Search Result
Results for "
K-562
" in MedChemExpress (MCE) Product Catalog:
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-116392D
-
|
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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-
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- HY-149805
-
|
Apoptosis
|
Cancer
|
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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-
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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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-
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- HY-N10678
-
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Others
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Cancer
|
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-155522
-
|
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-125136
-
(-)-Chaetominine
|
PI3K
Akt
Keap1-Nrf2
|
Cancer
|
Chaetominine is an alkaloidal metabolite. Chaetominine has cytotoxicity against human leukemia K562 and colon cancer SW1116 cell lines. Chaetominine reduces MRP1-mediated agent resistance via inhibiting PI3K/Akt/Nrf2 signaling pathway in K562/Adr human leukemia cells .
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-
-
- HY-154978
-
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Others
|
Cancer
|
Cisplatin-resistant cells-IN-1 (Compound 8) has high cytotoxicity against Cisplatin (HY-17394)-resistant cells. Cisplatin-resistant cells-IN-1 reduces the metabolic activity effectively in the low nanomolar range (IC50: 0.14–1.79 μM in A549/A549-R, K562/K562-R, and MCF-7/MCF-7TamR cells) .
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-
-
- HY-157483
-
|
P-glycoprotein
|
Cancer
|
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-155390
-
|
Caspase
Apoptosis
|
Cancer
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Caspase-3 activator 3 (compound 2h) induces apoptosis in HL-60 and K562 cells via significant caspase 3 activation. Caspase-3 activator 3 shows antileukemic acticity against HL-60 and K562 cells, with IC50 values of 42.89 and 33.61 μM, respectively .
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-
-
- HY-N2871
-
|
Apoptosis
|
Cancer
|
Angophorol is a flavonone compound. Angophorol exerts potential anticancer activity through growth inhibition and apoptosis in K562 cells .
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-
-
- HY-N3584
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Chonglou Saponin VII
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Cancer
|
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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-
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- HY-N0083
-
-
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- HY-125058
-
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Apoptosis
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Cancer
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Kinamycin C is a bacterial metabolite containing a diazo group with anticancer activities. Kinamycin C induces a rapid apoptotic response in K562 cells .
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-
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- HY-W700620
-
-
-
- HY-N10073
-
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Others
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Cancer
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Eupahualin C is a sesquiterpene lactone that can be isolated from Eupatorium hualienense. Eupahualin C shows cytotoxicity to K562 and U2OS cancer cells .
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-
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- HY-157484
-
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P-glycoprotein
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Cancer
|
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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-
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- HY-B0790
-
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Apoptosis
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Cancer
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TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells .
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-
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- HY-N8739
-
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Endogenous Metabolite
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Cancer
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2-Hydroxyxanthone (Compound 3) is an isoprene flavone derived from Calophyllum inophyllum. 2-Hydroxyxanthone has an obvious killing effect on K562 cells .
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-
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- HY-W027968
-
2-Oxochromene-3-carboxylic acid
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Others
|
Cancer
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Coumarin-3-carboxylic acid (2- Oxochromene-3-carboxylic acid) is an important initial compound for the synthesis of coumarins which are well known natural products for their diverse biological activities. Lanthanide complexes of Coumarin-3-carboxylic acid exhibit antiproliferative activity towards K-562 cell line .
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-
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- HY-141881
-
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PROTACs
Apoptosis
SF3B1
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Cancer
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PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells .
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- HY-N12153
-
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Others
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Cancer
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Theasaponin E2 shows cytotoxicity against K562 and HL60 cells (IC50: 14.7 μg/mL). Theasaponin E2 can be isolated from Camellia sinensis .
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- HY-11063
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Fingolimod
Maximum Cited Publications
33 Publications Verification
FTY720 free base
|
LPL Receptor
PAK
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Inflammation/Immunology
Cancer
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Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
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-
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- HY-N9339
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(+)-Norglaucine
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Others
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Cancer
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Norglaucine ((+)-Norglaucine), a cytotoxic alkaloid, exhibits cytotoxicity towards the tumor cell lines B16-F10, HepG2, K562 and HL-60 cells .
