Search Result
Results for "
MCF-7 cell
" in MedChemExpress (MCE) Product Catalog:
8
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-134964
-
-
-
- HY-13668
-
|
PaTrin-2
|
DNA Methyltransferase
|
Cancer
|
|
Lomeguatrib is a O 6-methylguanine-DNA methyltransferase (MGMT) inhibitor, with IC50s of 9 nM in cell-free assay and ～6?nM in MCF-7 cells.
|
-
-
- HY-B0543
-
|
Thiosinamine; N-Allylthiourea
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies .
|
-
-
- HY-13686
-
PQ401
2 Publications Verification
|
IGF-1R
Apoptosis
|
Cancer
|
|
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis .
|
-
-
- HY-W016794
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
NSC3852 exhibits anti-proliferative activity against cancer cell MCF-7. NSC3852 promotes the ROS generation, DNA damage, and apoptosis in MCF-7. NSC3852 exhibits anti-tumor against leukemia in mouse model
|
-
-
- HY-115997
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-153469
-
|
|
ADC Payload
|
Cancer
|
|
Benzyl DC-81 (Compound 6a) is an anticancer agent with antiproliferative activity against A375 and MCF-7 cells .
|
-
-
- HY-N2198
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents .
|
-
-
- HY-137099A
-
|
|
Fluorescent Dye
|
Endocrinology
|
|
Genistein 7-sulfate sodium is a metabolite of genistein that can reduce the activity of estrogen agonists in MCF-7 cells. Genistein 7-sulfate sodium can promote the growth of MCF-7 cells at concentrations of 10 μM and above .
|
-
-
- HY-N0435
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Isorhamnetin 3-gentiobioside is a flavonoid with activity of promoting cancer cell proliferation. Isorhamnetin 3-gentiobioside is an activator of DNA synthesis in MCF-7 human breast cancer cells with an EC50 of 3.1 μg/mL. Isorhamnetin 3-gentiobioside exhibits ABTS radical scavenging activity with an IC50 of 33.43 μg/mL. The compound can be used to study the bidirectional regulatory mechanism of cancer .
|
-
-
- HY-N2887
-
|
|
Others
|
Cancer
|
|
Araliadiol is a polyacetylenic compound isolated from the leaves of Aralia cordata Thunb. Araliadiol inhibits MCF-7 cells growth with an IC50 value of 6.41 μg/mL .
|
-
-
- HY-14585
-
|
Estrone 3-O-sulfamate
|
Steroid Sulfatase
|
Cancer
|
|
Estrone O-sulfamate (Estrone 3-O-sulfamate) is a potent steroid sulfatase (STS) inhibitor. Estrone O-sulfamate has inhibitory activity for STS in a placental microsomes (P.M.) preparation and in MCF-7 cells with IC50 values of 18 nM and 0.83 nM, respectively. Estrone O-sulfamate can be used for the research of cancer .
|
-
-
- HY-N4010
-
|
|
Others
|
Cancer
|
|
Iriflophenone, isolated from Aquilaria sinensis, stimulates MCF-7 and T-47D human breast cancer cells proliferation .
|
-
-
- HY-161740
-
|
|
AUTOTACs
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ .
|
-
-
- HY-148368
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
|
-
-
- HY-137099
-
|
|
Fluorescent Dye
|
Endocrinology
|
|
Genistein 7-sulfate is a metabolite of genistein that can reduce the activity of estrogen agonists in MCF-7 cells. Genistein 7-sulfate can promote the growth of MCF-7 cells at concentrations of 10 μM and above .
|
-
-
- HY-163281
-
|
|
Fluorescent Dye
|
Cancer
|
|
FSY-OSO2F shows an uptake in MCF-7 cells through the regulation of L-Tyr, ASC, and ASC2 transporters. FSY-OSO2F can be used as a PET tracer, when labeled with 18F, and exhibits good uptake and good contrast in MCF-7 and 22Rv1 subcutaneous tumors .
|
-
-
- HY-132247B
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(S)-ErSO is the dextrorotatory enantiomer of ErSO. (S)-ErSO is inactive in MCF-7 cells (from patent WO2020009958A1, compound (s)-105) .
|
-
-
- HY-N8679
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Physalin C is a natural product that can be found in physalis angulata. Physalin C shows cytotoxic activities against MCF-7 and HepG2 cells .
|
-
-
- HY-107550
-
|
|
HDAC
|
Cancer
|
|
NCT-14b is a HDAC6-selective inhibitor. NCT-14b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells .
|
-
-
- HY-175591
-
|
|
Photosensitizer
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Photosensitizer-7 is a endoplasmic reticulum (ER)-targeted photosensitizer (PS) (λab = 610 nm, λem = 622 nm). Photosensitizer-7shows an IC50 of 4.006 μM in HeLa cells and 3.28 μM in MCF-7 cells under light irradiation. Photosensitizer-7 exhibits dose-dependent cellular uptake and predominant colocalization with ER. Photosensitizer-7 induces dose-dependent intracellular ROS generation, reduces mitochondrial membrane potential, and increases apoptosis upon light irradiation in cells. Photosensitizer-7 significantly inhibits tumor growth in MCF-7 tumor-bearing mice. Photosensitizer-7 can be used for the study of photodynamic anticancer applications .
|
-
-
- HY-P5033
-
|
|
Bacterial
|
Cancer
|
Cyclo(Gly-His) is a liposome-encapsulated cyclic dipeptide with antimicrobial and anticancer activity. Cyclo(Gly-His) has cytotoxicity for HeLa and MCF-7 cell with IC50 values of 1.699 mM and 0.358 mM, respectively. Cyclo(Gly-His) can be used for the research of drug delivery systems .
|
-
-
- HY-175019
-
|
|
VEGFR
Apoptosis
Caspase
MDM-2/p53
Bcl-2 Family
|
Cancer
|
|
VEGFR-2-IN-70 is a potent VEGFR-2 inhibitor with an IC50 of 18.04 nM. VEGFR-2-IN-70 exhibits cytotoxicity against A549 and MCF-7 cancer cells with IC50 values of 0.43 μM and 3.8 μM, respectively. VEGFR-2-IN-70 induces G1 cell cycle arrest and apoptosis in lung cancer cells. VEGFR-2-IN-70 is useful in cancer research .
|
-
-
- HY-174404
-
|
|
Topoisomerase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC50 = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.
|
-
-
- HY-N5103
-
|
|
Others
|
Endocrinology
|
|
Genistein 7,4'-di-O-β-D-glucoside is a natural product with significantly estrogenic proliferative effect in MCF-7 cells .
|
-
-
- HY-W747516
-
|
|
Antibiotic
|
Infection
Cancer
|
|
Butylcycloheptylprodigiosin is the secondary metabolite produced by some bacteria, such as Streptomyces. Butylcycloheptylprodigiosin is a red-pigmented antibiotic and exhibits cytotoxicity against cancer cell MCF-7 and HDF .
|
-
-
- HY-103452
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
RU58668 is a steroidal antiestrogen that can be used as a potent antiproliferative agent on MCF-7 cells. RU58668 has the potential for the breast cancer research .
|
-
-
- HY-171755
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-40 (Compound 15b) is a heat shock protein 90 (Hsp90) C-terminal inhibitor. Hsp90-IN-40 exhibits antiproliferative activity against SKBr3 and MCF-7 breast cancer cells (IC50 of 2.57 µM and 2.43 µM, respectively). Hsp90-IN-40 inhibits cancer cell growth by inhibiting the Hsp90 C-terminal function, leading to Hsp90-dependent protein degradation. Hsp90-IN-40 can be used in breast cancer research .
|
-
-
- HY-148453
-
|
|
Drug Derivative
|
Cancer
|
|
Antiproliferative agent-16 is an indolyl hydrazide-hydrazone compound with anticancer activity. Antiproliferative agent-16 exhibits specificity toward breast cancer cells (IC50 of 6.94 μM for MCF-7 cells) .
|
-
-
- HY-153700
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
|
-
-
- HY-163126
-
|
|
Cholinesterase (ChE)
|
Cancer
|
|
AChE-IN-52 (compound A6) is an acetylcholinesterase (AChE) inhibitor. AChE-IN-52 shows antitumor efficacy, especially against breast cancer MCF-7 cells. AChE-IN-52 significantly disrupts the amino acid metabolism and inhibits migration of MCF-7. AChE-IN-52 plays anticancer role by regulating Best1 and HIST1H2BJ .
|
-
-
- HY-N4010R
-
-
-
- HY-147887
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 28 (compound 2g) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 28 shows anti-proliferative activity for MCF-7 cells .
|
-
-
- HY-170975
-
|
|
VD/VDR
|
Cancer
|
|
UG-650 is a non-Gemini analog of UVB1 that combines the structural features of UVB1 and MC 1288. UG-650 can bind to the vitamin D receptor (VDR) and inhibit the proliferation of MCF-7 cells and the migration of MC3T3-E1 cells .
|
-
-
- HY-162695
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Antitumor agent-168 (compound 21b) disrupts the microtubule network in tumor cells leading to G2/M cell cycle arrest and apoptosis induction. Antitumor agent-168 inhibits MCF-7 growth with an IC50 value of 1.4 nM .
|
-
-
- HY-N15584
-
|
Isoheraclenin
|
Others
|
Cancer
|
|
Pabularinone is a compound found in the plant Clausena lansium. Pabularinone has potent cytotoxic activity, and its activity showed inhibitory effects in human breast cancer (MCF-7) cells (IC50: 33.74 μg/mL). Pabularinone can be used in anti-tumor research .
|
-
-
- HY-100219
-
|
|
VD/VDR
|
Cancer
|
|
CB1151 is a 20-epi analogue of 1,25 dihydroxyvitamin D3 (VD) with potent anti-tumor effects. CB1151 inhibits MCF-7 cell growth with an IC50 value of 0.82 nM .
|
-
-
- HY-134964R
-
-
-
- HY-175177
-
|
|
Apoptosis
Caspase
β-catenin
|
Cancer
|
|
Xiap-casp7 PPI-IN-1 is a reversible XIAP: CASP7 inhibitor with specifically disrupting the interaction between XIAP and CASP7. XIAP-CASP7 PPI-IN-1 selectively induce MCF-7 and other caspase-3 down-regulation (CASP3/DR) triple-negative breast cancer cell apoptosis. XIAP-CASP7 PPI-IN-1 overcomes chemoresistance via down-regulating β-catenin and its associated ABC transporters in Paclitaxel (HY-B0015)-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 can be used for the study of breast cancer .
|
-
-
- HY-147882
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 6 (compound 3q6) is a potent anti-methicillin-resistant Staphylococcus aureus (anti-MRSA) agent. Anti-MRSA agent 6 shows low cytoxicity for MCF-7, A549 cells .
|
-
-
- HY-N10959
-
|
|
Others
|
Cancer
|
|
4,15-Isoatriplicolide methylacrylate is a germacrane-type sesquiterpene lactone. 4,15-Isoatriplicolide methylacrylate also is a cytotoxic agent. 4,15-Isoatriplicolide methylacrylate has cytotoxic activity for MCF-7 human breast cancer cell line .
|
-
-
- HY-144791
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
-
- HY-144792
-
|
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
-
- HY-146988
-
|
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
hCAIX/XII-IN-1 is a potent CAIX/XII inhibitor with the KI values of 0.48 µM and 0.83 µM for CAIX and CAXII, respectively. hCAIX/XII-IN-1 shows antiproliferative activity in vitro. hCAIX/XII-IN-1 induces apoptosis in MCF-7 cells .
|
-
-
- HY-155348
-
|
|
PARP
|
Cancer
|
|
Ru3 is a poly(ADP-ribose) polymerase 1 inhibitor. Ru3 induces apoptosisin MCF-7 cells by multiple modes, inclusive of inducing DNA damage, suppressing DNA damage repair, disturbing cell cycle distribution, decreasing the mitochondrial membrane potential, and increasing the intracellular reactive oxygen species levels .
|
-
-
- HY-175173
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-166 (Compound 2) is a EGFR inhibitor. EGFR-IN-166 has potent anticancer activity against breast cancer cells with IC50s of 69.63 and 22.84 μM for MCF-7 and MDA-MB-231 cells, respectively. EGFR-IN-166 significantly inhibits cell migration and EGFR expression. EGFR-IN-166 can be used for breast cancer research .
|
-
-
- HY-147888
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 29 (compound 3c) is a potent tubulin inhibitor with an IC50 value of 1.2 µM. Tubulin inhibitor 29 shows antiproliferative effects with an IC50 value of 7.5 µM for MCF-7 cells. Tubulin inhibitor 29 inhibits tubulin assembly and bounds in the colchicine site .
|
-
-
- HY-N11973
-
|
|
Others
|
Cancer
|
|
5,7-Dimethoxy-2,3-phenanthrenediol is a compound with estrogenic activity. 5,7-Dimethoxy-2,3-phenanthrenediol increases the proliferation of MCF-7 cell and the expression of ERβ in the MCF-7 cell line .
|
-
-
- HY-144637
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer .
|
-
-
- HY-169122
-
|
|
Drug Derivative
|
Cancer
|
|
LLC1 is an Amiloride (HY-B0285) derivative with cytotoxicity against breast cancer cells, particularly those resistant to treatment. The IC50 values of LLC1 for MCF7, MCF7 MX-100, MCF7 TS, MCF7 TR-1, and MCF7 TR-5 are 13, 12, 25, 26, and 19 mM, respectively. LLC1 shows potential for research in the field of cancer therapy .
|
-
- HY-101989
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-24 (compound HMBA) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-24 inhibits MCF-7 cells proliferation. Tubulin polymerization-IN-24 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-24 increase the GTP hydrolysis rate and inhibits microtubule assembly .
|
-
- HY-161858
-
|
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
EpskA21 is an inhibitor for PI3K/AKT signaling pathway, and inhibits the proliferation of cancer cells MCF-7, A549, MIA-PaCa-2, Panc-1 and HepG2, with IC50 of 1.3-7.24 μM. EpskA21 inhibits the cell migration, arrests the cell cycle at G2/M (MCF-7) and S (MIA-PaCa-2) phase, and induces apoptosis in MCF-7 and MIA-PaCa-2. EpskA21 causes the mitochondrial dysfunction .
|
-
- HY-162000
-
|
|
Apoptosis
|
Cancer
|
hCAIX/XII-IN-13 is an inhibitor of human carbonic anhydrases (hCA). hCAIX/XII-IN-13 shows good inhibitory activity against the tumor-related CA subtypes IX and XII, with Ki values of 0.08 µM and 0.06 µM, respectively. Under hypoxic conditions, hCAIX/XII-IN-13 can restore the cytotoxicity of Doxorubicin (HY-15142A) on MCF-7 cells, increasing G2/M phase cell cycle arrest and apoptosis .
|
-
- HY-144306
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα degrader 4 is an excellent and selective estrogen receptor α (ERα) degrader (IC50 of 0.31, 0.41 and 0.48 μM in MDA-MB-231, MCF-7 and MCF-7/ADR cells, respectively). ERα degrader 4 has potent inhibitory activity against MCF-7 cell lines. ERα degrader 4 is a potential SERDs candidate for the research of breast cancer .
|
-
- HY-147913
-
|
|
PI3K
Akt
mTOR
Apoptosis
|
Cancer
|
|
PI3K/Akt/mTOR-IN-3 (compound 3d) is a potent PI3K/AKT/mTOR inhibitor. PI3K/Akt/mTOR-IN-3 displays the inhibitory activity in MCF-7, HeLa and HepG2 cells, with IC50 values of 0.77, 1.23, and 4.57μM, respectively. PI3K/Akt/mTOR-IN-3 inhibits the migration of MCF-7 and HeLa cells at the concentration of 4 μM. PI3K/Akt/mTOR-IN-3 induces cell apoptosis and S phase arrest .
|
-
- HY-169477
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
PAMAM Dendrimer G0.5 Carboxylate sodium is a polyamidoamine (PAMAM) dendrimer with carboxylate termini. PAMAM Dendrimer G0.5 Carboxylate sodium conjugated with DACHPt is cytotoxic to A2780 ovarian cancer cells, MCF-7 breast cancer cells, Caco-2 colon cancer cells and BJ fibroblasts with IC50 values of 0.03, 1.6, 0.18 and 3 µM, respectively .
|
-
- HY-W082856A
-
|
|
BCRP
|
Cancer
|
|
Butein tetramethyl ether (Compound 20) is a potent and selective breast cancer resistance protein/ATP-binding cassette subfamily G member 2 (BCRP/ABCG2) inhibitor. Butein tetramethyl ether has inhibitory potencies against MCF-7 MX and MDCK BCRP cells with IC50 values of 2.2 and 1.03 μM, respectively. Butein tetramethyl ether is promising for research of cancers .
|
-
- HY-170590
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
VEGFR-2-IN-61 (Compound 7b) is an inhibitor for VEGFR-2 with an IC50 of 2.83 µM. VEGFR-2-IN-61 inhibits the proliferation of multi cancer cells (IC50 for MCF-7 is 2.12 μM). VEGFR-2-IN-61 inhibits the cell migration, induces oxidative stress and apoptosis in MCF-7 .
|
-
- HY-145866
-
|
|
Drug Intermediate
|
Cancer
|
|
Antiproliferative agent-3 (comp 4) shows the highest potency for MCF-7 cells (IC50 = 0.19 nM) .
|
-
- HY-116377
-
|
|
Steroid Sulfatase
|
Neurological Disease
|
|
DU-14 is a potent steroid sulfatase inhibitor with an IC50 of 55.8 nM. DU-14 inhibits the MCF-7 cell proliferation (IC50 = 38.7 nM). DU-14 has neuroprotective effects against neurotoxic Aβ, suggesting that up-regulation of endogenous DHEAS by DU-14 could be beneficial to the alleviation of Aβ-induced impairments in spatial memory and synaptic plasticity .
|
-
- HY-172621
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-159 (compound 12), a dihydropyrimidine, is a potent EGFR inhibitor with an IC50 value of 29.00 nM. EGFR-IN-159 exhibits dose-dependent inhibition against EGFR and HER2. EGFR-IN-159 shows cytotoxicity against MCF-7 breast cancer cells and Vero cells with IC50 values of 16.07 μg/mL and 35.98 μg/mL, respectively. EGFR-IN-159 has no BBB permeation. EGFR-IN-159 shows appreciable anti-cancer activity .
|
-
- HY-162885
-
|
|
Proteasome
JAK
STAT
Interleukin Related
|
Cancer
|
|
YSY01A is a proteasome inhibitor that can suppress cancer cell survival by inducing apoptosis (Apoptosis). Its IC50 values are 51.0 nM for HEK293T, 9.2 nM for A549, 5.2 nM for MCF-7, 8.9 nM for MGC-803, and 35.4 nM for PC-3M cells. Additionally, YSY01A eliminates constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A holds promise for research in the field of cancer therapy .
