
Cancer
|
|
(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
|
-
- HY-170689
-
|
|
FLT3
Bcl-2 Family
|
Cancer
|
|
CG-3-246 is a dual inhibitor of FLT3/BCL-2, with the Kds of 63 and 4.25 nM, respectibely. CG-3-246 plays an important role in acute myeloid leukemias research .
|
-
- HY-172399
-
|
|
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
|
Cancer
|
|
FTO-IN-14 (Compound F97) is the inhibitor for the RNA demethylase Fat mass and obesity-associated protein FTO with IC50 of 0.45 μM. FTO-IN-14 regulates the protein expression of ASB2, RARA and MYC. FTO-IN-14 exhibits antiproliferative activity in AML cancer cells (IC50 for MOLM13, NB4, HEL, OCI-AML3, MV4-11 and MONOMAC6 is 0.7-5.5 μM), induces apoptosis in NB4 cell. FTO-IN-14 exhibits antitumor activity in mouse NB4 xenograft models .
|
-
- HY-N10079
-
|
Jatrophan
|
SHP2
|
Cancer
|
|
Suchilactone (Jatrophan) is a lignan extracted from Monsonia angustifolia E.Mey. Suchilactone binds to SHP2 and inhibits SHP2 activation, thereby inhibiting ERK-mediated cell proliferation. Suchilactone can be ued in acute myeloid leukaemia (AML) .
|
-
- HY-147716
-
|
|
CDK
|
Cancer
|
|
CDK8-IN-6 (compound 9) is a potent cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 13 nM. CDK8-IN-6 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 11.2, 7.5, 8.6, 20.5, 12.5-25 µM, respectively. CDK8-IN-6 has the potential for the research of AML-cancer .
|
-
- HY-122670
-
|
|
Pim
Apoptosis
AMPK
DYRK
STAT
MDM-2/p53
|
Cancer
|
|
VS-II-173 is a pan-Pim kinase inhibitor with IC50 values of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
|
-
- HY-179466
-
|
|
Microtubule/Tubulin
Apoptosis
Caspase
|
Cancer
|
|
BKT300 is a potent and selective protein regulator of cytokinesis 1 (PRC1) inhibitor. BKT300 inhibits PRC1 dephosphorylation at T481, disrupts actin and microtubule formation, induces G2/M cell cycle arrest, triggers mitotic catastrophe, and promotes apoptosis, thereby inhibiting proliferation and migration of acute myeloid leukemia (AML) cells while sparing normal cells. BKT300 inhibits tumor growth in mouse xenograft AML models. BKT300 can be used for the research of AML .
|
-
- HY-182019
-
|
|
HDAC
SHMT
Apoptosis
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia .
|
-
- HY-186013
-
|
|
Apoptosis
|
Cancer
|
|
CML-07-119 is a selective inhibitor of GGPP synthase (GGPPS) with an IC50 of ~27 nM. CML-07-119 induces apoptosis and exhibits anticancer activity against acute myeloid leukemia (AML) cells, including those harbouring TP53 mutations. CML-07-119 inhibits tumor growth in an AML mouse xenograft model. CML-07-119 can be used for AML research .
|
-
- HY-124693
-
|
|
Apoptosis
|
Cancer
|
|
DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34+ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia[1].
|
-
- HY-183354
-
|
|
Histone Methyltransferase
WDR5
Apoptosis
Caspase
|
Cancer
|
|
HLC40 is a MLL1 histone methyltransferase inhibitor with an IC50 of 0.82 μM by binding to WDR5. HLC40 inhibits proliferation of cancer cells, induces apoptosis and upregulates cleaved caspase-3 levels. HLC40 exhibits antitumor efficacy in a murine AML xenograft model .
|
-
- HY-182892
-
|
|
Histone Demethylase
Histone Methyltransferase
|
Cancer
|
|
MC4491 is a selective LSD1/PRMT5 inhibitor, with an IC50 of 0.152 μM against the LSD1/CoREST complex and an IC50 of 0.043 μM against the PRMT5/MEP50 complex. MC4491 induces transcriptomic changes and splicing alterations in AML cells. MC4491 is applicable for the research of acute myeloid leukemia .
|
-
- HY-145743
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
CP-17 is a potent and selective IDH2/R140Q inhibitor with an IC50 of 40.75 nM. CP-17 exhibits excellent selectivity of >55-fold against the wild-type IDH2. CP-17 exhibits robust D-2-HG suppression activity in TF-1 (IDH2/R140Q) cells and reverses the cellular differentiation block induced by the R140Q mutation. CP-17 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-181678
-
|
|
DNA-PK
HDAC
Apoptosis
Mitochondrial Metabolism
DNA/RNA Synthesis
|
Cancer
|
|
DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia .
|
-
- HY-182937
-
|
|
FLT3
STAT
Akt
ERK
Caspase
PARP
Bcl-2 Family
Apoptosis
|
Cancer
|
|
FLC-8 is an orally active FLT3 inhibitor with IC50 values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia .
|
-
- HY-181834
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC MLLT1 Degrader-1 is a PROTAC degrader targeting MLLT1. PROTAC MLLT1 Degrader-1 inhibits AML cell proliferation and viability, suppresses tumor growth in human AML xenograft models, and can block the oncogene transcriptional program. PROTAC MLLT1 Degrader-1 can be used for the research of MLL-rearranged acute myeloid leukemia (AML) .
|
-
- HY-182891
-
|
|
Histone Demethylase
|
Cancer
|
|
MC4455 is a LSD1/PRMT5 dual inhibitor. MC4455 inhibits the LSD1/CoREST and PRMT5/MEP50 complex with IC50 values of 0.104 μM and 0.014 μM. MC4455 covalently binds to LSD1’s FAD cofactor, stabilizes the LSD1/CoREST complex. MC4455 induces myeloid differentiation, alters transcriptomic profiles, drives alternative splicing changes, and impairs leukemic cell viability in AML cells. MC4455 can be used for the research of acute myeloid leukemia .
|
-
- HY-106326
-
|
FAD 104
|
Others
|
Cancer
|
|
ME 2303 (FAD 104) is a fluoro-pyranosyl adriamycin analogue with anti-tumor potential. ME 2303 can inhibit the proliferation of acute undifferentiated myeloblastic leukemia (AML) blast cells in a dose-dependent manner. ME 2303 can be used for the study of acute undifferentiated myeloblastic leukemia (AML) .
|
-
- HY-177714
-
|
|
Drug Derivative
|
Cancer
|
|
14-Acetoxy parthenolide (compound 6a) is a parthenolide (PTL) derivative. 14-Acetoxy parthenolide exhibits potent anti-acute myeloid leukemia (AML) activity against HL-60 and KG1a cells, with IC50 values of 2.8 µM and 6.3 µM, respectively. 14-Acetoxy parthenolide can be used for AML research .
|
-
- HY-181735
-
|
|
Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
|
Cancer
|
|
BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML .
|
-
- HY-176457
-
|
|
Small Interfering RNA (siRNA)
MDM-2/p53
PROTACs
|
Cancer
|
|
ZS3-046 is a TAF1 PROTAC degrader. ZS3-046 promotes the ubiquitination and degradation of TAF1. ZS3-046 activates p53 and induces apoptosis in acute myeloid leukemia (AML) cells. ZS3-046 has antitumor activity in an AML tumor xenograft mouse model. (Target protein ligand (HY-176467); CRBN ligase (HY-41547); Linker (HY-176469); CRBN ligase + Linker (HY-176470)) .
|
-
- HY-170558
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FW-1 is a type I inhibitor for FLT3 with IC50 of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13 .
|
-
- HY-132182
-
HPA-12
1 Publications Verification
|
Ceramidase
Autophagy
Apoptosis
ATF6
|
Neurological Disease
Cancer
|
|
HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .
|
-
- HY-168927
-
|
|
Apoptosis
Pyroptosis
PANoptosis
|
Cancer
|
|
Apoptosis inducer 36 (Compound 42) exhibits anti-leukemic activity through reduction of leukemia stem cells (LSCs) and induction of differentiation. Apoptosis inducer 36 inhibits the proliferation of AML cells, arrests cell cycle at G1 phase, and induces PANoptosis including apoptosis, pyroptosis and necrosis. Prodrug of apoptosis inducer 36 exhibits orally active antitumor efficacy in mouse model .
|
-
- HY-136688
-
|
|
PROTACs
|
Cancer
|
|
MI-389 is a PROTAC translation termination factor GSPT1 degrader. MI-389 disrupts a target that is a shared dependency in different AML and ALL cell lines, and that MI-389 action is dependent on the CRL4 CRBN E3 ligase .
|
-
- 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-158783
-
|
|
Ceramidase
Bcl-2 Family
LPL Receptor
Apoptosis
|
Neurological Disease
|
|
SACLAC, a Ceramide analog, is a potent and covalent acid ceramidase (ASAH1; AC) inhibitor with a Ki of 97.1 nM. SACLAC effectively blocks AC activity and induces a decrease in sphingosine 1-phosphate (S1P) and total ceramide levels. SACLAC reduces the levels of splicing factor SF3B1 and alternative Mcl-1 mRNA splicing, increases pro-apoptotic Mcl-1S levels to induce apoptosis in acute myeloid leukemia (AML) cells. SACLAC reduces the leukemic burden in human AML xenograft mouse models .
|
-
- HY-147717
-
|
|
CDK
|
Cancer
|
|
CDK8-IN-7 (compound 12) is a potent and selective cyclin-dependent kinase 8 (CDK8) inhibitor with an Kd of 3.5 nM. CDK8-IN-7 shows cytotoxicity for MOLM-13, OCI-AML3, MV4-11, NRK and H9c2 cells with IC50s of 5.9, 4.8, 5.4, 16.2, 12.5-25 µM, respectively. CDK8-IN-7 has the potential for the research of AML-cancer .
|
-
- HY-142690A
-
|
|
Apoptosis
HDAC
|
Cancer
|
|
HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC50 values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 dihydrochloride exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 dihydrochloride demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 dihydrochloride can be used for research in acute myeloid leukemia (AML) .
|
-
- HY-142690
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC-IN-27 (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC50 values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 can be used for research in acute myeloid leukemia (AML) .
|
-
- HY-154997
-
|
|
METTL3
|
Cancer
|
|
7OQL (compound 54) is a selective METTL3 inhibitor (IC50=0.054 µM). 7OQL has the potential to be used in the study of cancer .
|
-
- HY-13680R
-
|
Dian III (Standard); N-Methylisoindigotin (Standard); Natura-α (Standard)
|
Apoptosis
Reference Standards
|
Cancer
|
|
Meisoindigo (Standard) is the analytical standard of Meisoindigo. This product is intended for research and analytical applications. 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-112041
-
|
PTC596
|
BMI1
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-121725
-
|
|
STAT
|
Cancer
|
|
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 .
|
-
- HY-170451
-
|
KT-253
|
PROTACs
MDM-2/p53
Apoptosis
|
Cancer
|
|
Seldegamadlin (KT-253) is a selective p53 stabilizer and a MDM2 PROTAC degrader (DC50 = 0.4 nM). Seldegamadlin inhibits the proliferation of cancer cell RS4;11 with an IC50 of 0.3 nM, arrests the cell cycle at G2/M phase, and induces apoptosis. Seldegamadlin upregulates p53 activity and overcomes the p53-MDM2 feedback loop. Seldegamadlin can be used for the study of hematologic and solid tumors, such as acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL). (Pink: ligand for target protein MDM2 ligand 4 (HY-170452); Black: linker (HY-W001478); Blue: ligand for E3 ligase cereblon (HY-163927)) .