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-
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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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-
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- HY-158025
-
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DNA/RNA Synthesis
|
Cancer
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Anticancer agent 198 (compound 18b) is a potent anticancer agent and potential WRN protein inhibitor. Anticancer agent 198 was significantly toxic to K562 cells and WRN-overexpressing PC3 cells .
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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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-
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- HY-144232
-
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Others
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Cancer
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Anticancer agent 28 showed good antitumor activity in H22 allogeneic mice in vivo. Its potency in K562 cells was 50 times that of oridonin, and its < b > IC < sub > 50 < / sub > < / b > value was 0.09 μ M。
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-
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- HY-N4029
-
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Others
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Cancer
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Humulene oxide II is an essential oil component from Zingiber striolatum Diels flowers, leaves and stems. Humulene oxide II has cytotoxicity against A549, PC-3 and K562 cell lines .
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-
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- HY-12757
-
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BCRP
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Cancer
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YHO-13177 is a potent and specific inhibitor of BCRP; potentiated the cytotoxicity of SN-38 in cancer cells and no effect on P-glycoprotein–mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells.
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-
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- HY-148284
-
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Others
|
Cancer
|
Berbamine acetate (Compound 3a) is the derivative of Berbamine (HY-N0714). Berbamine acetate exhibits antitumor activity, inhibits growth of Imatinib (HY-15463)-resistant K562 leukemia cells, with IC50 of 6.6 μM .
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-
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- HY-80012
-
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Deubiquitinase
|
Cancer
|
SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
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-
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- HY-108969
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NSC 366140; PD 115934
|
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-N8105
-
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Fungal
|
Infection
Cancer
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Protoneogracillin, a furostanol glycoside, shows anti-fungal activity against the plant pathogenic fungus P.oryzae (MMDC=94.0 μM) and cytotoxic activity on K562 cancer cells (IC50=6.6 μM) .
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- HY-N10188
-
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Others
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Cancer
|
Nidurufin is a potent cell cycle inhibitor with antitumor activity.Nidurufin induces in vitro cell cycle arrest at G2/M transition in the K562 cell line in a concentration and time dependent manner(IC50=12.6 μM) .
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-
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- HY-110104
-
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Others
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Others
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8MDP is a potent equilibrative nucleoside transporter 1 (ENT1) inhibitor with an IC50 of 0.43 nM. 8MDP inhibits hENT1 and hENT2 uptake of [H 3] uridine by K562 cells and K15NTD cells .
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-
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- HY-11063S1
-
FTY720-d4
|
LPL Receptor
PAK
|
Inflammation/Immunology
Cancer
|
Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant[1].
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-
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- HY-11063S
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FTY720 free based-d4
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LPL Receptor
PAK
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Inflammation/Immunology
Cancer
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Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].
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-
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- HY-136121
-
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Microtubule/Tubulin
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Cancer
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM .
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- HY-136123
-
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Microtubule/Tubulin
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Cancer
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM .
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- HY-136122
-
|
Microtubule/Tubulin
|
Cancer
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Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM .
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-
-
- HY-129592
-
|
Apoptosis
|
Cancer
|
p-Tolylmaleimide (compound 9) is a naphthalimide derivative that has cytotoxic effects on cancer cells. p-Tolylmaleimide can arrest the cell cycle of human acute myeloid leukemia cells K562 in the sub-G0/G1 phase and induce apoptosis .
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-
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- HY-155359
-
|
Microtubule/Tubulin
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Cancer
|
Tubulin polymerization-IN-55 is a potent inhibitor of Tubulin Polymerization. Tubulin polymerization-IN-55 has antiproliferative activity against A549, K562, HepG2, MDA-MB-231 and HFL-1 with IC50 s of 8, 3, 9, 24 and 62 nM, respectively .
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-
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- HY-N3862
-
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Others
|
Cancer
|
Erythrodiol 3-O-palmitate is a natural product isolated from Dicranostigma leptopodum (Maxim) Fedde, Gentiana rhodantha Franch or Swertia kouitchensis. Erythrodiol 3-O-palmitate has antitumor activity, and inhibits the proliferation of K562 cells with the inhibition rate of 47% at 100 ug/mL .
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-
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- HY-157327
-
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Bcr-Abl
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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 .
