Search Result
Results for "
leukemic
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-115740A
-
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Ara-CTP trisodium
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DNA/RNA Synthesis
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Cancer
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Cytarabine triphosphate (Ara-CTP) trisodiu, an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate trisodiu levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine .
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-
-
- HY-N9359
-
|
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Apoptosis
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Cardiovascular Disease
|
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Toddaculin is a natural coumarin that can induce differentiation and apoptosis in leukemic cells. Toddaculin suppresses excess osteoclast activity and enhances osteoblast differentiation and mineralization. Toddaculin also exhibits anti-inflammatory activity .
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-
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- HY-160415A
-
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PROTACs
Apoptosis
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Cancer
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WD6305 TFA is a potent METTL3-targeted PROTAC degrader. WD6305 TFA selectively reduces the METTL3 and METTL14 complex. WD6305 TFA inhibits m 6A modification and the proliferation of AML cells and promotes apoptosis. WD6305 TFA can be used for the research of leukemic .
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-
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- HY-100490B
-
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Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Cancer
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Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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-
-
- HY-100490A
-
|
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Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Cancer
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Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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-
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- HY-115740
-
|
Ara-CTP
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DNA/RNA Synthesis
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Cancer
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Cytarabine triphosphate (Ara-CTP), an active metabolite of Cytarabine, is a competitive inhibitor of DNA synthesis. Intracellular Cytarabine triphosphate levels can be used to predict chemosensitivity of leukemic blasts to Cytarabine .
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-
-
- HY-117220
-
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Others
|
Cancer
|
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Aspochalasin M is a colorless solid. Aspochalasin M shows modest activity against HL-60 cells with an IC50 of 20.0 μM. Aspochalasin M has the potential for the research of leukemic disease .
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-
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- HY-160415
-
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PROTACs
Apoptosis
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Cancer
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WD6305 is a potent METTL3-targeted PROTAC degrader. WD6305 selectively reduces the METTL3 and METTL14 complex. WD6305 inhibits m 6A modification and the proliferation of AML cells and promotes apoptosis. WD6305 can be used for the research of leukemic .
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-
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- HY-148994
-
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Dihydrofolate reductase (DHFR)
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Cancer
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Methotrexate-γ-aspartate is a Ll210 cell dihydrofolate reductase inhibitor. Methotrexate-γ-aspartate is apparently more resistant to enzymic cleavage than is methotrexate-y-glutamate. Methotrexate-γ-aspartate can be used in antibody-targeted liposomes and is promising for research of leukemic .
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-
-
- HY-100490
-
|
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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-
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- HY-150566
-
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Bcr-Abl
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Cancer
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BCR-ABL-IN-5 (compound II) is a Bcr-Abl kinase (Breakpoint cluster region-Abelson) inhibitor. BCR-ABL-IN-5 inhibits Bcr-Abl WT and Bcr-Abl T3151 with the IC50 value of 0.014 μM and 0.45 μM, respectively. BCR-ABL-IN-5 has some anti-proliferative activity against leukemic cells .
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-
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- HY-112041
-
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PTC596
|
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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- 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-118452
-
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Microtubule/Tubulin
Apoptosis
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Cancer
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cis-3,4',5-Trimethoxy-3'-hydroxystilbene is a stilbene. cis-3,4',5-Trimethoxy-3'-hydroxystilbene induces cytochrome c release to the cytoplasm. cis-3,4',5-Trimethoxy-3'-hydroxystilbene-induced apoptosis is associated with mitochondrial release of cytochrome c. cis-3,4',5-Trimethoxy-3'-hydroxystilbene also suppresses tubulin polymerization. cis-3,4',5-Trimethoxy-3'-hydroxystilbene can be used for leukemic research .
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-
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- HY-119827
-
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F 860191
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Others
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Cancer
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Moflomycin (F 860191) is a compound with strong anti-leukemic activity and low mutagenicity. Moflomycin has an antiproliferative effect on the leukemic cell line HL60 in vitro (IC50=2.9 nM) .
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- HY-128067
-
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Hexamethylene amiloride; HMA
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Sodium Channel
HIV
Apoptosis
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Infection
Cancer
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5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively .
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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 a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
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- HY-133900
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Others
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Cancer
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Deoxyharringtonine is an alkaloid isolated from Cephalotaxus genus with significant anti-leukemic activity .
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- HY-N3401
-
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Others
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Cancer
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Lasiodiplodin is a potent anti-leukemic macrolide can be isolated from Euphorbia splendens .
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-
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- HY-164393
-
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JAK
Bcr-Abl
Apoptosis
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Cancer
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ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
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-
-
- HY-135190
-
-
-
- HY-169091
-
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Others
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Cancer
|
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TS-002266 is a small molecule TUT4/7 inhibitor with anti-leukemic effects. TS-002266 is promising for research of cancers .
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-
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- HY-100423
-
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KPT-8602
|
CRM1
|
Cancer
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Eltanexor (KPT-8602) is a second-generation, highly specific and orally active exportin-1 (XPO1) inhibitor with potent anti-leukemic activity. Eltanexor (KPT-8602) inhibits XPO1-dependent nuclear export (EC50=60.9 nM) by directly targeting XPO1. Eltanexor (KPT-8602) induces Caspase-dependent apoptosis in a panel of leukemic cell lines .
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- HY-N3514
-
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Others
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Cancer
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Kuwanon E is a flavonoid isolated from Morus alba, cytotoxic to human monocytic leukemic cell lines, and reduces the level of IL-1β .
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-
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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-N10071
-
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Others
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Cancer
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Poricoic acid G is a triterpenoid that can be isolated from Poria cocos. Poricoic acid G has a significant cytotoxic effect on leukemia cells and is a potential potent anti-leukemic compound in humans .
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-
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- HY-N8402
-
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Others
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Cancer
|
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Germacrone 4,5-epoxide is a sesquiterpene that can be isolated from Curcuma cf. viridiflora. Germacrone 4,5-epoxide has excellent anti-leukemic activities .
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- HY-111617
-
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Apoptosis
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Cancer
|
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BTR-1 is an active anti-cancer agent, causes S phase arrest, and affects DNA replication in leukemic cells. BTR-1 activates apoptosis and induces cell death .
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- HY-149334
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-
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- HY-N10789
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Others
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Cancer
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(2S)-4'-Hydroxy-7-methoxyflavan is a Flavan. Flavan (4′-hydroxy-7-methoxyflavan) showed an important cytotoxic effect on human leukemic Molt 4 cells .
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-
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- HY-119361
-
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(Rac)-Deoxysappanone B 7,4' dimethyl ether
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Microtubule/Tubulin
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Cancer
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(Rac)-Deox B 7,4, a homoisoflavanoid compound, inhibits microtubule polymerization via binding near the colchicine site and promote reversible G2 arrest. (Rac)-Deox B 7,4 possesses nanomolar anti-leukemic activity .
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-
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- HY-112885A
-
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Nω-Hydroxy-nor-L-arginine acetate
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Arginase
Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
|
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nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism .
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- HY-141430
-
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Histone Methyltransferase
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Cancer
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AS-85 is a potent ASH1L histone methyltransferase inhibitor (IC50=0.6 µM) with anti-leukemic activity. AS-85 strongly binds to the ASH1L SET domain, with the Kd value of 0.78 µM .
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- HY-147934
-
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HDAC
Apoptosis
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Cancer
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HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC50 value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines .
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- HY-153274A
-
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Apoptosis
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Cancer
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CWI1-2 hydrochloride is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects .
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- HY-153274
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Apoptosis
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Cancer
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CWI1-2 is an IGF2BP2 inhibitor that binds IGF2BP2 and inhibits its interaction with m6A-modified target transcripts, induces apoptosis and differentiation, and shows promising anti-leukemic effects .
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- HY-N0732
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Apoptosis
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Cancer
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Jolkinolide B, a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud, is known to induce apoptosis in cancer cells .
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- HY-120297
-
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Others
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Cancer
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S 9788 is a triazinoaminopiperidine derivative that acts as multidrug-resistance modulator .
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- HY-123380
-
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Methyl bruneomycin; NSC-45384
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Others
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Cancer
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Methyl streptonigrin (Methyl bruneomycin) is a derivative of streptonigrin. Methyl streptonigrin has anti-tumor activity .