|
-
- HY-174844
-
|
|
p97
|
Cancer
|
|
p97-IN-1 is an orally active p97 inhibitor (IC50 = 26 nM). p97-IN-1 can significantly inhibit the proliferation of tumor cells. p97-IN-1 can be used for research on acute myeloid leukemia (AML) .
|
-
- HY-162265A
-
|
|
Apoptosis
|
Cancer
|
|
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells. UCM-13369 can be used for leukemia research .
|
-
- HY-175520
-
|
|
SHP2
Phosphatase
Apoptosis
|
Cancer
|
|
SHP2-IN-42 is a src homology 2 domain-containing phosphatase 2 (SHP2) inhibitor with an IC50 of 15 nM. SHP2-IN-42 inhibits cell proliferation and induces apoptosis and G1 phase cell cycle arrest. SHP2-IN-42 can be used for the research of cancer, such as acute myeloid leukemia (AML) .
|
-
- HY-W965550
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 40 is an apoptosis inducer. Apoptosis inducer 40 exhibits potent cytotoxic effects against jurkat and NB4 cells with IC50 values of 4.5 μM and 3.6μM. Apoptosis inducer 40 induces apoptosis and arrests cell cycle. Apoptosis inducer 40 can be used for the research of cancer, such as acute myeloid leukemia (AML) .
|
-
- HY-160638
-
|
|
TET Protein
|
Cancer
|
|
NSC-311068 is TET1 inhibitor. NSC-311068 selectively suppress TET1 transcription and 5-hydroxymethylcytosine (5hmC) modification. NSC-311068 represses the level of TET1 expression and the global 5hmC level. NSC-311068 effectively inhibits cell viability in AML cells with high expression of TET1 .
|
-
- HY-136175
-
Revumenib
Maximum Cited Publications
15 Publications Verification
SNDX-5613
|
Epigenetic Reader Domain
|
Cancer
|
|
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) .
|
-
- HY-124629A
-
|
|
Apoptosis
|
Cancer
|
|
DB2313 tetrahydrochloride is a potent transcription factor PU.1 inhibitor with an apoptosis of 14 nM. DB2313 tetrahydrochloride disrupts the interaction of PU.1 with target gene promoters. DB2313 tetrahydrochloride induces apoptosis of acute myeloid leukemia (AML) cells, and has anticancer effects .
|
-
- HY-P11451
-
|
|
CXCR
|
Cancer
|
|
Pentixather is a radiolabeled peptide that can target CXCR4. Pentixather can disrupt the interaction between leukemic cells and the bone marrow microenvironment by targeting the CXCR4/CXCL12 signaling axis, reduce the retention of leukemic cells in the protective bone marrow niche, and thereby enhance the sensitivity of leukemic cells to treatment. Pentixather can be used for the study of acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .
|
-
- HY-118970
-
|
|
VD/VDR
TGF-β Receptor
Interleukin Related
|
Cancer
|
|
LG190155 is a nonsteroidal vitamin D receptor (VDR) agonist. LG190155 activates VDR in mesenchymal stem cells, thereby upregulating the BMP6-IL6 autocrine axis. Pretreatment of mesenchymal stem cells with LG190155 significantly enhances their ability to induce differentiation of acute myeloid leukemia cells, without inducing hypercalcemia. LG190155 is applicable to research related to acute myeloid leukemia (AML) .
|
-
- HY-P990901
-
|
IGM-8444
|
TNF Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Aplitabart (IGM-8444) is a a pentameric IgM DR5 agonist antibody with 10 binding sites specific for DR5. Aplitabart multimerizes DR5 to selectively and potently induce tumor cell apoptosis. Aplitabart can be used for the study of lung cancer, breast cancer, cute myeloid leukemia (AML) and low-grade B-cell non-Hodgkin lymphoma (B-NHL) .
|
-
- HY-120089
-
|
|
FLT3
ERK
Akt
STAT
Apoptosis
|
Cancer
|
|
UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 reduces the phosphorylation levels of Mer and Flt3, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia .
|
-
- HY-123577
-
|
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
TPC-144 is a LSD1/KDM1A inhibitor. TPC-144 inhibits LSD1, and leads to a decrease in the protein level of DNMT1, causing low methylation of the LINE-1 element. TPC-144 can also produce a synergistic effect with Decitabine (HY-A0004) (a DNMT inhibitor), jointly promoting DNA demethylation and thereby inducing differentiation and apoptosis of leukemia cells. TPC-144 has also demonstrated anti-tumor efficacy in acute myeloid leukemia (AML) models. TPC-144 can be used for the study of 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-P11288
-
|
|
PACAP Receptor
Apoptosis
|
Cancer
|
|
ANT308 is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 significantly enhances the activation and proliferation of T cells. ANT308 inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 can be used for the studies of acute myeloid leukemia (AML) and uveal melanoma (UVM) .
|
-
- HY-P990928
-
|
APVO-436
|
CD3
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Mipletamig (APVO-436) is a bispecific CD123 x CD3 monoclonal antibody. Mipletamig simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This results in the activation and proliferation of T-cells and causes CTL-mediated cell lysis of CD123-expressing tumor cells. Mipletamig can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-104072
-
-
- HY-163541
-
SMS121
3 Publications Verification
|
Scavenger Receptor Class B type I (SR-BI）
|
Cancer
|
|
SMS121 is a CD36 inhibitor with a KD values of about 5 µM. SMS121 reduces the uptake of lipids and inhibits cell viability in acute myeloid leukemia cells. SMS121 has antitumor activity .
|
-
- HY-149735
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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-175886
-
-
- HY-173141
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor-26 (Compound HPT-11) is an inhibitor of mTOR with an IC50 of 0.7 nM. It effectively inhibits the proliferation of AML cell lines Molm-13 and MV-4-11. mTOR inhibitor-26 exhibits antitumor activity and favorable metabolic stability, making it a promising candidate for cancer research .
|
-
- HY-151381
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
hDHODH-IN-10 is a selective, potent and orally active hDHODH inhibitor, with an IC50 value of 10.9 nM. hDHODH-IN-10 forms hydrogen bonds with key residues Arg136 and Gln47. hDHODH-IN-10 inhibits the proliferation of cancer cells. hDHODH-IN-10 can be used in the research of cancers, such as AML, colorectal cancer .
|
-
- HY-112852A
-
|
|
Src
Apoptosis
|
Cancer
|
|
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 .
|
-
- 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-P991648
-
|
|
Interleukin Related
|
Cancer
|
|
CSL-360 is a chimeric unconjugated IgG1 monoclonal antibody targeting CD123. CSL-360 efficiently prevents the binding of IL-3 to CD123, abolishing IL-3 induced cell proliferation. CSL-360 can be used for acute myeloid leukemia (AML) research .
|
-
- 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-112852
-
|
|
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 .
|
-
- HY-160733
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL-IN-32 (compound 51) is a Menin-MLL interaction inhibitor with an IC50 of 0.042 nM in HTRF assay. Menin-MLL-IN-32 inhibits MEIS1 mRNA expression with an IC50 of 11 nM. Menin-MLL-IN-32 shows anti-proliferative effects, with IC50 values of 8 nM, 24 nM and 1900 nM for MOLM14 cells, OCI-AML3 cells and KO-52 cells, respectively. Menin-MLL-IN-32 can be used for the study of leukemia .
|
-
- HY-164607
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
YL-5092 is a selective YT521-B homology (YTH) domain-containing protein 1 (YTHDC1) inhibitor with an IC50 of 7.4 nM and a KD of 29.6 nM. YL-5092 can suppress cancer cell proliferation and induce cell G0/G1 phase arrest and apoptosis. YL-5092 can be used for the research of cancer, such as acute myeloid leukemia (AML) .
|
-
- HY-P11288A
-
|
|
PACAP Receptor
Apoptosis
|
Cancer
|
|
ANT308 TFA is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 TFA significantly enhances the activation and proliferation of T cells. ANT308 TFA inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 TFA can be used for the study of acute myeloid leukemia (AML) and uveal melanoma (UVM) .
|
-
- HY-30272
-
|
|
Hapten
|
Cancer
|
|
Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and exhibits good potential for vitiligo research. Monobenzone is a potent inhibitor of RNR (Ribonucleotide reductase) enzyme activity by targeting RRM2 (a regulatory small subunit M2 of RNR) protein, and thus has significant anti-leukemia efficacy in vitro and in vivo. Monobenzone inhibits acute myeloid leukemia (AML) cells proliferation and DNA synthesis, induces cell cycle arrest, and Apoptosis .
|
-
- HY-162293
-
|
|
CDK
|
Cancer
|
|
CDK8-IN-14 (compound 12) inhibits CDK8 with an IC50 value of 39.2 nM and has anti-AML cell proliferation activity (molm-13 GC50 = 0.02±0.01μM, MV4-11 GC50 = 0.03±0.01μM) .
|
-
- HY-183251
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC p300 degrader-1 is a paralog-selective, PROTAC-based degrader targeting the p300/CBP protein. It exhibits potent antiproliferative, cell cycle arrest and pro-apoptotic activities, and can be used in the research and development of antitumor drugs and related mechanism studies for hematological malignancies (AML, MM, NHL) .
|
-
- HY-173284
-
|
|
Discoidin Domain Receptor
|
Cancer
|
|
DDR1-IN-11 (Compound 4) is an inhibitor of Discoidin domain receptor 1 (DDR1) with an IC50 of 46.16 nM. DDR1-IN-11 can achieve an inhibition rate of 99.86% against Z-138 cells at a concentration of 10 μM, and it can be used in the research of acute myeloid leukemia (AML) .
|
-
- HY-101266R
-
|
DS-3032 (Standard)
|
MDM-2/p53
Reference Standards
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Milademetan (Standard) is the analytical standard of Milademetan (HY-101266). This product is intended for research and analytical applications. 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-162282
-
|
|
PROTACs
DNA Methyltransferase
|
Cancer
|
|
PROTAC METTL3-14 degrader 1 (compound 30) is a PROTAC degrader of METTL3-14. PROTAC METTL3-14 degrader 1 shows a 50% or higher degradation of METTL3 and/or METTL14(Pink: Ligand for target protein (HY-115717); Black: Linker (HY-168686); Blue: Ligand for E3 ligase (HY-10984)) .
|
-
- HY-161280
-
|
|
PROTACs
FLT3
|
Cancer
|
|
PROTAC FLT-3 degrader 3 (compound 35) is a PROTACs degrader of FLT. PROTAC FLT-3 degrader 3 has antiproliferative activity, with IC50 of 7.55 nM in MV4-11 cells .
|
-
- HY-139193
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
TH1760 is an inhibitor of NUDIX-type 15 (NUDT15) with an IC50 value of 25 nM. TH1760 sensitizes cells to 6-thioguanine by enhancing the accumulation of 6-thio- (d) GTP in nucleic acids. TH1760 enhances the anti-leukemia effect of thiopurine .
