Search Result
Results for "
myeloid leukemia cells
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P99014
-
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ARGX-110
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Apoptosis
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Inflammation/Immunology
Cancer
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Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML) .
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-
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- HY-158341
-
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
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Cancer
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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 .
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-
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- HY-169067
-
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Mtx-C
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p38 MAPK
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Cancer
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0-Methoxy-canthin-6-one (Mtx-C) is a DNA damage inducer. 0-Methoxy-canthin-6-one promotes cell cycle arrest at the G2/M phase by intercalating into DNA, thereby inducing myeloid differentiation of acute myeloid leukemia (AML) cells and leukemic stem cells (LSCs). The myeloid differentiation in AML and LSC cells is characterized by increased expression of myeloperoxidase, CD15, CD11b, and CD14, as well as activation of p38 MAPK. 0-Methoxy-canthin-6-one can be used in leukemia research .
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-
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- HY-129592
-
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Apoptosis
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Cancer
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p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
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-
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- HY-112218
-
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S-64315
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Bcl-2 Family
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Cancer
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MIK665 (S-64315), derived from S63845, is a myeloid cell leukemia sequence 1 (MCL1) inhibitor . MIK665 has an IC50 of 1.81 nM for MCL1 .
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-
-
- HY-162489
-
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Bcr-Abl
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Others
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Tyrosine kinase-IN-8 (compound 4e) is a BCR‐ABL1 tyrosine kinase inhibitor (TKI). Tyrosine kinase-IN-8 shows anti-proliferative activity against K562 cells, a chronic myeloid leukemia (CML) cell line (CC50=0.8 µM). Tyrosine kinase-IN-8 can be used in the study of chronic leukemia .
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-
-
- HY-162906
-
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HDAC
FLT3
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Cancer
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FLT3/HDAC-IN-2 is (compound 25h) a FLT3/HDAC dual inhibitor. FLT3/HDAC-IN-2 has antiproliferative activity against MOLM-13 cells. FLT3/HDAC-IN-2 can be used in acute myeloid leukemia research .
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-
-
- HY-168605
-
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MMP
Apoptosis
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Cancer
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DH-18 is a matrix metalloproteinase-2 (MMP-2) inhibitor with the IC50 values of 139.45 nM, 518.11 nM and 833.34 nM for MMP-2, MMP-9 and MMP-8, respectively. DH-18 induces cell apoptosis and arrests cell cycle in the G0/G1 phase. DH-18 inhibits cell growth and can be used for study of chronic myeloid leukemia .
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-
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- HY-126920
-
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FLT3
Apoptosis
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Cancer
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AFG206 is a first-generation ATP competitive “type II” FLT3 inhibitor. AFG206 potently inhibits cell proliferation (IC50 around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia .
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-
-
- HY-142690
-
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HDAC
Apoptosis
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Cancer
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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) .
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-
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- HY-142690A
-
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Apoptosis
HDAC
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Cancer
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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) .
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-
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- HY-16271
-
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4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
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MDM-2/p53
Apoptosis
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Cancer
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Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
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-
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- HY-144782
-
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HDAC
Autophagy
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Cancer
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HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
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-
-
- HY-144782A
-
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HDAC
Autophagy
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Cancer
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HDAC10-IN-2 hydrochloride (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 hydrochloride modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
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- HY-144779
-
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HDAC
Autophagy
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Cancer
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HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells .
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- HY-128888B
-
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Isocitrate Dehydrogenase (IDH)
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Cancer
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(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 .
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- HY-12892
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SphK
Apoptosis
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Cancer
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SKI-178 is a potent sphingosine kinase-1 (SphK1) and SphK2 inhibitor. SKI-178 is cytotoxic at IC50 concentrations ranging from 1.8 to 0.1 μM in both agent sensitive and multi-agent resistant cancer cell lines (i.e., MTR3, NCI-ADR and HL60/VCR cells). SKI-178 induces apoptosis in a CDK1-dependent manner in human acute myeloid leukemia cell lines .
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- HY-162936
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FLT3
Apoptosis
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Cancer
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SILA-123 is a FLT3 inhibitor (FLT3-WT: IC50=2.1 nM; FLT3-ITD: IC50=1.0 nM). SILA-123 inhibits FLT3 phosphorylation and downstream signaling pathways, leading to apoptosis by arresting cell cycle progression at the G0/G1 phase. SILA-123 can be used in the study of acute myeloid leukemia .
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-
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- HY-144675A
-
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Histone Demethylase
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Cancer
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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 .
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- HY-144675
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Histone Demethylase
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Cancer
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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 .
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- HY-115906
-
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FLT3
MNK
Apoptosis
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Cancer
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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 .
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- HY-123486
-
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Apoptosis
Bcr-Abl
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Cancer
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HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML) .
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- HY-12083
-
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Bcr-Abl
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Cancer
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PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
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- HY-142696
-
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CDK
Pim
Apoptosis
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Cancer
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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 .
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- HY-164542
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Isocitrate Dehydrogenase (IDH)
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Cancer
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TQ05310 is an orally available inhibitor of IDH2 mutants, targeting both IDH2-R140Q (IC50=136.9 nM) and IDH2-R172K (IC50=37.9 nM) mutants. TQ05310 inhibits the production of 2-hydroxyglutarate (2-HG) and induces differentiation of cells expressing IDH2-R140Q and IDH2-R172K by inhibiting the enzymatic activity of mutant IDH2. TQ05310 can be used for the study of acute myeloid leukemia .