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- HY-N0732R
-
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Apoptosis
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Cancer
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Jolkinolide B (Standard) is the analytical standard of Jolkinolide B. This product is intended for research and analytical applications. Jolkinolide B, a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud, is known to induce apoptosis in cancer cells .
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- HY-123159
-
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Aurora Kinase
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Cancer
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AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells .
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- HY-123954
-
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Casein Kinase inhibitor A51
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Casein Kinase
CDK
Apoptosis
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Cancer
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BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
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-
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- HY-112885C
-
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Nω-Hydroxy-nor-L-arginine dihydrochloride
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Apoptosis
Arginase
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Metabolic Disease
Inflammation/Immunology
Cancer
|
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nor-NOHA dihydrochloride is a selective and reversible arginase inhibitor. nor-NOHA dihydrochloride induces apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA dihydrochloride has anti-leukemic activity. nor-NOHA dihydrochloride can used in study endothelial dysfunction, immunosuppression and metabolism .
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-
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- HY-W588250
-
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Integrin
|
Inflammation/Immunology
|
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Surfactin C1 is an amphiphilic biosurfactants. Surfactin C1 inhibits leukemic cell (HL-60) adhesion to human umbilical vein endothelial cells (HUVEC). Surfactin C1 inhibits adhesion melecules expression, such as ICAM-1 and VCAM-1 .
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-
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- HY-112885
-
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Nω-Hydroxy-nor-L-arginine
|
Apoptosis
Arginase
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Metabolic Disease
Inflammation/Immunology
Cancer
|
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nor-NOHA is a selective and reversible arginase inhibitor. nor-NOHA induces apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA has anti-leukemic activity. nor-NOHA can used in study of endothelial dysfunction, immunosuppression and metabolism .
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-
-
- HY-168182
-
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Epigenetic Reader Domain
|
Cancer
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Menin-MLL inhibitor 34 (Compound 37) is a selective and potent Menin-MLL inhibitor, with an IC50 of 18.21 nM for Menin. Menin-MLL inhibitor 34 has long-lasting anti-leukemic effects by reducing Menin protein levels and down-regulating MEN1 transcription .
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-
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- HY-N0928
-
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Apoptosis
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Inflammation/Immunology
Cancer
|
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Mimosine, a tyrosine analog , can act as an antioxidant by its potent iron-binding activity . Mimosine is a known chelator of Fe(III) . Mimosine induces apoptosis through metal ion chelation, mitochondrial activation and ROS production in human leukemic cells . Anti-cancer, antiinflammation.
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-
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- HY-134333
-
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Apoptosis
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Cancer
|
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ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc) .
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-
-
- HY-112885B
-
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Nω-Hydroxy-nor-L-arginine monoacetate
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Arginase
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Metabolic Disease
|
|
nor-NOHA monoacetate is a selective and reversible arginase inhibitor. nor-NOHA monoacetate induces apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA monoacetate has anti-leukemic activity. nor-NOHA monoacetate can used in study of endothelial dysfunction, immunosuppression and metabolism .
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-
-
- HY-101991
-
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PERK
Eukaryotic Initiation Factor (eIF)
Apoptosis
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Cancer
|
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ML291 is a UPR (unfolded protein response)-inducing sulfonamidebenzamide. ML291 overwhelms the adaptive capacity of the UPR and induces apoptosis in a variety of solid cancer models. ML291 can activate the PERK/eIF2a/CHOP (apoptotic) arm of the UPR and reduce leukemic cell burden .
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- HY-155556
-
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ClpP
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Cancer
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ZG36 is a human Caseinolytic protease P (ClpP) agonist. ZG36 non-selectively degrades respiratory chain complexes and reduces mitochondrial DNA, ultimately leading to mitochondrial dysfunction and leukemic cell death. ZG36 also inhibits the development of acute myeloid leukemia in a xenograft mouse model .
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- HY-16786
-
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Others
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Inflammation/Immunology
Cancer
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AI-10-49 is an inhibitor of leukemic oncoprotein CBFβ-SMHHC. AI-10-49 inhibits the binding of CBFβ-SMMHCto the RUNX1 Runt domain with IC50 value of 0.26 μM. AI-10-49 can be used for the research of leukemia .