|
-
- HY-157334
-
DEG-77
1 Publications Verification
|
Molecular Glues
Casein Kinase
IKZF Family
Bcl-2 Family
CDK
Apoptosis
|
Cancer
|
|
DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC50 values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.
|
-
- 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-175273
-
|
|
PROTACs
FLT3
HSP
ERK
STAT
Akt
Apoptosis
|
Cancer
|
|
MA191 is a FLT3 PROTAC degrader. MA191 abrogates FLT3 inhibitor resistance from rebound activation of mitogen-activated kinases. MA191 mediates rapid FLT3-ITD degradation through a mechanism requiring VHL, neddylation, and BIM. MA191 reduces FLT3-ITD levels before inducing apoptosis. MA191 halts AML cell proliferation in Danio rerio. MA191 can be used for the study of acute myeloid leukemia (AML) (Pink: FLT3 ligand: (HY-175311), Blue: E3 ligase CRBN Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175312)) .
|
-
- HY-101266BR
-
|
DS-3032b (Standard); DS-3032 tosylate hydrate (Standard)
|
MDM-2/p53
Reference Standards
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Milademetan (tosylate hydrate) (Standard) is the analytical standard of Milademetan (tosylate hydrate) (HY-101266B). This product is intended for research and analytical applications. 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 .
|
-
- HY-164515
-
|
|
Apoptosis
Mitochondrial Metabolism
Caspase
PARP
|
Cancer
|
|
ONC213 is an orally active αKGDH inhibitor. ONC213 can suppress mitochondrial respiration and elevate α-ketoglutarate levels by inhibiting αKGDH activity. ONC213 can induce cells apoptosis by inducing mitochondrial stress response and inhibiting translation of MCL-1. ONC213 can be used for the research of cancer, such as acute myeloid leukemia research (AML) .
|
-
- HY-124629
-
|
|
Apoptosis
|
Cancer
|
|
DB2313 is a potent inhibitor of transcription factor PU.1. DB2313 inhibits PU.1-dependent reporter gene transactivation with an IC50 of 5 μM. DB2313 disrupts the interaction of PU.1 with target gene promoters. DB2313 induces apoptosis in acute myeloid leukemia (AML) cells and has anticancer effects .
|
-
- HY-164460
-
|
|
Pim
|
Cancer
|
|
AZD1897 is a PIM1, PIM2, and PIM3 inhibitor with IC50 values of less than 3 nM for these three PIM kinases. AZD1897 exhibits anticancer activity and synergistically inhibits the activity of acute myeloid leukemia (AML) cells in combination with Capivasertib (HY-15431). This synergistic inhibitory effect is achieved through the inhibition of the mTOR and MCL1 pathways .
|
-
- HY-P99394
-
|
JNJ-64407564
|
CD3
|
Cancer
|
|
Talquetamab (JNJ-64407564) is a humanized bispecific antibody that binds to GPRC5D (member of G protein-coupled receptor family C5 group D) and CD3 to induce T cell-mediated killing of GPRC5D-expressing MM cells through T cell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .
|
-
- HY-136175B
-
|
cis-SNDX-5613
|
Epigenetic Reader Domain
|
Cancer
|
|
cis-Revumenib (cis-SNDX-5613) is an isomer of Revumenib (HY-136175). 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) .
|
-
- HY-158160
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
|
-
- HY-171792
-
|
ORM-6151
|
Transmembrane Glycoprotein
|
Cancer
|
|
BMS-986497 (ORM-6151) is a CD33-targeting antibody-conjugated GSPT1 degrader. BMS-986497 delivers the GSPT1 degrader SMol006 to CD33-expressing cells and induces GSPT1 protein degradation. BMS-986497 shows potential for research on acute myeloid leukemia (AML) .
|
-
- HY-129937A
-
GNE-987
1 Publications Verification
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer .
|
-
- HY-181690
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
Menin-MLL-IN-37 is an orally active Menin-MLL protein complex inhibitor with an IC50 of 820.50 nM. Menin-MLL-IN-37 disrupts the interaction between menin and MLL proteins. Menin-MLL-IN-37 induces differentiation of acute myeloid leukemia cells and selectively inhibits the proliferation of MLL-rearranged and DNMT3A/NPM1-mutant leukemia cells. Menin-MLL-IN-37 can be used for the research of acute myeloid leukemia (AML) .
|
-
- HY-116129
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
BPR1J-340 is a potent FLT3 inhibitor with an IC50 of ~25 nM. BPR1J-340 inhibits the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD + acute myeloid leukemia (AML) cells. BPR1J-340 exhibits significant anti-tumor activities .
|
-
- HY-122209
-
|
|
HBV
|
Infection
|
|
DVR-01 is a HBV inhibitor with EC50 values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. DVR-01 shows antiviral activity against drug-resistant HBV mutants with EC50s of 2.403-3.273 μM. DVR-01 can be used for the research of HBV infection and related diseases .
|
-
- HY-174873
-
|
|
PROTACs
METTL3
Apoptosis
Bcl-2 Family
|
Cancer
|
|
AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML). (Pink: METTL3 Ligand (HY-174874); Blue: VHL Ligand (HY-125845); Black: Linker; VHL Ligand+Linker (HY-174875)) .
|
-
- HY-178908
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-35 (Compound 4K) is an orally active, covalent, irreversible FLT3 inhibitor. FLT3-IN-35 inhibits the phosphorylation of FLT3 and its downstream signaling factors, as well as induces cell cycle arrest and apoptosis. FLT3-IN-35 inhibits the phosphorylation of FLT3 and its downstream signaling factors, as well as induced cell cycle arrest and apoptosis. FLT3-IN-35 can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-129079
-
-
- HY-180430
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-208, a Bufalin (HY-N0877) analogue, is a potent and orally active antitumor agent. Antitumor agent-208 exhibits antiproliferative activity against tumor cell line (IC50 =0.30-1.09 nM). Antitumor agent-208 inhibits tumor growth in a MV-4-11 xenograft mouse model. Antitumor agent-208 can be used for cancer research, such as acute myeloid leukemia (AML) and non-small cell lung cancer (NSCLC) .
|
-
- HY-125236
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BET-IN-19 (Compound 146) is a BET inhibitor. BET-IN-19 inhibits hlL-6 mRNA transcription (IC50 ≤0.3 uM), and c-myc activity in human AML MV4-11 cell (IC50 ≤0.3 uM)。BET-IN-19 inhibits tetra-acetylated histone H4 binding to BRD4 bromodomain 1 (IC50 ≤0.3 uM) .
|
-
- 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-148014
-
-
- HY-172581
-
|
|
FLT3
Apoptosis
Ras
p38 MAPK
PI3K
Akt
JAK
STAT
|
Cancer
|
|
Clifutinib is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib exerts strong antiproliferative effects on FLT3-ITD acute myeloid leukemia (AML) cell lines (MV-4-11: IC50 = 1.5 nM; MOLM-13: IC50 = 1.4 nM). Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib demonstrates significant antitumor efficacy in mice bearing MV-4-11 or MOLM-13 xenografts. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia .
|
-
- HY-P991656
-
|
|
CXCR
Apoptosis
p38 MAPK
Akt
|
Cancer
|
|
LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research .
|
-
- HY-P990002
-
|
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD117/c-Kit Antibody (2B8) is an IgG2b antibody, targeting to mouse CD117/c-Kit. Anti-Mouse CD117/c-Kit Antibody (2B8) reacts with mouse c-Kit (also known as CD117), which is expressed on hematopoietic progenitor cells, mast cells, and acute myeloid leukemia (AML) cells. Anti-Mouse CD117/c-Kit Antibody (2B8) can be used for the detection of flow cytometry, immunofluorescence and immunohistochemistry in cancer and inflammation .
|
-
- HY-179734
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
c-Myc
|
Cancer
|
|
PROTAC BRD4 Degrader-41 (Compound A5) is a BRD4 PROTAC degrader with a DC50 of 0.97 nM. PROTAC BRD4 Degrader-41 exhibits potent anti-proliferative activity against various types of cancer cells such as AML, lymphoma, breast cancer, ovarian cancer, and non-small cell lung cancer. PROTAC BRD4 Degrader-41 can induce G0/G1 phase arrest and apoptosis in MV4-11 cells. PROTAC BRD4 Degrader-41 downregulates the transcriptional level of c-Myc .
|
-
- HY-158974
-
|
|
DNA/RNA Synthesis
Apoptosis
PARP
|
Cancer
|
|
YTHDC1-IN-1 is a selective YTHDC1 inhibitor with a Kd of 49 nM and an IC50 of 0.35 μM. YTHDC1-IN-1 can inhibit the proliferation and induce apoptosis of acute myeloid leukemia cell lines. YTHDC1-IN-1 has anti-tumor activity .
|
-
- HY-12344A
-
|
|
FLT3
|
Cancer
|
|
UNC2025 hydrochloride is a potent, ATP-competitive, highly orally active and BBB-permeable 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 .
|
-
- HY-125008
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
JH-IX-179 is an FLT3 inhibitor (IC50 = 4 nM (FLT3-ITD), 10 nM (FLT3-D835Y)). JH-IX-179 inhibits G1 phase arrest and induces apoptosis in FLT3-ITD-expressing cells. JH-IX-179 can be used in acute myeloid leukemia (AML) research .
|
-
- HY-N12641
-
|
|
Apoptosis
Pyroptosis
|
Cancer
|
|
Ardisianone is a component with an alkyl benzoquinone structure that can be isolated from Ardisia virens Kurz and Ardisia compressa tea extract. Ardisianone exhibits potent antileukemic activity, particularly against HL-60 cells, with IC50 values of 1.87 μM (24 h) and 1.67 μM (48 h). Ardisianone induces caspase-dependent apoptosis and triggers pyroptosis. Ardisianone can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-15222
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
Menin-MLL inhibitor MI-2 is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL) .
|
-
- HY-182912
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Cancer
|
|
PLX-4104 is an orally active BRD4 molecular glue degrader with a DC50 of 2 nM. PLX-4104 selectively promotes BRD4 degradation via DCAF11 recruitment, triggering ubiquitination and proteasomal breakdown. PLX-4104 inhibits cancer cell proliferation. PLX-4104 induces complete regression of AML xenograft tumors. PLX-4104 can be used for the research of acute myeloid leukemia .
|
-
- HY-173214
-
|
|
FLT3
Apoptosis
|
Cancer
|
FLT3-ITD-IN-3 (13v), an orally active FLT3-ITD (FLT3 internal tandem duplication) inhibitor, disrupts FLT3 signal transduction and induced G0/G1 cell cycle arrest and apoptosis. FLT3-ITD-IN-3 (13v) is used in the research of acute myeloid leukemia (AML) .
|
-
- HY-15222A
-
|
|
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
Menin-MLL inhibitor MI-2 dihydrochloride is a competitive and selective Menin-MLL interaction inhibitor with an IC50 value of 446 nM and a Ki value of 158 nM. Menin-MLL inhibitor MI-2 dihydrochloride downregulates the expression of target genes such as HOXA9 and MEIS1, inhibits proliferation of leukemia cells and induces apoptosis and differentiation. Menin-MLL inhibitor MI-2 dihydrochloride is proming for rasearch of MLL-rearranged acute leukemias (e.g., AML, ALL) .