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- HY-128607
-
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Bcl-2 Family
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Cancer
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Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM .
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- HY-139877
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Microtubule/Tubulin
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Cancer
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OXS007417 induces differentiation of acute myeloid leukemia cells (EC50 = 48 nM) in vitro and shows antitumor effects in vivo.
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-
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- HY-148422
-
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Eukaryotic Initiation Factor (eIF)
Apoptosis
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Cancer
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Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .
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- HY-171146
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FLT3
Bcr-Abl
RET
PDGFR
MNK
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Cancer
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HSN748 is a Ponatinib (HY-12047) analogue and a multikinase inhibitor. HSN748 has inhibitory activity on FLT3, ABL1, RET, PDGFRα/β, MNK1, MNK2 and other kinases. HSN748 can inhibit the growth of chronic myeloid leukemia and acute myeloid leukemia cell lines and can be used in the study of leukemia .
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- HY-150507
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Bcl-2 Family
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Cancer
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JNJ-4355 is a highly potent MCL-1 (myeloid cell leukemia-1) inhibitor, with KI of 18 pM. JNJ-4355 shows antitumor activity .
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- HY-146749
-
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FLT3
Trk Receptor
Apoptosis
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Cancer
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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) .
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-
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- HY-168475
-
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Apoptosis
WDR5
HDAC
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Cancer
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DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. DD0-2363 inhibits cells proliferation and induces apoptosis in acute myeloid leukemia cells. DD0-2363 has antitumor activity and can be used in the research of acute myeloid leukemia .
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- HY-154961
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 14 (Compound (Ra)-10) is an inhibitor of myeloid cell leukemia-1 (MCL-1) with an Ki of 0.018 nM and can be used for anticancer research .
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- HY-100741
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S63845
Maximum Cited Publications
83 Publications Verification
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Bcl-2 Family
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Cancer
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S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1 .
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-
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- HY-125908
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-
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- HY-110071
-
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c-Kit
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Cancer
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APcK110 is a potent Kit inhibitor that can be used for the research of acute myeloid leukemia (AML). APcK110 induces AML cell apoptosis .
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- HY-B0722
-
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Endogenous Metabolite
Reactive Oxygen Species
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Metabolic Disease
Cancer
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Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
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- HY-163293
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 18 (compound 57) is a myeloid cell leukemia 1 (Mcl-1) inhibitor, and can be used for study of cancer .
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- HY-136175
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SNDX-5613
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Epigenetic Reader Domain
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Cancer
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Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .
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- HY-162008
-
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HSP
Bcl-2 Family
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Cancer
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S1g-10 is a Hsp70/Bim inhibitor, and shows antitumor activity in chronic myeloid leukemia cells .
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- HY-172154
-
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CXCR
Apoptosis
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Cancer
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SSB-2548 is a CXCR-4 inhibitor. SSB-2548 can inhibit the proliferation, migration and induce apoptosis of acute myeloid leukemia cells. SSB-2548 has good gastrointestinal absorption and can be used in the research of leukemia .
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-
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- HY-163541
-
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Scavenger Receptor Class B type I (SR-BI）
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Cancer
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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 .
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-
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- HY-19527
-
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N6-Benzyladenosine-5'-phosphate
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STAT
Apoptosis
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Cancer
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IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML) .
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- HY-123718
-
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Parasite
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Others
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6-Benzylthioinosine is a compound with antileukemic activity that increases cytotoxicity against acute myeloid leukemia cells when combined with metformin, modulating cellular metabolism and signaling pathways through multiple mechanisms.
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-
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- HY-B0722R
-
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Endogenous Metabolite
Reactive Oxygen Species
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Metabolic Disease
Cancer
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Histamine (dihydrochloride) (Standard) is the analytical standard of Histamine (dihydrochloride). This product is intended for research and analytical applications. Histamine dihydrochloride is a reactive oxygen species (ROS) inhibitor. Histamine dihydrochloride can suppress ROS production and work together with IL-2 to activate T cells and NK cells, leading to immune activation in the tumor microenvironment, which consequently kills acute myeloid leukemia (AML) cells. Histamine dihydrochloride can cause a reduction in vaginal tetrazo reduction, increased epithelial growth, and heightened keratinization in mouse models of ovariectomy. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma .
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-
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- HY-115406A
-
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Apoptosis
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Cancer
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CPTH6 hydrobromide is a thiazole derivative which activates apoptotic program and increases autophagic features in human acute myeloid leukemia cell lines. CPTH6 can be used for cancer research .
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-
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- HY-112041
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PTC596
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BMI1
Apoptosis
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Cancer
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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 .
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-
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- HY-13297
-
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E1/E2/E3 Enzyme
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Cancer
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PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells .
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- HY-169843
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c-Myc
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Cancer
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Cotylenin A is a type of phenanthraquinone compound that works alongside vitamin K2 to induce the differentiation of monocytes and halt their growth, while also inhibiting the expression of c-Myc and inducing the expression of cyclin G2 in human leukemia HL-60 cells. Cotylenin A can be used in studies on acute myeloid leukemia .
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- HY-161149
-
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HDAC
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Cancer
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CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells .
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- HY-18626
-
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Topoisomerase
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Cancer
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NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM .
