Search Result
Results for "
K-562 leukemia cells
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-125771
-
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18:0 Lyso-PC; LPC(18:0)
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Endogenous Metabolite
HDAC
STAT
Apoptosis
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Cancer
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1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
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-
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- HY-N3584
-
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Chonglou Saponin VII
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Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
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Cancer
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Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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- HY-G0017
-
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Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588
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Drug Metabolite
P-glycoprotein
Apoptosis
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Neurological Disease
Cancer
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N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-147831
-
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Eukaryotic Initiation Factor (eIF)
Epigenetic Reader Domain
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Cancer
|
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HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia) .
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- HY-149470
-
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Histone Acetyltransferase
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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-103274
-
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Bcr-Abl
Src
c-Kit
Apoptosis
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Neurological Disease
Cancer
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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 .
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- HY-114570
-
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NSC 286193; Riboxamide
|
Nucleoside Antimetabolite/Analog
Orthopoxvirus
|
Infection
Neurological Disease
Cancer
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Tiazofurin (NSC 286193) is a synthetic nucleoside analogue with antineoplastic activity. Tiazofurin is anabolized intracellularly to tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH). Tiazofurin enhances the autosecretion of IL-6 in K562 cells. Tiazofurin also has anti-orthopoxvirus and anti-variola activities. Tiazofurin can be used for the study of leukemia and lung cancer .
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- HY-125834
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PROTACs
Bcr-Abl
Apoptosis
STAT
JAK
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Cancer
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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)) .
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- HY-116392D
-
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Glucosylceramide Synthase (GCS)
Apoptosis
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Cancer
|
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PDMP hydrochloride is a glucosylceramide synthase (GCS) inhibitor. PDMP hydrochloride induces apoptosis in K562/A02 cells. PDMP hydrochloride can be used in cancer (such as leukemia) research .
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- HY-N10678
-
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Others
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Cancer
|
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R-30-Hydroxygambogic acid is polyprenylated xanthone epimer that can be isolated from gamboges of Garcinia hanburyi. R-30-Hydroxygambogic acid shows cytotoxicities to Human Leukemia K562 cell lines of IC50 values of 2.89 and 1.27 μM for K562/R and K562/S, respectively. R-30-Hydroxygambogic acid can be used for the research of cancer .
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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
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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-17563R
-
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Deoxyguanosine (Standard); Guanine deoxyriboside (Standard)
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Reference Standards
Endogenous Metabolite
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Cancer
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2'-Deoxyguanosine (Standard) is the analytical standard of 2'-Deoxyguanosine. This product is intended for research and analytical applications. 2’-Deoxyguanosine (Deoxyguanosine) is a purine nucleoside with a variety of biological activities. 2’-Deoxyguanosine can induce DNA division in mouse thymus cells. 2’-Deoxyguanosine is a potent cell division inhibitor in plant cells .
In Vitro: 2'-Deoxyguanosine inhibits the clonal growth of HL-60 and K562 leukemia cells with IC50 values of 50 and 80 μM, respectively .
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- HY-G0017S
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Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8
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Isotope-Labeled Compounds
Drug Metabolite
P-glycoprotein
Apoptosis
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Neurological Disease
Cancer
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N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-163854
-
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HSP
Bcl-2 Family
Apoptosis
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Cancer
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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) .
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- HY-W231513
-
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MASTL
Ser/Thr Protease
Aurora Kinase
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Cancer
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MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis .
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- HY-125771S
-
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18:0 Lyso-PC-d35; LPC(18:0)-d35
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Isotope-Labeled Compounds
Endogenous Metabolite
HDAC
STAT
Apoptosis
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Cancer
|
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1-Stearoyl-sn-glycero-3-phosphocholine-d35 is deuterium labeled 1-Stearoyl-sn-glycero-3-phosphocholine (HY-125771). 1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
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- HY-169021
-
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JNK
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Cancer
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JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .
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- HY-129592
-
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Apoptosis
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Cancer
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p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
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- HY-162658
-
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HDAC
Apoptosis
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Cancer
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Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models .