|
-
- HY-164526
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
SH1573 is an orally active mIDH2 inhibitor. SH1573 has a strong and selective inhibitory effect on mIDH2 R140Q protein (IC50=4.78 nmol/L), and can effectively reduce the production of the carcinogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum and tumors. SH1573 can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-115529
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
(-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2 protein family, inhibiting Mcl-1, Bcl-2, Bcl-xL and Bcl-1 with IC50 values of 0.025, 0.031, 0.076 and 0.122 μM, respectively. (-)BI97D6 stimulates cell death through the Bak and Bax mediated mitochondrial apoptosis pathway. In addition, (-)BI97D6 inhibits Mcl-1 and can effectively induce apoptosis in acute myeloid leukemia (AML) cells .
|
-
- 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-155226
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
|
-
- 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-172262
-
|
|
VDAC
Bcl-2 Family
Apoptosis
|
Cancer
|
|
WEHI-3773 is a VDAC2 ligand and apoptosis modulator. WEHI-3773 directly binds to the β7-β10 region of VDAC2 and disrupts its interaction with BAX and BAK. WEHI-3773 regulates BAX-mediated apoptosis in BAK-deficient cells by modulating conformational activation of BAX, mitochondrial redistribution, and cytochrome c release. WEHI-3773 overcomes Venetoclax (HY-15531) resistance, resensitizes leukemia cells carrying BAX mutations to BH3 mimetics, and enables long-term clonogenic survival of BAK-deficient cells treated with BH3 mimetics. WEHI-3773 is applicable to research related to acute myeloid leukemia .
|
-
- HY-168741
-
|
|
FLT3
|
Cancer
|
|
FLT3-ITD-IN-2 (Compound A1) is an inhibitor for FLT3-ITD kinase with an IC50 of 2.12 nM. FLT3-ITD-IN-2 inhibits the proliferation of FLT3-dependent human AML cell line MOLM-13 with an IC50 of 25.65 nM. FLT3-ITD-IN-2 exhibits antitumor efficacy against acute myeloid leukemia .
|
-
- HY-112852S
-
|
|
Isotope-Labeled Compounds
Src
Apoptosis
|
Cancer
|
|
TL02-59-d5 is the deuterium labeled TL02-59 (HY-112852). TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an ICC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with ICC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
|
-
- HY-158325
-
|
|
PROTACs
FLT3
Apoptosis
|
Cancer
|
|
PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor) .
|
-
- HY-185207
-
|
|
Pyroptosis
|
Infection
Cancer
|
|
CQ80 is a PEPD/XPNPEP1 inhibitor and selective CARD8 inflammasome activator. CQ80 has IC50 values of 0.91 μM for PEPD, 43 μM for XPNPEP1. CQ80 promotes the accumulation of Xaa-Pro peptides by inhibiting PEPD and XPNPEP1, releases the fragment of CARD8 for inflammasome formation, and induces pyroptosis via GSDMD cleavage. CQ80 can be used for research on inflammasome, CARD8-expressing cancer cells, HIV-1-infected cell clearance, acute myeloid leukemia (AML) .
|
-
- HY-155112
-
|
|
Microtubule/Tubulin
FLT3
Bcr-Abl
|
Cancer
|
|
Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
|
-
- HY-175282
-
|
|
Apoptosis
Caspase
CDK
PARP
Akt
Autophagy
Atg8/LC3
|
Cancer
|
|
ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC50 = 0.113 μM, Ki = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers .
|
-
- HY-175164
-
|
|
Apoptosis
c-Myc
|
Cancer
|
|
SVC112 is a translation elongation inhibitor that prevents the cyclic dissociation of EF2 from the ribosome, thereby inhibiting the elongation step of translation. SVC112 shows activity in growth inhibition among cancer cell lines of various origins (acute myeloid leukemia (AML), multiple myeloma (Myeloma), colorectal cancer (CRC), and head and neck squamous cell carcinoma (HNSCC)). SVC112 preferentially impedes ribosomal processing of mRNAs, and decreaseds CSC-related proteins including Myc and Sox2. SVC112 induces apoptosis in hematologic cancer cell lines, while phosphorylation of c-Myc correlates with sensitivity to SVC112 in colorectal cancer cell lines. SVC112 inactivates HNSCC stem cells in vitro and prevents the regrowth of HNSCC tumor xenografts in mice. SVC112 can be used for the study of HNSCC .
|
-
- HY-168936
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
DP-15 is the degrader for GSPT1 and BRD4 with DC50s of 5.25 nM and 0.48 nM. DP-15 exhibits anti-proliferative activity of AML cells and NHL cells with an IC50 of nanomolar levels, arrests the cell cycle at G1 phase, and induces apoptosis in MOLM13. DP-15 exhibits anti-leukemia activity in MOLM-13 xenograft mouse models . (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W262798); Blue: ligand for E3 ligase Cereblon Thalidomide-5-OH (HY-23095))
|
-
- HY-175502
-
|
|
Molecular Glues
IKZF Family
Apoptosis
|
Cancer
|
|
MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL) .
|
-
- HY-161710
-
|
|
PROTACs
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
XYD129 is an effective CBP/p300 PROTAC degrader. XYD129 has antiproliferative activity on MV4-11 cell line (IC 50=0.044 μM). XYD129 can be used for the study of acute myeloid leukemia (AML). (Structure Note: Pink, CBP/p300 ligand 5 (HY-161711); Blue, E3 ligase ligand (HY-41547); Black, Linker (HY-40178)) .
|
-
- HY-108417
-
|
|
STAT
JAK
Bcr-Abl
|
Cancer
|
|
Debio 0617B, a multi-kinase inhibitor, reduces maintenance and self-renewal of primary human AML CD34 + stem/progenitor cells. Debio 0617B has a unique profile targeting key kinases upstream of STAT3/STAT5 signaling such as JAK, SRC, ABL, and class III/V receptor tyrosine kinases (TKs). Debio 0617B has documented efficacy in STAT3-driven solid tumors .
|
-
- HY-129079A
-
|
|
DNA Methyltransferase
Wnt
β-catenin
|
Endocrinology
Cancer
|
|
TFMB-(S)-2-HG is a potent TET2 inhibitor. TFMB-(S)-2-HG also inhibits the EglN prolyl hydroxylases. TFMB-(S)-2-HG downregulates Wnt3a, β-catenin (intranuclear) protein expression. TFMB-(S)-2-HG inhibits osteogenic differentiation of cells. TFMB-(S)-2-HG has the potential for the research of acute myeloid leukemia (AML) .
|
-
- HY-144433
-
|
|
DNA Methyltransferase
|
Infection
|
|
DNMT3A-IN-1 (compound 1) is an effective and selective DNMT3A inhibitor. DNMT3A-IN-1 exhibits inhibitory activity against DNMT3A, with KI values ranging from 9.16 to 18.85 μM (AdoMet) and 11.37 to 23.34 μM (poly dI-dC). DNMT3A-IN-1 can induce apoptosis in acute myeloid leukemia (AML) cell lines (Apoptosis) .
|
-
- HY-155175
-
|
|
Tim3
IFNAR
|
Cancer
|
|
TIM-3-IN-2 is a TIM-3 inhibitor. TIM-3-IN-2 blocks the interactions of TIM-3 with PtdSer, CEACAM1 and Gal-9, and inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 restores IFNγ release from peripheral blood mononuclear cells. TIM-3-IN-2 inhibits the proliferation of acute myeloid leukemia cells. TIM-3-IN-2 can be used for the research of acute myeloid leukemia .
|
-
- HY-114414
-
|
|
HDAC
mTOR
Apoptosis
|
Cancer
|
|
HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies .
|
-
- HY-P99971
-
|
|
ADC Antibody
Transmembrane Glycoprotein
|
Cancer
|
|
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen. Gemtuzumab affects cell necrosis by specifically targeting CD33 expressed on the surface of leukaemic cell blasts in 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. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
-
- HY-153775
-
|
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
UC-764864 is a selective UBE2N inhibitor. UC-764864 covalently binds UBE2N catalytic Cys87, blocks ubiquitin-UBE2N thioester formation and polyubiquitin chain synthesis. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates, and induces cell apoptosis. UC-764864 can be used for the research of acute myeloid leukemia .
|
-
- HY-182956
-
|
|
Molecular Glues
DNA Methyltransferase
|
Cancer
|
|
DNMT1 Degrader-1 is a selective DNMT1 degrader with an IC50 of 202.87 nM and a Kd value of 122 nM. As a molecular glue, DNMT1 Degrader-1 forms a ternary complex with DNMT1 and UHRF1, thereby triggering UHRF1-mediated ubiquitination and degradation of DNMT1, and inhibiting the enzymatic activity of DNMT1. DNMT1 Degrader-1 inhibits the proliferation of primary acute myeloid leukemia cells and exerts anti-tumor activity. DNMT1 Degrader-1 can be used for the research of acute myeloid leukemia .
|
-
- HY-173481
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-37 (Compound 24) is a CDK9 inhibitor (EC50: 5.5 nM) with weak inhibition on other CDK isoforms, showing high selectivity. CDK9-IN-37 has significant antiproliferative activity against acute myeloid leukemia MOLM-13 cells (IC50: 0.034 μM). CDK9-IN-37 inhibits the CDK9 signaling pathway, reduces the phosphorylation level of RNAP II CTD (Ser2), downregulates the anti-apoptotic protein McI-1, induces cell apoptosis, and arrests the cell cycle at the G2/M phase. CDK9-IN-37 can be used in the study of acute myeloid leukemia (AML) .
|
-
- HY-173212
-
|
|
Polo-like Kinase (PLK)
c-Myc
Apoptosis
|
Cancer
|
|
PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC50: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC50: 12.72 nM) and PLK3 (IC50: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-174437A
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-32 TFA is a potent FLT3 inhibitor with an IC50s of 2.40 nM and 3.83 nM against FLT3-ITD and FLT3-D835Y. FLT3-IN-32 TFA inhibits proliferation/survival of human MV4-11 cells with an IC50 of 0.07 nM. FLT3-IN-32 TFA can be used for the study of acute myeloid leukemia (AML) .
|
-
- 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-138195
-
|
|
DNA/RNA Synthesis
Apoptosis
FAK
Src
MMP
Autophagy
|
Cancer
|
|
NEO212 is an orally active, blood-brain barrier permeable conjugate of Temozolomide (TMZ) (HY-17364) and Perillyl Alcohol (POH) (HY-N7000), with potent anticancer activity. NEO212 overcomes classical TMZ resistance and DNA alkylation by depleting MGMT. By inhibiting the FAK/Src signaling pathway, NEO212 reduces the production of MMP2 and MMP9, induces mesenchymal-epithelial transition, and inhibits the migration, invasion and tumor progression of glioma stem cells. NEO212 disrupts autophagy flux to enhance mitochondrial apoptosis; it induces differentiation of acute myeloid leukemia (AML) cells into macrophages and proliferation arrest .
|
-
- HY-183265
-
|
|
Creatine Kinase
ATP Synthase
Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
|
Cancer
|
|
GO847 is an orally active casein kinase 2 (CK2) inhibitor with an IC50 of 40.2 nM. GO847 increases intracellular ATP levels, impairs Mitochondrial metabolic flexibility, and promotes excessive mitochondrial ROS production. GO847 alters the period length of cellular circadian rhythms. GO847 inhibits the growth of acute myeloid leukemia cells. GO847 can be used for the research of acute myeloid leukemia .