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- HY-P3083
-
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PKC
|
Inflammation/Immunology
|
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N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC50 value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat .
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-
- HY-P99412
-
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OSE-127
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Interleukin Related
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Cancer
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Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research .
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- HY-113221
-
-
- HY-113221R
-
|
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Proteasome
Endogenous Metabolite
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Metabolic Disease
|
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Isovalerylcarnitine (Standard) is the analytical standard of Isovalerylcarnitine. This product is intended for research and analytical applications. Isovalerylcarnitine is a product of the catabolism of L-leucine. Isovalerylcarnitine is also a selective and reversible calpain activator that induces apoptosis .
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- HY-135231
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NL-1
1 Publications Verification
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Mitochondrial Metabolism
Autophagy
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Cancer
|
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NL-1 is a mitoNEET inhibitor with antileukemic effect. NL-1 inhibits REH and REH/Ara-C cells growth with IC50s of 47.35 µM and 56.26 µM, respectively. NL-1-mediated death in leukemic cells requires the activation of the autophagic pathway .
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- HY-141429
-
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Histone Methyltransferase
Apoptosis
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Cancer
|
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AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
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- HY-141429C
-
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Histone Methyltransferase
Apoptosis
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Cancer
|
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AS-99 is a first-in-class, potent, and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
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-
- HY-146230
-
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VEGFR
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Cancer
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VEGFR-2-IN-26 (compound 5h) is a highly potent VEGFR-2 inhibitor with an IC50 value of 15.5 nM. VEGFR-2-IN-26 has good antiproliferative activity against the leukemic, non-small lung, CNS, ovarian, renal, prostate and breast cancer cells .
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- HY-126566
-
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Fungal
HDAC
Apoptosis
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Infection
Cancer
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Trichostatin C is an inhibitor for histone deacetylase (HDAC), induces apoptosis and arrests cell cycle at G2/M phase, and exhibits anticancer activity against lung cancer and urothelial bladder cancer . Trichostatin C induces differentation of Friend leukemic cells . Trichostatin C exhibits antifungal activity .
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- HY-141429A
-
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Histone Methyltransferase
Apoptosis
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Cancer
|
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AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
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- HY-163803
-
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HDAC
DNA Methyltransferase
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Cancer
|
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CM-444 is inhibitor for HDAC (IC50 is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC50 is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models .
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- HY-16209
-
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BCX-1777 hydrochloride; Immucillin-H hydrochloride
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Nucleoside Antimetabolite/Analog
Apoptosis
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Cancer
|
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Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels .
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- HY-16210
-
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BCX-1777; Immucillin-H
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Nucleoside Antimetabolite/Analog
Apoptosis
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Cancer
|
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Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels .
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- HY-10971A
-
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MLN 8237 sodium
|
Aurora Kinase
Autophagy
Apoptosis
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Cancer
|
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Alisertib (MLN 8237) sodium is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib sodium induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
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-
- HY-123955
-
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Casein Kinase
CDK
Apoptosis
|
Cancer
|
|
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
|
-
- HY-10971
-
Alisertib
Maximum Cited Publications
43 Publications Verification
MLN 8237
|
Aurora Kinase
Autophagy
Apoptosis
|
Cancer
|
|
Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity .
|
-
- HY-153775
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
UC-764864 is a UBE2N inhibitor. UC-764864 inhibits UBE2N enzymatic activity. UC-764864 has cytotoxic effects and inhibition of UBE2N-dependent signaling in leukemic cells. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines .
|
-
- HY-124134
-
|
LCL102
|
Ceramidase
Caspase
PARP
|
Cancer
|
|
AD-2646 (LCL102), a ceramide analog, can kill leukemic T cells (EC50: 40 μM). AD-2646 triggers the cleavage of caspase-8, -9 and -3, as well as the caspase substrate PARP. AD-2646 is a ceramidase inhibitor. AD-2646 induces an accumulation of endogenous ceramide owing to perturbed ceramide metabolism .