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- HY-122359A
-
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rel-L-Centchroman; Ormeloxifene
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Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species (ROS)
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Cancer
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rel-Levormeloxifene (rel-L-Centchroman) is the relative configuration of Levormeloxifene (HY-122359). rel-Levormeloxifene is a selective estrogen receptor modulator (SERM). rel-Levormeloxifene inhibits proliferation of leukemia cells with IC50 about 7 μM, arrests cell cycle at G0/G1 phase, and induces apoptosis. rel-Levormeloxifene induces differentation of myelogenesis leukemia, and enhances ROS production in K562 cells .
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- HY-179247
-
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Bcr-Abl
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Cancer
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BCR-ABL1-IN-2 (compound 8) is a potent BCR-ABL1 tyrosine kinase inhibitor. BCR-ABL1-IN-2 exhibits activity in Imatinib (HY-15463) resistant K562/DOX cells with LC50 of 5.29 μM. BCR-ABL1-IN-2 shows no significant toxicity in nontumor cells. BCR-ABL1-IN-2 can be used for chronic myeloid leukemia research .
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- HY-116971
-
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Histone Methyltransferase
Apoptosis
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Cancer
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DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562 .
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- HY-177768
-
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HDAC
Apoptosis
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Cancer
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HDAC-IN-96 (Compound 3f) is a selective HDAC1/2 inhibitor with IC50 values of 457.1 and 433.7 nM. HDAC-IN-96 has strong inhibitory activity against multiple hematological tumor cells (RS4;11, K562, RPMI-8226, U266), with IC50 values ranging from 2.11 to 5.35 μM. HDAC-IN-96 can induce cancer cells apoptosis and S phase arrest. HDAC-IN-96 can be used for the research of cancer, such as acute lymphoblastic leukemia .
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- HY-N15582
-
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Apoptosis
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Inflammation/Immunology
Cancer
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Perezone is a sesquiterpenoid benzoquinone found in the roots of Acourtia species. Perezone inhibits the activity of leukemia cell line K-562 and human glioma cell line U-251 (IC50: 6.83 μM). Perezone increases the expression of caspase 3, 8, and 9 genes associated with apoptosis. Perezone has antioxidant and anti-inflammatory activities .
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- HY-N10677
-
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Others
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Cancer
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S-30-Hydroxygambogic acid is polyprenylated xanthone epimer that can be isolated from gamboges of Garcinia hanburyi. S-30-Hydroxygambogic acid shows cytotoxicities to Human Leukemia K562 cell lines of IC50 values of 4.49 and 3.61 μM for K562/R and K562/S, respectively. S-30-Hydroxygambogic acid can be used for the research of cancer .
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- HY-170323
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Apoptosis
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Cancer
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4-TM.P binds to the minor groove of DNA, inhibits proliferation of cancer cell K562 with an IC50 of 25 µM, arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell K562. 4-TM.P can be used in anti-leukemia research .
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- HY-149805
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Apoptosis
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Cancer
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Anticancer agent 110 is an anticancer agent with in vitro anticancer activity and excellent anti-leukemia potency. Anticancer agent 110 is highly cytotoxic to K-562 lineage chronic myelogenous leukemia cells at nanomolar concentrations. Anticancer agent 110 causes DNA damage and leads to apoptosis .
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- HY-157483
-
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P-glycoprotein
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Cancer
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P-gp inhibitor 18 (compound 6G) is a potent inhibitor of P-gp. P-gp inhibitor 18 inhibits rhodamine 123 efflux in the P-gp overexpressed leukemia cells, K562/Dox .
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- HY-157484
-
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P-glycoprotein
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Cancer
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P-gp inhibitor 19 (Compound 6i) is a P-gp inhibitor. P-gp inhibitor 19 can inhibit the efflux of rhodamine 123 (HY-D0816) in P-gp-overexpressing leukemia cells K562/Dox and also restore the sensitivity of DOX-resistant cells .