|
-
- HY-155841
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
Tubulin polymerization-IN-46 (compound 9q) is a microtubule/Tubulin inhibitor that inhibits tubulin polymerization and induces apoptosis. Tubulin polymerization-IN-46 inhibits mitosis and arrests MCF-7 cells in the G2/M phase. Tubulin polymerization-IN-46 has anti-proliferative activity against MCF-7 breast cancer cells with an IC50 of 10 nM .
|
-
- HY-155177
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-27 (Compound 6a) is a CDK9 inhibitor (IC50s: 0.424 μM). CDK9-IN-27 induces apoptosis and cell cycle arrest at S stage. CDK9-IN-27 has cytotoxic action against HepG2, HCT-116 and MCF-7 cell lines, with IC50s of 10.31-40.34 μM. CDK9-IN-27 can be used for cancer research .
|
-
- HY-138089
-
|
|
Androgen Receptor
Estrogen Receptor/ERR
LDLR
|
Metabolic Disease
Cancer
|
|
17β-Hydroxy exemestane (17-H-EXE) is the primary active metabolite of Exemestane (HY-13632). 17β-Hydroxy exemestane is an aromatase inhibitor (IC50 = 69 nM) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). 17β-Hydroxy exemestane stimulates growth of AR- and ERα-positive MCF-7 (EC50= 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7 cells. 17β-Hydroxy exemestane inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae in ovariectomized rats .
|
-
- HY-158388
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 215 (1) is a Camptothecin compound, with IC50 values of 5.2 nM and 8.2 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-158389
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 216 (34A) is a Camptothecin compound, with IC50 values of 9.6 nM and 11.6 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-158387
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 214 (2) is a Camptothecin compound, with IC50 values of 2.6 nM and 15.7 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-147853
-
|
|
Raf
|
Cancer
|
|
B-Raf IN 8 (compound 7g) is a potent B-Raf inhibitor, with an IC50 of 70.65 nM. B-Raf IN 8 exhibits antitumor activity against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells, with IC50 values of 9.78, 13.78, 18.52 and 29.85 µM .
|
-
- HY-N3042
-
|
Platyphyllone
|
Others
|
Cancer
|
|
Platyphyllonol (Platyphyllone) can be isolated from A. japonica. Platyphyllonol shows cytotoxic effects on MCF-7 cells with IC50 values of 46.9 μg/mL .
|
-
- HY-147967
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-63 is an EGFR inhibition (IC50: 0.096 μM) and it has anticancer activity in MCF-7 cells (IC50: 2.49 μM).
|
-
- HY-N14603
-
|
|
Fungal
|
Infection
|
|
Chandrananimycin A has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
|
-
- HY-158390
-
|
|
Topoisomerase
|
Cancer
|
|
Anticancer agent 217 (35B) is a Camptothecin compound, with IC50 values of 6.2 nM and 7.1 nM in MCF-7 cells and MDA-MB-231 cells, respectively .
|
-
- HY-156115
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-3 (compound 4b) is a dual inhibitor of EGFR and CDK-2 with IC50s of 71.7 and 113.7 nM, respectively. EGFR/CDK2-IN-3 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-3 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 3.16 μM .
|
-
- HY-156114
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-2 (compound 6a) is a dual inhibitor of EGFR and CDK-2 with IC50s of 19.6 and 87.9 nM, respectively. EGFR/CDK2-IN-2 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-2 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 0.39 μM .
|
-
- HY-156116
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-4 (compound 4c) is a dual inhibitor of EGFR and CDK-2 with IC50s of 89.6 and 165.4 nM, respectively. EGFR/CDK2-IN-4 induces apoptosis in MCF-7 cells and arrests the cell cycle in the S phase. EGFR/CDK2-IN-4 has significant anti-cancer cell toxicity and inhibits MCF-7 with an IC50 of 2.74 μM .
|
-
- HY-118129
-
|
Ganwuweizic acid
|
PARP
Apoptosis
|
Cancer
|
|
Schisandronic acid is a triterpenoid antioxidant and anticancer agent extracted from Schisandra chinensis, which has potent cytotoxicity against human breast cancer cells, especially MCF-7. Schisandronic acid induces apoptosis and reduces cell viability in a time-dependent manner (MCF-7, IC50=8.06 μM). Schisandronic acid can upregulate active caspase-3 expression and cleave PARP, reduce the generation of reactive oxygen species and exhibit antioxidant effects .
|
-
- HY-175567
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apoptosis inducer 41 is an apoptosis inducer that induces apoptosis through the mitochondrial pathway. Apoptosis inducer 41 exhibits remarkable inhibitory effects against MCF-7 cells (IC50 = 6.2 μM). Apoptosis inducer 41 significantly arrests MCF-7 cells in the G2/M phase, increases ROS accumulation, induces mitochondrial membrane potential depolarization. Apoptosis inducer 41 can used for the study of breast cancer .
|
-
- HY-163125
-
|
|
VEGFR
|
Cancer
|
|
BHEPN is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR-2). BHEPN has inhibition of VEGFR-2 with an IC50 value of 0.320 μM. BHEPN also exhibits remarkable cytotoxic effects against HepG2 and MCF-7 cancer cell lines, with IC50 values of 0.19 μM and 1.18 μM, respectively. BHEPN can be used for anticancer research .
|
-
- HY-168589
-
|
|
Apoptosis
Cytochrome P450
Caspase
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer .
|
-
- HY-147852
-
|
|
Raf
|
Cancer
|
|
B-Raf IN 7 (compound 6a) is a potent B-Raf inhibitor, with an IC50 of 110.23 nM. B-Raf IN 7 exhibits antitumor activity against colon carcinoma (HCT-116), mammary gland (MCF-7), hepatocellular carcinoma (HEPG-2), human cervical carcinoma (Hela) and human prostate cancer (PC-3) cells, with IC50 values of 7.50, 9.87, 10.57, 11.63 and 12.83 µM .
|
-
- HY-173492
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-156 (Compound 7f) is an EGFR inhibitor that also has inhibitory activity against mutations EGFRL858R and EGFRT790M (IC50 values are 0.186, 0.131, and 0.107 μM, respectively). EGFR-IN-156 has significant anticancer activity against human cancer cell lines HepG-29 (liver cancer), MCF-7 (breast cancer), and HCT-116 (colon cancer) (IC50 values are 1.67, 5.32, and 6.56 μM, respectively). EGFR-IN-156 inhibits cancer cell proliferation by inducing cell cycle arrest at the G/G1 phase and triggering apoptosis. EGFR-IN-156 shows promise in EGFR-related cancers .
|
-
- HY-175174
-
|
|
Glutaminase
|
Cancer
|
|
Antiproliferative agent-73 (Compound 7) is an antiproliferative agent. Antiproliferative agent-73 significantly inhibits proliferation of human cancer cells with excellent cytotoxicity. Antiproliferative agent-73 has potent anticancer activity with IC50s of 15.20, 18.18, 20.20 and 13.23 μM for HepG2, MCF-7, HCT-116 and WI38 cells, respectively. Antiproliferative agent-73 can be used for cancers research, such as breast, colorectal and liver cancer .
|
-
- HY-N10305
-
|
|
Autophagy
|
Cancer
|
|
Clionamine B is an autophagy stimulating aminosteroid isolated from the sponge Cliona celata. Clionamine B strongly stimulates autophagy in human breast cancer MCF-7 cells .
|
-
- HY-N7464
-
|
|
Others
|
Others
|
|
Jolkinolide E is a casbane diterpenoid from the roots of Euphorbia rapulum. Jolkinolide E shows weak selective activity against HepG2, MCF-7, and C6 cell lines .
|
-
- HY-N2863
-
|
|
Others
|
Cancer
|
|
Goniothalenol is a styryl lactone that can be isolated from Goniothalamus griffithii. Goniothalenol exhibits cytatoxic activity against A2780, HCT-8, KB and MCF-7 cell lines .
|
-
- HY-173040
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 266 (Compound 3B) is an anticancer agent that can inhibit the proliferation of tumor cells. Anticancer agent 266 has an IC50 of 0.13 μM for MCF-7 breast cancer cell line .
|
-
- HY-N9391
-
|
|
Apoptosis
|
Cancer
|
|
7,3′,5′-Trihydroxyflavanone, a flavanoid derivative, induces the apoptotic cell death of MCF-7 cells by increasing Bax expression level. 7,3′,5′-Trihydroxyflavanone also exhibits antioxidant activity .
|
-
- HY-161692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERα degrader 8 (Compound 18j) is a selective Estrogen Receptor degrader. ERα degrader 8 is degrader to MCF-7 cells with IC50 value of 0.15 μM .
|
-
- HY-179103
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK4-IN-5 (compound 5f) is a PLK4 (IC50 = 0.8 nM) inhibitor. PLK4-IN-5 can inhibit MCF-7 cell clone formation, induce cell cycle arrest (S/G2 phase), and apoptosis. PLK4-IN-5 has anti proliferative activity against MCF-7 cells (IC50 = 0.48 μM). PLK4-IN-5 can be used in the research of cancer such as breast cancer .
|
-
- HY-173528
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
Antimicrobial agent-40 (Compound 5a) has antimicrobial activity against fungi, Gram-negative and Gram-positive bacteria. Antimicrobial agent-40 has good cytotoxicity against MCF-7 cells (IC50: 33.52 μM) and exhibits anticancer activity .
|
-
- HY-173368
-
|
|
PI3K
|
Cancer
|
|
Antiproliferative agent-67 (Compound 5g) is a PI3K inhibitor with a selectivity index SI of 7.72 for breast cancer cells (MCF-7). Antiproliferative agent-67 inhibits the activity of PI3K protein by forming hydrogen bonds and intermolecular hydrophobic forces with it, exerting anti - proliferative activity against breast cancer cells (MCF-7), and can be used in the research of breast cancer .
|
-
- HY-180827
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-79 (Compound 17) is a VEGFR-2 inhibitor with an IC50 of 2.32 μM. VEGFR-2-IN-79 exhibits potent and broad-spectrum cytotoxicity and can induce apoptosis in MCF-7 cells. VEGFR-2-IN-79 does not cause a significant decrease in the mitochondrial membrane potential of MCF-7 cells. VEGFR-2-IN-79 can be used for research on breast cancer .
|
-
- HY-N14604
-
|
|
Fungal
|
Infection
|
|
Chandrananimycin B has anti-mucor activity, as well as anti-tumor cell activity such as CCL HT29, MFXF 529L, MACL McF-7 .
|
-
- HY-159994
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
AUPF02, a 5-arylurea uracil derivative, is a potent anti-breast cancer agent, with an IC50 of 23.4 µM for MCF-7 cells .
|
-
- HY-186161
-
|
|
Others
|
Cancer
|
|
Antiproliferative agent-77 is an anticancer cell proliferation agent that exerts significant antiproliferative effects on HCT116, HepG2, H1299 and MCF-7 .
|
-
- HY-N15306
-
|
|
Apoptosis
|
Cancer
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-168644
-
-
- HY-180541
-
|
|
COX
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-190 (Compound 3o) is an inhibitor that targets both EGFR (IC₅₀ = 0.028 μM) and COX-2 (IC₅₀ = 0.208 μM). EGFR-IN-190 exhibits potent inhibitory activity against MCF-7 cells and induces apoptosis (apoptosis). EGFR-IN-190 can be used for research on breast cancer .
|
-
- HY-N16759
-
|
|
Others
|
Cancer
|
|
Apparicine is a monoterpene indole alkaloid that can be naturally extracted from the stems of Tabernaemontana divaricata. Apparicine shows no cytotoxicity against MCF-7 human breast cancer cells and A-549 human lung cancer cells .
|
-
- HY-162035
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2-IN-23 (compound 5d) is an inhibitor of MDM2. MDM2-IN-23 has an IC50 of 60.09 μM on MCF-7 cells .
|
-
- HY-176956
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 13 (Compound 37) is an estrogen receptor (ER) degrader. ER degrader 13 has a significant inhibitory effect on the proliferation of ER-positive breast cancer MCF-7 cells .
|
-
- HY-N6990
-
|
|
Others
|
Cancer
|
|
Anhydrosecoisolariciresinol is from the flower of Wedelia biflora, has anti-tumor activities .
Anhydrosecoisolariciresinol decreases the growth of human breast cancer MCF-7 and MDA-MB-231 cell lines .
|
-
- HY-147504
-
|
|
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity .
|
-
- HY-162239
-
|
|
Drug Intermediate
|
Cancer
|
|
Anticancer agent 187 (Compound 4) is an anticancer agent that can target sarcoma cells in tumor-bearing mouse models. Anticancer agent 187 exhibits cytotoxic activity against HepG2, Caco2, and MCF-7 cells .
|
-
- HY-147782
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 67 (Compound 13g) is an anti-cancer agent. Anticancer agent 67 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 67 is a ciprofloxacin analog .
|
-
- HY-147781
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 66 (Compound 13e) is an anti-cancer agent. Anticancer agent 66 induces apoptosis and increases sub-G1 cell population in MCF-7 cells. Anticancer agent 66 is a ciprofloxacin analog .
|
-
- HY-113319
-
|
|
Drug Intermediate
|
Cancer
|
|
β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
-
- HY-155167
-
|
|
Antibiotic
Fungal
|
Cancer
|
|
Anticancer agent 151 (compound 6C) is an anticancer agent. Anticancer agent 151 exhibits excellent in vitro cytotoxic activity against MCF-7 cells with an IC50 value of 6.3 μM .
|
-
- HY-158743
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Indium (III) thiosemicarbazone 5b (compound 5b) is an Indium (III) thiosemicarbazone agent. Indium (III) thiosemicarbazone 5b effectively inhibits MCF-7 and DDP tumor cells growth .
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
- HY-143233
-
|
|
Pim
HDAC
Apoptosis
|
Cancer
|
|
PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-N3443
-
|
|
Others
|
Cancer
|
|
Jolkinol A is a natural product that can be found in Euphorbia pubescens. Jolkinol A inhibits cell growth with GI50s of 95.3, 57.3, >100 µM for MCF-7, NCI-460, SF-268 cells, respectively .
|
-
- HY-W702106
-
|
|
Endogenous Metabolite
|
Cancer
|
2-Methyl estradiol, an endogenous metabolite of Estradiol (HY-B0141), inhibits cell proliferation and angiogenesis, with IC50 values of 3 and 2.39 μM for HUVEC and MCF-7 human breast cancer cell proliferation, respectively .
|
-
- HY-N8859
-
|
16-Hydroxyiridal
|
Others
|
Others
|
|
Isoiridogermanal can be isolated from the extract of rhizomes of Iris tectorum Maxim. Isoiridogermanal is cytotoxic with IC50 values of 11 μM and 23 μM against MCF-7 and C32 cell lines.
|
-
- HY-P5956
-
|
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-LEHD-CHO is an inhibitor of caspases 4, 5 and 9. Ac-AAVALLPAVLLALLAP-LEHD-CHO shows protective effects upon Neocarzinostatin (HY-111183)-treated MCF-7 cells .
|
-
- HY-W288480
-
|
|
Apoptosis
|
Cancer
|
|
Trihexyl phosphate is an organophosphate flame retardant. Trihexyl phosphate causes mitochondrial impairment and induces cell apoptosis in CHO cells. Trihexyl phosphate promotes the proliferation of human breast cancer cells (MCF-7) in a dose-dependent manner and exerts estrogenicity via ERα-independent pathways .
|
-
- HY-113796
-
|
|
Others
|
Cancer
|
|
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
|
-
- HY-N13213
-
|
|
Others
|
Cancer
|
|
Fenugreek Seed Extract is a fenugreek extract. Fenugreek Seed Extract has potential antibacterial and anticancer activities, can inhibit Staphylococcus aureus and Pseudomonas aeruginosa, and inhibit the proliferation of MCF-7 breast cancer cells (no significant effect on liver cancer cells). .
|
-
- HY-111524
-
|
|
HSP
Apoptosis
|
Cancer
|
|
CPUY201112 is a potent heat shock protein Hsp90 inhibitor with Kd of 27 nM. CPUY201112 induces p53-mediated apoptosis in MCF-7 cells, resulting in cell cycle arrest, which can be used in cancer research .
|
-
- HY-175003
-
|
|
Proton Pump
|
Cancer
|
|
HV1-IN-2 (Compound 14c) is a human voltage-gated proton channel (HV1) inhibitor with an IC50 of 2.14 μM. HV1-IN-2 has a potent anticancer activity with significant antiproliferative effects against THP-1 and MCF-7 cells. HV1-IN-2 can be used for cancers research, such as colorectal tumours, leukaemia, and breast cancer .
|
-
- HY-170402
-
|
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT6-IN-4 (Compound 10d) is a selective inhibitor for SIRT6 with an IC50 of 5.68 μM. SIRT6-IN-4 inhibits the proliferation of MCF-7 with an IC50 of 8.30 μM. SIRT6-IN-4 arrests the cell cycle at G2/M phase, inhibits thecell migration and invasion of MCF-7, and induces apoptosis. SIRT6-IN-4 exhibits antitumor efficacy in mouse models .
|
-
- HY-115948
-
|
|
Others
|
Cancer
|
|
Antitumor agent-46 (Compound 2h) is an anti-tumor agent. Antitumor agent-46 demonstrates markedly higher antiproliferative activity on MCF-7 cells with an IC50 value of 2.08 µM .
|
-
- HY-183197
-
|
|
Drug Derivative
|
Cancer
|
|
SR 13915 is a structural analog of EGCG (HY-13653), a green tea polyphenol, and exhibits an IC50 greater than 100 μM against both MCF‑7 and MDA‑MB‑231 cell lines .
|
-
- HY-178774
-
|
Isopentyl-deoxynboquinone
|
Quinone Reductase
|
Cancer
|
|
IP-DNQ is an efficient NQO1 dependent cytotoxic agent. IP-DNQ has a potent killing effect on MCF-7 cells (IC50 = 0.18 µM). IP-DNQ can be used for cancer research .
|
-
- HY-163812
-
|
|
Molecular Glues
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 9 (compound 1), a bifunctional molecular glue, is a potent estrogen receptor (ER) degrader with a DC50 of ≤10 nM in MCF-7 cells. ER degrader 9 can be used for the research of breast cancer .
|
-
- HY-146440
-
|
|
Histone Demethylase
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has high affinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
|
-
- HY-N7654
-
|
|
Apoptosis
|
Cancer
|
|
(-)-Epipodophyllotoxin (2) is an antiproliferative agent against cancer cells isolated from American mayapple Podophyllum peltatum, with GI50s of 0.36 and 0.24 μM in HeLa cells and MCF-7 cells, respectively. (-)-Epipodophyllotoxin can inhibit mitotic spindle assembly in vitro .