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-
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- HY-155389
-
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Caspase
|
Cancer
|
Caspase-3 activator 2 (Compound 2f) is a caspase 3 activator that induces apoptosis and can be used in cancer research. Caspase-3 activator 2 is cytotoxic to HL-60 cells and K562 cells, with IC50 values of 33.52 μM and 76.90 μM respectively .
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-
-
- HY-142922
-
|
Bcr-Abl
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Cancer
|
BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .
|
-
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- HY-150239
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BAY-299N
|
DNA/RNA Synthesis
|
Cancer
|
BAY-364 (BAY-299N) is an inhibitor of the second bromine domain in TAF1. BAY-364 inhibits the TAF1 of Kasumi-1 cells, CD34 + cells and K562 cells with IC50 values of 1.0 µM, 10.4 µM and 10.0 µM respectively .
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-
-
- HY-N11709
-
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Others
|
Cancer
|
Theasaponin E1 is a tea saponin isolated from tea seeds. Theasaponin E1 exhibits potential antitumor activity against human tumor cell lines K562 and HL60. Theasaponin E1 also has quinone reductase (QR)-inducing activity and can act as an anti-tumor agent for cancer prevention .
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-
-
- HY-146718
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
Tubulin polymerization-IN-9 is a potent tubulin inhibitor with IC50 of 1.82 μM. Tubulin polymerization-IN-9 causes cell cycle arrest at G2/M phase, and induces cell apoptosis and depolarized mitochondria of K562 cells. Tubulin polymerization-IN-9 has potent anti-vascular and antitumor activities .
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-
-
- HY-153415
-
|
PROTACs
Bcr-Abl
|
Cancer
|
PROTAC BCR-ABL Degrader-1 (compound PROTAC 1) is a PROTAC with a 2-oxoethyl linker. PROTAC BCR-ABL Degrader-1 induces Bcr-Abl degradation in a ubiquitinproteasom-dependent manner. PROTAC BCR-ABL Degrader-1 exhibits antiproliferative activity against K562 cells, and has the potential to study cancer .
|
-
- HY-149470
-
|
Histone Acetyltransferase
|
Cancer
|
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-W728151
-
|
Endogenous Metabolite
|
Cancer
|
3-O-Caffeoylshikimic acid (Compound 8) is a phenolic and can be isolated from Livistona chinensis. 3-O-Caffeoylshikimic acid is an antioxidant agent. 3-O-Caffeoylshikimic acid inhibits the proliferation of human cancer cells HepG2, HL-60, K562, and CNE-1 with IC50s of 5–150 μM .
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- HY-111193
-
3-Chloroprocainamide
|
NF-κB
Apoptosis
|
Cancer
|
Declopramide (3-Chloroprocainamide) is an orally active antitumor agent, which inhibits proliferation of cancer cells HL60 and K562, and inhibits tumor growth of human brain astrocytoma (T24) in mouse model. Declopramide induces apoptosis, inhibits NF-κB through inhibition of IκBα degradation. Declopramide serves also as chemosensitizer in research .
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-
- HY-W178011
-
4,4'-Sulfonylbis(2-methylphenol)
|
Topoisomerase
|
Cancer
|
Topoisomerase IIα-IN-9 (NSC85582) is a bisphenol compound that has a moderate inhibitory effect on DNA topoisomerase Topoisomerase II (IC50: 571 μM). Topoisomerase IIα-IN-9 also exhibits a certain cell growth inhibitory effect, with IC50s of 117 μM and 218 μM for K562 and CHO, respectively .
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-
- HY-151361
-
|
AMPK
|
Cancer
|
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer .
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-
- HY-162489
-
|
Bcr-Abl
|
Others
|
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-136747
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Nec2/Hec1 inhibitor
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Others
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Cancer
|
N-[4-(2,4-Dimethylphenyl)-2-thiazolyl]-4-pyridinecarboxamide is a derivative of INH1 with anticancer activity. It is cytotoxic to MDA-MB-231, MDA-MB-488, HeLa, and K562 cells (IC50s=1.1, 3.4, 1.6, and 1.2 μM, respectively).
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-
- HY-N0678
-
Anhydroicaritin
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Autophagy
Apoptosis
|
Cancer
|
Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis [3.
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- 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 .