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- HY-158968
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MDM-2/p53
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Cancer
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MMs02943764 is a 1,2,4-triazole derivative with anticancer activity. MMs02943764 has significant antiproliferative effects on multiple cancer cell lines. PAC, a structural analog of MMs02943764, has significant cytotoxicity against the leukemia cell line K562 (IC50=35.264 μM), reduces the degradation of p53 by inhibiting Mdm2 and Pirh2, and induces K562 cell cycle arrest .
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- HY-N1056
-
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Zerumbetol
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Others
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Cancer
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Yunnancoronarin A (Zerumbetol) can be isolated from Hedychium forrestii. Yunnancoronarin A is cytotoxic, with IC50 values of 11.08 and 2.19 μM against lung adenocarcinoma cells A549 and leukemia cells K562, respectively .
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- HY-126556
-
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Microtubule/Tubulin
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Cancer
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Cytochalasin J is a cytochalasin detivative. Cytochalasin J affects mitotic spindel microtubule organization and kinetochore structure, and exhibits cytotoxicity in human leukemia K562 cell with IC50 of 1.5 μM .
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- HY-169608
-
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Bcr-Abl
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Cancer
|
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BCR-ABL-IN-11 (Compound 2) is a BCR-ABL inhibitor. BCR-ABL-IN-11 shows anticancer activity against chronic myelogenous leukemia (CML) (IC50 of 129.61 μM for K562 cells) .
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- HY-10212A
-
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CNF2024 mesylate
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HSP
β-catenin
c-Myc
Autophagy
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Cancer
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BIIB021 (CNF2024) mesylate is the mesylate of BIIB021 (HY-10212). BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML .
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- HY-155522
-
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Carbonic Anhydrase
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Cancer
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WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
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- HY-N3584R
-
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Chonglou Saponin VII (Standard)
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Reference Standards
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
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Cancer
|
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Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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- HY-16958R
-
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Antibiotic
Dimethylargininase (DDAH)
Reference Standards
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Inflammation/Immunology
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Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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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-108969R
-
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NSC 366140 (Standard); PD 115934 (Standard)
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Topoisomerase
Apoptosis
Reference Standards
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Cancer
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Pyrazoloacridine (Standard) is the analytical standard of Pyrazoloacridine. This product is intended for research and analytical applications. 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-117285
-
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Lactoquinomycin A; LQM-A
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Antibiotic
Bacterial
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Infection
Cancer
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Lactoquinomycin A is a quinone antibiotic. Lactoquinomycin A has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin A inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.02, 0.006, 0.008, 0.033, 0.013 and 0.03, respectively .
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- HY-N14774
-
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Antibiotic
Bacterial
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Infection
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Lactoquinomycin B is a quinone antibiotic. Lactoquinomycin B has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin B inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.43, 0.21, 0.19, 0.16, 0.2 and 0.12, respectively .
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- HY-170604
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MMP
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Cardiovascular Disease
Cancer
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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) .
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- HY-125322
-
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Bacterial
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Infection
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Reveromycin C is a polyketide originally isolated from Streptomyces that has antifungal activity against C. albicans (MICs=2.0 and >500 μg/mL at pH 3 and 7.4, respectively). Reveromycin C inhibits EGF-induced mitogenic activity in the Balb/MK mouse epidermal cell line. It also reverses the morphology of sarcoma-virus-transformed NRK rat kidney cells (EC50=1.58 μg/mL) and inhibits proliferation of KB cells and K562 human chronic myelogenous leukemia cells (IC50=2.0 μg/mL for both).
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- HY-128634
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Apoptosis
PI3K
MEK
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Cancer
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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 .