|
-
- HY-146162
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Colletotrichalactones A is a polyketide that display moderate-to-potent cytotoxic activities against MCF7 cells with an IC50 of 35.06 µM .
|
-
- HY-178472
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
AurAP14 is an Aurora A PROTAC degrader (DC50 = 120 nM). AurAP14 shows significant inhibitory activity against various tumor cell lines, with IC50s of 0.294 μM in A549 cells and 0.534 μM in MCF-7 cells. AurAP14 induces apoptosis and arrests A549 cells in the S and G2/M phases. AurAP14 demonstrates anti-tumor efficacy in nude mouse xenograft models of A549 and A549/PTR. AurAP14can be used in the research on the treatment of Aurora A-overexpressing NSCLC. (Pink: Aurora A ligand (HY-10971), Blue: E3 ligase Ligand (HY-W437598), Black: Linker) .
|
-
- HY-N10846
-
|
|
Others
|
Others
|
|
Neotriptonoterpene, a compound isolated from T. regelii, shows weak cytotoxic activity against A2780, HepG2 and MCF-7 cells with IC50 values of 65.80, 35.45 and 64.80 µM respectively .
|
-
- HY-13762
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-135590
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6 .
|
-
- HY-135584
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6 .
|
-
- HY-13762A
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
|
-
- HY-N3316
-
|
|
Others
|
|
|
Martynoside protects ex vivo bone marrow cells from 5-fluorouracil (5-FU)-induced cell death and inflammation response by down-regulating the TNF signaling pathway .Martynoside is a potent antiestrogen in MCF-7 cells, increasing IGFBP3 levels
|
-
- HY-161641
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
|
-
- HY-178099
-
|
|
Apoptosis
Caspase
PARP
Bcl-2 Family
|
Cancer
|
|
Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer .
|
-
- HY-161852
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3K-IN-55 (Compound 6a) is a potent inhibitor for PI3K. PI3K-IN-55 affects PI3K/Akt/p53 signaling pathway, inhibits the proliferation of cancer cells A549, Hela, HepG2, MCF-7 and HT-29, with IC50s of 1.03-6.78 μM. PI3K-IN-55 induces apoptosis in cell MCF-7 .
|
-
- HY-175638
-
|
|
Carbonic Anhydrase
Apoptosis
Bcl-2 Family
CDK
|
Cancer
|
|
Carbonic anhydrase-IN-35 is a selective carbonic anhydrase (CA) inhibitor. Carbonic anhydrase-IN-35 potently inhibits tumor-associated hCA IX (Ki = 0.6 nM) and hCA XII (Ki = 2.2 nM). Carbonic anhydrase-IN-35 induces apoptosis in MCF-7 cells by elevating Bax, reducing Bcl-2, and downregulating CDK4/6. Carbonic anhydrase-IN-35 exhibits potent cytotoxicity against MCF-7 (IC50 = 0.3975 μM normoxic/0.6575 μM hypoxic), MCF-7-ADR (IC50> = 0.3975 μM normoxic/4.488 μM hypoxic), MDA-MB-231, and 4T1 breast cancer cells. Carbonic anhydrase-IN-35 can be used for the study of breast cancer .
|
-
- HY-112589
-
|
|
Bacterial
|
Infection
Cancer
|
|
BRITE-338733 is an inhibitor of E. coli RecA ATPase activity (IC50: 4.7 μM). BRITE-338733 also inhibits the ATP hydrolysis activity of RSC chromatin remodeling enzyme by binding to its ATP-binding pocket and DNA (IC50: 0.316 μM). BRITE-338733 exhibits cytotoxicity against MCF-7 and MDA-MB-231 breast cancer cells. BRITE-338733 can be used in studies on antibacterial adjuvants and anticancer research .
|
-
- HY-112721
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
FDI-6 is an inhibitor of FOXM1. FDI-6 binds directly to FOXM1 protein, to displace FOXM1 from genomic targets in MCF-7 breast cancer cells, and induce concomitant transcriptional down-regulation.
|
-
- HY-N3318
-
|
|
HIV
|
Infection
|
|
Marsdenoside F is a polyoxygenated pregnane glycoside isolated from the stems of Marsdenia tenacissima. Marsdenoside F showed no significant cytotoxicity against A549 and MCF-7 cell lines, nor did it exhibit significant anti-HIV activity .
|
-
- HY-N16642
-
|
|
Others
|
Cancer
|
|
Rabdoternin D is an Ent-Kaurane diterpenoid found in Rabdosia rubescens. Rabdoternin D shows no significant cytotoxicity to Hep G2, COLO 205, MCF-7 and HL-60 cancer cells with IC50 values >100 μM .
|
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
Cancer
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
-
- HY-160811
-
|
|
VEGFR
|
Cancer
|
|
hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC50s of 61, 142, and 114 μM .
|
-
- HY-N11438
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
3'-Hydroxymirificin (compound 3) is a naural compound that can be isolated from Pueraria lobata roots. 3'-Hydroxymirificin (compound 3) possesses estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
|
-
- HY-B1029
-
Danazol
4 Publications Verification
|
PKC
Apoptosis
Tyrosinase
|
Endocrinology
Cancer
|
|
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
|
-
- HY-168128
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin polymerization-IN-69 (compund 6c) significantly inhibits microtubule/tubulin polymerization in vitro (78.3% inhibition) with an IC50 value of 6.53 μM, and rapidly induces apoptotic cell death and G2/M cell cycle arrest in MCF-7 cells .
|
-
- HY-N3261
-
|
|
AP-1
ERK
STAT
|
Inflammation/Immunology
Cancer
|
|
Methyllinderone is an inhibitor of AP-1/STAT/ERK. Methyllinderone has anti-inflammatory effect. Methyllinderone reduce the invasion and migration rate of TPA-stimulated MCF-7 cells. Methyllinderone can be used in study breast cancer metastasis .
|
-
- HY-164923
-
|
Hemiasterlin methyl ester
|
Microtubule/Tubulin
|
Cancer
|
|
SPA107 (Hemiasterlin methyl ester) is a Hemiasterlin (HY-117371) analog. SPA107 inhibits the polymerization of tubulin, exhibits antimitotic activity (IC50 of 0.5 nM) and cytotoxicity in p53 mutated MCF-7 cell with IC50 of 0.5 nM .
|
-
- HY-13734
-
|
IV-2
|
Apoptosis
|
Cancer
|
|
PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
|
-
- HY-N11919
-
|
|
Others
|
Cancer
|
|
Anticancer agent 149 (compound 3) is an anticancer agent isolated from the rhizome of Dioscorea dioscorea (DM). Anticancer agent 149 exhibits selective cytotoxic activity against MCF-7 cells (IC50=31.41 μM) .
|
-
- HY-N4227
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Conicasterol is a 4-mercaptosteroid with significant cytotoxic activity. Conicasterol showed an IC50 value of 6.23 μg/mL in a test on a human breast adenocarcinoma cell line (MCF-7). Conicasterol's antitumor activity makes it a potential bioactive lead molecule .
|
-
- HY-181235
-
|
|
COX
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
COX-2/Aromatase-IN-1 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-1 can simultaneously inhibit COX-2 and aromatase, significantly suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-1 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-1 can be used for the study of inflammation and breast cancer .
|
-
- HY-N1366
-
|
Methylumbelliferone
|
Apoptosis
Bacterial
|
Infection
Cancer
|
|
Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
|
-
- HY-118474
-
|
NSC 721648
|
Aryl Hydrocarbon Receptor
Cytochrome P450
|
Cancer
|
|
GW 610 (NSC 721648), an antitumor agent, is a potent AhR ligand with a Ki of 6.8 nM. GW 610 induces CYP1A1 expression in MCF-7 cells. GW 610 shows potent and selective anticancer activity against lung, colon, and breast cancer cell lines .
|
-
- HY-B1029R
-
-
- HY-141877
-
MS4322
1 Publications Verification
YS43-22
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-161769
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model. (Pink: ligand for target protein JQ-1 (HY-78695); Black: linker (HY-W004640); blue: ligand for E3 ligase HL389 (HY-161770))
|
-
- HY-N7302
-
|
|
Others
|
Cancer
|
|
Anthracophyllone is an aristolane sesquiterpene that can be isolated from the mushroom Anthracophyllum. Anthracophyllone has cytotoxicity against MCF-7, KB, NCI-H187, Vero cells (IC50: 32.97, 18.02, 15.17, 18.06 μM) .
|
-
- HY-153697
-
|
|
FAK
|
Cancer
|
|
FAK-IN-10 is an inhibitor of FAK with an IC50 of 76.3 μM. FAK-IN-10 exhibits antitumor activity against MCF-7 and A431 cell lines with IC50s of 4.23 and 0.78 μM,respectively .
|
-
- HY-163947
-
|
|
VD/VDR
|
Cancer
|
|
UG-480 is a gemini analog that effectively stabilizes the active VDR conformation. UG-480 has antiproliferative effects in estrogen receptor-positive MCF-7 breast adenocarcinoma cells. UG-480 can be used in cancer research .
|
-
- HY-N5052
-
|
|
Others
|
Cancer
|
|
Asiaticoside B is a 9,19-cycloartane triterpene glycoside found in Actaea asiatica. Asiaticoside B has cytotoxicity against HepG2 and MCF-7 cancer cells with IC50 values of 9.74 µM and 8.32 µM, respectively .
|
-
- HY-144733
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells .
|
-
- HY-178143
-
|
|
KLF
|
Cancer
|
|
Sp1-IN-1 is a selective specificity protein 1 (Sp1) inhibitor. Sp1-IN-1 inhibits the proliferation of Hela cells and MCF-7 cells. Sp1-IN-1 can be used to the studies of cervical cancer and breast cancer .
|
-
- HY-N10351
-
|
|
Apoptosis
|
Cancer
|
|
27-O-(tert-Butyldimethylsilyl)withaferin A (compound 9a), a natural withanolide, is an apoptosis inducer. 27-O-(tert-Butyldimethylsilyl)withaferin A shows antiproliferative activity against HeLa, A-549 and MCF-7 human cancer cell lines, and against normal Vero cells .
|
-
- HY-W038396
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Ferrotrace (Compound dppt) is a ligand. Ferrotrace can bind to DNA and BSA (Kb = 0.14 x 10 4 M -1). Ferrotrace shows an IC50 of 17.35 μM for MCF-7 cells. Ferrotrace can be used for the research of breast cancer .
|
-
- HY-121149
-
|
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-N1252
-
|
|
Others
|
Cancer
|
|
Scillascillin (compound 10) is a homoisoflavanone. Scillascillin can be isolated from S. scilloides. Scillascillin shows anticancer activity towards MCF-7 (breast cancer) and DU-145 (prostate cancer) cells with the IC50 of 9.59 and 11.32 ug/ml, respectively .
|
-
- HY-13847
-
|
|
mTOR
|
Cancer
|
|
GNE-555 is a selective, metabolically stable mTOR inhibitor (Ki=1.5 nM) that also has good oral bioavailability. GNE-555 exhibits antiproliferative activity on PC3 and MCF-7 cells and can be used in cancer research .
|
-
- HY-N10871
-
|
|
SARS-CoV
|
Cancer
|
|
Neocryptomerin, a biflavonoid, shows inhibitory activity against U251, MCF-7, HeLa cell. Neocryptomerin has favorable binding affinities in the active pocket of SARS-CoV-2. Neocryptomerin is the leading compound of rational compounds against COVID-19 .
|
-
- HY-144337
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
DNA crosslinker 4 (dihydrochloride) is a potent DNA minor groove binder. DNA crosslinker 4 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 4 (dihydrochloride) can be used for researching anticancer .
|
-
- HY-135309
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-4 is a von Hippel-Lindau-based PROATC estrogen receptor (ER) degrader, binding to ER with an IC50 of 0.8 nM. PROTAC ER Degrader-4 induces ER degradation in MCF-7 cells with an IC50 of 0.3 nM .
|
-
- HY-18351A
-
|
LMP-400 hydrochloride; NSC-724998 hydrochloride
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan hydrochloride, an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan hydrochloride prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-155969
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-83 (Compound 9) is an EGFR inhibitor (IC50: 2.53 nM). EGFR-IN-83 has antiproliferative activity against MCF-7 and MDA-MB-231 cells, with IC50 of 2.50 μM and 1.96 μM. EGFR-IN-83 can induce cell apoptosis .
|
-
- HY-151624
-
|
|
PARP
Apoptosis
|
Cancer
|
|
PARP-2-IN-2 (compound 27) is a PARP 2 inhibitor with an IC50 value of 0.057 μM. PARP-2-IN-2 induces cell cycle arrest and apoptosis of MCF-7 breast cancer cells. PARP-2-IN-2 can be used for the research of cancer .
|
-
- HY-N2298
-
|
|
Apoptosis
|
Cancer
|
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population .
|
-
- HY-114310
-
|
|
VD/VDR
Apoptosis
|
Cancer
|
|
VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2 .
|
-
- HY-N14893
-
|
|
Others
|
Cancer
|
|
Cetoniacytone B can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 4.4 μM .
|
-
- HY-172932
-
|
|
YAP
|
Cancer
|
|
TEAD-IN-20 is a TEAD inhibitor. The IC50 values of TEAD-IN-20 in TEAD4 FRET and TEAD4 MCF7-Tead cell lines are 0.021 and 0.044 μM, respectively. TEAD-IN-20 can be used in cancer research .
|
-
- HY-126803
-
|
|
Antibiotic
|
Infection
Cancer
|
|
Saquayamycin B (compound 3) is a new angucycline antibiotic. Saquayamycin B has antitumor activities against a human lung (H-460) and a human breast cancer cell line (MCF-7) with GI50 values of 12.2 and 15.2 µM respectively .
|
-
- HY-170580
-
|
|
Topoisomerase
|
Cancer
|
|
Topo I/II-IN-1 (compound 7t) is a potent Topo I and Topo II dual inhibitor. Topo I/II-IN-1 exhibits significant cytotoxicity against MCF-7 breast cancer cell line with an IC50 of 7.45 μM .
|
-
- HY-161146
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-100 (compound 3f) is a EGFR inhibitor with IC50 range of 0.137-0.507 μM. EGFR-IN-100 has antiproliferative activity and induces the apoptosis pathway. EGFR-IN-100 arrests the MCF-7 cell cycle at the S phase .
|
-
- HY-144314
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PSDalpha is an ERα degrader conjugating photosensitizer (PS), triphenylamine benzothiadiazole (TB) and 17β-estradiol via an acetylene bond. PSDalpha shows excellent anti-proliferation performance on MCF-7 cells. The maximum absorption wavelength of PSDalpha in the visible region is located at 465 nm .
|
-
- HY-152774
-
|
|
Akt
PI3K
|
Cancer
|
|
Antitumor agent-86 (compound 5a) inhibits MCF-7 breast cancer cells with an IC50 value of 2.62 µM. Antitumor agent-86 induces cell apoptosis and cell cycle arrest, and shows antineoplastic activity by targeting RAS/PI3K/Akt/JNK signaling cascades .
|
-
- HY-173182
-
|
|
Microtubule/Tubulin
P-glycoprotein
|
Cancer
|
|
Antitumor agent-200 (Compound 2g) is a microtubule synthesis inhibitor. By binding to the colchicine site of tubulin, it causes G2/M cell cycle arrest and generates reactive oxygen species (ROS). Antitumor agent-200 exhibits significant inhibitory activity against MCF7/ADR and KBV200 cell lines with overexpression of P-glycoprotein (P-gp), with drug resistance indices (DRI) of 0.83 and 0.58 respectively. In the MCF-7 xenograft model, Antitumor agent-200 (25 mg/kg, intraperitoneal injection) can achieve a tumor growth inhibition rate of 57.2%. Antitumor agent-200 can be used in the research of the anti-cancer field .
|
-
- HY-156378
-
|
|
Aurora Kinase
|
Cancer
|
|
Aurora A inhibitor 3 (Compound 5h) inhibits Aurora-A kinase with an IC50 value of 0.78 μM. Aurora A inhibitor 3 is cytotoxic, with GI50 values of 0.12 μM and 0.63 μM for MCF-7 and MDA-MB-231 cells, respectively .
|
-
- HY-161770
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-169253
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
ROS inducer 5 (compound 6e) can induce intracellular ROS accumulation and subsequent nuclear fragmentation. ROS inducer 5 can induce apoptosis in MCF-7 cells, with an IC50 value of 3.85 μM. ROS inducer 5 can be used in anticancer research .
|
-
- HY-W560574
-
|
|
Xanthine Oxidase
|
Cancer
|
|
Xanthine oxidase-IN-14 (Compound 3f) is an inhibitor for xanthine oxidase, with IC50 >100 μM. Xanthine oxidase-IN-14 inhibits proliferations of cancer cells MCF-7, NCI-H460 and SF-268, with IC50 greater than 150 μM .
|
-
- HY-N6885
-
|
|
Others
|
Cancer
|
|
Puerarin-4'-O-β-D-glucopyranoside (compound 8) is a isoflavone from Pueraria lobata root (PLR). Puerarin-4'-O-β-D-glucopyranoside has estrogenic activity and anti-proliferation of MCF-7 human breast carcinoma cells .
|
-
- HY-N3615
-
|
|
Others
|
Cancer
|
|
Confluentin can be isolated from Rhododendron dauricum. Confluentin shows weak cytotoxicity against human tumor cells (IC50: 15.05, 17.08, 18.48, and 23.01 μM for HL-60, SMMC-7712, A-549, and MCF-7) .
|
-
- HY-W106688
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Triisopropyl phosphate inhibits TFF1 and EGR3 gene expression, exhibits anti-estrogenic activity that inhibits Estradiol (HY-B0141)-induced MCF-7 cell proliferation with an EC50 of 341 μM. Triisopropyl phosphate inhibits the estrogen response element (ERE)-stimulated luciferase activity in MVLN cells with an EC50 of 900 μM .
|
-
- HY-181459
-
|
|
PARP
DNA/RNA Synthesis
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
PARP1-IN-55 is a potent and selective PARP1 inhibitor with an IC50 value of 0.019 μM. PARP1-IN-55 exhibits anti-proliferative selective activity against MCF-7 breast cancer cells (IC50 = 3.6 μM). PARP1-IN-55 inhibits the PARP1-mediated DNA damage repair pathway, induces ROS accumulation, disrupts mitochondrial membrane potential, induced apoptosis and suppresses cancer cell migration, invasion, and colony formation. PARP1-IN-55 can be used for the study of breast cancer .