|
-
- HY-14518
-
|
4-Aminofolic acid; APGA
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
- HY-14518R
-
|
|
Antifolate
|
Inflammation/Immunology
Cancer
|
|
Aminopterin (Standard) is the analytical standard of Aminopterin. This product is intended for research and analytical applications. Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia .
|
-
- HY-14518A
-
|
4-Aminofolic acid sodium; APGA sodium
|
Antifolate
|
Cancer
|
|
Aminopterin sodium (4-Aminofolic acid sodium) is an anti-tumor drug with immunosuppressive activity. Aminopterin sodium blocks the metabolism of folic acid by inhibiting the activity of dihydrofolate reductase, thereby affecting nucleic acid synthesis. Aminopterin sodium is mainly used to inhibit acute lymphoblastic leukemia and certain other types of cancer. Aminopterin sodium is also used clinically as an immunosuppressant to suppress autoimmune diseases .
|
-
- HY-103274
-
|
|
Bcr-Abl
Src
c-Kit
Apoptosis
|
Neurological Disease
Cancer
|
|
PD180970 is a highly potent and ATP-competitive p210 Bcr-Abl kinase inhibitor, with an IC50 of 5 nM for inhibiting the autophosphorylation of p210 Bcr-Abl. PD180970 also inhibits Src and KIT kinase with IC50s of 0.8 nM and 50 nM, respectively. PD180970 indcues apoptosis of K562 leukemic cells, and can be used for chronic myelogenous leukemia research .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-139108
-
|
|
Histone Acetyltransferase
Apoptosis
|
Cancer
|
|
DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P99971
-
|
|
ADC Antibody
|
Cancer
|
|
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen, which present on leukemic myeloblasts of acute myeloid leukemia (AML). Gemtuzumab can be used for synthesis of antibody-drug conjugate (ADC), Gemtuzumab ozogamicin (HY-109539). Gemtuzumab ozogamicin consists of a cytotoxic derivative of Calicheamicin (a cytotoxic antibiotic), and a monoclonal antibody. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia .
|
-
- HY-N1255
-
|
(-)-Scoulerine; Discretamine
|
Microtubule/Tubulin
Beta-secretase
Apoptosis
|
Cancer
|
|
Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (?-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
|
-
- HY-115768
-
|
Poly-p-methoxyphenethylmethylamine
|
Others
|
Neurological Disease
Cancer
|
|
Compound 48/80 (Poly-p-methoxyphenethylmethylamine) is widely used in animal and tissue models as a "selective" mast cell activator. Compound 48/80 acts at the mast cell membrane to stimulate trimeric G-proteins and induces degranulation via phospholipase C and D pathways .
|
-
- HY-N0097A
-
|
AraG
|
Others
|
Cancer
|
|
9-β-D-Arabinofuranosylguanine is a Guanosine (HY-N0097) analog and shows high affinity for deoxyguanosine kinase (dGK) with a Km of 8.0 μM. 9-β-D-Arabinofuranosylguanine can be used for the research of T-cell lymphoblastic disease .
|
-
- HY-159588
-
|
|
Bcl-2 Family
|
Cancer
|
|
Mcl-1 inhibitor 20 (compound 47) is a Mcl-1 inhibitor with anti-leukemic effects. Mcl-1 inhibitor 20 can bind to the BH3 binding groove of Mcl-1 (Ki=24 nM), occupy the P1 pocket in Mcl-1, and form interactions with Lys234 and Val249. Mcl-1 inhibitor 20 has good microsomal stability, pharmacokinetic characteristics and low cardiotoxicity .
|
-
- HY-19619
-
|
|
Phospholipase
Apoptosis
|
Cancer
|
|
m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis .
|
-
- HY-158019
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 196 (compound 1) shows cell cytotoxicity with IC50 values of 7.69 µM and 54.2 µM for HL-60 cells and A549 cells, respectively. Anticancer agent 196 can induce DNA damage .
|
-
- HY-158020
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Anticancer agent 197 (compound 2b) shows cell cytotoxicity with IC50 values of 10.03 µM and 73.54 µM for HL-60 cells and A549 cells, respectively. Anticancer agent 197 can induce DNA damage .