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-
- HY-156376
-
|
Cuproptosis
Apoptosis
Topoisomerase
|
Cancer
|
Cu(II)-Elesclomol is a Cu 2+ complex of Elesclomol (HY-12040). Cu(II)-Elesclomol induces cuproptosis. Cu(II)-Elesclomol also inducesapoptosis, causes a G1 cell cycle block and induces DNA double strand breaks in K562 cells. Cu(II)-Elesclomol also weakly inhibits DNA topoisomerase I. Cu(II)-Elesclomol has anticancer activity .
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- HY-122359A
-
rel-L-Centchroman; Ormeloxifene
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Estrogen Receptor/ERR
Apoptosis
Reactive Oxygen Species
|
Cancer
|
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-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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-
- HY-100490B
-
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
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-147831
-
|
Eukaryotic Initiation Factor (eIF)
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Cancer
|
EIF2α activator 1 (Compound 40) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 1 increases the expression level of eIF2α downstream proteins, ATF and CHOP. EIF2α activator 1 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.00 and 19.3 μM, respectively .
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- HY-125066
-
|
Bacterial
|
Infection
|
Reveromycin B is a spiroketal bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells (IC50=6 μg/mL) and exhibits pH-dependent antifungal activity against C. albicans (MICs=15.6 and >500 μg/mL at pH 3.0 and 7.4, respectively). Unlike reveromycin A and reveromycin C, reveromycin B does not inhibit proliferation of KB and K562 cells.
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-
- HY-100490A
-
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
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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-
- HY-147832
-
|
Eukaryotic Initiation Factor (eIF)
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Cancer
|
EIF2α activator 2 (Compound 1) is an activator of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. EIF2α activator 2 exhibits high potency in SRB cell proliferation assays (IC50=0.46 μM). EIF2α activator 2 exhibits antiproliferative activity againist K562 and PBMC cells with IC50s of 4.79 and 10.52 μM, respectively .
|
-
- HY-116971
-
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
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-161324
-
|
Microtubule/Tubulin
|
Cancer
|
Tubulin degrader 1 (Compound 5i) is a BML284 (HY-19987) derivative that is an orally active colchicine-site noncovalent tubulin degradation agent with IC50 values ranging from 0.02 to 0.05 μM against the five tumor cell lines (Hela, HCT116, MCF-7, K562 and Molm-13). Tubulin degrader 1 has antiproliferative activity that effectively suppressed tumor growth .
|
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- HY-W747507
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Bacterial
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Infection
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Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb/MK cells and has pH-dependent antifungal activity against C. albicans (MICs=2 and >500 μg/mL at pH 3 and 7.4, respectively).2 Reveromycin D also inhibits proliferation of KB and K562 cells (IC50s=1.6 and 1.3 μg/mL, respectively).
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- HY-100490S
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Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Cancer
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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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- HY-N12253
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Others
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Cancer
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(19R)-13-Deoxy-19-hydroxyenmein is the parent compound of enmein-type diterpenoid analogs. (19R)-13-Deoxy-19-hydroxyenmein has anti-proliferative activities with IC50 values of 0.41, 0.85, 0.43, 1.89 μM against human cancer cell lines K562, MGC-803, CaEs-17, and Bel-7402, respectively .
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- HY-156182
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JNK
Cytochrome P450
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Cancer
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JNK-IN-14 is a potent JNK inhibitor with IC50 values of 1.81, 12.7 and 10.5 nM for JNK1, JNK2 and JNK3, respectively. JNK-IN-14 induces early-stage apoptosis. JNK-IN-14 shows cell population arrest at the G2/M phase and slightly inhibits beclin-1 production at K562 leukemia cells relative to SP600125 (HY-12041), showing higher inhibitory ability.