|
-
- HY-173060
-
|
|
ERK
Apoptosis
Autophagy
|
Cancer
|
|
ERK1/2 inhibitor 13 (Compound 21y) is the orally active inhibitor for ERK that inhibits ERK1 and ERK2 with IC50 of 91.71 nM and 97.87 nM. ERK1/2 inhibitor 13 inhibits the proliferation of MCF-7, 4T1, MDA-MB-468, and HCC1970 (IC50 of 0.67, 2.76, 2.15 and 1.68 μM), inhibits the cancer cell migration, induces apoptosis and autophagy in MCF-7. ERK1/2 inhibitor 13 exhibits antitumor and anti-metastatic effect in 4T1 xenograft mouse model .
|
-
- HY-172767
-
|
|
PROTACs
STAT
Apoptosis
|
Cancer
|
|
STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting Signal Transducer and Activator of Transcription 3 (STAT3). STAT3-D11-PROTAC-VHL exhibits anti-tumor activity with IC50 values of 1335 nM and 1973 nM against HeLa and MCF-7 cells, respectively. STAT3-D11-PROTAC-VHL binds to the DNA-binding domain of STAT3 and recruits the E3 ligase VHL to form a ternary complex, leading to the ubiquitination of STAT3 and subsequent degradation by the proteasome. STAT3-D11-PROTAC-VHL also inhibits tumor cell growth, induces cell cycle arrest and apoptosis, and suppresses tumor immune evasion .
|
-
- HY-155239
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-35 (compound 7) is a potent VEGFR-2 inhibitor with IC50=37 nM. VEGFR-2-IN-35 inhibits MCF-7 and HCT 116 cancer cells with IC50 values of 10.56 and 7.07 μM, respectively .
|
-
- HY-157402
-
|
|
Topoisomerase
EGFR
|
Cancer
|
|
Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer .
|
-
- HY-18351
-
|
LMP-400; NSC-724998
|
Topoisomerase
|
Infection
Cancer
|
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis .
|
-
- HY-N16645
-
|
|
Cholinesterase (ChE)
|
Cancer
|
|
Plasiaticine B (Compound 2) is an indole alkaloid found in Plantago asiatica. Plasiaticine B shows no significant cytotoxicity to HL-60, A-549 and MCF-7 cells with IC50 >40 μM. Plasiaticine B shows no significant inhibitory effect on AChE, with an inhibition rate <60% .
|
-
- HY-N11651
-
|
|
Others
|
Others
|
|
Peganumine A is a natural product that can be found in Peganum harmala. Peganumine A shows cytotoxicity with IC50s of5.8, 38.5, 40.2, 55.4 µM for HL-60, MCF-7, PC-3, and HepG2 cells ,respectively .
|
-
- HY-N12299
-
|
Quercetin 3-O-β-D-glucuronide butyl ester
|
Others
|
Cancer
|
|
Parthenosin (Quercetin 3-O-β-D-glucuronide butyl ester) is a flavonoid, that can be isolated from the aerial parts of Calligoum polygonoides. Parthenosin shows cytotoxic activity against HepG2 and MCF-7 cell lines with IC50 values of 60.46 and 61.4 μg/mL, respectively .
|
-
- HY-N14378
-
|
|
Bacterial
|
Infection
|
|
Parimycin has activity against Gram-positive bacteria, negative bacteria and tumors, and no effect on fungal. Parimycin can inhibit tumor cells including GXF 251L, H640, LXFA 629L, MCF-7, MEXF 514L with IC70s of 0.9-6.7 μg/mL .
|
-
- HY-147788
-
|
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
hDHODH-IN-9 (Compound 3k) is a potent inhibitor of hDHODH with an IC50 of 0.34 μM. hDHODH-IN-9 demonstrates high cytotoxic activity against MCF-7 and A375 cells and good selectivity. hDHODH-IN-9 has the potential for the research of cancer diseases .
|
-
- HY-W317408
-
|
|
Biochemical Assay Reagents
|
Others
|
|
(+)-Menthyl acetate is a compound isolated from natural Cunila angustifolia Benth essential oil. The selectivity of (+)-Menthyl acetate is higher than that of MCF-7 cell line, IC50=34.0 μg?mL -1, and lower than that of SK-Mel-28 cell line, IC50=279.9 μg?mL -1, on A549 cell without fatal .
|
-
- HY-162227
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antitumor agent-138 (compound 5b) is an inhibitor against tubulin polymerization at tubulin colchicine-binding sites, with IC50 of 1.87 μM. Antitumor agent-138 arrests the cell cycle at G2/M phase and induces an apoptosis in MCF-7 cells. Antitumor agent-138 inhibits cells migration and angiogenesis .
|
-
- HY-N14255
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Memnobotrin A is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin A has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
|
-
- HY-176834
-
|
|
GLUT
|
Cancer
|
|
3-Deoxy-3-fluoro-D-fructose (Compound 12) is a derivative of 2,5-Anhydro-D-mannitol. 3-Deoxy-3-fluoro-D-fructose is a selective probe of Hexose transporter 5 (GLUT5). 3-Deoxy-3-fluoro-D-fructose inhibits the transport of D-fructose labeled with 14C by GLUT5 with IC50s of 1.16 and 2.37 µM in EMT-6 and MCF-7 cells. 3-Deoxy-3-fluoro-D-fructose can be used for positron emission tomography (PET) imaging of cancers .
|
-
- HY-168608
-
|
|
TRP Channel
Apoptosis
PI3K
Akt
|
Cancer
|
|
TRPM7-IN-1 (compound SUD), a benzoylurea derivative, is an effective TRPM7 inhibitor. TRPM7-IN-1 induces cell cycle arrest and apoptosis, decreases the migration of MCF-7 and BGC-823 cells. TRPM7-IN-1 decreases vimentin expression and increases E-cadherin expression. TRPM7-IN-1 potentially reduces the TRPM7-like current and decreases TRPM7 expression through the PI3K/Akt signaling pathway. TRPM7-IN-1 is a potential agent to suppress the metastasis of breast and gastric cancer by inhibiting TRPM7 expression and function .
|
-
- HY-155441
-
|
|
CDK
|
Cancer
|
CDK2-IN-20 (compound 3b) is an inhibitor of CDK2. CDK2-IN-20 has cytotoxicity on tumor cells presenting an IC50 range of 5.52-17.09 µM. CDK2-IN-20 arrests the MCF-7 cell cycle at the S phase and induces apoptosis .
|
-
- HY-173151
-
|
|
Reactive Oxygen Species (ROS)
|
Cancer
|
|
BRCA2-IN-1 (Compound 3j) is a potential BRCA2 inhibitor that exhibits antiproliferative activity against the breast cancer MCF-7 cell lines. BRCA2-IN-1 also demonstrates DPPH radical scavenging ability, with an IC50 of 12.36 µM .
|
-
- HY-115994
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 10 is a potent hCA IX inhibitor with a Ki value of 6.2 nM. Carbonic anhydrase inhibitor 10 exhibits anti-proliferative activity against MCF-7 cancer cell line with an IC50 of 11.9 μM. Carbonic anhydrase inhibitor 10 can be used for cancer research .
|
-
- HY-N11928
-
|
|
Others
|
Cancer
|
|
Changnanic acid (schisandrin) is a triterpene compound with potential anti-tumor effects. Changnanic acid exhibits moderate cytotoxic activity against human tumor cell lines Bel-7402, MCF-7 and HL-60, with IC50s of 100 μM, 100 μM and 50.51 μM respectively .
|
-
- HY-168901
-
|
|
Src
|
Cancer
|
|
Hck-IN-2 (Compound 8e) is an HCK inhibitor. Hck-IN-2 is cytotoxic to tumor cells, with IC50 values of 19.58 μM and 1.42 μM against MDA-MB231 and MCF-7, respectively. Hck-IN-2 has anti-tumor activity .
|
-
- HY-N10777
-
|
|
Others
|
Cancer
|
|
1-Ketoaethiopinone is an abietane-diterpenoid. 1-Ketoaethiopinone has an α, β-unsaturated carbonyl function. 1-Ketoaethiopinone shows cytotoxic activity against human cancer cell lines MOLT-4 (human lymphoblastic leukemia) and MCF-7 (human breast adenocarcinoma) .
|
-
- HY-13636
-
Fulvestrant
Maximum Cited Publications
133 Publications Verification
ICI 182780; ZD 9238; ZM 182780
|
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-157487
-
|
|
Drug Derivative
|
Cancer
|
|
Anticancer agent 185 (compound 9d) is a glycohybrid derivative of pyrazolopyrimidine [1,5-a]. Anticancer agent 185 has good anti-breast cancer activity. Anticancer agent 185 shows good cytotoxic activity against MCF-7 cells with IC50 value of 15.3 μM .
|
-
- HY-138098
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Sartorypyrone B is a 2β-acetoxyl analogue of chevalone C. Sartorypyrone B is yielded from the ethyl acetate extract of the culture of the marine sponge-associated fungus Neosartorya tsunodae (KUFC 9213). Sartorypyrone B exhibits strong growth inhibitory activity, having GI50s of 17.8, 20.5, and 25.0 μM, respectively, for MCF-7, NCI-H460, and A375-C5. Sartorypyrone B has the potential for the research of breast adenocarcinoma, non-small cell lung cancer, and melanoma diseases .
|
-
- HY-112811
-
|
|
PROTACs
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-2 (compound 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin (CDK ligand) binds ubiquitin E3 ligase Cereblon (CRBN) via a linker to form PROTAC .
|
-
- HY-N1833
-
|
|
Others
|
Cancer
|
|
3'-Geranyl-3-prenyl-2',4',5,7-tetrahydroxyflavone displays cytotoxicity of 1.32, 3.92 and 5.22 μm against the human cervical carcinoma HeLa, human breast carcinoma MCF-7, and human hepatocarcinoma Hep3B cells .
|
-
- HY-145379
-
|
|
Parasite
Endogenous Metabolite
|
Infection
|
|
Miaosporone A, an angucyclic quinone, exhibits antimalarial activity against Plasmodium falciparum K1 and antibacterial activity against Mycobacterium tuberculosis with respective IC50 values of 2.5 and 2.4 μM and displays cytotoxic activities against both cancerous (MCF-7 and NCI-H187) and nonmalignant (Vero) cells .
|
-
- HY-13762S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-117872
-
|
20-O-Acetylsartorypyrone D
|
Fungal
|
Infection
|
|
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
|
-
- HY-N10023
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
Physalin O is a physalin that can be isolated from Physalis angulata. Physalin O shows cytotoxicity to Hep G2 and MCF-7 cancer cells with IC50 values of 31.1 and 11.4 µM, respectively. Physalin O inhibits the production of nitric oxide (NO) and shows anti-inflammatory activities .
|
-
- HY-151519
-
|
|
Sirtuin
|
Cancer
|
|
SIRT2-IN-9 (compound 12) is a selective inhibitor of SRIT2 with an IC50 value of 1.3 μM. SIRT2-IN-9 inhibits proliferative activity of MCF-7 breast cancer cells. SIRT2-IN-9 can be used for the research of cancer .
|
-
- HY-N1107
-
|
NSC 119993; NSC 277290; Odorigeni
|
Others
|
Cancer
|
|
Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively .
|
-
- HY-167694
-
|
|
Quinone Reductase
|
Cancer
|
|
Antiproliferative agent-62 (compound 5) is a functionalized benzylidene-indolin-2-one with notable antiproliferative activity and NQO1 activity induciton funciton, particularly in inducing NQO1 expression in murine Hepa1c1c7 cells and demonstrating effectiveness against human cancer cell lines, including MCF-7 and HCT116.
|
-
- HY-160563
-
-
- HY-N14280
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Memnobotrin B is an antibiotic found in Memnoniella echinata (JS6308). Memnobotrin B has inhibitory effect on NCI-460, MCF7 and SF-268 cell lines .
|
-
- HY-175698
-
|
|
ACSL Family
Ferroptosis
Microtubule/Tubulin
COX
Glutathione Peroxidase
|
Cancer
|
|
Ferroptosis inducer-9 is a ferroptosis inducer and colchicine site tubulin polymerization inhibitor. Ferroptosis inducer-9 inhibits MCF-7 cell growth with an IC50 of 14 nM and inhibits [ 3H]colchicine binding. Ferroptosis inducer-9 reduces expression of GPX4 and FTH, increases COX2 and ACSL4, lowers GSH, NADP+, and NADPH levels, increases LPO, MDA, and Fe(II) levels, and decreases SOD concentrations. Ferroptosis inducer-9 demonstrates significant anti-tumor efficacy in HCT116 CRC xenograft model. Ferroptosis inducer-9 can be used for the study of triple negative breast cancer (TNBC) and colorectal cancer (CRC) .
|
-
- HY-182275
-
|
|
PROTACs
Histone Methyltransferase
|
Cancer
|
|
PROTAC PRMT1 degrader-1 (compound 4) is a PRMT1 PROTAC degrader, with a DC50 of 0.77 μM (MCF-7 cells). PROTAC PRMT1 degrader-1 recruits the CRBN E3 ubiquitin ligase to induce proteasome-dependent degradation of PRMT1; it also forms a ternary complex with PRMT1 and CRBN, promoting ubiquitination and subsequent proteasomal degradation of PRMT1. PROTAC PRMT1 degrader-1 reduces the level of asymmetric dimethylarginine in cancer cells, as well as the level of asymmetric dimethylation of arginine 3 on histone H4, while inhibiting the growth of various cancer cells. PROTAC PRMT1 degrader-1 can be used in the research of breast cancer and melanoma .
|
-
- HY-144335
-
|
|
DNA Alkylator/Crosslinker
|
Cancer
|
|
DNA crosslinker 2 (dihydrochloride) is a potent DNA minor groove binder with DNA binding affinity (ΔTm) of 1.2 °C. DNA crosslinker 2 (dihydrochloride) has certain inhibitory activity against cancer cells NCI-H460, A2780 and MCF-7. DNA crosslinker 2 (dihydrochloride) can be used for researching anticancer .
|
-
- HY-147921
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor, with an IC50 of 0.67 μM. PIM1-IN-7 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively .
|
-
- HY-147920
-
|
|
Pim
|
Cancer
|
|
PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor, with an IC50 of 0.60 μM. PIM1-IN-6 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 1.51 and 15.2 μM, respectively .
|
-
- HY-N10354
-
|
|
Apoptosis
|
Cancer
|
|
27-Methyl withaferin A (comppund 26) is an apoptosis inducer with anticancer effects. 27-Methyl withaferin A shows antiproliferative effects against HeLa, A-549 and MCF-7 human tumor cell lines with IC50 values of 3.2 μM, 4.2 μM and 1.4 μM, respectively .
|
-
- HY-161755
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Anticancer agent 232 (compound 12f) is a glycohybrid designed using 1-azidoglycosides derived from d-glucose, d-galactose, and d-mannose. The IC50 values of anticancer agent 232 against MCF-7 and MDA-MB231 cells are 1.05 μM and 18.03 μM, respectively .
|
-
- HY-W080443
-
|
|
Endogenous Metabolite
|
Others
Cancer
|
|
O-allylvanillin is O-allylchalcone derivative with anti-cancer effects . O-allylvanillin inhibits THP-1, HL60, Hep-G2, MCF-7 cells growth with IC50 values of 74.76 μM, 63.52 μM, 90.99 μM, and 90.11 μM, respectively .
|
-
- HY-152945
-
|
|
NF-κB
|
Cancer
|
|
Antiproliferative agent-22 (compound 2) is an anticancer agent. Antiproliferative agent-22 shoes anti-proliferative activities against MCF-7, MDA-MB-231 and MDA-MB-468 cells with IC50 values of 6.2 μM, 3.3 μM and 3.3 μM, respectively .
|
-
- HY-126618
-
|
|
Tyrosinase
|
Cancer
|
|
Aspochalasin I exhibits cytotoxicity against cancer cells NCIH460, MCF-7 and SF-268, with IC50s of 22.1, 33.4 and 19.9 μM. Aspochalasin I inhibits melanogenesis (IC50 of 22.4 μM) through inhibition of tyrosinase, and can thus be used as whitening agent .
|
-
- HY-P4523
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
FA-Ala-Arg is a dipeptide with furylacryloyl group. FA-Ala-Arg breaks down to produce arginine. While cell-surface Carboxypeptidase-D (CPD) also increases intracellular Arg, which is converted to nitric oxide (NO). FA-Ala-Arg enhances NO production in MCF-7 cells. FA-Ala-Arg also increases the cell survival of prolactin (PRL)-treated cells, PRL regulates CPD mRNA levels in cells .
|
-
- HY-169019
-
|
|
PI3K
Apoptosis
|
Cancer
|
XJTU-L453 is a PI3Kα inhibitor with an IC50 value of 0.4 nM. XJTU-L453 can inhibit the proliferation of breast cancer cell lines T47D and MCF7, with IC50 values of 0.2 μM and 0.5 μM, respectively. XJTU-L453 can inhibit the PI3K pathway, induce cell cycle arrest, and trigger cell apoptosis (apoptosis). XJTU-L453 also has antitumor activity in MCF7 xenograft mice .
|
-
- HY-N1366S
-
|
7-Methoxycoumarin-d3; Methyl umbelliferyl ether-d3
|
Isotope-Labeled Compounds
Apoptosis
Bacterial
|
Infection
Cancer
|
|
Herniarin-d3 is the deuterium labeled Herniarin (HY-N1366). Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
|
-
- HY-173361
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Anticancer agent 270 (Compound 8e) is an inhibitor that acts on tubulin. Its IC50 value against MCF-7 breast cancer cells is 1.02 μM. Through a dual mechanism of action, namely inducing Apoptosis and destabilizing microtubules, it exerts significant anti-proliferative activity against breast cancer cells. Anticancer agent 270 can be applied to research in the field of cancer .
|
-
- HY-172783
-
|
|
Cytochrome P450
Apoptosis
|
Cancer
|
|
Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. Aromatase-IN-5 effectively blocks estrogen production. Aromatase-IN-5 inhibits the proliferation of breast cancer cell lines like MCF-7, arrests the cell cycle at the G1 phase, and induces apoptosis. Aromatase-IN-5 is promising for research of breast cancer .
|
-
- HY-149995
-
|
|
Pim
|
Cancer
|
|
Pim-1 kinase inhibitor 5 (Compound 4c) is a Pim-1 kinase inhibitor (IC50: 0.61 μM). Pim-1 kinase inhibitor 5 shows cytotoxicity against cancer cells, with IC50s of 6.95-20.19 μM for HepG2, MCF-7, PC3, and HCT-116 cells .
|
-
- HY-179150
-
|
|
EGFR
Tyrosinase
|
Cancer
|
|
EGFR-TK-IN-6 (compound 10B) is an EGFR-TK inhibitor (IC50 = 0.65 μM). EGFR-TK-IN-6 has anti proliferative activity against MCF-7 cells (IC50 = 37.7 μM). EGFR-TK-IN-6 has low toxicity to normal cells. EGFR-TK-IN-6 can be used for cancer research .