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- HY-170763
-
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Apoptosis
Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 22 (Example 36) is a myeloid cell leukemia-1 (MCL-1) inhibitor which inhibits the antiapoptotoic activity of MCL-1 by inhibiting its interaction with proapototic proteins. Mcl-1 inhibitor 22 exhibits anti-proliferation activities against various cancer cell lines and can be utilized in cancer research .
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- HY-170763A
-
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Apoptosis
Bcl-2 Family
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Cancer
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(+)-Mcl-1 inhibitor 22 (Example 37) is a myeloid cell leukemia-1 (MCL-1) inhibitor which inhibits the antiapoptotoic activity of MCL-1 by inhibiting its interaction with proapototic proteins. (+)-Mcl-1 inhibitor 22 exhibits anti-proliferation activities against various cancer cell lines and can be utilized in cancer research .
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- HY-125151
-
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STAT
Apoptosis
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Cancer
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BP-1-108 is a selective inhibitor of STAT5 (Ki=8.3 μM) with anticancer activity. BP-1-108 induces apoptosis of leukemia cells by inhibiting the phosphorylation of STAT5. BP-1-108 can be used in the study of acute myeloid leukemia and prostate cancer .
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- HY-127130
-
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Bcl-2 Family
Apoptosis
Fungal
Antibiotic
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Infection
Cancer
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Spicamycin, an adenine nucleoside antibiotic with antifungal and antitumor activities. Spicamycin is also a potent inducer of differentiation of myeloid leukemia cells. Spicamycin induces apoptosis in NB4 cells via down-regulation of Bcl-2 expression and modulation of PML protein .
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- HY-148203
-
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 9 (example 2) is a myeloid cell leukemia 1 (Mcl-1) inhibitor with IC50 value of 0.21889 nM. Mcl-1 inhibitor 9 shows anti-tumor activity .
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- HY-164515
-
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Apoptosis
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Cancer
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ONC213 is an αKGDH inhibitor that suppresses mitochondrial respiration and elevates α-ketoglutarate levels by inhibiting αKGDH activity, leading to apoptosis (Apoptosis) in AML cells. ONC213 can be used in acute myeloid leukemia research .
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- HY-13680
-
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Dian III; N-Methylisoindigotin; Natura-α
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Apoptosis
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Cancer
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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 .
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- HY-139535
-
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CG-806
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FLT3
Btk
Apoptosis
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Cancer
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Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .
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- HY-168213
-
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FLT3
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Cancer
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FLT3-IN-27 (compound 49) is a FLT3-ITD inhibitor with the IC50 of 174 nM. FLT3-IN-27 inhibits cell growth and increases the number of cells in the G1 phase of the cell cycle and can be used for study of acute myeloid leukemia .
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- HY-173158
-
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Histone Acetyltransferase
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Cancer
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AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer) .
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- HY-101266B
-
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DS-3032b; DS-3032 tosylate hydrate
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
|
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Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis .
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- HY-108969
-
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NSC 366140; PD 115934
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Topoisomerase
Apoptosis
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Cancer
|
|
Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment .
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- HY-101266
-
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DS-3032
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MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
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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 .
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-
- HY-103275
-
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NSC 680410
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Bcr-Abl
Apoptosis
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Cancer
|
|
Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210 bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells .
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- HY-100741A
-
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Bcl-2 Family
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Cancer
|
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(S,R)-S63845 is the isomer of S63845 (HY-100741), and can be used as an experimental control. S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1 .
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-
- HY-100741C
-
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Bcl-2 Family
Drug Isomer
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Cancer
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(R,R)-S63845 is the isomer of S63845 (HY-100741), and can be used as an experimental control. S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a Kd of 0.19 nM for human MCL1 .
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- HY-N0071
-
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Isoguanosine
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FLT3
HDAC
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Cancer
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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 .
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-
- HY-B1336
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Bacterial
Apoptosis
Antibiotic
Parasite
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Infection
Cancer
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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].
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- HY-30272
-
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Biochemical Assay Reagents
Apoptosis
DNA/RNA Synthesis
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Cancer
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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 .
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- HY-152133
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PROTACs
HDAC
Apoptosis
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Cancer
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PROTAC HDAC6 degrader (Compound A6) is a potent and selective PROTAC HDAC6 degrader with a DC50 of 3.5 nM. PROTAC HDAC6 degrader shows promising antiproliferative activity via inducing apoptosis in myeloid leukemia cell lines .
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- HY-N2492
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Methyl trans-p-coumarate
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Bacterial
Apoptosis
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Infection
Cancer
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(E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
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- HY-129079
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Estrogen Receptor/ERR
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Cancer
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TFMB-(R)-2-HG, a cell membrane-permeable version of (R)-2-HG, is a carcinogenic factor in Acute myeloid leukemia (AML).
TFMB-(R)-2-HG impairs SCF ER-Hoxb8 cells differentiation in response to estrogen withdrawal .
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- HY-121725
-
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STAT
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Cancer
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MM-206, a STAT3 activity inhibitor, potently inhibits the STAT3 SH2 domain-phosphopeptide interaction with IC50 of 1.2 μM. MM-206 demonstrates dose-dependent induction of apoptosis in acute myeloid leukemia (AML) cell lines .
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- HY-149981
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P-glycoprotein
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Cancer
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P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia .
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- HY-168983
-
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Bcl-2 Family
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Cancer
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Lonitoclax is a B-cell lymphoma 2 (Bcl-2) inhibitor. Lonitoclax has comparable anti-tumor efficacy to Venetoclax (HY-15531) in both B cell and myeloid malignancy models. Lonitoclax is promising for research of relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas .
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- HY-103275R
-
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NSC 680410 (Standard)
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Bcr-Abl
Apoptosis
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Cancer
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Adaphostin (Standard) is the analytical standard of Adaphostin. This product is intended for research and analytical applications. Adaphostin (NSC 680410), the adamantyl ester of AG957, is a potent p210bcr/abl inhibitor (IC50=14 μM). Adaphostin induces apoptosis in T-lymphoblastic human leukemia cell lines (IC50 ranging from 17 to 216 nM). Adaphostin has significant and selective activity against chronic and acute myeloid leukemia cells. Adaphostin increased the level of reactive oxygen species (ROS) within CLL B cells[1][2][3].
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- HY-128360
-
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PROTACs
Bcl-2 Family
Apoptosis
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Cancer
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dMCL1-2 is a potent and selective PROTAC of myeloid cell leukemia 1 (MCL1) (Bcl-2 family member) based on Cereblon, which binds to MCL1 with a KD of 30 nM. dMCL1-2 activats the cellular apoptosis machinery by degradation of MCL1 .
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- HY-124629A
-
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Apoptosis
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Cancer
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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 .
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-
- HY-155556
-
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ClpP
|
Cancer
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ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
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- HY-19541A
-
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Epigenetic Reader Domain
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Cancer
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I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin .
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-
- HY-114162B
-
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Epigenetic Reader Domain
Apoptosis
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Cancer
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VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
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-
- HY-162386
-
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Cuproptosis
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Cancer
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UM4118 is a copper ionophore that can initiate a mitochondrial-based noncanonical form of cell death known as cuproptosis. UM4118 exhibits high sensitivity in SF3B1-mutated and adverse risk acute myeloid leukemia (AML), and can be used for AML research .
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-
- HY-121917
-
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c-Myc
Apoptosis
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Inflammation/Immunology
|
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APTO-253 (LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4 (KLF4) tumor suppressor. APTO-253 hydrochloride exhibits antiarthritic activity.
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- HY-155153
-
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Apoptosis
CDK
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Others
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CDK9-IN-24 (compound 21a) is a highly selective CDK9 inhibitor with significant inhibitory effect on tumor growth. CDK9-IN-24 effectively blocks cell proliferation and induces apoptosis by downregulating Mcl-1 and c-Myc, and can be used in acute myeloid leukemia research .
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-
- HY-P99623
-
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MGD006; S80880
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CD3
|
Cancer
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Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
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-
- HY-163707
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Apoptosis
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Cancer
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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 .
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- HY-129388A
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CC-90011; LSD1-IN-7
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Histone Demethylase
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Cancer
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Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
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- HY-163803
-
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HDAC
DNA Methyltransferase
|
Cancer
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CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models .
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- HY-162250
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PROTACs
Histone Methyltransferase
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Cancer
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MS8847 is a highly potent EZH2 PROTAC degrader that recruits the E3 ligase von Hippel-Lindau (VHL). MS8847 potently degrades EZH2 in a ubiquitin-proteasome system-dependent manner. MS8847 effectively inhibits the growth of acute myeloid leukemia (AML) and triple-negative breast cancer (TNBC) cells .
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-
- HY-W286906
-
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Bcl-2 Family
Apoptosis
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Cancer
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Mcl1-IN-15 (Compound 7) is the inhibitor for myeloid cell leukemia 1 (Mcl-1) with an IC50 of 8.73 μM. Mcl1-IN-15 inhibits Mcl1-BH3 peptide interaction, activates the Bak/Bax-mediated apoptosis and exhibits antitumor activity .
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-
- HY-163160
-
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Apoptosis
Epigenetic Reader Domain
|
Cancer
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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 .
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-
- HY-122240
-
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FLT3
|
Cancer
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AAE871 is a potent type I FLT3 inhibitor with an IC50 value of 0.034 µM. AE871 has the potential for the research of acute myeloid leukemia (AML) .
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- HY-129388B
-
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CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
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Histone Demethylase
|
Cancer
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CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
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- HY-16291
-
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LOR-253; LT-253
|
c-Myc
KLF
Apoptosis
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Inflammation/Immunology
Cancer
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APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor . APTO-253 has antiarthritic activity .
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- HY-N3210
-
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Others
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Cancer
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Nb-Demethylechitamine is an alkaloid isolated from the methanol extract of Alstonia rostrata twigs. Nb-Demethylechitamine has in vitro cytotoxic activity against several human cancer cell lines, including human myeloid leukemia HL-60, liver cancer SMMC-7721, lung cancer A-549, breast cancer MCF-7, and colon cancer SW480 cells .
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-
- HY-173123
-
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Histone Demethylase
Apoptosis
|
Cancer
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LSD1-IN-40 (Compound 9e) is a potent LSD1 inhibitor, with an IC50 of 9.85 nM. LSD1-IN-40 exhibits exceptional selectivity for LSD1 over both MAOs and hERG. LSD1-IN-40 exhibits significant inhibitory activity against leukemia cells (MV-4-11, HL-60, and THP-1 cells). LSD1-IN-40 can induce apoptosis in MV-4-11 cells. LSD1-IN-40 has the potential for the research of acute myeloid leukemia .