|
-
- HY-101287
-
|
|
Microtubule/Tubulin
JNK
Apoptosis
Caspase
|
Cancer
|
|
MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line .
|
-
- HY-100490S
-
|
|
Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
|
-
- HY-122214
-
AC-73
4 Publications Verification
|
Autophagy
|
Cancer
|
|
AC-73 is a first specific, orally active inhibitor of cluster of differentiation 147 (CD147), which specifically disrupts CD147 dimerization, thereby mainly suppressing the CD147/ERK1/2/STAT3/MMP-2 pathways. AC-73 inhibits the motility and invasion of hepatocellular carcinoma cells . AC-73 is also an anti-proliferative agent and an inducer of autophagy in leukemic cells .
|
-
- HY-106777
-
|
CPEC; NSC 375575
|
Apoptosis
Necroptosis
|
Cancer
|
|
Cyclopentenylcytosine (CPC) is a nucleoside analog that reduces the levels of cytidine triphosphate (CTP) and deoxycytidine triphosphate (dCTP) in leukemic cells by inhibiting CTP synthetase. Cyclopentenylcytosine also promotes the phosphorylation of 1-β-D-arabinorubosylmannosylcytidine (araC) and its DNA intercalation activity. Cyclopentenylcytosine induces apoptosis and necrosis in the human T lymphocyte line MOLT-3 in a concentration (50-300 nM) and time (8-16 h) dependent manner. Co-treatment of cyclopentenylcytosine with araC enhances the effects of induction of apoptosis and necrosis, as well as its cytotoxicity in T lymphoblasts .
|
-
- 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-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-157327
-
|
|
Bcr-Abl
|
Cancer
|
|
AKE-72 (compound 5) is a potent inhibitor of Pan-BCR-ABL. AKE-72 inhibits BCR-ABL WT, BCR-ABL T315, BCR-ABL E255K, BCR-ABL F3171, BCR-ABL H396P and BCR-ABL Q252H with IC50s of < 0.5, 9, 8.98, 3.12, < 1.0 and 3.88 nM, respectively. AKE-72 has anti-leukemic activity against K-562 cell line .
|
-
- 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-112654A
-
|
|
Others
|
Cancer
|
|
GCN2iB acetate is a GCN2 inhibitor that enhances Gcn2 activity and Atf4 expression. GCN2iB can activate Gcn2 mutants lacking functional regulatory regions or certain kinase domain substitution mutants. GCN2iB increases eIF2 phosphorylation by Gcn2 at low concentrations, thereby enhancing the cellular response to nutritional stress. GCN2iB may have potential benefits for the inhibition of cancer cells expressing low basal levels of aspartate synthetase, enhancing their sensitivity to the anti-leukemic compound L-aspartase .
|
-
- HY-118084
-
|
Tyrene CR-4
|
JAK
Bcr-Abl
FLT3
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
LS-104 (Tyrene CR-4) is a non-ATP-competitive kinase inhibitor against JAK2, Bcr-Abl and FLT3. LS-104 potently induces apoptosis in JAK2V617F-positive cells and inhibits JAK2 autophosphorylation and downstream signal transduction. LS-104 also inhibits proliferation and induces potent cytotoxic effects in FLT3 expressing leukemic cells. LS-104 is a hydroxystyryl-acrylonitrile compound, which is promising for research of myeloproliferative disorders and refractory/relapsed hematologic malignancies .
|
-
- HY-102078
-
|
|
Ras
Apoptosis
|
Cancer
|
|
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects .
|
-
- 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-151411
-
|
|
Others
|
Cancer
|
|
RUNX1/ETO tetramerization-IN-1 is a small-molecule inhibitor of RUNX1/ETO tetramerization, exhibits anti-leukemic effect. RUNX1/ETO tetramerization-IN-1 specifically targets to NHR2 of RUNX1/ETO (EC50=0.25 μM), restores gene expression down-regulated by RUNX1/ETO. RUNX1/ETO tetramerization-IN-1 inhibits the proliferation of RUNX1/ETO-depending SKNO-1 cells, and reduces the RUNX1/ETO-related tumor growth in a mouse model .