|
-
- HY-161267
-
-
- HY-151564
-
|
|
Others
|
Cancer
|
|
Anticancer agent 85 (compound 6j) is an anticancer agent that shows good cytotoxicity against MCF7 cells. Anticancer agent 85 can be used in breast cancer and other cancer studies .
|
-
- HY-157138
-
|
|
MMP
|
Cancer
|
|
MMP-9-IN-8 (Compound 3) is an MMP-9 inhibitor with inhibitory activities of 42.16% and 58.28% at 10 μM and 50 μM concentrations, respectively. MMP-9-IN-8 has anti-cancer activity and can induce apoptosis in MCF-7 cells with an IC50 value of 23.42 μM .
|
-
- HY-130431
-
|
|
Parasite
|
Infection
|
|
Vinclozolin M2 is an active metabolite of vinclozolin. It is formed from vinclozolin by successive esterase activity and decarboxylation of vinclozolin in C. elegans and by decarboxylation in human liver microsomes. Vinclozolin M2 is an antagonist of the mineralocorticoid receptor (IC50=1,400 nM) and androgen receptor (IC50=0.17 nM) in reporter assays using MCF-7 cells.
|
-
- HY-Y0598
-
|
Benzylideneacetophenone
|
Fatty Acid Synthase (FASN)
Apoptosis
Fungal
|
Inflammation/Immunology
Cancer
|
|
trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity .
|
-
- HY-N13162
-
|
|
Others
|
Cancer
|
|
Hemsleyadin D is a triterpenoid compound derived from Hemsleya penxianensis with antitumor activity. Its IC50 values against K562, MGC-803, U118, HepG2, A549, and MCF-7 cells are 93.9, 47.1, 25.9, 56.1, 66.3, and 67.6 μM, respectively .
|
-
- HY-176955
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC50 values for ERα and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC50 of 1.53 nM. ER degrader 12 can be used for research on breast cancer .
|
-
- HY-150692
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor α antagonist 1 (compound 35) is a highly selective antagonist of estrogen receptor α, with IC50s of 0.02, 6.55 and 7.73 μM for estrogen receptor α, estrogen receptor β and MCF-7 cells, respectively. Estrogen receptor α antagonist 1 can be used for the research of cancer .
|
-
- HY-162002A
-
|
|
ATM/ATR
|
Cancer
|
|
(S)-WSD0628 (Compound 28) is the S-isomer of WSD0628 (HY-162002). (S)-WSD0628 is the inhibitor for ATM that inhibits the phosphorylation of ATM in MCF-7 cell with IC50 <100 nM. (S)-WSD0628 exhibits radiosensitizing activity. (S)-WSD0628 can cross blood-brain barrier .
|
-
- HY-146467
-
|
|
Drug Derivative
|
Cancer
|
|
Anticancer agent 62 (compound 4c) is a potent anticancer agent. Anticancer agent 62 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 0.019, 0.060 and 0.016 μM, respectively. Anticancer agent 62 shows effective tumor growth inhibition .
|
-
- HY-W587738
-
|
|
Apoptosis
|
Cancer
|
|
Viridiflorol is an active natural molecule with anti-cancer effect. Viridiflorol induces anti-neoplastic effects on breast (MCF-7, IC50 = 10 µM), lung (A549, IC50 = 30 µM), and brain (Daoy, IC50 = 0.1 µM) cancer cells through apoptosis. Viridiflorol can be used for breast, lung, and brain cancer research .
|
-
- HY-124403
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
D 15413 is an orally active antagonist for nonsteroidal estrogen. D 15413 inhibits growth of estrogen receptor positive MCF-7 cell with an inhibition rate of 70% at 10 -7 M. D 15413 exhibits antitumor efficacy against DMBA (HY-W011845) or MNU (HY-34758)-induced breast cancer .
|
-
- HY-N10949
-
|
|
Others
|
Cancer
|
|
Viscosalactone B is a withanolide found in Withania somnifera. Viscosalactone B shows potent inhibitory activities to NCI-H460, HCT-116, MCF-7 and SF-268 cancer cells with IC50 values of 0.32, 0.47, 0.4 and 0.45 μg/mL. Viscosalactone B can be used for the research of cancer .
|
-
- HY-153588
-
|
|
HSP
|
Cancer
|
|
HSP90-IN-22 (Compound 35) is an Hsp90 inhibitor with antiproliferative properties on cells with IC50 values of 3.65 μM for MCF7 breast cancer cells and 2.71 μM for SKBr3 breast cancer cells, respectively.
|
-
- HY-163632
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-112 (SPP10) is an EGFR kinase inhibitor which exhibits IC50s of 2.31 ± 0.3, 3.16 ± 0.8, and 4.2 ± 0.2 μM, against MCF-7, H69AR, and PC-3 cancer cells, respectively. EGFR-IN-112 also demonstrates selective cytotoxicity against cancer cells .
|
-
- HY-144774
-
|
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin .
|
-
- HY-N1366R
-
|
Methylumbelliferone (Standard)
|
Reference Standards
Apoptosis
Bacterial
|
Cancer
|
|
Herniarin (Standard) (Methylumbelliferone (Standard)) is the analytical standard of Herniarin (HY-N1366). This product is intended for research and analytical applications. Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer.
|
-
- HY-146454
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Antiproliferative agent-6 (compound 8a) is a potent antitumor agent. Antiproliferative agent-6 has antiproliferative activity against cancer cell lines HCT116, MCF-7, H460 and non-tumor aneuploid immortal keratinocyte HaCaT cells with GI50s of 0.5 μM, 2 μM, 0.7 μM and 3.5 μM, respectively .
|
-
- HY-N3210
-
|
|
Others
|
Cancer
|
|
Nb-Demethylechitamine is an alkaloid isolated from the methanol extract of Alstonia rostrata twigs. Nb-Demethylechitamine has in vitro cytotoxic activity against several human cancer cell lines, including human myeloid leukemia HL-60, liver cancer SMMC-7721, lung cancer A-549, breast cancer MCF-7, and colon cancer SW480 cells .
|
-
- HY-116904
-
|
|
Apoptosis
Akt
|
Cancer
|
|
Anticancer agent 253 (Compound 26) has anti-cancer activity against breast cancer cells, with IC50s of 6 μM (MCF-7), 10 μM (MDA-MB-231) and 6.4 μM (4T1 cells). Anticancer agent 253 arrests cell cycle and induces mitochondria-mediated apoptosis in cancer cells. Anticancer agent 253 inhibits Akt phosphorylation in human breast and prostate cancer .
|
-
- HY-162593
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 45 (compound 5) is an inhibitor of tubulin protein active sites. Tubulin inhibitor 45 against MCF7 and HePG2 cancer cells with IC50 values of 11 μM and 13 μM .
|
-
- HY-N13709
-
|
|
Others
|
Cancer
|
|
12β-Acetoxy-7β-hydroxy-3,11,15,23-tetraoxo-5a-lanosta-8,20-dien-26-oic acid, a lanostanoid triterpene that can be isolated from Ganoderma lingzhi, exhibits an IC50 of 80.8 μM in MCF-7 cells .
|
-
- HY-N2741
-
|
|
Bcl-2 Family
|
Cancer
|
|
Vitexin B-1 is an inhibitor of Bcl-2 and the agonist of Caspase. Vitexin B-1 has cytotoxic effect and induces apoptosis in MCF-7, ZR-75-1, MDA-MB-231, and COC1 cells with IC50s of 3.2, 2.1, 1.8 and 0.39 μM, respectively .
|
-
- HY-13734R
-
|
IV-2 (Standard)
|
Apoptosis
Reference Standards
|
Cancer
|
|
PX-12 (Standard) is the analytical standard of PX-12. This product is intended for research and analytical applications. PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
|
-
- HY-N15479
-
|
|
Bacterial
|
Infection
Cancer
|
|
Nanangenine F is a drimane sesquiterpenoid with weak antibacterial and anticancer activities. Nanangenine F inhibits Bacillus subtilis (ATCC 6633) with an IC50 of 78 µg/mL. Nanangenine F inhibits NS-1, DU-145, MCF-7 and human fibroblast NFF cells with IC50s of 49 µg/mL, 95 µg/mL, 49 µg/mL, and 84 µg/mL, respectively .
|
-
- HY-N15652
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Versimide (Compound 15) can be isolated from the insect pathogenic fungus Gibellula sp. BCC36964. Versimide exhibits cytotoxicity in cell lines including MCF-7, KB, NCI-H187, and Vero with IC50s of 3.59, 4.83, 1.89, and 3.49 μg/mL, respectively, demonstrating its anticancer activity .
|
-
- HY-146466
-
|
|
Others
|
Cancer
|
|
Anticancer agent 61 (compound 3v) is an orally active and potent anticancer agent. Anticancer agent 61 shows antiproliferative activity in HepG2, Bel-7402 and MCF-7 cancer cells, with IC50 values of 1.12, 1.97 and 1.08 μM, respectively. Anticancer agent 61 shows effective tumor growth inhibition .
|
-
- HY-111846
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
PROTAC ERα Degrader-2 (Compound 11) is a ERα PROTAC degrader. PROTAC ERα Degrader-2 significantly down-regulates the level of ERα in MCF-7 cells.(Pink: AR ligand (HY-43962), Blue: IAP Ligand (HY-177389), Black: Linker (HY-128833)) .
|
-
- HY-N12232
-
|
|
Parasite
Bacterial
|
Infection
Cancer
|
|
Carbazomycin D exhibits antituberculosis and antimalarial activities, that inhibits Plasmodium falciparum with an IC50 > 10 μg/mL, inhibits Mycobacterium tuberculosis with MIC of 25 μg/mL. Carbazomycin D exhibits cytotoxicity in cell MCF-7, KB, NCI-H187 and Vero, with IC50s of 21.3, 33.2, 12.9, and 34.3 μg/mL, respectively .
|
-
- HY-138210
-
|
|
Fungal
|
Infection
|
|
N,O-Diacetyltyramine is a compound with antibacterial activity and cytotoxicity that can be isolated from the actinomycete Pseudonocardia endophytica VUK-10. N,O-Diacetyltyramine has antibacterial activity against Gram-positive and Gram-negative bacteria and fungi. N,O-Diacetyltyramine is cytotoxic to MDA-MB-231, HeLa, MCF-7 and OAW-42 cells .
|
-
- HY-13636S
-
|
ICI 182780-d3; ZD 9238-d3; ZM 182780-d3
|
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
|
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-158090
-
|
|
Drug Derivative
|
Cancer
|
|
Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC50 of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier .
|
-
- HY-119358
-
|
|
Reactive Oxygen Species (ROS)
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis .
|
-
- HY-147174
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: 100 nM in MCF-7 cells). PROTAC_ERRα induces proteasomal degradation and has capable of specifically degrading ERRα protein by >80%. Blue: VHL ligand (HY-125845), Pink: ERRα ligand (HY-U00425), black: linker .
|
-
- HY-143301
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer .
|
-
- HY-W177546
-
|
|
Phosphodiesterase (PDE)
Apoptosis
Caspase
DNA/RNA Synthesis
|
Cancer
|
|
CD00509 is a tyrosyl-DNA phosphodiesterase (PDE) Tdp1 inhibitor with an IC50 of 0.71 μM. CD00509 increases DNA damage and promotes apoptosis of MCF-7 cells. CD00509 can sensitize breast cancer cells and wild-type murine embryonic fibroblasts (MEFs) to Camptothecin (CPT) (HY-16560). CD00509 can be used for the study of cancers such as breast cancer .
|
-
- HY-157419
-
|
7-(4-Ethylphenyl)-FL118
|
Apoptosis
|
Cancer
|
|
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
|
-
- HY-N14892
-
|
|
Bacterial
|
Infection
Cancer
|
|
Cetoniacytone A has weak activity against Gram-positive and negative bacteria. Cetoniacytone A can inhibit the growth of HEPG2 and MCF7 human tumor cell lines, with GI50 values of 3.2 μM .
|
-
- HY-147839
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 10 (compound 32a) is a potent topoisomerase II inhibitor with an IC50 value of 7.45 μM. Topoisomerase II inhibitor 10 causes cell cycle arrest at G2-M phase and induces apoptosis of HepG-2 cells. Topoisomerase II inhibitor 10 has excellent anti-proliferative activities against HepG-2, MCF-7, and HCT-116 cells .
|
-
- HY-174336
-
|
|
Survivin
Apoptosis
|
Cancer
|
|
Survivin-IN-1 (Compound II₃) is a potent Survivin (a member of the Inhibitor of Apoptosis Protein family) inhibitor with an IC50 value of 8.1 μM against human lung cancer A549 cells and 9.0 μM against breast cancer MCF-7 cells. Survivin-IN-1 reduces Survivin protein levels and induces tumor cell apoptosis. Survivin-IN-1 is promising for research of malignant tumors such as lung cancer and breast cancer .
|
-
- HY-149149
-
|
|
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Incadronic acid inhibits growth of Dictyostelium discoideum with an IC50 of 1.6 μM. Incadronic acid binds the farnesyl diphosphate synthase (FPPS) in Leishmania major with the Ki of 23 nM. Incadronic acid inhibits the bone resorption and reduces bone loss, that can be used in osteoporosis research. Incadronic acid inhibits the proliferation of cells RAW264.7, PC-3 and MCF-7 with IC50 of 48 to 228.6 µM .
|
-
- HY-113319R
-
|
|
Reference Standards
Drug Intermediate
|
Cancer
|
|
β-D-Fructose, (Standard) is the analytical standard of β-D-Fructose (HY-113319R). This product is intended for research and analytical applications. β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
-
- HY-155105
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-30 (compound 8c) is a potent, orally active, competitive inhibitor against α-glucosidase, with Ki of 40.0 µM and IC50 value of 49.0 µM. α-Glucosidase-IN-30 is non-cytotoxic against the cancer and normal cell lines MCF-7 and HDF, and can be used for Type 2 diabetes study .
|
-
- HY-N14056
-
|
|
Bacterial
|
Infection
Cancer
|
|
Chrolactomycin is found in the strain of Streptomyces sp. 569N-3. The IC50 of Chrolactomycin for ACHN, A431, McF-7 and T24 cells are 1.2 μM, 1.6 μM, 0.69 μM and 0.45 μM, respectively. Chrolactomycin has only anti-Gram-positive bacteria activity with the MIC of 5.2-10.4 μg/mL .
|
-
- HY-115950
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively .
|
-
- HY-13636R
-
|
ICI 182780(Standard); ZD 9238(Standard); ZM 182780 (Standard)
|
Reference Standards
Estrogen Receptor/ERR
Autophagy
Apoptosis
|
Cancer
|
|
Fulvestrant (Standard) is the analytical standard of Fulvestrant. This product is intended for research and analytical applications. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
- HY-144070
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO (HY-132247). ErSO-DFP displays antitumor activity against MCF-7 in mice. ErSO-DFP can cross the blood brain barrier .
|
-
- HY-145865
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative against-3 (comp 33) shows a prominent activity against Hela (IC50 = 0.21 µM), A549 (IC50 = 0.39 µM), and MCF-7 (IC50 = 0.33 µM), respectively. Antiproliferative against-3 (comp 33) also dose dependently induces apoptosis by arresting A549 cells at G1 phase .
|
-
- HY-163566
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 18, a potent inducer of apoptosis, shows significant cytotoxicity to the breast cancer cell line MCF-7 (IC50=0.559 μM). Apoptosis inducer 18 inhibits cell cycle progression and promotes apoptosis by binding to DNA and causing damage, and by binding to the active site of CDK-2, interfering with its kinase activity. Apoptosis inducer 18 can be used in anti-breast cancer research .
|
-
- HY-150108
-
|
|
mTOR
Apoptosis
Caspase
|
Cancer
|
|
RMC-4745 is a selective dual-site inhibitor of mTORC1, with a selectivity of 35 times for mTORC1 and mTORC2. RMC-4745 inhibits the proliferation of MCF-7 cells and upregulates Caspase-3/7 activity to induce cell apoptosis. RMC-4745 does not cause the upregulation of HER3 due to the inhibition of mTORC2. RMC-4745 can be used for the study of breast cancer .
|
-
- HY-146819
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Compound 9 is the most effective against tumor specific Ca ix/ca XII (ki=29.1 and 8.8 nm), so it is possible to evaluate its cytotoxicity and selectivity to HepG-2, HCT-116 and MCF-7 cancer cell lines in vitro, and its IC50 values to tumor cells are 1.78, 1.94 and 3.07, respectively μ M. It showed that it had obvious cytotoxicity.
|
-
- HY-173232
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-66 (Compound 6) is an orally active VEGFR-2 inhibitor with an IC50 value of 0.509 µM and an IC50 value of 7.48 μM for inhibiting the proliferation of MCF-7 cells. VEGFR-2-IN-66 exerts its anti-cancer activity by arresting the cell cycle, inducing apoptosis, and regulating gene expression, and can be used in the research of the breast cancer field .
|
-
- HY-155337
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
eIF4E-IN-6(compound 4b) is a GMP analogs synthesized to targeteIF4Eand restrain its binding to cap mRNA.eIF4E-IN-6shows cell cytotoxicity against Caco-2, HepG-2,and MCF-7 cells, withIC50values of 31, 27, and 21 μM, respectively .
|
-
- HY-119539
-
|
|
Phosphatase
|
Endocrinology
Cancer
|
|
Limocitrin is a natural product that can be isolated from the buds of P. acerifolia and P. orientalis. Limocitrin suppresses estradiol-dependent proliferation of MCF7 cells weakly but estradiol-induced AlkP (alkaline phosphatase) expression only marginally .
|
-
- HY-174870
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
Fluorescent Dye
|
Cancer
|
|
PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)) .
|
-
- HY-10815
-
|
|
Sigma Receptor
Apoptosis
|
Neurological Disease
Cancer
|
|
σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells .
|
-
- HY-N7340
-
|
|
Others
|
Cancer
|
|
Withaperuvin C is a withanolide that can be isolated from Physalis Minima. Withaperuvin C has moderate cytotoxicity against cancer cells such as HepG2, SK-LU-1, and MCF7 cells (IC50: 19.5, 14.65, 11.74 μg/mL) .
|
-
- HY-157960
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-42 (compound 8c) is a potent VEGFR-2 inhibitor. VEGFR-2-IN-42 shows anti-proliferative effect against MCF7 cells with the IC50 of 25 µM .
|
-
- HY-W016887
-
|
H-Gly-Pro-OH; Gly-Pro
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Cancer
|
|
Glycyl-L-proline (H-Gly-Pro-OH) is a dipeptide. Glycyl-L-proline can induce MCF-7 cells apoptosis. Glycyl-L-proline can enhance the inhibitory effect of the PRODH/POX knockout on collagen and DNA biosynthesis. Glycyl-L-proline can inhibit Gly-Sar and L-proline transport. Glycyl-L-proline can be used for the researches of cancer and metabolic disease, such as breast cancer .