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-
- HY-P3508
-
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MDM-2/p53
|
Cancer
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|
PNC-27, a chimeric p53-penetratin peptide binds to HDM-2 in a p53 peptide-like structure, induces selective membrane-pore formation and leads to cancer cell lysis. PNC-27 is an anticancer peptide. PNC-27 can be used in acute myeloid leukemia research .
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- HY-123121
-
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Antibiotic
Apoptosis
Bacterial
NF-κB
|
Infection
Inflammation/Immunology
Cancer
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Nargenicin A1 is an antibiotic agent against various Gram-positive bacteria. Nargenicin A1 shows anti-inflammatory activity. Nargenicin A1 protects HINAE cells against Tacrolimus (HY-13756)-induced DNA damage and apoptosis. Nargenicin A1 can also be used for the research of acute myeloid leukemia .
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- HY-149470
-
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Histone Acetyltransferase
|
Cancer
|
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MOZ-IN-3 (Compound 6j) is a KAT6A (MOZ) acetyltransferase inhibitor (IC50: 30 nM). MOZ-IN-3 has antitumor activity against four different myeloid leukemia cell lines (HL-60, U937, SKNO-1, K562). MOZ-IN-3 has favorable metabolic stability and pharmacokinetics .
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-
- HY-164607
-
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DNA/RNA Synthesis
|
Cancer
|
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YL-5092 is an inhibitor for YT521-B homology (YTH) domain-containing protein 1 (YTHDC1). YL-5092 inhibits acute myeloid leukemia cell with IC50 of 0.28-2.87 μM. YL-5092 exhibits antitumor efficacy in MOLM-13 or U937 xenograft mice .
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-
- HY-P3508A
-
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MDM-2/p53
|
Cancer
|
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PNC-27 acetate, a chimeric p53-penetratin peptide binds to HDM-2 in a p53 peptide-like structure, induces selective membrane-pore formation and leads to cancer cell lysis. PNC-27 acetate is an anticancer peptide. PNC-27 acetate can be used in acute myeloid leukemia research .
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-
- HY-149474
-
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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) .
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-
- HY-132231
-
|
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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 .
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-
- HY-172153
-
|
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CDK
Reactive Oxygen Species
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-149735
-
|
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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 .
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-
- 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 .
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-
- HY-124629
-
DB2313
2 Publications Verification
|
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-170952
-
|
|
Molecular Glues
|
Cancer
|
|
LYG-409 is an orally active degrader of GSPT1. LYG-409 shows excellent anti-acute myeloid leukemia and prostate cancer in vivo with TGI of 94.34% and 104.49%, respectively. LYG-409 inhibits KG-1 cells mediated by the degradation of GSPT1 with an IC50 of 9.50 nM, with a DC50 of 7.87 nM in vitro .
|
-
- HY-13653
-
|
EGCG; Epigallocatechol Gallate
|
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
|
-
- HY-16291A
-
|
LOR-253 hydrochloride; LT-253 hydrochloride
|
c-Myc
|
Inflammation/Immunology
|
|
APTO-253?(LOR-253) hydrochloride is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253?hydrochloride mediates anticancer activity via induction of Kruppel-like factor 4?(KLF4)?tumor suppressor. APTO-253?hydrochloride exhibits antiarthritic activity .
|
-
- HY-129388
-
|
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-125090
-
|
|
Aurora Kinase
c-Myc
Bcr-Abl
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PHA-680626 is an effective inhibitor of the interaction between Aurora-A and N-Myc. PHA-680626 inhibits kinase activity of AURKA and Bcr-Abl, and induces N-Myc degradation. PHA-680626 decreases phosphorylation of CrkL and histone H3. PHA-680626 shows anti-proliferative and pro-apoptotic activity on Imatinib (HY-15463)-resistant chronic myeloid leukemia cell lines and primary CD34+ cells .
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-
- HY-N2492R
-
|
|
Bacterial
Apoptosis
|
Infection
Cancer
|
|
(E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate. This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
|
-
- HY-B1899AR
-
|
|
G protein-coupled Bile Acid Receptor 1
Endogenous Metabolite
|
Metabolic Disease
|
|
(E)-Methyl 4-coumarate (Standard) is the analytical standard of (E)-Methyl 4-coumarate. This product is intended for research and analytical applications. (E)-Methyl 4-coumarate (Methyl 4-hydroxycinnamate), found in several plants, such as Allium cepa or Morinda citrifolia L. leaves. (E)-Methyl 4-coumarate cooperates with Carnosic Acid in inducing apoptosis and killing acute myeloid leukemia cells, but not normal peripheral blood mononuclear cells. Antioxidant and antimicrobial activity.