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- HY-G0017A
-
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Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate
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Drug Metabolite
P-glycoprotein
Apoptosis
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Neurological Disease
Cancer
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N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-G0017S1
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Norimatinib-d4; Imatinib metabolite N-Desmethyl imatinib-d4; CGP 74588-d4
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Isotope-Labeled Compounds
Drug Metabolite
P-glycoprotein
Apoptosis
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Neurological Disease
Cancer
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N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-G0017R
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Norimatinib (Standard); Imatinib metabolite N-Desmethyl imatinib (Standard); CGP 74588 (Standard)
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Reference Standards
Drug Metabolite
P-glycoprotein
Apoptosis
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Others
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N‑Desmethyl imatinib (Standard) is the analytical standard of N‑Desmethyl imatinib (Norimatinib) (HY-G0017R). This product is intended for research and analytical applications. N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-180968
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PROTACs
Bcr-Abl
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Cancer
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GMB-805 is a BCR-Abl PROTAC degrader with a DC50 of 30 nM in K562 cells. GMB-805 exerts antiproliferative activity in K562 cells. GMB-805 exhibits potent anti-tumor activity with favorable safety profile in vivo. GMB-805 can be used for chronic myeloid leukemia research .
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- HY-180963
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PROTACs
Bcr-Abl
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Cancer
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Lys-PEG1-Dasa is a BCR-ABL PROTAC degrader with an DC50 of 0.98 nM in K562 cells. Lys-PEG1-Dasa exerts growth inhibitory with IC50 of 0.4569 nM in K562 cells. Lys-PEG1-Dasa can be used for chronic myeloid leukemia research .
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- HY-180969
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PROTACs
Bcr-Abl
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Cancer
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SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research .
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- HY-N16684
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P-glycoprotein
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Cancer
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Clausarin is a selective inhibitor of P-glycoprotein (P-gp), inhibiting P-gp-mediated drug efflux. Clausarin significantly inhibits Daunorubicin (HY-13062A) efflux in K562/R7 human leukemia cells overexpressing P-gp (with Cyclosporin A (HY-B0579) as a positive control). Clausarin can be naturally extracted from the roots of Citrus sinensis (sweet orange) and can be used in research related to overcoming multidrug resistance (MDR) in tumors .
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- HY-186016
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PROTACs
Bcr-Abl
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Cancer
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Arg-PEG1-Dasa is a mini-PROTAC targeting BCR-ABL. Arg-PEG1-Dasa induces BCR-ABL degradation (EC50 = 0.85 nM) and shows antiproliferative activity in K562 cells (IC50 = 0.36 nM). Arg-PEG1-Dasa can be used for chronic myeloid leukemia research .
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- HY-180766
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JAK
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Cancer
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JAK2-IN-19 (Compound 3p) is a JAK2 inhibitor with a KD value of 1.11 μM. JAK2-IN-19 inhibits the proliferation of K562 cells and HeLa cells. JAK2-IN-19 significantly reduces the level of p-JAK2. JAK2-IN-19 can be used for research on cervical cancer and leukemia .
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- HY-115797
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MDM-2/p53
Caspase
c-Myc
Apoptosis
NF-κB
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Cancer
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LQFM030 is a novel small molecule MDM2 inhibitor. LQFM030 exhibits concentration dependent cytotoxicity in K562 cells (IC50 = 0.28 mM). LQFM030 induces cell apoptosis through G0/G1 phase cell cycle arrest and increased Caspase activity. LQFM030 downregulates the mRNA expression of MDM2, MDMX, p73, MYC, and NF-κB. LQFM030 is commonly used in research on cancers such as leukemia .
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- HY-180979
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PROTACs
Bcr-Abl
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Cancer
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P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia .
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- HY-N15121
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Drug Derivative
Apoptosis
c-Myc
AMPK
mTOR
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Cancer
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4-O-Methyl-ascochlorin (Compound MAC) is a derivative of Ascochlorin (HY-101021). 4-O-Methyl-ascochlorin can selectively induce apoptosis of K562 leukemia cells, cause G1 phase arrest and downregulate c-Myc expression. 4-O-Methyl-ascochlorin can promote the phosphorylation of AMPK and inhibit the phosphorylation of mTOR and its target proteins, including p70S6 K and 4E-BP-1. 4-O-Methyl-ascochlorin can be used for research of leukemia .
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- HY-402815
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Drug Intermediate
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Cancer
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(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 .