|
-
- 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-111447
-
|
|
NADPH Oxidase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
VAS 3947, a specific NADPH oxidase (NOX) inhibitor, exerts a potent antiplatelet effect. VAS3947 induces apoptosis independently of anti-NOX activity, via UPR activation, mainly due to aggregation and misfolding of proteins .
|
-
- HY-118304A
-
|
|
FLT3
Apoptosis
Caspase
|
Cancer
|
|
AKN-028 TFA, 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 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML) .
|
-
- HY-P990164
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse RGMb Antibody (307.9D1) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse RGMb. Anti-Mouse RGMb Antibody (307.9D1) blocks RGMb binding to PD-L2. Anti-Mouse RGMb Antibody (307.9D1) can be used for the researches of cancer inflammation and immunology, such as acute myeloid leukemia (AML) and graft versus-host disease (GVHD) .
|
-
- HY-124676A
-
|
|
Apoptosis
|
Cancer
|
|
DB2115 tetrahydrochloride is a highly selective PU.1 inhibitor that suppresses the binding of PU.1 to DNA (IC50: 2.3 nM). DB2115 tetrahydrochloride can inhibit tumor cell proliferation and induce apoptosis. DB2115 tetrahydrochloride can be used in the research of tumors such as leukemia .
|
-
- 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-181869
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia .
|
-
- HY-171334A
-
|
|
PROTACs
PIN1
CDK
Akt
c-Myc
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. P1D-34 also down-regulates Pin1 client proteins such as Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. P1D-34 shows anti-proliferative activities in a panel of acute myeloid leukemia (AML) cell lines. P1D-34 induces cell DNA damage and apoptosis by releasing ROS generation. Pink: PIN1 ligand (HY-171442A), Blue: CRBN ligand (HY-14658), Black: Linker (HY-W014883) .
|
-
- HY-176735
-
|
|
IRAK
FLT3
Apoptosis
|
Cancer
|
FLT3/IRAK4-IN-1 is a selective FLT3/IRAK4 inhibitor with the remarkable activity towards FLT3-WT (IC50 = 1.95 nM), FLT3-D835Y (IC50 = 3.22 nM) and IRAK4 (IC50 = 53.72 nM). LT3/IRAK4-IN-1 has relatively low toxicity to normal bone marrow cells, can effectively promote cell apoptosis, and has the potential to overcome drug resistance. FLT3/IRAK4-IN-1 can be used for research on acute myeloid leukemia (AML) .
|
-
- HY-155066
-
|
|
PI3K
mTOR
Apoptosis
|
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 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
|
-
- 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-139996
-
|
|
PROTACs
Apoptosis
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
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-164977
-
|
|
PROTACs
Phosphatase
|
Cancer
|
|
JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3
ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)) .
|
-
- HY-P99014
-
|
ARGX-110
|
Fc Receptor (FcR)
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
|
-
- HY-128724
-
CB-5339
2 Publications Verification
|
p97
|
Cancer
|
|
CB-5339 is an oral activity potent p97 inhibitor with an IC50 <30 nM. CB-5339 can be used for leukemia research . CB-5339 extracted from WO2015109285A1 compound FF07.
|
-
- HY-150797
-
|
QA-68-ZU81
|
PROTACs
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
QA-68 (QA-68-ZU81) is an effective PROTAC-class 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 can be formed by a target protein ligand (red part) EA-89 (HY-170314), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-I (HY-131318), and a PROTAC linker (black part) Ethyne-C2-Pip-CO-Pip-Boc (HY-170315). E3 ubiquitin ligase and linker can form Lenalidomide-ethyne-C2-Pip-CO-Pip (HY-170319).
|
-
- 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-P9S0124
-
|
ORM-6151 Antibody; BMS-986497 Antibody
|
|
Cancer
|
|
Anti-CD33 Antibody (OR000283) (ORM-6151 Antibody; BMS-986497 Antibody) is an antibody targeting CD33. It is generated by grafting the FAb (H&L) sequence of Gemtuzumab (HY-P99971) onto an IgG1 Fc carrying the N297A mutation, which inhibits Fc-γR binding. Anti-CD33 Antibody (OR000283) can be used to construct degrader-antibody conjugates (DACs), such as ORM-6151 (HY-171792) .
|
-
- HY-174367
-
|
|
RUNX
Apoptosis
|
Cancer
|
|
RUNX1/ETO-IN-1 is a RUNX1-ETO oncogenic fusion protein inhibitor that specifically targets the NHR2 oligomerization domain. RUNX1/ETO-IN-1 directly interacts with the NHR2 (KD,app = 39 μM). RUNX1/ETO-IN-1 exhibits anti-leukemic activity by inducing apoptosis and promoting differentiation in RUNX1/ETO-translocated AML cells. RUNX1/ETO-IN-1 remains essentially uncharged at physiological pH, demonstrating superior membrane permeability.
|
-
- HY-E70723
-
|
|
FLT3
|
Cancer
|
|
FLT3 (FMS-like tyrosine kinase 3, CD135) is a type 3 receptor tyrosine kinase that plays important roles in cell survival, proliferation, and differentiation during normal hematopoiesis. FLT3 is one of the most frequently mutated genes in acute myeloid leukemia (AML). FLT3 D835Y is the most frequent kinase domain mutation, converting aspartic acid to tyrosine. FLT3 D835Y Recombinant Human Active Protein Kinase is a recombinant FLT3 D835Y protein that can be used to study FLT3 D835Y-related functions .
|
-
- HY-161615
-
|
|
PROTACs
ATM/ATR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC50 of 29.6 nM against ATR, and its IC50 values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia .
|
-
- HY-P992333
-
|
|
C-type Lectin-like Receptors (CTLRs)
|
Cancer
|
|
CLT030 Antibody is a human monoclonal antibody targeting CLL1/CLEC12A/CD371, with a Kd value of 7.32 nM against human targets. CLT030 Antibody can be used to synthesize the ADC CLT030. It is applicable to research related to acute myeloid leukemia .
|
-
- HY-13559A
-
|
Azaspirane dimaleate; SKF 106615-12 dimaleate; SKF 106615A12 dimaleate
|
STAT
Apoptosis
Caspase
Interleukin Related
Autophagy
Reactive Oxygen Species (ROS)
Atg8/LC3
p62
JAK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Atiprimod (Azaspirane) (dimaleate) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
|
-
- HY-110102
-
|
Azaspirane hydrochloride; SKF 106615-12 hydrochloride; SKF 106615
|
JAK
STAT
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Atg8/LC3
p62
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Atiprimod (Azaspirane) hydrochloride is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
|
-
- HY-149359
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
|
-
- HY-13559
-
|
Azaspirane ; SKF 106615-12; SKF 106615A12
|
STAT
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
p62
Atg8/LC3
PARP
NF-κB
PERK
JAK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Atiprimod (Azaspirane) is a STAT3 inhibitor with antitumor, anti-inflammatory, and anti-angiogenic activities. Atiprimod blocks the signaling pathways of IL-6 and VEGF by inhibiting the phosphorylation of signal transducer and activator of STAT3. Atiprimod blocks the JAK-STAT signaling pathway by inhibiting the phosphorylation of JAK2 and JAK3. Atiprimod also inhibits cell proliferation, induces cell cycle arrest, and induces autophagy and apoptosis. Atiprimod triggers persistent ER stress-mediated apoptosis in breast cancer cells by activating the PERK/eIF2α/ATF4/CHOP axis and inhibiting the nuclear translocation of STAT3/NF-κB. Atiprimod shows great anti-tumor activities in tumor xenograft mouse models. Atiprimod can be used for the study of pituitary adenoma, breast cancer, multiple myeloma and acute myeloid leukemia (AML) .
|
-
- 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-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-18948
-
GSK321
1 Publications Verification
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
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. GSK321 induces decrease in intracellular α-Hydroxyglutaric acid (2-HG) (HY-113038B), abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
|
-
- HY-177578
-
|
|
Antibody-Drug Conjugates (ADCs)
c-Kit
Apoptosis
Microtubule/Tubulin
ERK
Akt
Caspase
|
Cancer
|
|
NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research [1][2].
|
-
- HY-128888B
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
(S,R)-GSK321 is the (S,R)-enantiomer of GSK321 (HY-18948). 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. 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. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
|
-
- HY-155770
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-20 (compound 34f) is a potent FLT3 inhibitor with IC50 values of 1 and 4 nM for FLT3-D835Y and FLT3-ITD, respectively. FLT3-IN-20 has anti-proliferation efficacy in FLT3-ITD-positive AML cell lines MV4-11 and MOLM-13 (7 and 9 nM, respectively) and the MOLM-13 variant (4 nM) with the FLT3-ITD-D835Y mutation. FLT3-IN-20 can be used in research of cancer .
|
-
- HY-145939
-
|
BRD5846
|
Casein Kinase
|
Cancer
|
|
BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
|
-
- HY-175282A
-
|
|
Apoptosis
Caspase
CDK
PARP
Autophagy
|
Cancer
|
|
(2S,3R,4S)-ASX-173 is the (2S,3R,4S)-enantiomer of ASX-173 (HY-175282). ASX-173 is an orally active inhibitor of asparagine synthetase (ASNS) (IC50 = 0.113 μM, Ki = 0.4 nM). ASX-173 enhances the anticancer activity of L-asparaginase (ASNase) (HY-P1923). ASX-173 disrupts nucleotide synthesis and induces leukemia cell cycle arrest, apoptosis and autophagy in leukemia cells in combination with ASNase. ASX-173 slows the growth of OCI-AML2 xenografts in combination with ASNase. ASX-173 is indicated for the study of acute lymphoblastic leukemia, acute myeloid leukemia, colorectal cancer, and other cancers .
|
-
- HY-178020
-
|
|
FLT3
ERK
Akt
Apoptosis
|
Cancer
|
|
FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML) .
|
-
- HY-179272
-
|
|
Wee1
HDAC
Apoptosis
|
Cancer
|
|
Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC50 of 1.2 nM for Wee1 and IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC50 of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML) .
|
-
- HY-182356
-
|
|
Methylenetetrahydrofolate Dehydrogenase (MTHFD)
|
Cancer
|
|
MTHFD1/2-IN-1 is an orally active dual MTHFD1/MTHFD2 inhibitor, with IC50 values of 0.26 μM and 0.031 μM against human MTHFD1 and MTHFD2, respectively. MTHFD1/2-IN-1 blocks one-carbon metabolism by inhibiting the dehydrogenase activity of MTHFD1 as well as the dehydrogenase and cyclohydrolase activities of MTHFD2, thereby disrupting nucleotide biosynthesis and redox homeostasis in cancer cells. MTHFD1/2-IN-1 exhibits favorable Caco-2 permeability and hepatic microsomal metabolic stability. MTHFD1/2-IN-1 shows significant anti-leukemic activity, which not only reduces the viability of various leukemia cells but also inhibits tumor growth of acute myeloid leukemia (AML) in mouse models .