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- HY-149511
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c-Met/HGFR
Apoptosis
PDGFR
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Cancer
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MET/PDGFRA-IN-2 (compound 8h) is a MET and PDGFRA protein inhibitor. MET/PDGFRA-IN-2 induces cell apoptosis. MET/PDGFRA-IN-2 inhibits proliferation of MET-positive cells (IC50s: 9.7, 6.1, 12.0, 11.5, 8.6, 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
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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-149510
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c-Met/HGFR
Apoptosis
PDGFR
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Cancer
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MET/PDGFRA-IN-1 (compound 8c) is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET). MET/PDGFRA-IN-1 inhibits MET phosphorylation and induces cell apoptosis. MET/PDGFRA-IN-1 inhibits proliferation of MET-positive cells (IC50s: 15.3, 19.0, 22.0, 25.6, 21.0, 31.5 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
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- HY-160214
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Others
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Inflammation/Immunology
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Perforin-IN-2 is a benzosulfonamide perforin inhibitor that alleviates transplant rejection during allogeneic bone marrow/stem cell transplantation. Perforin-IN-2 binds to plasma proteins with a binding rate of 99.8%. Perforin-IN-2 requires a higher concentration (> 900 μM) to achieve optimal perforin inhibition in vivo. Perforin-in-2 can effectively inhibit the lytic activity of recombinant perforin on Jurkat T (IC50=6.65 μM) leukemia cells, and also inhibit the death of K562 leukemia target cells .
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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-155112
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Microtubule/Tubulin
FLT3
Bcr-Abl
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Cancer
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Antiproliferative agent-30 (Compound 8g) inhibits tubulin assembly and inhibits FLT3 and Abl1. Antiproliferative agent-30 has vascular-disrupting activity. Antiproliferative agent-30 has broad antiproliferative activities against cancer cell lines (IC50s: 0.054 nM, 0.008 nM, 0.144 nM for HCT-116, K562, MV-4-11 cells respectively). Antiproliferative agent-30 also has anticancer effect against AML with FLT3-ITD-TKD mutation .
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- HY-161694
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DNA Methyltransferase
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Cancer
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DNMT1-IN-3 (compound 7t-S) is an effective DNA methyltransferase 1 (DNMT1) inhibitor with an IC50 value of 0.777 μM and a KD value of 0.183 μM. DNMT1-IN-3 can bind to the methyl donor S-adenosyl-l-methionine (SAM) site in DNMT1. DNMT1-IN-3 can inhibit cell proliferation in K562 cells by inducing cells apoptosis and arresting cell cycle at G0 / G1 phase, which has the potential to be used for the research of hematologic tumor .
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- HY-156016
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HDAC
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Cancer
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HDAC/CD13-IN-1 (Compound 12) is a HDAC/CD13 inhibitor (IC50: 0.34 μM for hCD13, 0.53 μM for porcine CD13, 0.03, 0.06, 0.02 μM for HDAC1/2/3). HDAC/CD13-IN-1 inhibits MV4-11, K562, Jeko-1, and HL60 cell proliferation (IC50: 0.25-2.04 μM). HDAC/CD13-IN-1 induces cancer cell apoptosis. HDAC/CD13-IN-1 has anti-metastasis and anti-invasion efficacy .
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- HY-N6972
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SARS-CoV
Cytochrome P450
Apoptosis
Parasite
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Infection
Inflammation/Immunology
Cancer
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Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
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- HY-151916
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Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
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Cancer
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Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.36, 1.35, 3.00, 0.88, 1.02 μM for NPP1, NPP2, NPP3, CA-II, CA-IX respectively. Enpp/Carbonic anhydrase-IN-1 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-1 induces Apoptosis .
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- HY-151917
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Apoptosis
Carbonic Anhydrase
Phosphodiesterase (PDE)
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Cancer
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Enpp/Carbonic anhydrase-IN-2 (compound 1i) is a potent Enpp and carbonic anhydrase inhibitor with IC50s of 1.13, 1.07, 0.74, 0.33, 0.68 for NPP1, NPP2, NPP3, CA-IX, CA-XII respectively. Enpp/Carbonic anhydrase-IN-2 shows antiproliferative activity for cancer cells and low cytotoxic against normal cells. Enpp/Carbonic anhydrase-IN-2 induces Apoptosis .
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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-146444
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Apoptosis
Bcl-2 Family
Caspase
Reactive Oxygen Species
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Cancer
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Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC50<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9 .
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- HY-151372
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PKD
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Cancer
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Protein kinase D inhibitor 1 (compound 17m) is a pan-PKD inhibitor, with IC50 values ranging from 17 to 35 nM. Protein kinase D inhibitor 1 inhibits PKD-dependent cortactin phosphorylation .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-11063S1
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Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant[1].
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- HY-11063S
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Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].
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- HY-100490S
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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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