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- HY-180925
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PROTACs
Bcr-Abl
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Cancer
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Leu-PEG1-Dasa is a potent BCR-ABL PROTAC degrader with a DC50 of 0.48 nM. Leu-PEG1-Dasa uses a single amino acid as the E3 ligand and belongs to a mini-PROTAC, functioning through the N-terminal canonical pathway. Leu-PEG1-Dasa exhibits potent anti-proliferative activity against K562 cells. Leu-PEG1-Dasa can be used for the study of chronic myeloid leukemia (CML) .
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- HY-180983
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PROTACs
Bcr-Abl
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Cancer
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Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that can efficiently degrade the BCR-ABL fusion protein and ABL protein. Azo-PROTAC-4C-trans exhibits potent selective anti-proliferative activity against K562 cells. Azo-PROTAC-4C-trans allows real-time, reversible regulation of its activity via UV (to inactivate it) /visible light (to activate it) irradiation. Azo-PROTAC-4C-trans can be used for the study of myeloid leukemia .
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- HY-180962
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PROTACs
Bcr-Abl
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Cancer
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Phe-PEG1-Dasa is a BCR-ABL PROTAC degrader, with its DC50 being 1.56 nM. Phe-PEG1-Dasa uses a single amino acid (Phe) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, thus being called a mini-PROTAC. Phe-PEG1-Dasa significantly inhibits the proliferation of K562 cells. Phe-PEG1-Dasa can be used for the study of leukemia .
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- HY-N17753
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NSC-698789
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Others
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Cancer
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Protoneodioscin is a furostanol saponin found in the rhizomes of Dioscorea collettii var. hypoglauca. It exhibits selective activity against various cancer cell lines, including leukemia, but shows no activity against colon and renal cancer cells. Protoneodioscin can be used in research on cancers such as leukemia .
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| Cat. No. |
Product Name |
Type |
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- HY-125771
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18:0 Lyso-PC; LPC(18:0)
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Biochemical Assay Reagents
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1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-125771
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- HY-N3584
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- HY-N10678
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- HY-17563R
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- HY-N15582
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- HY-N10677
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- HY-N1056
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- HY-126556
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- HY-N3584R
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Chonglou Saponin VII (Standard)
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Structural Classification
Liliaceae
Trillium tschonoskii Maxim.
Plants
Steroids
Source Classification
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Reference Standards
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
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Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
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- HY-117285
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Lactoquinomycin A; LQM-A
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Microorganisms
Antibiotics
Other Antibiotics
Source Classification
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Antibiotic
Bacterial
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Lactoquinomycin A is a quinone antibiotic. Lactoquinomycin A has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin A inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.02, 0.006, 0.008, 0.033, 0.013 and 0.03, respectively .
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- HY-N14774
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Microorganisms
Antibiotics
Other Antibiotics
Source Classification
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Antibiotic
Bacterial
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Lactoquinomycin B is a quinone antibiotic. Lactoquinomycin B has the activity of anti-Gram-positive bacteria and some Gram-negative bacteria, but the effect of anti-Gram-negative bacteria is weak and has no effect on fungi. Lactoquinomycin B inhibits a variety of cell lines including lymphoma L5178Y progenitor, Adriamycin resistant, Bleomycin-resistant, human leukemia K562, mouse leukemia L-1210 and mouse leukemia P 388 with ID50 (μg/mL) of 0.43, 0.21, 0.19, 0.16, 0.2 and 0.12, respectively .
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- HY-N16684
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- HY-N15121
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- HY-N17753
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-G0017S
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N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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- HY-125771S
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1-Stearoyl-sn-glycero-3-phosphocholine-d35 is deuterium labeled 1-Stearoyl-sn-glycero-3-phosphocholine (HY-125771). 1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
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- HY-G0017S1
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N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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| Cat. No. |
Product Name |
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Classification |
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- HY-125771
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18:0 Lyso-PC; LPC(18:0)
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Phospholipids
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1-Stearoyl-sn-glycero-3-phosphocholine is a lysophosphatidylcholine that inhibits HDAC3 activity and phosphorylation of STAT3 in K562 cells. 1-Stearoyl-sn-glycero-3-phosphocholine induces apoptosis and exhibits anticancer activity in chronic myelogenous leukemia (CML) K562 cells .
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