|
-
- HY-170576
-
|
|
FLT3
STAT
Apoptosis
|
Cancer
|
|
FLT3-IN-28 (Compound 12y) is an orally active FLT3 inhibitor with antitumor activity. FLT3-IN-28 selectively inhibits cancer cells harboring the FLT3 internal tandem duplication (ITD) mutation, with IC50 values of 85, 290, 130, 65, and 220 nM for BaF3-FLT3-ITD, BaF3-TEL-VEGFR2, MV4-11, MOLM-13, and MOLM-14 cell lines respectively (MV4-11 and MOLM-13/14 are acute myeloid leukemia (AML) cell lines carrying the FLT3-ITD mutation). Additionally, FLT3-IN-28 can downregulate the phosphorylation levels of FLT3 and STAT5 in MOLM-13 cells and induce cell cycle arrest and Apoptosis. FLT3-IN-28 has an oral bioavailability of 19.2% in SD rats and can prolong survival in a dose-dependent manner in NSG mice xenografted with MOLM-13 cells. FLT3-IN-28 holds promise for research in cancer fields related to FLT3-ITD .
|
-
- HY-151411
-
|
|
RUNX
|
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-174847
-
|
|
p97
|
Cancer
|
|
VCP/p97 IN-2 (Compound V13) is a VCP/p97 inhibitor with IC50 of 32 nM for p97. VCP/p97 IN-2 has excellent antitumor activities and significantly inhibits tumor growth in Molm-13 xenograft mice model. VCP/p97 IN-2 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-P99488
-
|
JSP-191; AMG-191
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
Briquilimab (JSP-191 or AMG-191) is a humanized IgG1 monoclonal antibody that binds human CD117 (c-Kit). Briquilimab blocks the interaction between CD117 receptor and stem cell factor on various CD117 expressing tissues. Briquilimab can lead to inhibition of SCF/c-Kit signaling and MC apoptosis. Briquilimab is a non-toxic approach to target and deplete HSC, enabling blood and immune reconstitution with minimal toxicity with the other agents being used for transient immune suppression to prevent immunologic rejection. Briquilimab can be used in various disease research such as severe combined immunodeficiency (SCID), myelodyplastic syndromes (MDS), acute myeloid leukemia (AML), chronic spontaneous urticarial (CSU), chronic inducible urticarial (CIndU) and asthema .
|
-
- HY-179497
-
|
|
FLT3
VEGFR
Akt
STAT
ERK
Apoptosis
|
Cancer
|
FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 and 3.4 nM for FLT3-ITD and TEL-VEGFR2, respectively. FLT3-IN-37 exhibits high selectivity for wild-type FLT3 (WT) and c-Kit. FLT3-IN-37 inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. FLT3-IN-37 exerts anti-leukemia effects by blocking the cell cycle and inducing apoptosis (apoptosis). FLT3-IN-37 can be used for research on acute myeloid leukemia (AML) .
|
-
- HY-180277
-
|
|
PROTACs
CDK
Apoptosis
|
Cancer
|
|
PROTAC CDK6 Degrader 1 (compound 48a) is a potent and selective PROTAC CDK6 degrader with a DC50 of 0.037 μM. PROTAC CDK6 Degrader 1 exhibits selectivity over CDK4 (DC50 > 10 μM). PROTAC CDK6 Degrader 1 induces G0/G1 cell-cycle arrest and apoptosis through inhibition of CDK6 downstream signaling. PROTAC CDK6 Degrader 1 reduces tumor burden and CDK6 levels in a MOLM-14 xenograft mouse model. PROTAC CDK6 Degrader 1 can be used for CDK6-driven cancers research, such as acute myeloid leukemia (AML) .
|
-
- HY-120877
-
|
|
MARK
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-173333
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
PROTAC SMARCA2/4 degrader-38 is a degrader SMARCA2/4 PROTAC (DC50: 3.0 nM and 4.0 nM respectively). PROTAC SMARCA2/4 degrader-38 promotes the ubiquitination and degradation of SMARCA2/4. PROTAC SMARCA2/4 degrader-38 blocks the G0/G1 cell cycle and induces apoptosis. PROTAC SMARCA2/4 degrader-38 can be used in acute myeloid leukemia (AML) research. (Pink: SMARCA2/4 ligand; Blue: VHL ligand (HY-112078); Black: linker; Target Protein Ligand-Linker Conjugates (HY-173343)) .
|
-
- HY-181767
-
|
|
PROTACs
HDAC
Bcl-2 Family
Apoptosis
|
Cancer
|
|
PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia .
|
-
- HY-143877
-
|
|
HDAC
|
Cancer
|
|
NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
|
-
- HY-121708
-
|
|
c-Kit
|
Cancer
|
|
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
|
-
- HY-153718
-
|
|
Ligands for Target Protein for PROTAC
CDK
c-Myc
|
Cancer
|
|
KI-ARv-03 is a potent and selective ATP-competitive CDK9 inhibitor with an IC₅₀ of 0.15 μM (at 45 μM ATP), exhibiting over 130-fold selectivity against other CDKs (including CDK1-7). KI-ARv-03 reduces androgen receptor (AR)-driven transcription and proliferation in prostate cancer cells. KI-ARv-03 can be used for leukemia, pancreatic cancer, alveolar rhabdomyosarcoma (ARMS) and castration-resistant prostate cancer (CRPC) research. KI-ARv-03 is a ligand for target protein for PROTAC. KI-ARv-03 can be used to synthesize PROTAC KI-CDK9d-32 (HY-173523) [1][2].
|
-
- HY-16398
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
|
Cancer
|
|
Pipobroman is a bromide derivative of piperazine and acts as an alkylating agent. Pipobroman plays its role by inhibiting DNA and RNA polymerase or by reducing pyrimidine nucleotide incorporation into DNA. Pipobroman can be used for the cancer research, including polycythemia vera, myeloproliferative neoplasm, and AML et.al .
|
-
- HY-16398R
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Reference Standards
|
Cancer
|
|
Pipobroman (Standard) is the analytical standard of Pipobroman. This product is intended for research and analytical applications. Pipobroman is a bromide derivative of piperazine and acts as an alkylating agent. Pipobroman plays its role by inhibiting DNA and RNA polymerase or by reducing pyrimidine nucleotide incorporation into DNA. Pipobroman can be used for the cancer research, including polycythemia vera, myeloproliferative neoplasm, and AML et.al .
|
-
- HY-153495
-
|
BP1001
|
Bcl-2 Family
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Prexigebersen (BP1001) is an antisense oligonucleotide targeting Bcl-2 and Grb2. Prexigebersen exhibits antileukemic activity in cell models. Prexigebersen induces apoptosis (apoptosis), cell cycle arrest and ROS production in leukemia cells. Prexigebersen inhibits Grb2 expression, thereby suppressing tumor growth and survival. Prexigebersen can be used in studies related to acute myeloid leukemia .
|
-
- HY-175885
-
|
|
PROTACs
Fat Mass and Obesity-associated Protein (FTO)
Apoptosis
Caspase
PARP
YTHDF
|
Cancer
|
|
PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML) . (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))
|
-
- HY-174437B
-
|
|
FLT3
Apoptosis
STAT
p38 MAPK
Akt
|
Cancer
|
|
FLT3-IN-32 hydrochloride is a potent and orally active FLT3 inhibitor with an IC50s of 0.29 nM, 0.77 nM and 2.07 nM against FLT3-ITD, FLT3-D835Y and FLT-N676K. FLT3-IN-32 hydrochloride reduces the phosphorylation of FLT3 and its downstream signaling molecules (STAT5, MAPK, AKT) to induce FLT3-mutated Ba/F3 cells apoptosis. FLT3-IN-32 hydrochloride shows significant anti-tumor efficacy in n the MV4-11 xenograft model. FLT3-IN-32 hydrochloride can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-120877A
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
(R)-MRT199665 is an isomer of MRT199665 (HY-120877). 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-153803
-
|
|
PROTACs
Molecular Glues
Btk
|
Cancer
|
GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
|
-
- HY-181078
-
|
|
c-Myc
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is an anti-leukemic agent with potent ribosome-targeting protein synthesis inhibition. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) downregulates short-lived oncoproteins, including c-Myc and Mcl-1, by inhibiting protein synthesis. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) induces cell cycle arrest at the G0/G1 phase and triggers mitochondrial pathway-mediated apoptosis in acute myeloid leukemia (AML) cells. Cephalotaxine-ester-(R)-1-ethoxy-3-mercaptopropan-2-ol-Ph (3,4OMe) is applicable for research on leukemia .
|
-
- HY-175342
-
|
LOXO-338
|
Bcl-2 Family
|
Cancer
|
|
FCN-338 (LOXO-338) is an orally active and selective Bcl-2 inhibitor with an IC50 of 4.5 nM for Bcl-2/BAK interaction. FCN-338 potently inhibits tumor growth in follicular lymphoma (FL), acute myeloid leukemia (AML), and acute lymphoblastic leukemia (ALL) xenograft mice model without significant weight loss. FCN-338 has a broad-spectrum anti-cancer activity, such as FL, CLL/SLL, AML, and ALL .
|
-
- HY-181695
-
|
|
PROTACs
Histone Acetyltransferase
|
Cancer
|
|
PROTAC KAT2A/B degrader-1 is an orally active CRBN-baed histone acetyltransferase KAT2A/KAT2B PROTAC degrader. PROTAC KAT2A/B degrader-1 induces degradation of KAT2A and KAT2B proteins. PROTAC KAT2A/B degrader-1 inhibits proliferation of acute myeloid leukemia and small cell lung cancer cells. PROTAC KAT2A/B degrader-1 can be used for the research of acute myeloid leukemia, small cell lung cance .
|
-
- HY-123153
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
GSK990 is an inactive mutant IDH1 inhibitor with no significant inhibitory activity against wild-type or mutant IDH1/IDH2 enzymes. In experiments, GSK990 can serve as an inactive negative control for the IDH1 inhibitor GSK321 (HY-18948). GSK990 is applicable to the research of acute myeloid leukemia .
|
-
- HY-P992439
-
|
|
CXCR
|
Cancer
|
|
PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies .
|
-
- HY-162386
-
|
|
Cuproptosis
Mitochondrial Metabolism
|
Cancer
|
|
UM4118 is a potent copper-selective non-genotoxic copper ionophore that induces cuproptosis in acute myeloid leukemia cells. UM4118 exhibits stronger activity against SF3B1G12C mutant acute myeloid leukemia cells. UM4118 transports extracellular copper into cells, elevates intracellular and mitochondrial copper levels, and triggers lipoylated DLAT aggregation, proteotoxic stress, iron-sulfur cluster protein depletion, reduced lipoylated protein levels, and maximal mitochondrial respiratory damage. UM4118 cytotoxicity can be enhanced by supplementation with extracellular copper, abolished by copper chelation, and shows synthetic lethal effects in the absence of iron-sulfur cluster biosynthesis/transport genes. UM4118 can be used for the study of acute myeloid leukemia .
|
-
- HY-169067
-
|
Mtx-C
|
DNA/RNA Synthesis
p38 MAPK
Bacterial
|
Infection
Cancer
|
|
10-Methoxy-canthin-6-one (Mtx-C) is analkaloid derivative. 10-Methoxy-canthin-6-one can induce DNA damage by intercalating into DNA. 10-Methoxy-canthin-6-one can inhibit cancer cells proliferation, cause G2/M phase arrest and induce myeloid differentiation. T10-Methoxy-canthin-6-one can upregulate the expression of myeloperoxidase, CD15, CD11b, and CD14, as well as activation of p38 MAPK. 10-Methoxy-canthin-6-one also exhibits anti-bacterial activity. 10-Methoxy-canthin-6-one can be used for the researches of cancer and infection, such as acute myeloid leukemias (AML) .