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-
- HY-149539
-
|
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FLT3
RET
|
Cancer
|
|
PLM-101 is an orally available anticancer agent targeting FLT3 and RET with inhibitory activity against acute myeloid leukemia cells. PLM-101 inhibits RET, thereby inducing autophagic degradation of FLT3; and it inhibits the PI3K and Ras/ERK pathways, resulting in anti-leukemia activity. PLM-101 has anti-tumor efficacy in a mouse MV4-11 flank xenograft model (dose: 3, 10 mg/kg; po) and an allogeneic xenograft mouse model (dose: 40 mg/kg; po) .
|
-
- HY-158147
-
|
|
PI3K
|
Cancer
|
|
PI3Kδ-IN-20 (compound (S)-36) is a potent inhibitor of PI3Kδ, with the IC50 of 6.4 nM. PI3Kδ-IN-20 has oral bioactivity. PI3Kδ-IN-20 shows significant suppression of cell proliferation and remarkable induction of apoptosis both in vitro and in vivo .
|
-
- HY-112378
-
|
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FLT3
|
Cancer
|
|
D-65476 is an inhibitor of type Ⅲ receptor tyrosine kinase (Flt3). In the absence of IL-3, D-65476 inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells (IC50= 0.2 μM), which can be used in the study of Flt3-driven leukemia .
|
-
- HY-148036
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-16 is a potent FLT3 inhibitor with an IC50 of 1.1 μM. FLT3-IN-16 can be used for researching acute myeloid leukemia .
|
-
- 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-111158
-
|
|
c-Met/HGFR
|
Cancer
|
|
BMS-748730 is an oral tyrosine kinase inhibitor. BMS-748730 inhibits tyrosine kinase activity by competing with the ATP binding site of the tyrosine kinase, which prevents the kinase from phosphorylating the substrate protein, thereby inhibiting signaling pathways associated with cell proliferation and tumor growth. BMS-748730 can be used in the study of certain types of cancer, including chronic myeloid leukemia (CML) .
|
-
- 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-170604
-
|
|
MMP
|
Cardiovascular Disease
Cancer
|
|
MMP-2 Inhibitor-4 (Compound 5g) is an MMP-2 inhibitor with an IC50 of 152.62 nM. MMP-2 Inhibitor-4 can reduce the levels of MMP-2 in the K562 cell line through stable binding at the MMP-2 active site, and it demonstrates strong antiangiogenic effects in the ACHN cell line. MMP-2 Inhibitor-4 holds promise for research in chronic myeloid leukemia (CML) .
|
-
- HY-150526
-
|
|
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGCG-4″-sulfate is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate sulfate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. EGCG-4″-sulfate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
|
-
- 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-144709
-
|
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FLT3
|
Cancer
|
|
FLT3/ITD-IN-1 (Compound 1) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 38.2 nM and 144.1 nM against FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-1 displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
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-
- HY-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-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-169400
-
|
|
HDAC
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
|
-
- 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-168493
-
|
|
FLT3
VEGFR
HDAC
STAT
PERK
|
Cancer
|
|
FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia .
|
-
- HY-128634
-
|
|
Apoptosis
PI3K
MEK
|
Cancer
|
|
CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer .
|
-
- HY-13653R
-
|
EGCG(Standard); Epigallocatechol Gallate (Standard)
|
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(-)-Epigallocatechin Gallate (Standard) is the analytical standard of (-)-Epigallocatechin Gallate. This product is intended for research and analytical applications. (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
|
-
- HY-163854
-
|
|
HSP
Bcl-2 Family
Apoptosis
|
Cancer
|
|
HSP70-IN-6 (Compound JL-15) is an inhibitor of Hsp70-Bim protein-protein interaction (PPI) (IC50: 70 nM). HSP70-IN-6 induces apoptosis in chronic myeloid leukemia (CML) cells, with EC50s of 0.43 μM(BV173), 0.88 μM (K562), 0.19 μM (K562-R3) .
|
-
- 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-123201
-
|
|
FLT3
|
Cancer
|
|
KRN383 analog is an analog of KRN383. KRN383 is an orally active Flt3 inhibitor that inhibits the autophosphorylation of Flt3 bearing internal tandem duplications (ITDs) and the Asp835Tyr (D835Y) point mutation with IC50 values of < or =5.9 and 43 nM, respectively. KRN383 also inhibits the proliferation of the ITD-positive cell lines with IC50 values of < or =2.9 nM. KRN383 can be used for the research of acute myeloid leukemia .
|
-
- HY-173631
-
|
|
PROTACs
|
Cancer
|
|
(S)-dHTC1 is a molecular glue degrader targeting the transcriptional co-activator ENL. (S)-dHTC1 binds the ligase with high affinity only after forming the ENL:dHTC1 complex with an IC50 value of 93 nM. (S)-dHTC1 degrades ENL in MV4;11 cells with a DC50 value of 26 nM. (S)-dHTC1 can be used for acute myeloid leukemia study .
|
-
- 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-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-N1746
-
|
2'-O-Methylkurarinone
|
RANKL/RANK
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
(2S)-2'-Methoxykurarinone, a compound isolated from the roots of Sophora flavescens, has anti-inflammatory, antipyretic, antidiabetic, and antineoplastic effects. (2S)-2'-Methoxykurarinone (MK) inhibits osteoclastogenesis and bone resorption through down-regulation of RANKL signaling. (2S)-2'-Methoxykurarinone (MK) displays cytotoxic activity against human myeloid leukemia HL-60 cells .
|
-
- HY-145015
-
|
HM43239
|
FLT3
Apoptosis
|
Cancer
|
|
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-145015A
-
|
HM43239 hydrate
|
FLT3
Apoptosis
|
Cancer
|
|
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-135664
-
-
- HY-160174
-
|
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL kinase-IN-3 (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research .
|
-
- HY-160174A
-
|
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL kinase-IN-3 (dihydrocholide) (example 1) is a potent inhibitor of BCR-ABL that plays an important role in acute myeloid leukemia (AML) research .