|
-
- HY-162312
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-158371
-
|
|
HDAC
Casein Kinase
|
Cancer
|
|
HDAC/CK2-IN-1 (compound 38) is a HDAC1 (IC50 = 1.46 μM), HDAC6 (IC50 = 0.66 μM), and CK2 (IC50 = 3.67 μM) inhibitor. HDAC/CK2-IN-1 exhibits promising antproliferative activity against Jurkat, MCF-7, HCT-116, and HL-60 cell lines .
|
-
- HY-168720
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, showing anti-tumor activity. Apoptosis inducer 32 caused significant cellular morphological changes in MDA-MB-231 cells, including membrane bubbling, nuclear fragmentation, and apoptotic body formation. The IC50 of Apoptosis inducer 32 in MCF-7, MDA-MB-231, and HEK cells is 4.77, 6.56 and 337.8 μM respectively .
|
-
- HY-161868
-
|
|
PARP
HDAC
Apoptosis
|
Cancer
|
|
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC50 of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase .
|
-
- HY-170382
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
|
-
- HY-50936S
-
|
Ecteinascidin 743-d3; ET-743-d3
|
Isotope-Labeled Compounds
Reactive Oxygen Species (ROS)
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
|
-
- HY-168164
-
|
|
Histone Methyltransferase
|
Cancer
|
|
4-Methoxycinnamyl alcohol is an anticancer compound with cytotoxic activity against MCF-7, HeLa, and DU145 cancer cell lines with IC50 values of 14.24, 7.82, and 22.10 μg/mL, respectively. 4-Methoxycinnamyl alcohol showed the ability to induce cell necrosis, rather than apoptosis, after a 48-hour DNA fragmentation assay. 4-Methoxycinnamyl alcohol was isolated from Foeniculum vulgare .
|
-
- HY-169476
-
|
|
Drug Derivative
|
Cancer
|
|
Pyrrolidine linoleamide is a derivative of linoleic acid amide with anticancer activity. Pyrrolidine linoleamide exhibits antiproliferative activity against a range of cancer cell lines, with IC50 values of 12.0, 27.5, 7.7, 21.9, 36.6, 32.6, and 33.9 μg/mL against U251, MCF-7, NCI-ADR/RES, 786-0, NCI-H460, PC-3, and OVCAR-3 cell lines, respectively .
|
-
- HY-146452
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 57 (compound 14) potently inhibits MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC50s of 6.43 ~ 8.00 μM. Anticancer agent 57 induces cell cycle arrest and significantly promotes apoptosis. Anticancer agent 57 inhibits tumor growth in nude mice xenografted with MADMB-231 cells. Anticancer agent 57 can be used for researching triple negative breast cancer (TNBC) .
|
-
- HY-173075
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Cancer
|
|
Anticancer agent 267 (Compound 5q) is the activator for RIPK3 and MLKL. Anticancer agent 267 inhibits the proliferation in a variety of cancer cell lines (IC50 for MDA-MB-231, MDA-MB-486 and MCF-7 is 9.79, 10.77 and 5.94 μM, respectively), arrests cell cycle at subG1 phase, and induces necroptosis in cell MDA-MB-231. Anticancer agent 267 exhibits antitumor activity in mouse xenograft models .
|
-
- HY-N12208
-
|
|
Others
|
Cancer
|
|
Neohelmanthicin B is a phenylpropanoid that can be isolated from Thapsia garganica. Neohelmanthicin B exhibits cytotoxicity against EL4, S180 and MCF7 cell lines with IC50s of 10, 5 and12 μM, respectively .
|
-
- HY-N12209
-
|
|
Others
|
Cancer
|
|
Neohelmanthicin A (compound 3A) is a phenylpropanoid compound with antitumor activity. The IC50s of Neohelmanthicin A for inhibiting leukemia cell line EL4, breast cancer cell line S180 and breast cancer cell line MCF7 are 0.13 μM, 7 μM and 23 μM respectively .
|
-
- HY-175779
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
TDP1-IN-4 (Compound 33) is a Tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 0.90 μM. TDP1-IN-4 has a strong synergistic effect with Camptothecin (HY-16560) in SK-Mel-2 cells, but not in cancer cells (A549, HCT-116 and MCF-7 cells) and non-cancerous Ges-1 cells. TDP1-IN-4 can be used for cancer chemotherapy and radiotherapy research .
|
-
- HY-149132
-
|
DDA
|
LXR
|
Cancer
|
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
- HY-143232
-
|
|
Fungal
Bacterial
|
Infection
Cancer
|
|
Antibacterial agent 73 (compound 7a) is a potent antimicrobial agent. Antibacterial agent 73 exhibits very good antitubercular activity (MIC=0.65 µg/mL) against Mtb H37Rv. Antibacterial agent 73 shows good activity against fungal and bacterial. Antibacterial agent 73 also shows cytotoxicity in MCF-7 breast cancer cell lines, with IC50 of 8.20 μM .
|
-
- HY-155118
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-81 (Compound 10i) is an EGFR inhibitor. EGFR-IN-81 inhibits EGFR WT and L858R/T790M with IC50s 4.38 nM and 5.69 nM. EGFR-IN-81 has cytotoxic activity against MCF-7 and HCT116 cells with of 2.07 μM and 6.72 μM respectively .
|
-
- HY-170910
-
|
|
HSP
|
Cancer
|
|
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
|
-
- HY-157151
-
|
|
Histone Methyltransferase
|
Cancer
|
|
iPRMT1 is a potent and selective PRMT1 inhibitor for breast cancer research. iPRMT1 inhibits breast cancer cell growth in vitro and in vivo with EC50 values of 90, 70, and 9 nM in MCF7, T47D, and MDA-MB-231 cells, respectively .
|
-
- HY-156919
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 8 (compound 5) is a p53 activator. p53 Activator 8 has potent anti-proliferative activity against MCF7 breast cancer cell lines with an IC 50 value of 0.5 μM .
|
-
- HY-117102
-
|
|
Aryl Hydrocarbon Receptor
Checkpoint Kinase (Chk)
|
Cancer
|
|
ANI-7 is an activator of aryl hydrocarbon receptor (AhR) pathway. ANI-7 inhibits the growth of multiple cancer cells, and potently and selectively inhibits the growth of MCF-7 breast cancer cells with a GI50 of 0.56 μM. ANI-7 induces CYP1-metabolizing mono-oxygenases by activating AhR pathway, and also induces DNA damage, checkpoint Kinase 2 (Chk2) activation, S-phase cell cycle arrest, and cell death in sensitive breast cancer cell lines .
|
-
- HY-156470
-
|
|
Trk Receptor
Anaplastic lymphoma kinase (ALK)
c-Kit
EGFR
Pim
Casein Kinase
Checkpoint Kinase (Chk)
CDK
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect .
|
-
- HY-174414
-
|
|
EGFR
|
Cancer
|
EGFR/HER2-IN-18 is a stable EGFR/HER2 dual inhibitor with IC50 values of 0.09 (EGFR) and 0.08 μM (HER2) respectively. EGFR/HER2-IN-18 exhibits broad-spectrum anti-cancer activity. EGFR/HER2-IN-18 induces MCF-7 cells apoptosis and inhibits the cell cycle. EGFR/HER2-IN-18 can be used for the study of breast cancer .
|
-
- HY-177966
-
|
|
Drug Metabolite
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
ETM-305 is a degradation product of the anticancer agent ET-743 (HY-50936). ET-743 (Ecteinascidin 743; Trabectedin) is a tetrahydroisoquinoline alkaloid that binds to the minor groove of DNA, blocks the transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cell apoptosis, and increases ROS production in MCF-7 and MDA-MB-453 cells. Trabectedin is used in the research of soft tissue sarcoma and ovarian cancer .
|
-
- HY-162887
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-53 (Compound 15w) is a VEGFR-2 inhibitor with an IC50 of 4.34 μM. VEGFR-2-IN-53 induces apoptosis by inhibiting VEGFR-2 activity and preventing cell migration, thereby exhibiting anti-angiogenic effects. The IC50 value of VEGFR-2-IN-53 for inhibiting MCF-7 cell growth is 3.87 μM. VEGFR-2-IN-53 can be used in cancer research .
|
-
- HY-146228
-
|
|
HSP
Apoptosis
Topoisomerase
EGFR
VEGFR
|
Cancer
|
|
HSP90-IN-13 (compound 5k) is a highly potent HSP90 pan inhibitor with an IC50 value of 25.07 nM. HSP90-IN-13 has multi-target activity against EGFR, VEGFR-2 and Topoisomerase-2. HSP90-IN-13 causes cell cycle arrest at G2/M phase and induces apoptosis of MCF-7 cells through mitochondrial-mediated pathway .
|
-
- HY-N15577
-
|
|
Drug Derivative
|
Cancer
|
|
Antiproliferative agent-69 (Compound 1) is a prenylated kaempferol derivative found in the fresh bud’s fur of Platanus acerifolia. Antiproliferative agent-69 shows significant antiproliferative effects against human breast cancer cells (MCF-7) and human hepatocellular carcinoma cells (Hep-G2) with IC50 values of 38.2 μM and 39.5 μM, respectively. Antiproliferative agent-69 is promising for research of breast cancer and liver cancer .
|
-
- HY-N8508
-
|
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
Cancer
|
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-155061
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
|
Cancer
|
|
hCYP1B1-IN-1 (compound B18) is a hCYP1B1 inhibitor (IC50=3.6 nM)，as well as an antagonist of Aryl Hydrocarbon Receptor. hCYP1B1-IN-1 exhibtis suitable metabolic stability and good cell-permeability. hCYP1B1-IN-1 inhibits migration of MCF-7 cells .
|
-
- HY-155203
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
Ferroptosis
|
Cancer
|
|
Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC50s of 1.0-1.9 μM .
|
-
- HY-162751
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Anticancer agent 249 (Compound 89) is an inhibitor for Hsp90β with IC50 of 16.5 μM in PC3MM2 cell. Anticancer agent 249 inhibits proliferation of cancer cells MCF-7, T47D, MDA-MB-231, MDA-MB-468 and SKBr3 with IC50 of 1.8-5.3 μM. Anticancer agent 249 induces apoptosis in MDA-MB-231. Anticancer agent 249 exhibits antitumor efficacy in mice .
|
-
- HY-174131
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
PVTX-321 (Compound 16a) is an orally active estrogen receptor α (ERα) degrader. PVTX-321 can potently degrade ERα (DC50=0.15 nM in MCF-7 cells) and also has inhibitory activity against mutant ERα (IC50=59 nM). PVTX-321 is promising for research of ER+/HER2- breast cancer .
|
-
- HY-170483
-
|
|
HSV
HIV
|
Infection
Cancer
|
|
Antitumor agent-191 (Compound 7) exhibits antiviral activity against HSV-1 and HIV with EC50 of 0.03 μM and 0.81 μM. Antitumor agent-191 exhibits potential antitumor efficacy, that inhibits cancer cell HepG2, WI-38, Vero and MCF-7, with IC50s of 19.6, 39.3, 18.3 and 28 μM, respectively .
|
-
- HY-157516
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC50 of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC50 values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively .
|
-
- HY-171777
-
|
ErPC3; Erucylphosphohomocholine
|
PI3K
Akt
Ras
Raf
p38 MAPK
|
Cancer
|
|
Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC50: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia .
|
-
- HY-12520
-
|
|
Dopamine Receptor
|
Neurological Disease
Cancer
|
|
SKF 38393 is a selective dopamine D1 receptor agonist. SKF 38393 activates the cAMP signaling pathway and promotes dopamine release in the developing rat striatum. SKF 38393 inhibits MCF-7 breast cancer cell proliferation (IC50=0.1 μM). SKF 38393 is promising for research of neurodevelopmental disorders, dopamine-related diseases (e.g., Parkinson’s, dopamine deficiency), and cancers .
|
-
- HY-145864
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-12 (compound 6g), a 2-oxoquinoxalinyl-1,2,4-triazole, is a potent VEGFR-2 inhibitor with an IC50 of 0.037 µM. VEGFR-2-IN-12 shows high growth inhibition against MCF-7 cells (GI50=1.6 µM). VEGFR-2-IN-12 has antitumor activity .
|
-
- HY-13636S1
-
|
ICI 182780-d5; ZD 9238-d5; ZM 182780-d5
|
Isotope-Labeled Compounds
|
Others
|
|
Fulvestrant-d5 (ICI 182780-d5) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
|
-
- HY-W047131
-
|
|
Bacterial
|
Infection
Cancer
|
|
IPrAgCl is an antibacterial agent. IPrAgCl exhibits antiproliferative activity against MCF7 cell line with an IC50 of 30 nM. IPrAgCl has an IC50 of 35 nM against KB cancer cell line. IPrAgCl induces apoptosis in HL60 cell line. IPrAgCl promotes apoptosis-inducing factor translocation from the mitochondrial to the nuclear compartment .
|
-
- HY-172097
-
|
|
Drug Derivative
|
Cancer
|
|
HL22 is a harmaline derivative. HL22 significantly inhibits HCT116, MGC803 and MCF7 cancer cell lines, and inhibits MGC803 cell migration and monoclonal formation. The anti-cancer mechanism of HL22 is related to a variety of metabolic pathways and can be used in the study of cancer .
|
-
- HY-179045
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
ERα degrader 14 (Compound B7) is a potent ERα degrader. ERα degrader 14 exhibits significantly potent and selective anti-proliferative activity on two ERα-positive breast cancer cell lines (MCF-7 and T47D). ERα degrader 14 induces cell cycle arrest, inhibits cell migration, and induces cell apoptosis. ERα degrader 14 effectively inhibits tumor growth in mouse models. ERα degrader 14 can be used for the study of breast cancer .
|
-
- HY-147710
-
|
|
MicroRNA
|
Cancer
|
|
PIN1 inhibitor 2 (compound 12) is a potent PIN1 inhibitor. PIN1 inhibitor 2 shows antitumor activity with an IC50 of 9.55 µM for MCF7 cells. PIN1 inhibitor 2 has the potential for the research of breast cancer .
|
-
- HY-119358R
-
|
|
Reference Standards
Reactive Oxygen Species (ROS)
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Traumatic Acid (Standard) is the analytical standard of Traumatic Acid. This product is intended for research and analytical applications. Traumatic Acid is a wound healing agent and a cytokinin (phytohormone). Traumatic Acid enhances the biosynthesis of collagen in cultured human skin fibroblasts. Traumatic Acid inhibits MCF-7 breast cancer cells viability and enhances apoptosis and oxidative stress. Traumatic Acid can be used in studies of cancer, circulatory disorders (including arterial hypertension), and skin diseases associated with oxidative stress and impaired collagen biosynthesis[1][2].
|
-
- HY-N13115A
-
|
(E)-21-Angeloyl-protoaescigenin
|
Others
|
Cancer
|
|
Protoescigenin 21-tiglate (compound 10) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. However, the antitumor activity of Protoescigenin 21-tiglate is relatively weak, with IC50 values of >80 μM and 80 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-N13115
-
|
(Z)-Protoescigenin 21-tiglate
|
Others
|
Cancer
|
|
21-Angeloyl-protoaescigenin (compound 11) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. Protoescigenin 21-tiglate has antitumor activity, with IC50 values of 38.2 μM and 33 μM against MCF-7 and HeLa cells, respectively .
|
-
- 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 .
|
-
- HY-170999
-
|
|
Caspase
Apoptosis
Ferroptosis
|
Cancer
|
|
Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer activity, showing an IC50 of 90 nM against MCF-7 breast cancer cells.
Antitumor agent-196 promotes Apoptosis by regulating the Bax-caspase 3 signaling pathway, and induces Ferroptosis through the modulation of key signaling molecules, including GPX4.
Antitumor agent-196 holds promising potential for further research in the field of cancer therapy .
|
-
- HY-155242
-
|
|
VEGFR
Bcl-2 Family
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM) .
|
-
- HY-175465
-
|
|
Interleukin Related
STAT
|
Cancer
|
|
SMI-10B13 is an Oncostatin M (OSM) inhibitor with a KD of 6.6 μM. SMI-10B13 inhibits OSM-mediated STAT3 phosphorylation in T47D and MCF-7 cell lines (IC50 = 136 and 164 nM, respectively). SMI-10B13 shows anti-tumor effect in human breast cancer mice models .
|
-
- HY-161855
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-50 (Compound 10f) is a VEGFR-2 inhibitor and apoptosis inducer, with an IC50 value of 0.33 μM. VEGFR-2-IN-50 (Compound 10f) has growth inhibitory activity on MCF-7 and MDA-MB-231 breast cancer cell lines, with IC50 values of 19.86 μM and 10.88 μM, respectively, which is expected to be used in the study of breast cancer diseases .
|
-
- HY-179398
-
|
|
Keap1-Nrf2
|
Cancer
|
|
Keap1-Nrf2-IN-29 (Compound 1a), a Curcumin (HY-N0005) analog, is a Keap1 protein inhibitor. Keap1-Nrf2-IN-29 exhibits significant inhibitory activity against A549, PC-3 and MCF-7 cells. Keap1-Nrf2-IN-29 can be used for the study of prostate cancer .
|
-
- HY-164533
-
|
|
STAT
|
Cancer
|
|
STAT3-IN-33 (compound 7f) is a potent STAT3 inhibitor with anti-cancer activity. STAT3-IN-33 exhibits antiproliferative activity in HCT116, MCF-7, and MDA-MB-231 cells, with IC50s of 6.44, 3.29, and 4.86 μM, respectively. STAT3-IN-33 can be used for breast and colon cancer research .
|
-
- HY-157942
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP1B1-IN-7 (compound 2a) is a selective inhibitor of CYP1B1 (IC50: 75 nM). CYP1B1-IN-7 also reverses resistance (IC50: 29 μM) and exhibits cytotoxicity in the CYP1B1-overexpressing MCF-7 cell line that is resistant to Docetaxel (HY-B0011) .
|
-
- HY-179160
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-61 is a tubulin polymerization inhibitor with an IC50 of ≤7.63 μM. Tubulin-IN-61 induces early apoptosis and triggers significant G2/M phase arrest. Tubulin-IN-61 elevates intracellular ROS levels. Tubulin-IN-61 shows high activity against MCF-7 cells with an IC50 of 5.61 μM. Tubulin-IN-61 can be used for the research of breast cancer .
|
-
- HY-172748
-
|
|
Drug Derivative
|
Neurological Disease
Cancer
|
|
9β-Hydroxyhexahydrocannabinol is a synthetic cannabinoid derivative. 9β-Hydroxyhexahydrocannabinol exhibits cytotoxicity against various tumor cell lines, such as HCT-116, MCF-7, K562, MIAPaCa-2, PANC-1, A549, PC-3 and SW-620, with IC50 values ranging from 15.23 to 33.74 μM. 9β-Hydroxyhexahydrocannabinol can be used in the study of cancer .