|
-
- HY-161708
-
|
|
PROTACs
CDK
FLT3
|
Cancer
|
|
PROTAC FLT3/CDKs degrader-1 (Compound C3) is a degrader for cyclin-dependent kinases (DC50 is 18.73 nM for CDK2) and the FMS-like tyrosine kinase 3 (FLT3). PROTAC FLT3/CDKs degrader-1 induces differentation of HL-60 (72.77% differentation at 6.25 nM), inhibits proliferation of AML cells, with IC50s of 2.9-37 nM. PROTAC FLT3/CDKs degrader-1 is potential for ameliorating acute myeloid leukemia. (Pink: ligand for target protein FLT3/CDKs ligand-1 (HY-161709); Black: linker (HY-W012935); Black: ligand for E3 ligase Thalidomide 5-fluoride (HY-W087383))
|
-
- HY-181976
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Others
|
|
dHTC3 is a selective BRD4 molecular glue degrader. dHTC3 specifically recruits the first bromodomain of BRD4 to the E3 ubiquitin ligase complex (SCF FBXO3), thereby triggering the ubiquitination and degradation of BRD4 .
|
-
- HY-P991228
-
|
|
Galectin
|
Cancer
|
|
LYT-200 is a humanized monoclonal antibody against galectin-9 (Galectin-9). LYT-200 binds to galectin-9 expressed on the surface of hematologic malignant cells, inhibits pro-leukemic functions and induces cell death. LYT-200 can be used in research related to hematologic malignancies .
|
-
- HY-138632
-
|
|
PROTACs
Epigenetic Reader Domain
PROTAC-Linker Conjugates for PAC
|
Cancer
|
|
PROTAC BRD4 Degrader linker conjugate is a linker-payload conjugate as well as a bifunctional degrader of BRD4 that binds to VHL, consisting of PROTAC and a linker. PROTAC BRD4 Degrader linker conjugate can be conjugated with STEAP1 and CLL1 antibodies to degrade BRD4 protein, with DC50 values of 0.86 nM and 7.6 nM, respectively. PROTAC BRD4 Degrader linker conjugate can be used in research related to prostate cancer and acute myeloid leukemia (BRD4 ligand: (HY-129939); VHL ligand: (HY-125845)) .\n
|
-
- HY-181959
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
APL-4098 is an orally active, selective, ATP-competitive GCN2 inhibitor with a Ki of 4.39 nM and a Kd of 2.9 nM. APL-4098 reduces the phosphorylation level of eIF2α and the expression level of ATF4. APL-4098 impairs mitochondrial function and exerts cytotoxic effects on primary acute myeloid leukemia cells. APL-4098 is applicable to research related to acute myeloid leukemia .
|
-
- HY-175610
-
|
|
PROTACs
FLT3
JAK
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
|
-
- HY-P991998
-
|
|
Fc Receptor (FcR)
|
Inflammation/Immunology
Cancer
|
|
Anti-Human/Monkey CD16a Antibody (3G8) is a monoclonal antibody targeting CD16a. Anti-Human/Monkey CD16a Antibody (3G8) blocks FcγRIII/CD16a, upregulates the metabolic activity of CD16+ cells, downregulates CD87, a poor prognostic marker, and inhibits the engraftment and growth of leukemia cells in acute myeloid leukemia, and rapidly increases platelet counts in immune thrombocytopenia. Anti-Human/Monkey CD16a Antibody (3G8) is applicable to research related to tumor immunology .
|
-
- HY-155033
-
|
|
Stearoyl-CoA Desaturase (SCD)
DNA/RNA Synthesis
Apoptosis
Autophagy
mTOR
Influenza Virus
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
SSI-4 is an orally active stearoyl-CoA desaturase (SCD1) inhibitor with an EC50 of 1.9 nM against mouse SCD1. SSI-4 blocks the conversion of saturated fatty acids to monounsaturated fatty acids, reducing the production of oleic acid and palmitoleic acid. SSI-4 induces lipid peroxidation, endoplasmic reticulum stress, DNA damage and activates apoptotic mechanisms. SSI-4 inhibits mTORC1 activity, suppresses B cell proliferation and antibody production, and induces autophagy. SSI-4 is applicable to research on cancers such as acute myeloid leukemia and renal cell carcinoma, as well as influenza infections .
|
-
- HY-170403
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-38 (Compound 23e) is a reversible, orally active inhibitor for lysine specific demethylase 1 (LSD1) with an IC50 of 1.2 nM. LSD1-IN-38 inhibits the proliferation of cancer cells MV4-11, Kasumi-1 and NCI-H526, with IC50 of 5, 4 and 11 nM, respectively. LSD1-IN-38 activates CD86 expression with an EC50 of 0.034 μM, and induces differentiation in MV4−11 cell. LSD1-IN-38 exhibits antitumor efficacy in mouse models .
|
-
- HY-159657
-
|
|
Salt-inducible Kinase (SIK)
Interleukin Related
|
Inflammation/Immunology
|
|
PF-07899895 (Compound 34) is a SIK inhibitor, with IC50 values of 1.2 nM, 0.9 nM, and 1.8 nM against SIK1, SIK2, and SIK3, respectively. PF-07899895 modulates the anti-inflammatory cytokine IL-10 in immune cells. PF-07899895 is applicable to research related to inflammatory diseases .
|
-
- HY-162250
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC50=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .
|
-
- HY-108894
-
|
|
Ferroptosis
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Ferumoxytol is an FDA-approved ultrasmall superparamagnetic iron oxide preparation and iron replacement agent that exerts selective activity against leukemia cells with low ferroportin expression. Ferumoxytol increases intracellular iron levels, induces reactive oxygen species (ROS) production via the Fenton reaction, and triggers oxidative stress and cell death. Ferumoxytol reduces disease burden in mouse models and patient-derived leukemia models. As an MRI contrast agent, Ferumoxytol enables imaging of vascular lesions, tumors and lymph nodes. Ferumoxytol can be used in research related to acute myeloid leukemia and blast-phase chronic myeloid leukemia .
|
-
- HY-13560
-
AVN-944
5 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-178858
-
|
|
PROTACs
FLT3
Checkpoint Kinase (Chk)
STAT
ERK
c-Myc
Akt
|
Cancer
|
|
PROTAC FLT3/CHK1 Degrader-1 is a PROTAC FLT3/CHK1 degrader, with DC50 values of 5.88 nM (FLT3) and 4.17 nM (CHK1), respectively. PROTAC FLT3/CHK1 Degrader-1 can inhibit the phosphorylation of FLT3 downstream signaling effectors STAT5 (Tyr694), AKT (Ser473), and ERK (Tyr204), downregulate the protein level of c-Myc and maintain the expression of p53 protein. PROTAC FLT3/CHK1 Degrader-1 induces apoptosis in MV-4-11 cells. PROTAC FLT3/CHK1 Degrader-1 shows significant anti-tumor efficacy in mice bearing MV-4-11 subcutaneous xenografts. PROTAC FLT3/CHK1 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/CHK1 ligand (HY-178869 ), Blue: CRBN Ligand (HY-W093272), Black: Linker, E3 ligase ligand-linker conjugate (HY-W998238)) .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P11288
-
|
|
PACAP Receptor
Apoptosis
|
Cancer
|
|
ANT308 is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 significantly enhances the activation and proliferation of T cells. ANT308 inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 can be used for the studies of acute myeloid leukemia (AML) and uveal melanoma (UVM) .
|
-
- HY-P11288A
-
|
|
PACAP Receptor
Apoptosis
|
Cancer
|
|
ANT308 TFA is a vasoactive intestinal polypeptide (VIP receptor) antagonist. ANT308 TFA significantly enhances the activation and proliferation of T cells. ANT308 TFA inhibits the migration and metastasis, induces apoptosis of melanoma tumor cells by inhibiting VIP-VPAC2 signaling and reducing the expression of MCAM and N-cadherin. ANT308 TFA can be used for the study of acute myeloid leukemia (AML) and uveal melanoma (UVM) .
|
-
- HY-P11451
-
|
|
CXCR
|
Cancer
|
|
Pentixather is a radiolabeled peptide that can target CXCR4. Pentixather can disrupt the interaction between leukemic cells and the bone marrow microenvironment by targeting the CXCR4/CXCL12 signaling axis, reduce the retention of leukemic cells in the protective bone marrow niche, and thereby enhance the sensitivity of leukemic cells to treatment. Pentixather can be used for the study of acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .
|
-
- HY-P11076
-
|
|
Complement System
|
Cancer
|
|
CP-EPS8-NLS is a peptide with anti-AML property. CP-EPS8-NLS interferes with EPS8-associated signaling and exerts anti-AML activity in various AML cell types. CP-EPS8-NLS has potent antitumor activity in xenograft tumor models. CP-EPS8-NLS downregulates EPS8 expression and its downstream pathway .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99014
-
|
ARGX-110
|
Fc Receptor (FcR)
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
|
-
(5)
-
- HY-P99394
-
|
JNJ-64407564
|
CD3
|
Cancer
|
|
Talquetamab (JNJ-64407564) is a humanized bispecific antibody that binds to GPRC5D (member of G protein-coupled receptor family C5 group D) and CD3 to induce T cell-mediated killing of GPRC5D-expressing MM cells through T cell recruitment and activation. Talquetamab (JNJ-64407564) has antitumor activity .
|
-
(5)
-
- HY-P99971
-
|
|
ADC Antibody
Transmembrane Glycoprotein
|
Cancer
|
|
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen. Gemtuzumab affects cell necrosis by specifically targeting CD33 expressed on the surface of leukaemic cell blasts in 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. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
|
-
(5)
-
- HY-P99488
-
|
JSP-191; AMG-191
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
Briquilimab (JSP-191 or AMG-191) is a humanized IgG1 monoclonal antibody that binds human CD117 (c-Kit). Briquilimab blocks the interaction between CD117 receptor and stem cell factor on various CD117 expressing tissues. Briquilimab can lead to inhibition of SCF/c-Kit signaling and MC apoptosis. Briquilimab is a non-toxic approach to target and deplete HSC, enabling blood and immune reconstitution with minimal toxicity with the other agents being used for transient immune suppression to prevent immunologic rejection. Briquilimab can be used in various disease research such as severe combined immunodeficiency (SCID), myelodyplastic syndromes (MDS), acute myeloid leukemia (AML), chronic spontaneous urticarial (CSU), chronic inducible urticarial (CIndU) and asthema .
|
-
(5)
-
- HY-P9983
-
|
SGN-33; HuM-195; GLK-33 Antibody
|
Transmembrane Glycoprotein
Radionuclide-Drug Conjugates (RDCs)
|
Inflammation/Immunology
|
|
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
|
-
(5)
-
- 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) .
|
-
(5)
-
- HY-P991669
-
|
AML-01
|
Caspase
Apoptosis
|
Cancer
|
|
IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers. .