|
-
- 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-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-13653S1
-
|
EGCG-d4; Epigallocatechol Gallate-d4
|
Isotope-Labeled Compounds
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(-)-Epigallocatechin Gallate-d4 (EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
|
-
- 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-402815
-
|
|
Drug Intermediate
|
Cancer
|
|
(E)-4-(Naphthalen-2-yl)but-3-en-2-one (Compound 7) is a small active molecule that can be used as building block. (E)-4-(Naphthalen-2-yl)but-3-en-2-one exhibits anti-leukemic activity, that inhibits the proliferation of human chronic myeloid leukemia cell K562 with an IC50 of 7.6 μM .
|
-
- 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-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-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-132307
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Mcl-1 inhibitor 6 is an orally active, selective myeloid cell leukemia 1 (Mcl-1) protein inhibitor with a Kd of 0.23 nM and a Ki of 0.02 μM. Mcl-1 inhibitor 6 possesses superior selectivity over other Bcl-2 family members (Bcl-2, Bcl2A1, Bcl-xL, and Bcl-w, Kd>10 μM). Mcl-1 inhibitor 6 is a potent antitumor agent .
|
-
- HY-125834
-
|
|
PROTACs
Bcr-Abl
Apoptosis
STAT
JAK
|
Cancer
|
|
GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
|
-
- HY-15815
-
|
|
Epigenetic Reader Domain
Apoptosis
CDK
HIV
|
Cancer
|
|
Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
|
-
- HY-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-121245
-
-
- 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-144711
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-3 (Compound 19) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 0.9 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-3 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-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-144710
-
|
|
FLT3
|
Cancer
|
|
FLT3/ITD-IN-2 (Compound 17) is a potent FLT3 internal tandem duplications (FLT3-ITD) inhibitor with IC50 values of 0.3, 0.4 and 1.0 nM against FLT3 D835Y, FLT3 and FLT3-ITD, respectively. FLT3/ITD-IN-2 potently inhibits the phosphorylation of FLT3 and displays excellent antiproliferative activities against acute myeloid leukemia cell lines .
|
-
- HY-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-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-161615
-
|
|
Apoptosis
PROTACs
|
Cancer
|
|
PROTAC ATR degrader-2 (Compound 8i) is a PROTAC degrader for ATR, through of . PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC50 of 22.9 and 34.5 nM. APROTAC ATR degrader-2 induces apoptosis, inhibits proliferations of AML cells. PROTAC ATR degrader-2 exhibits good pharmacokinetics charachers and antitumor efficacy against AML in mouse model. (Pink: ATR ligand (HY-161616); Blue:E3 ligase ligand Lenalidomide (HY-A0003); Black: linker)
|
-
- 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-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-111517
-
|
|
Apoptosis
SF3B1
|
Cancer
|
|
H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant .
|
-
- HY-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-164469
-
|
|
Bcr-Abl
Apoptosis
STAT
|
Cancer
|
|
CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
|
-
- 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-167673
-
|
|
E1/E2/E3 Enzyme
|
Infection
Inflammation/Immunology
Cancer
|
|
RNF5-IN-1 (FX12) is a selective RNF5 degrader. RNF5-IN-1 binds to RNF5 and inhibits its E3 activity, and promotes proteasomal degradation of RNF5 in an endoplasmic reticulum (ER)-associated degradation (ERAD) way in cells. RNF5-IN-1 inhibits α-1-antitrypsin (NHK) dislocation with an IC50 value of 2.7 μM. RNF5-IN-1 can be used for research of cystic fibrosis, acute myeloid leukemia, and certain viral infections .
|
-
- HY-149819
-
|
|
HDAC
CDK
|
Cancer
|
CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
|
-
- HY-155066
-
|
|
PI3K
mTOR
|
Cancer
|
|
FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
|
-
- HY-164099
-
|
|
HDAC
Monoamine Oxidase
Histone Demethylase
|
Cancer
|
|
LSD1/HDAC6-IN-2 (JBI-802) is an orally active LSD1/HDAC6/MAO-A inhibitor, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. LSD1/HDAC6-IN-2 can inhibit the growth of multiple myeloma cells MM.1S, MM.1R, and RPMI-8226. LSD1/HDAC6-IN-2 can be used for research on diseases such as acute myeloid leukemia and lymphoma .
|
-
- HY-171334A
-
|
|
PROTACs
PIN1
CDK
Akt
c-Myc
|
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-120044
-
|
|
Farnesyl Transferase
Ras
|
Cancer
|
|
L-739749 is a farnesyl transferase inhibitor. L-739749 inhibits the selective hypersensitivity of JMML cells to granulocyte-macrophage colony-stimulating factor (GM-CSF) by blocking the prenylation of Ras. L-739749 exhibits a strong inhibitory effect on the growth of primary human JMML cells in vitro .
|
-
- 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.
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- HY-156158
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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) .
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- HY-P99395
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JNJ 56022473; CSL 362
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Interleukin Related
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Cancer
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Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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- HY-150797
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QA-68-ZU81
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PROTACs
Epigenetic Reader Domain
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Inflammation/Immunology
Cancer
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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).
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- HY-170669
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PROTACs
CRM1
Apoptosis
NF-κB
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Cancer
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PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies (Pink: Target Protein Ligand (HY-170672); Black: Linker (HY-W010525); Blue: E3 Ligase Ligand (HY-170671); E3 Ligase Ligand-Linker Conjugate (HY-170673)) .