|
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W588250
-
|
|
Integrin
|
Inflammation/Immunology
|
|
Surfactin C1 is an amphiphilic biosurfactants. Surfactin C1 inhibits leukemic cell (HL-60) adhesion to human umbilical vein endothelial cells (HUVEC). Surfactin C1 inhibits adhesion melecules expression, such as ICAM-1 and VCAM-1 .
|
-
- HY-P3245A
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 hydrochloride is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 hydrochloride antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 hydrochloride selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
-
- HY-P3083
-
|
|
PKC
|
Inflammation/Immunology
|
|
N-Myristoyl-Lys-Arg-Thr-Leu-Arg is a protein kinase C (PKC) inhibitor with an IC50 value of 75 μM. N-Myristoyl-Lys-Arg-Thr-Leu-Arg inhibits IL-2 receptor induction and IL-2 production in the human leukemic cell line Jurkat .
|
-
- HY-P3245
-
|
|
Apoptosis
|
Cancer
|
|
HXR9 is a cell-permeable peptide and a competitive antagonist of HOX/PBX interaction. HXR9 antagonizes the interaction between HOX and a second transcrip-tion factor (PBX), which binds to HOX proteins in paralogue groups1 to 8. HXR9 selectively decreases cell proliferation and promotes apoptosis in cells with a high level of expression of the HOXA/PBX3 genes, such as MLL-rearranged leukemic cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Interleukin Related
|
Cancer
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
- HY-P99412
-
|
OSE-127
|
Interleukin Related
|
Cancer
|
|
Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research .
|
-
- HY-P99971
-
|
|
ADC Antibody
|
Cancer
|
|
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen, which present on leukemic myeloblasts of acute myeloid leukemia (AML). Gemtuzumab can be used for synthesis of antibody-drug conjugate (ADC), Gemtuzumab ozogamicin (HY-109539). Gemtuzumab ozogamicin consists of a cytotoxic derivative of Calicheamicin (a cytotoxic antibiotic), and a monoclonal antibody. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N9359
-
-
-
- HY-135190
-
-
-
- HY-N3514
-
-
-
- HY-P99395
-
|
JNJ 56022473; CSL 362
|
Classification of Application Fields
Disease Research Fields
Cancer
|
Interleukin Related
|
|
Talacotuzumab (JNJ 56022473; CSL 362) is an IgG1-type fully humanized, CD123-neutralizing monoclonal antibody containing a modified Fc structure. Talacotuzumab has KDs of 0.43 nM, 188 nM, 46 nM, 16.8 nM for CD123, CD32b/c, CD16-158F, CD16-158V, respectively. Talacotuzumab inhibits IL-3 binding to CD123, antagonizing IL-3 signaling in target cells. Talacotuzumab has mutated the Fc region to increase affinity for CD16 (FcγRIIIa), thereby enhancing antibody-dependent cell-mediated cytotoxicity (ADCC). Talacotuzumab is highly effective in vivo reducing leukemic cell growth in acute myeloid leukemia (AML) xenograft mouse models .
|
-
-
- HY-N0732
-
-
-
- HY-117220
-
-
-
- HY-N3401
-
-
-
- HY-N10071
-
-
-
- HY-N8402
-
-
-
- HY-N10789
-
-
-
- HY-N0732R
-
-
-
- HY-N0928
-
-
-
- HY-113221
-
-
-
- HY-113221R
-
-
-
- HY-126566
-
-
-
- HY-P99971
-
|
|
Classification of Application Fields
Disease Research Fields
Cancer
|
ADC Antibody
|
|
Gemtuzumab is a monoclonal IgG4-κ antibody targeting CD33 antigen, which present on leukemic myeloblasts of acute myeloid leukemia (AML). Gemtuzumab can be used for synthesis of antibody-drug conjugate (ADC), Gemtuzumab ozogamicin (HY-109539). Gemtuzumab ozogamicin consists of a cytotoxic derivative of Calicheamicin (a cytotoxic antibiotic), and a monoclonal antibody. Gemtuzumab ozogamicin can be used for the research of acute myeloid leukemia .
|
-
-
- HY-N1255
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-100490S
-
|
|
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells[1][2][3].
|
-
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