|
-
(5)
-
- HY-P99390
-
|
MCLA 117
|
CD3
Interleukin Related
IFNAR
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Tepoditamab (MCLA-117) is a full-length human IgG1 bispecific monoclonal antibody that binds to CLEC12A of myeloid cells and CD3 of cytotoxic T cells. Among others, CLEC12A is a myeloid differentiation antigen. Tepoditamab kills AML leukaemia mother cells and AML leukaemia stem cells, induces T cell-mediated proliferative lysis of AML cells. Tepoditamab induces upto 30-fold T-cell expansion. Tepoditamab results in moderate to strong cytokine (IFNγ, IL-6, IL-8, IL-10, and TNFα) and IFNγ release in human whole blood and PBMC, respectively. Tepoditamab can be used in acute myeloid leukaemia (AML) research .
|
-
(5)
-
- HY-P99916
-
|
AMG-427
|
FLT3
CD3
TNF Receptor
|
Inflammation/Immunology
Cancer
|
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
|
-
(5)
-
- 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 .
|
-
(5)
-
- HY-P991228
-
|
|
Galectin
|
Cancer
|
|
LYT-200 is a humanized monoclonal antibody against galectin-9 (Galectin-9). LYT-200 binds to galectin-9 expressed on the surface of hematologic malignant cells, inhibits pro-leukemic functions and induces cell death. LYT-200 can be used in research related to hematologic malignancies .
|
-
(5)
-
- HY-P991517
-
|
|
Transmembrane Glycoprotein
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Cancer
|
|
BI-836858 is a fully human anti-CD33 monoclonal antibody. BI-836858 reduces CD33+ cells via antibody-dependent cellular cytotoxicity (ADCC), blocks downstream signaling of S100A9/CD33, decreases the secretion of immunosuppressive cytokines and reactive oxygen species-induced genomic instability, and restores bone marrow hematopoietic function. BI-836858 is applicable to the research of myelodysplastic syndrome (MDS) and AML .
|
-
(5)
-
- HY-P990002
-
|
|
c-Kit
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD117/c-Kit Antibody (2B8) is an IgG2b antibody, targeting to mouse CD117/c-Kit. Anti-Mouse CD117/c-Kit Antibody (2B8) reacts with mouse c-Kit (also known as CD117), which is expressed on hematopoietic progenitor cells, mast cells, and acute myeloid leukemia (AML) cells. Anti-Mouse CD117/c-Kit Antibody (2B8) can be used for the detection of flow cytometry, immunofluorescence and immunohistochemistry in cancer and inflammation .
|
-
(5)
-
- HY-P991665
-
|
OBT357NF; OBT357
|
Transmembrane Glycoprotein
|
Cancer
|
|
MEN1112 (OBT357NF) is a selective humanized monoclonal antibody targeting the Bst1/CD157 antigen (EC50=1 nM). MEN1112 exerts potent antitumor activity against acute myeloid leukemia (AML) cells. MEN1112 is promising for research of hematological malignancies such as AML .
|
-
(5)
-
- HY-P990905
-
|
SAR-443579
|
Interleukin Related
|
Cancer
|
|
Bexatamig (SAR-443579) is a trifunctional natural killer cell engager targeting IL-3R α/CD123, NKp46/NCR1/CD335 and Fc gamma RIIIA/CD16a. Bexatamig forms a cytolytic synapse between natural killer cells and CD123-positive tumor cells. By activating natural killer cells to induce tumor cell death, Bexatamig effectively reduces the burden of CD123-positive acute myeloid leukemia (AML) blasts. Bexatamig has been granted FDA Fast Track designation, and is primarily investigated for relapsed or refractory acute myeloid leukemia, B-cell acute lymphoblastic leukemia, and high-risk myelodysplastic syndromes .
|
-
(5)
-
- HY-P990928
-
|
APVO-436
|
CD3
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Mipletamig (APVO-436) is a bispecific CD123 x CD3 monoclonal antibody. Mipletamig simultaneously binds to both CD3-expressing T cells and CD123-expressing cancer cells, thereby crosslinking CD123-expressing tumor cells and cytotoxic T lymphocytes (CTLs). This results in the activation and proliferation of T-cells and causes CTL-mediated cell lysis of CD123-expressing tumor cells. Mipletamig can be used for the study of acute myeloid leukemia (AML) .
|
-
(5)
-
- HY-P991656
-
|
|
CXCR
Apoptosis
p38 MAPK
Akt
|
Cancer
|
|
LY-2624587 is a humanized IgG4 monoclonal antibody antagonist targeting CXCR4. LY-2624587 blocks SDF-1/CXCR4 interaction and SDF-1-induced GTP binding. LY-2624587 significantly inhibits cell migration and induces apoptosis in human lymphoma and leukemia cells. LY-2624587 also inhibits CXCR4 and SDF-1 mediated cell signaling including activation of MAPK and AKT. LY-2624587 can be used for human hematological malignancies like acute myeloid leukemia (AML) research .
|
-
(5)
-
- HY-P990164
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse RGMb Antibody (307.9D1) is a rat-derived IgG2a κ type antibody inhibitor, targeting to mouse RGMb. Anti-Mouse RGMb Antibody (307.9D1) blocks RGMb binding to PD-L2. Anti-Mouse RGMb Antibody (307.9D1) can be used for the researches of cancer inflammation and immunology, such as acute myeloid leukemia (AML) and graft versus-host disease (GVHD) .
|
-
(5)
-
- HY-P991294
-
|
|
ADC Antibody
|
Cancer
|
|
MGTA-117 is a humanized monoclonal antibody targeting CD117. MGTA-117 can be used for synthesis of antibody-drug conjugate (ADC), utilizing an amanitin payload. MGTA-117 has potent anti-tumor activity and increases survival in three acute myeloid leukemia (AML) xenograft hNSG mice models (Kasumi-1, AML PDX 1 and AML PDX 2). MGTA-117 enables hematopoietic stem cell transplantation (HSCT) preprocessing in AML, myelodysplasia with excess blasts (MDS-EB) and gene therapy .
|
-
(5)
-
- HY-P991425
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
AT-1413 is a human monoclonal antibody (mAb) targeting CD43. AT-1413 induces antibody-dependent cell-mediated cytotoxicity (ADCC) in melanoma cell lines and acute myeloid leukemia (AML) cells. AT-1413 has antitumor activity in AML mouse models. AT-1413 can be used in Acute myeloid leukaemia, Breast cancer, Malignant melanoma and Myelodysplastic syndromes research. Recommended isotype control: Human IgG1 kappa, Isotype Control (HY-P99001) .
|
-
(5)
-
- HY-P990901
-
|
IGM-8444
|
TNF Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Aplitabart (IGM-8444) is a a pentameric IgM DR5 agonist antibody with 10 binding sites specific for DR5. Aplitabart multimerizes DR5 to selectively and potently induce tumor cell apoptosis. Aplitabart can be used for the study of lung cancer, breast cancer, cute myeloid leukemia (AML) and low-grade B-cell non-Hodgkin lymphoma (B-NHL) .
|
-
(5)
-
- HY-P991648
-
|
|
Interleukin Related
|
Cancer
|
|
CSL-360 is a chimeric unconjugated IgG1 monoclonal antibody targeting CD123. CSL-360 efficiently prevents the binding of IL-3 to CD123, abolishing IL-3 induced cell proliferation. CSL-360 can be used for acute myeloid leukemia (AML) research .
|
-
(5)
-
- HY-P9S0124
-
|
ORM-6151 Antibody; BMS-986497 Antibody
|
|
Cancer
|
|
Anti-CD33 Antibody (OR000283) (ORM-6151 Antibody; BMS-986497 Antibody) is an antibody targeting CD33. It is generated by grafting the FAb (H&L) sequence of Gemtuzumab (HY-P99971) onto an IgG1 Fc carrying the N297A mutation, which inhibits Fc-γR binding. Anti-CD33 Antibody (OR000283) can be used to construct degrader-antibody conjugates (DACs), such as ORM-6151 (HY-171792) .
|
-
(5)
-
- HY-P992333
-
|
|
C-type Lectin-like Receptors (CTLRs)
|
Cancer
|
|
CLT030 Antibody is a human monoclonal antibody targeting CLL1/CLEC12A/CD371, with a Kd value of 7.32 nM against human targets. CLT030 Antibody can be used to synthesize the ADC CLT030. It is applicable to research related to acute myeloid leukemia .
|
-
(5)
-
- HY-P992439
-
|
|
CXCR
|
Cancer
|
|
PF-06747143 is recombinant anti-human antibody targeting CXCR4. PF-06747143 blocks CXCL12-induced calcium flux, F-actin polymerization, chemotaxis, cell migration, and leukemic cell bone marrow homing. PF-06747143 reduces tumor burden and improves survival in mouse models of hematologic malignancies. PF-06747143 can be used for the research of chronic lymphocytic leukemia, acute myeloid leukemia, and hematologic malignancies .
|
-
(5)
-
- HY-P991998
-
|
|
Fc Receptor (FcR)
|
Inflammation/Immunology
Cancer
|
|
Anti-Human/Monkey CD16a Antibody (3G8) is a monoclonal antibody targeting CD16a. Anti-Human/Monkey CD16a Antibody (3G8) blocks FcγRIII/CD16a, upregulates the metabolic activity of CD16+ cells, downregulates CD87, a poor prognostic marker, and inhibits the engraftment and growth of leukemia cells in acute myeloid leukemia, and rapidly increases platelet counts in immune thrombocytopenia. Anti-Human/Monkey CD16a Antibody (3G8) is applicable to research related to tumor immunology .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-112852S
-
|
|
|
TL02-59-d5 is the deuterium labeled TL02-59 (HY-112852). TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an ICC50 of 0.03 nM. TL02-59 inhibits Lyn and Hck with ICC50s of 0.1 nM and 160 nM, respectively. TL02-59 potently suppresses acute myelogenous leukemia (AML) cell growth.
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-150725
-
|
|
|
CpG ODNs
|
|
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-150725C
-
|
|
|
CpG ODNs
|
|
ODN 1585 sodium is a potent inducer of IFN and TNFα production. ODN 1585 sodium is a potent stimulator of NK (natural killer) function. ODN 1585 sodium increases CD8+ T-cell function, including the CD8+ T cell-mediated production of IFN-γ. ODN 1585 sodium induces regression of established melanomas in mice. ODN 1585 sodium can confer complete protection against malaria in mice. ODN 1585 sodium can be used for acute myelogenous leukemia (AML) and malaria research. ODN 1585 sodium can be used as a vaccine adjuvant .
|
-
- HY-153495
-
|
BP1001
|
|
Antisense Oligonucleotides
|
|
Prexigebersen (BP1001) is an antisense oligonucleotide targeting Bcl-2 and Grb2. Prexigebersen exhibits antileukemic activity in cell models. Prexigebersen induces apoptosis (apoptosis), cell cycle arrest and ROS production in leukemia cells. Prexigebersen inhibits Grb2 expression, thereby suppressing tumor growth and survival. Prexigebersen can be used in studies related to acute myeloid leukemia .
|
-
- HY-177821
-
|
|
|
Aptamers
|
|
CD117/c-Kit aptamer sodium is a single-strand DNA aptamer specific for the biomarker CD117, which is highly expressed on acute myeloid leukemia (AML) cells.
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