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- HY-169317
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- HY-169318
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- HY-144777
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FLT3
Apoptosis
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Cancer
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FLT3-IN-14 is a potent FLT3 inhibitor with IC50s of 5.6 nM and 1.4 nM for FLT3-WT and FLT3-ITD. FLT3-IN-14 reduces the phosphorylation of FLT3 (Y591), induces cell cycle arrest at G1 phase and apoptosis. FLT3-IN-14 significantly reduces the tumor growth in an MV4-11 xenograft mouse model .
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- HY-120877
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MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
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Cancer
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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 .
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- HY-173333
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PROTACs
Epigenetic Reader Domain
Apoptosis
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Cancer
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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)) .
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- HY-173320
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Wee1
HSP
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Cancer
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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) .
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- HY-145939
-
|
BRD5846
|
Casein Kinase
|
Cancer
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|
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 .
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- HY-151411
-
|
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RUNX
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Cancer
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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 .
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- HY-120877A
-
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|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
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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 .
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- HY-131061
-
|
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Epigenetic Reader Domain
|
Cancer
|
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BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with high affinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .
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- HY-10475G
-
|
CD336; NSC608001; Ro 40-6055
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RAR/RXR
|
Cancer
|
|
AM580 (CD336) (GMP) is AM580 (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist .
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- HY-170576
-
|
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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 .
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- HY-161708
-
|
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PROTACs
CDK
FLT3
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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))
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- HY-121708
-
|
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c-Kit
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Cancer
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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.
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-
- HY-143434
-
|
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FLT3
|
Cancer
|
|
FLT3/D835Y-IN-1 (compound 13a) is a orally active, potent and selective FLT3 and FLT3/D835Y inhibitor, with IC50 values of 0.26 nM and 0.18 nM, respectively. FLT3/D835Y-IN-1 also blocks tumor growth, has anticancer efficacy, and can be used to research for AML (acute myeloid leukemia) .
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- 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 .
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- HY-133136
-
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4 11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- HY-13560
-
AVN-944
4 Publications Verification
VX-944
|
Arenavirus
DNA/RNA Synthesis
Apoptosis
Caspase
Bcl-2 Family
|
Infection
Cancer
|
|
AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research .
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-
| Cat. No. |
Product Name |
Type |
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- HY-10475G
-
|
CD336 (GMP); NSC608001 (GMP); Ro 40-6055 (GMP)
|
Fluorescent Dye
|
|
AM580 (CD336) (GMP) is AM580 (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist .
|
| Cat. No. |
Product Name |
Type |
-
- HY-10475G
-
|
CD336 (GMP); NSC608001 (GMP); Ro 40-6055 (GMP)
|
Biochemical Assay Reagents
|
|
AM580 (CD336) (GMP) is AM580 (HY-10475) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. AM580 is a selective RARα agonist .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3508A
-
|
|
MDM-2/p53
|
Cancer
|
|
PNC-27 acetate, a chimeric p53-penetratin peptide binds to HDM-2 in a p53 peptide-like structure, induces selective membrane-pore formation and leads to cancer cell lysis. PNC-27 acetate is an anticancer peptide. PNC-27 acetate can be used in acute myeloid leukemia research .
|
-
- HY-P3508
-
|
|
MDM-2/p53
|
Cancer
|
|
PNC-27, a chimeric p53-penetratin peptide binds to HDM-2 in a p53 peptide-like structure, induces selective membrane-pore formation and leads to cancer cell lysis. PNC-27 is an anticancer peptide. PNC-27 can be used in acute myeloid leukemia research .
|
-
- HY-K3102
-
|
|
|
MCE Human Acute Myeloid Leukemia Cell Culture Medium is specially designed to promote the in vitro growth of primary human acute myeloid leukemia cells.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99014
-
|
ARGX-110
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Cusatuzumab is a human αCD70 monoclonal antibody. Cusatuzumab shows cytotoxicity activity with enhanced antibody-dependent cellular. Cusatuzumab reduces leukemia stem cells (LSCs) and triggers gene signatures related to myeloid differentiation and apoptosis. Cusatuzumab has the potential for the research of Acute myeloid leukemia (AML) .
|
-
- HY-P99623
-
|
MGD006; S80880
|
CD3
|
Cancer
|
|
Flotetuzumab (MGD006; S80880) is an investigational CD123/CD3 bispecific dual-affinity retargeting antibody (DART) molecule. Flotetuzumab reactivates T cells by simultaneously binding to CD123 in target cells and CD3 in effector T cells, leading to T-cell-mediated cytotoxicity in target cells. Flotetuzumab shows inhibitory effect on a mouse model of patient-derived xenograft (PDX) in acute myeloid leukemia (AML) .
|
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13653S1
-
|
|
|
(-)-Epigallocatechin Gallate-d4 (EGCG-d4) is the deuterium labeled (-)-Epigallocatechin Gallate (HY-13653). (-)-Epigallocatechin Gallate (EGCG) is a major polyphenol in green tea, which can inhibit cell proliferation and induce cell apoptosis. (-)-Epigallocatechin Gallate inhibits glutamate dehydrogenase 1/2 (GDH1/2, GLUD1/2) activity. (-)-Epigallocatechin Gallate has a potent anticancer, antioxidant and anti-inflammatory properties against various types of cancers such as colorectal cancer, myeloid leukemia, thyroid carcinoma .
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