|
-
- HY-172869
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Estrogen receptor antagonist 9 (Compound 5D) is an estrogen receptor antagonist. Estrogen receptor antagonist 9 shows significant cytotoxicity against MCF7 cells with an IC50 value of 8.50 μM. Estrogen receptor antagonist 9 is promising for research of breast cancers .
|
-
- HY-128600
-
ERD-308
1 Publications Verification
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-308 is a potent estrogen receptor (ER) PROTAC degrader. ERD-308 has DC50 values of 0.17 nM and 0.43 nM in MCF-7 and T47D ER+ cells. ERD-308 can inhibit the proliferation of breast cancer cells and exhibits anti-tumor activity. (Pink: Target Protein Ligand (HY-48027); Black: Linker (HY-172643); Blue: VHL Ligand (HY-112078); VHL Ligand+Linker：(HY-172645))
|
-
- HY-180537
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 57 is a apoptosis inducer and Thymidylate Synthase (TS) inhibitor. Apoptosis inducer 57 exhibits cytotoxic activity against SW480 and MCF-7 cancer cells with IC50 values of 15.7 and 16.5 µM, and induces dose-dependent apoptosis and S-phase cell cycle arrest. Apoptosis inducer 57 stalely binds the TS active site via interactions with Asp218 and Met311. TS-IN-9 can be used for breast cancer and colorectal cancer research .
|
-
- HY-171477
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Metahexestrol is an estrogen receptor (E2R) inhibitor with antitumor activity. It significantly inhibits the proliferation of estrogen receptor-positive MCF-7 human breast cancer cells (ED50 = 1.0 μM). Additionally, Metahexestrol also exhibits inhibitory effects in estrogen receptor-negative MDA-MB-231 cells, and its antiproliferative activity cannot be reversed by estrogen, suggesting that its mechanism of action may be partially independent of the E2R pathway. Metahexestrol can be used in research on estrogen-dependent breast cancer .
|
-
- HY-169408
-
|
|
Cytochrome P450
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-137 (Compound 4c) is an inhibitor for aromatase and EGFR with IC50s of 1.67 μg/mL and 0.08 μg/mL. EGFR-IN-137 inhibits the proliferation of cancer cell MCF-7 and MDA-MB-231 with IC50s of 1.62 µM and 4.14 µM. EGFR-IN-137 arrests the cell cycle at G0/G1 phase in MDA-MB-231, and induces apoptosis through caspase-dependent pathway .
|
-
- HY-178112
-
|
|
CDK
Apoptosis
|
Cancer
|
|
CDK2-IN-47 is a potent CDK2 inhibitor with an IC50 of 0.21 μM. CDK2-IN-47 exhibits outstanding anticancer activity against MCF-7, HCT-116, and MGC-803 cell lines. CDK2-IN-47 effectively induces G1 cell cycle arrest, retinoblastoma protein (Rb) dephosphorylation, and significant apoptosis. CDK2-IN-47 can be used for the studies of breast cancer, colorectal cancer and gastric cancer .
|
-
- HY-124053
-
|
|
HDAC
|
Cancer
|
|
BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC50s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively .
|
-
- HY-170955
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
HA-CD44 interaction inhibitor 3 (compound 5d) is a Hyaluronic acid (HY-B0633A) (HA)-CD44 interaction inhibitor with antiproliferative activities. HA-CD44 interaction inhibitor 3 inhibits MDA-MB-231 (CD44++) cells and MCF-7 cells (CD44--) with EC50s of 4.24 μM and 14.74 μM, respectively. HA-CD44 interaction inhibitor 3 shows the potential for cancer research .
|
-
- HY-163747
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-47 (compound 7g) is a potent VEGFR-2 inhibitor with an IC50 value of 0.072 µM. VEGFR-2-IN-47 can induce G2 / M phase cell cycle arrest, promote apoptosis, and boost immunomodulation by downregulating TNF-α expression and upregulating IL-2 levels in MCF-7 cells. VEGFR-2-IN-47 has the potential to be used for the research of cancer such as breast cancer and liver carcinoma .
|
-
- HY-120275
-
|
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer .
|
-
- HY-151154
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis .
|
-
- HY-179149
-
|
|
Polo-like Kinase (PLK)
Apoptosis
|
Cancer
|
|
PLK4-IN-6 (compound C05) is an PLK4 inhibitor (IC50 < 0.1 nM). PLK4-IN-6 has anti proliferative activity against various tumor cells, such as IMR-32 (IC50 = 0.948 μM), MCF-7 (IC50 = 0.979 μM), H460 (IC50 = 1.679 μM) cells. PLK4-IN-6 can significantly induce cell apoptosis and block the cell cycle. PLK4-IN-6 can be used for research on various types of cancer .
|
-
- HY-155965
-
|
|
VEGFR
PARP
Apoptosis
|
Cancer
|
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-163434
-
|
|
EGFR
Histone Methyltransferase
|
Cancer
|
|
PRMT5/EGFR-IN-1 (Compound 10p) is an orally active dual PRMT5/EGFR inhibitor, with IC50s of 15.47 and 19.31 μM, respectively. PRMT5/EGFR-IN-1 exhibits antiproliferative activity against A549, MCF7, HeLa, and MDA-MB-231 cell lines. PRMT5/EGFR-IN-1 has favorable in vivo PK and PD properties. PRMT5/EGFR-IN-1 can significantly inhibit the growth of MCF7 orthotopic xenograft tumors .
|
-
- HY-163615
-
|
|
Bacterial
|
Infection
|
|
Antimicrobial agent-32 (Compound 4g) is an antimicrobial agent that exhibits significant activity against various bacteria, including Staphylococcus aureus, Bacillus subtilis, Bacillus cereus (MIC=1000 µg/mL), Klebsiella pneumonia, and Staphylococcus aureus (MRSA) (MIC=500 µg/mL), as well as Escherichia coli (MIC=250 µg/mL). Additionally, Antimicrobial agent-32 inhibits the proliferation of MCF-7, HCT-116, and HepG-2 cells, demonstrating anticancer activity .
|
-
- HY-163616
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 221 (Compound 4h) is an orally active anticancer agent and an antioxidant agent. Anticancer agent 221 exhibits cytotoxicity to cancer cells A549 (IC50=22.09 µg/mL) and MCF-7 (IC50=6.40 µg/mL), and induces apoptosis. Anticancer agent 221 exhibits antioxidant efficacy with an IC50 of 42.46 μM in DPPH experiment. Anticancer agent 221 exhibits antitumor efficacy against breast cancer in mouse models .
|
-
- HY-114770
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
(E,E)-GLL398 is a selective estrogen receptor degrader with potent binding activity to ERα (IC50 = 1.14 nM). (E,E)-GLL398 can effectively degrade ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). The introduced boronic acid group of (E,E)-GLL398 gives it superior oral bioavailability, with an AUC of 36.9 μg·h/mL in rats, which is significantly higher than that of GW7604 .
|
-
- HY-151158
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-7 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2-IN-7 is a EGFR/HER2 kinase and DHFR inhibitor, with IC50s of 0.18 μM (EGFR), 0.146 μM (HER2), respectively. EGFR/HER2-IN-7 shows moderate inhibition on DHFR (IC50=0.907 μM) .
|
-
- HY-118761
-
|
5,6-epoxy atRA; 5,6-epoxy RA
|
RAR/RXR
|
Metabolic Disease
|
|
all-trans-5,6-epoxy Retinoic acid (5,6-epoxy RA) is an agonist of all isoforms of the retinoic acid receptor (RAR; EC50s=77, 35, and 4 nM for RARα, RARβ, and RARγ, respectively). 5,6-epoxy RA (1 μM) also induces growth arrest of MCF-7 and NB4 cells in vitro. It is a natural metabolite of all-trans retinoic acid, which is a metabolite of vitamin A.
|
-
- HY-146103
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antiproliferative agent-7 (compound 8f) is a potent anti-proliferative agent. Antiproliferative agent-7 has antiproliferative activity against cancer cell lines MCF-7, MDA-MB-231, HCT-116 and FR-2 with IC50s of 3.5 μM, 15.54 μM, 30.43 μM and 34.8 μM, respectively. Antiproliferative agent-7 can increase ROS production and induce apoptosis .
|
-
- HY-B0543R
-
|
Thiosinamine (Standard); N-Allylthiourea (Standard)
|
Reference Standards
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Allylthiourea (Standard) is the analytical standard of Allylthiourea. This product is intended for research and analytical applications. Allylthiourea can selectively inhibit the oxidation of ammonia. Allylthiourea is commonly used to inhibit nitrification by targeting ammonia monooxygenase and chelating copper in the active site to suppress its activity. Allylthiourea also exhibits anticancer activity, showing cytotoxicity against the MCF-7 cell line with an IC50 of 5.22 mM. Allylthiourea can be utilized in research related to micropollutant biodegradability and cancer studies [4].
|
-
- HY-Y0598R
-
|
|
Fatty Acid Synthase (FASN)
Reference Standards
Apoptosis
Fungal
|
Inflammation/Immunology
Cancer
|
|
trans-Chalcone (Standard) is the analytical standard of trans-Chalcone (HY-Y0598). This product is intended for research and analytical applications. trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity .
|
-
- HY-144749
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1C3-IN-5 (Compound 6e) is a potent inhibitor of AKR1C3. AKR1C3 enzyme is overexpressed in hormone-dependent prostate and breast tumors. AKR1C3-IN-5 derived from drupanin, which exhibits half-maximal inhibitory concentration (IC50) of 9.6 ± 3 μM and selectivity index (SI) of 5.5 against MCF-7 cells .
|
-
- HY-170508
-
|
|
Cytochrome P450
|
Endocrinology
|
|
Aromatase-IN-4 (Compound 6a) is an aromatase (Aromatase) inhibitor. Aromatase-IN-4 exhibits anticancer activity, with GI50 values of 2.95 μM, 3.35 μM, 2.27 μM, 8.46 nM, and 1.56 μM against the MDAMB-231, MCF-7, A-549, NCI-H23, and A-498 cell lines, respectively . Aromatase-IN-4 effectively blocks aromatase-dependent estrogen production .
|
-
- HY-156444
-
|
|
HDAC
CDK
Apoptosis
|
Cancer
|
|
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
|
-
- HY-175512
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer .
|
-
- HY-170551
-
|
|
Carbonic Anhydrase
VEGFR
|
Cancer
|
|
CA IX/VEGFR-2-IN-3 (Compound 6i) is an inhibitor of Carbonic Anhydrase IX and VEGFR-2, with IC50 values of 41 and 48 nM, respectively. CA IX/VEGFR-2-IN-3 exhibits anticancer activity, inhibiting the growth of MCF-7 breast cancer cells (with an IC50 of 22.33 μM) and mouse fibroblast cell line 3T3 (where cell viability is less than 40% at a concentration of 100 μM). CA IX/VEGFR-2-IN-3 can be used for research in the field of cancer treatment .
|
-
- HY-134997
-
|
4-oxo DHA
|
PPAR
|
Cancer
|
|
4-oxo Docosahexaenoic acid (4-oxo DHA) is a putative metabolite of Docosahexaenoic acid (HY-B2167) with antiproliferative and PPARγ agonist activity. It inhibits the growth of several triple negative breast cancer cell lines (MCF-10F, trMCF, bsMCF, MDA-MB-231, and BT549) at 50-100 μM, however it increased proliferation of MCF-7 cells. 4-oxo DHA binds covalently to PPARγ and activates gene transcription in luciferase reporter assays and in dendritic cells with EC50 values of approximately 8-16 μM.
|
-
- HY-168102
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC50 of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .
|
-
- HY-162670
-
|
|
CDK
|
Cancer
|
|
Anticancer agent 238 (compound 5) is an anticancer agent with a notably strong binding affinity towards the CDK-5 enzyme. Anticancer agent 238 shows a strong efficacy agains HCT116 and MCF7 cells, with IC50 values of 13.46 µM and 16.43 µM, respectively .
|
-
- HY-N15392
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Lactonamycin Z is an antitumor antibiotic. Lactonamycin Z has weak anti-Gram-positive bacterial activity. Lactonamycin Z can inhibit human tumor cells HMO2, MCF7 and Hep G2 with GI50 (μg/mL) of 1.9, 0.85 and 5.11, respectively .
|
-
- HY-186015
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Arg-TERRα is a mini-PROTAC targeting ERRα. Arg-TERRα induces ERRα degradation via the N-end rule pathway, thereby in inhibiting the proliferation and migration of MCF7 breast cancer cells. Arg-TERRα can be used for breast cancer research .
|
-
- HY-N13772
-
|
(+)-Dihydroisorhamnetin
|
Apoptosis
|
Cancer
|
|
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
|
-
- HY-149636
-
|
|
EGFR
CDK
VEGFR
Apoptosis
|
Cancer
|
|
Multi-target kinase inhibitor 2 is a multi-targeted kinase inhibitor, and exhibits activity against EGFR, Her2, VEGFR2, and CDK2 enzymes, with IC50 values of 79 nM, 40 nM,136 nM, and 204 nM, respectively. Multi-target kinase inhibitor 2 shows cytotoxic effects were observed against HepG2, HeLa , MDA-MB-231 and MCF-7, with IC50 of 41, 57, 51 and 59 μM. Multi-target kinase inhibitor 2 induces cell cycle arrest and apoptosis in HepG2 cells .
|
-
- HY-178161
-
|
|
HDAC
Apoptosis
|
Cancer
|
|
HDAC degrader-2 is a selective HDAC degrader with a DC50 values of 2.55 μM against HDAC1. HDAC degrader-2 effectively induces the degradation of HDAC1 and HDAC2, but has no significant effect on the degradation of HDAC3, 4, 6 and 8. HDAC degrader-2 exerts potent antiproliferative effects against MM.1S and MCF-7 cells. HDAC degrader-2 induces apoptosis in myeloma cells. HDAC degrader-2 can be used for the study of myeloma .
|
-
- HY-178350
-
|
|
CDK
HDAC
Apoptosis
Histamine Receptor
|
Cancer
|
|
MFDCH016 is a potent HDAC1/6 (IC50 = 38/59 nM) and CDK4/6 (IC50 = 680/720 nM) inhibitor. MFDCH016 induces apoptosis and cell cycle arrest in G2/M and G0/G1 phases in MCF-7 cells. MFDCH016 can modulate the HDAC-p21-CDK signaling pathway, increasing the levels of acetylated H3 and p21. MFDCH016 can be used for the study of breast cancer .
|
-
- HY-139434
-
|
|
Histone Demethylase
|
Cancer
|
|
JMJD6-IN-1 is a JMJD6 inhibitor, with an inhibition rate of 82% at 10 μM. JMJD6-IN-1 inhibits MCF-7 and HCC4006 cell proliferation with IC50 values of 19.2 μM and 25.2 μM. JMJD6-IN-1 inhibits JMJD6 demethylase activity. JMJD6-IN-1 can be used for the research of lung adenocarcinoma, prostate cancer, breast cancer, pancreatic cancer, colon cancer, oral squamous cell carcinoma, and glioblastoma .
|
-
- HY-W131302
-
|
N,N-Ethylenediglycine
|
Endogenous Metabolite
|
Cancer
|
|
Ethylenediaminediacetic acid (N,N-Ethylenediglycine) is an important ligand that enhances the antiproliferative activity of metal complexes. The complexes formed by ethylenediacetic acid and metal ions exhibited significant antiproliferative properties in MCF-7 cancer cell line. The metal complexes of ethylenediacetic acid were able to interact with DNA and were studied by CD and EPR spectroscopy techniques. Ethylenediaminediacetic acid and its metal complexes were able to induce cell cycle arrest at the G(0)/G(1) phase. The crystal structure analysis of ethylenediacetic acid provided important structural information for understanding its biological activity .
|
-
- HY-179062
-
|
|
Apoptosis
|
Cancer
|
Anticancer agent 280 (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 exhibits IC50 values of Anticancer agent 280 for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 can be used for the study of TNBC .
|
-
- HY-172889
-
|
|
PI3K
HDAC
Apoptosis
mTOR
Akt
|
Cancer
|
|
PI3K/HDAC-IN-4 (Compound 31f) is a PI3K/HDAC dual inhibitor (IC50: 0.2μM). PI3K/HDAC-IN-4 shows high selectivity for HDAC1-3 (IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively). PI3K/HDAC-IN-4 is a potent PIK3 inhibitor with IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. PI3K/HDAC-IN-4 significantly induces tumor cell apoptosis by simultaneously inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. PI3K/HDAC-IN-4 exhibits potent antiproliferative activity in a variety of tumor cell lines (e.g., MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively). PI3K/HDAC-IN-4 can be used in the study of lymphoma and leukemia .
|
-
- HY-147081
-
AS 1411
2 Publications Verification
AGRO-100
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
-
- HY-129152
-
|
|
Influenza Virus
|
Infection
|
|
Ganoderic acid T-N, a triterpenoid, is a H5N1 and H1N1 influenza neuraminidase (NA) inhibitor with IC50s of 2.7 μM and 42 μM, respectively. Ganoderic acid T-Q shows cytotoxicity against MCF7 cells (CC50=24.4 μM) .
|
-
- HY-151573
-
|
|
EGFR
CDK
|
Cancer
|
|
EGFR/CDK2-IN-1 (Compound 3b) is an EGFR/CDK2 inhibitor. EGFR/CDK2-IN-1 shows good cytotoxicity against MCF7 and HepG2 cells. EGFR/CDK2-IN-1 can be used in cancer research .
|
-
- HY-147202
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-24 (compound 3U) is a potent BRD4 inhibitor, BRD4 Inhibitor-24 shows antitumor activity against MCF7 and K652 cells, with IC50 values of 33.7 and 45.9 μM, respectively (extracted from patent CN107721975A) .
|
-
- HY-129672
-
|
25-Dihydrostichorrenoside E
|
Drug Derivative
|
Cancer
|
|
Thelenotoside B (25-Dihydrostichorrenoside E) shows strong cytotoxicities against five cancer cell lines as HepG2, KB, LNCaP, MCF7 and SK-Mel2 with the IC50 values from 0.95 ± 0.08 to 1.90 ± 0.13 μM. Thelenotoside B is a triterpene tetraglycoside .
|
-
- HY-178961
-
|
|
PROTACs
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-13 is an orally active PROTAC molecule that efficiently and selectively degrades ERα (DC50 = 3.78 nM). PROTAC ERα Degrader-13 has the characteristics of strong anti proliferation (IC50 = 0.6 nM), induction of apoptosis, and overcoming drug resistance in MCF-7 cells. PROTAC ERα Degrader-13 has good safety and no significant organ toxicity. PROTAC ERα Degrader-13 can be used for cancer research .
|
-
- HY-161776
-
|
|
P-glycoprotein
CDK
|
Cancer
|
|
P-gp/CDK2-IN-1 (Compound 4j) is an inhibitor for is inhibitor for P-glycoprotein (P-gp) and for cyclin-dependent kinase-2 (CDK2). P-gp/CDK2-IN-1 inhibits the proliferation of cancer cells SW-480 and MCF-7 wit IC50 of 38.6 μM and 26.6 μM. P-gp/CDK2-IN-1 exhibits antioxidant efficacy with EC50 of 580 μM in DPPH experiment .
|
-
- HY-169216
-
|
|
EGFR
VEGFR
CDK
|
Cancer
|
|
Multi-target kinase inhibitor 3 (compund 6i) is a multi-kinase target inhibitor with anticancer activity. Multi-target kinase inhibitor 3 inhibits EGFR, HER2, VEGFR-2, and CDK2 with IC50s of 0.063 μM, 0.054 μM, 0.119 μM, and 0.448 μM, respectively. Multi-target kinase inhibitor 3 has a good inhibitory effect on breast cancer cells MCF-7, with an IC50 of 6.10 μM .
|
-
- HY-155113
-
|
|
PROTACs
HSP
|
Cancer
|
|
PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
|
-
- HY-169058
-
|
|
Glutathione S-transferase
|
Cancer
|
|
GSTP1-1 inhibitor 2 (Compound 5g) is an hGSTP1-1 (glutathione S-transferase P1-1) inhibitor with an IC50 value of 12.2 μM. GSTP1-1 inhibitor 2 exhibits significant cytotoxicity against DU-145, PC3, and MCF-7 cell lines, with CC50 values of 36.6 μM, 11.9 μM, and 17.4 μM, respectively. It can be used in cancer research .
|
-
- HY-146169
-
|
|
Reactive Oxygen Species (ROS)
Microtubule/Tubulin
|
Cancer
|
|
Antitumor agent-68 is a potent tubulin inhibitor. Antitumor agent-68 shows potent anticancer activity with IC50s of 3.6 and 3.8 μM for HeLa and MCF-7 cells, respectively. Antitumor agent-68 exhibits good scavenging activity of ROS and DPPH radical in a dose-dependent manner . Antitumor agent-68 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-123656
-
|
|
Apoptosis
|
Cancer
|
|
Antiproliferative agent-61 is a synthetic β-carlinyl chalcone with significant antiproliferative activity. Antiproliferative agent-61 showed significant effects in a range of solid tumor cell lines, with the most prominent effects in breast cancer. Antiproliferative agent-61 showed IC50 values of 2.25 and 3.29 μM in the human breast cancer MCF-7 cell line. Antiproliferative agent-61 significantly induced DNA fragmentation and apoptosis in breast cancer cells. Antiproliferative agent-61 inhibited the interaction of MDM2 with p53 and promoted the degradation of MDM2 .
|
-
- HY-117649
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
RU-39411 is a steroidal anti-estrogen with mixed estrogenic/antiestrogen activity. RU-39411 has shown inhibitory effects on cell growth in the MCF-7 breast cancer model, with the effect being correlated with its binding affinity to the estrogen receptor. RU-39411 was able to downregulate the estrogen binding capacity of cells, but did not reduce estrogen receptor mRNA levels, indicating that the grafting of its side chain prevents the antagonistic effects usually associated with steroidal estrogens. The administration of RU-39411 can promote the synthesis of progesterone receptors, further supporting its activity as an estrogen .
|
-
- HY-155197
-
|
|
Microtubule/Tubulin
Estrogen Receptor/ERR
|
Cancer
|
|
ER degrader 7 (Compound 35t) is an ERα and ERβ degrader. ER degrader 7 inhibits tubulin polymerization. ER degrader 7 inhibits cell viability with IC50s of 0.06, 2.56, 15.84, 1.59, 1.67, 1.37 μM for MCF-7, T47D, MCF-10A, LCC2, T47D D538G, and T47D Y537S cells respectively. ER degrader 7 also inhibits breast cancer tumor growth .
|
-
- HY-170849
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Apoptosis
PERK
IRE1
|
Cancer
|
|
Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. Nur77 modulator 4 significantly induces Nur77 expression and apoptosis, showing excellent growth inhibition in HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, thereby inducing cell apoptosis. Nur77 modulator 4 can be used in cancer research applications .
|
-
- HY-178911
-
|
|
Thymidylate Synthase
Apoptosis
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
|
Cancer
|
|
TS-IN-8 is a potent thymidylate synthase (TS) inhibitor. TS-IN-8 can induce apoptosis and cause cell cycle arrest at the G2/M in MCF-7 cells. TS-IN-8 can induce nuclear morphological changes. TS-IN-8 can increase intracellular reactive oxygen species (ROS) levels. TS-IN-8 can activate intrinsic apoptosis pathways by regulating apoptosis-related proteins such as the bax/bcl-2 ratio and caspase activation. TS-IN-8 can be used for the study of breast cancer .
|
-
- HY-178496
-
|
|
Hsp-targeting Chimeras
PARP
HSP
|
Cancer
|
|
DDO3602 is a PARP1 HEMTAC degradation agent mediated by HSP90. DDO3602 has good anti-tumor activity and tumor selectivity. DDO3602 induces G2/M phase arrest, DNA damage, and inhibits cell migration by degrading PARP1 in MCF-7 cells (IC50 = 187 nM). DDO3602 can be used for research on cancer such as breast cancer. (Pink: PARP1 Ligand (HY-75706); Blue: HSP90 Ligand (HY-179203); Black: Linker (HY-W015300))
|
-
- HY-147081A
-
|
AGRO-100 sodium
|
Histone Methyltransferase
Bcl-2 Family
|
Cancer
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
|
-
- HY-148789
-
|
OP-1250
|
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
|
Palazestrant is an antiestrogen and antineoplastic agent. Palazestrant can completely inhibit the activity of 17b-estradiol (E2) with IC50 value of 6.4 nM, and inhibit the proliferation of MCF7 and CAMA-1 cells with IC50 value of 1.4-1.6 nM. Palazestrant can inhibit ER +/HER2 + cancer .
|
-
- HY-155382
-
|
|
Monocarboxylate Transporter
|
Others
Cancer
|
|
Lactate transportor 1 (compound 1) is an active lactate transporter in living cells. Lactate transportor 1 displays the cytotoxic effect, with IC50 values of 3.36, 3.27,5.58 and 7.66 μM in Hela, CAL27, MCF7 and MCF10A, respectively. Lactate transportor 1 has an additive effect with Cisplatin (HY-17394) observed in HeLa cells .
|
-
- HY-175269
-
|
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Topoisomerase
|
Cancer
|
|
MGB1Y is a noncovalent DNA minor groove binder (MGB). MGB1Y potently inhibits cancer cells proliferation and topoisomerase I activity. MGB1Y downregulates their breast cancer-related genes in MCF7 and MDA-MB-231 cells. MGB1Y has a broad-spectrum anticancer activity, such as breast cancer, colon cancer, and leukemia .
|
-
- HY-N8470
-
|
NSC 204855; U 40615
|
Bacterial
|
Infection
|
|
Steffimycin B is an anthracycline bacterial metabolite originally isolated from Streptomyces. It binds to DNA, preferentially intercalating at sites containing cytosine and guanine.2 Steffimycin B is cytotoxic to MCF-7, KB, NCI-H187, and Vero cells (IC50s=3.5, 6.75, 3.28, and 10.5 μM, respectively). It is active against M. tuberculosis (MIC=5.2 nM), B. cereus (MIC=1.56 μg/mL), and P. falciparum (IC50=2.19 μM).
|
-
- HY-161773
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
HL389-NHC2-PEG3-C2NH inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389-NHC2-PEG3-C2NH can be utilized as a conjugate of an E3 ligase ligand and a linker, for the synthesis of PROTAC degrader HL435 (HY-161769) .
|
-
- HY-170895
-
|
|
HSP
Na+/K+ ATPase
|
Cancer
|
|
Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
|
-
- HY-124456
-
|
|
Bacterial
|
Infection
|
|
Unguinol is a depsidone originally isolated from A. unguis. It is an inhibitor of pyruvate phosphate dikinase (PPDK; IC50=42.3 μM). It inhibits the growth of plants utilizing C4, but not C3, carbon fixation. Unguinol also inhibits the growth of the bacteria S. aureus and V. harveyi (GI50s=8.7 and 69.5 μM, respectively) and H460, MCF-7, and SF-268 cancer cells (GI50s=28.2, 50.8, and 44.3 μM, respectively).
|
-
- HY-124509
-
|
|
Bacterial
|
Infection
|
|
Pyrocoll is a bacterial metabolite originally isolated from Streptomyces. It inhibits the growth of A. aurescens, A. globiformis, A. oxydans, A. pascens, and R. erythropolis bacteria (MICs=10, 1, 10, 3, and 10 μg/mL, respectively) and HMO2, HepG2, and MCF-7 cancer cells (GI50s=0.28, 0.42, and 2.2 μg/mL, respectively) in vitro. Pyrocoll is also active against P. falciparum and T. rhodesiense (IC50s=1.19 and 1.97 μg/mL, respectively).
|
-
- HY-N12230
-
|
|
Bacterial
Parasite
Fungal
|
Infection
Cancer
|
|
Penicolinate B is a picolinic acid derivative that can be isolated from Penicillium sp. Penicolinate B exhibits antimalarial activity (IC50: 1.40 μg/mL), antitubercular activity (MIC: 25.0 μg/mL), activity against Bacillus cereus (IC50: 25.0 μg/mL), and activity against Candida albicans (IC50: 1.45 μg/mL). Penicolinate B also has certain cytotoxicity against cancer cells such as MCF-7, KB, and NCI-H187. Penicolinate B can be used in research on malaria, tuberculosis, bacterial/fungal infections and tumors .
|
-
- HY-168439
-
|
|
PROTACs
Aurora Kinase
|
Cancer
|
|
HLB-0532259 is a PROTAC degrader for Aurora-A and N-Myc. HLB-0532259 degrades Aurora-Ain a non-MYCN amplified MCF-7 with a DC50 of 20.2 nM, degrades N-Myc in MYCN amplified cells SK-N-BE and Kelly with DC50 of 179 nM and 229 nM. HLB-0532259 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-168440); Black: linker (HY-W007957); Blue: ligand for E3 ligase Cereblon (HY-41547))
|
-
- HY-175838
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp-IN-32 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-32 exhibits low cytotoxicity and potent multidrug resistance (MDR) reversal activity against Doxorubicin (HY-15142A) in MCF7/ADR cells (IC50 = 0.11 μM, reversal fold (RF) = 215.9). P-gp-IN-32 can bind to P-gp directly, induce a conformation change of P-gp and inhibit the efflux function. P-gp-IN-32 can be used for the research of cancer, such as breast cancer .
|
-
- HY-W348485
-
|
|
mTOR
|
Cancer
|
|
WRX606 is an orally active nonrapalog inhibitor for mTOR complex 1 (mTORC1M). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (S6K1) (IC50 = 10 nM) and eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50 = 0.27 μM) in MCF-7 cells. WRX606 suppresses tumor growth in mice without promotion of metastasis. WRX606 can be studied in research as an antitumor agent .
|
-
- HY-156912
-
|
|
EGFR
|
Cancer
|
|
Tyrosine kinase-IN-7 (compound 13h) is an inhibitor of the tyrosine kinase EGFR. The IC50s for inhibiting EGFR(WT) and EGFR(T790M) are 0.630 μM and 0.956 μM respectively. Tyrosine kinase-IN-7 has antitumor activity against four cancer cell lines (HepG2, HCT-116, MCF-7, and A431) with IC50s of 13.02 μM, 10.14 μM, 12.68 μM, and 47.05 μM, respectively .
|
-
- HY-178955
-
|
|
EGFR
HSP
PI3K
Caspase
Apoptosis
CDK
ERK
Akt
|
Cancer
|
|
EGFR-IN-182 (Compound 4) is an EGFR inhibitor with an IC50 value of 199 nM. EGFR-IN-182 inhibits HSP90 and PI3K, with IC50 values of 5.007 and 13.596 μM respectively. EGFR-IN-182 exhibits strong anti-proliferative activity against MCF-7 and MDA-MB-231 cells. EGFR-IN-182 downregulates Cyclin D1, inducing cell cycle arrest; it enhances the activity of caspase-9, inducing cell apoptosis. EGFR-IN-182 downregulates the expressions of ERK and AKT. EGFR-IN-182 can be used for research on breast cancer .
|
-
- HY-146080
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-61 (Compound 9b), Irinotecan (Ir) derivative, is a potential antitumor agent. Antitumor agent-61 displays potent activity with IC50s of 0.92, 1.39, 1.75, 2.20, 3.05 and 3.23 μM against five human cancer cells SK-OV-3, SK-OV-3/CDDP, U2OS, MCF-7, A549 and MG-63, respectively. Antitumor agent-61 induces SK-OV-3 cells apoptosis through mitochondrion pathways .
|
-
- HY-179070
-
|
|
Apoptosis
|
Cancer
|
Anticancer agent 280 TFA (Compound 65) is an anti-cancer agent targeting triple-negative breast cancer (TNBC). Anticancer agent 280 TFA exhibits IC50 values of Anticancer agent 280 TFA for MDA-MB-231, MDA-MB-231/LM2-4, Jurkat, and MCF-7 of 7.1, 11.65, 6.99, and 21.51 μM respectively. Anticancer agent 280 TFA can cause significant arrest of cells in the S phase and induce cell apoptosis. Anticancer agent 280 TFA can be used for the study of TNBC .
|
-
- HY-162805
-
|
|
NO Synthase
Topoisomerase
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
iNOS/TopoI-IN-1 (compound AuL9) is a multi-target hybrid molecule with anti-tumor, anti-inflammatory and antioxidant activities. iNOS/TopoI-IN-1 inhibits the growth of breast cancer cells MCF-7 and MDA MB-231 in vitro with IC50 of 3.5 μM and 6.3 μM, respectively, and induces DNA damage and apoptosis of breast cancer cells by inhibiting human topoisomerase I (TopoI) (Ki=2.72 μM). In addition, NOS/TopoI-IN-1 inhibits the expression of iNOS by inhibiting the activation of NF-kB (Ki=1.49 μM) .
|
-
- HY-181236
-
|
|
COX
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
COX-2/Aromatase-IN-2 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-2 can simultaneously inhibit COX-2 and aromatase, suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-2 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-2 can be used for the study of inflammation and breast cancer .
|
-
- HY-157161
-
|
|
11β-HSD
|
Cancer
|
|
11β-HSD2-IN-1 (compound CDSN) is a potent inhibitor of 11β-HSD2, inhibiting the metabolism of Cholestane-3β,5α,6β-triol (CT) in cells by 11β-HSD2 into the tumor promoter, carcinosterone. 11β-HSD2-IN-1 inhibits testosterone biosynthesis, thereby inhibiting MCF-7 cell proliferation. 11β-HSD2-IN-1 has immune activity and antiviral infection effects .
|
-
- HY-174800
-
|
|
Topoisomerase
|
Cancer
|
|
ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer .
|
-
- HY-156018
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC50: 2.5 nM). PI3Kα-IN-13 induces tumor cell apoptosis. PI3Kα-IN-13 inhibits cancer cell proliferation with IC50s of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), 9.85 μM (SW620), respectively. PI3Kα-IN-13 inhibits tumor cell colony formation, migration and invasion .
|
-
- HY-168714
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 12 (Compound 2k) is an inhibitor for microtubule polymerization with an IC50 of 22.23 μM. Microtubule inhibitor 12 arrests the cell cycle of B16-F10 at G2/M phase, induces apoptosis in B16-F10, and inhibits cell migration. Microtubule inhibitor 12 inhibits the proliferation of cancer cells B16-f10, A549, HepG2 and MCF-7, with IC50s of 0.098, 0.135, 0.109, and 0.259 μM, respectively. Microtubule inhibitor 12 exhibits antitumor efficacy in mouse model .
|
-
- HY-N10621
-
|
|
Others
|
Cancer
|
|
3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM .
|
-
- HY-149407
-
|
|
VEGFR
CDK
EGFR
Necroptosis
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-4 (compound 5d) is multi-targeted kinase inhibitor, including VEGFR2, EGFR, HER2, and CDK2, with IC50 values of 0.33, 0.22, 0.18 and 2.09 μM, respectively. Multi-kinase-IN-4 shows broad-spectrum anti-cancer activities against HepG2, MCF-7, MDA-231, and HeLa cell lines (IC50 = 1.94–7.1 µM), but exhibits lower toxicity in the WI-38 cells (IC50 = 40.85 µM). Multi-kinase-IN-4 induces apoptosis and arrests cell cycle at S phase in HepG2 cells. Multi-kinase-IN-4 has the potential for the research of cancer .
|
-
- HY-183618
-
|
|
PROTACs
Histone Demethylase
|
Cancer
|
|
DW-229 is a PROTAC degrader derived from Deferiprone (HY-B0568), targeting Fe(II)/α‑ketoglutarate‑dependent histone lysine demethylases (KDMs). DW-229 degrades KDM2A, KDM3A, KDM5B, KDM4A‑C, KDM5C, KDM6B in breast cancer cells. DW-229 shows IC50 < 0.5 μM against MCF‑7 cells and IC50 of 8.87 μM against MDA‑MB‑231 cells, with high cancer cell selectivity. DW-229 can be used for the research of breast cancer, liver cancer, prostate cancer, lung cancer .
|
-
- HY-130624
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549 .
|
-
- HY-N9174
-
|
|
Others
|
Cancer
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
- HY-179140
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR/VEGFR2-IN-8 (compound 10k) is a dual EGFR/VEGFR-2 inhibitor (EGFR IC50 = 57 nM, VEGFR-2 IC50 = 21 nM). EGFR/VEGFR2-IN-8 has anti proliferative activity against various tumor cells, such as MCF-7 (IC50 = 20 nM), Panc-1 (IC50 = 22 nM), A-549 (IC50 = 23 nM), HT-29 (IC50 = 23 nM) cells. EGFR/VEGFR2-IN-8 has antioxidant and apoptosis inducing activity. EGFR/VEGFR2-IN-8 can be used for research on various types of cancer .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-125620
-
|
|
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Rubiginone D2 is an antibiotic, which exhibits antimicrobial activities against Bacillus subtilis, Staphylococcus aureus and Escherichia coli. Rubiginone D2 exhibits antitumor efficacy, inhibits proliferations of cancer cells HM02, Kato III, HepG2 and MCF7, with GI50s of 0.1, 0.7, <0.1 and 7.5 μM, respectively .
|
-
- HY-146238
-
|
|
EGFR
Thymidylate Synthase
Apoptosis
|
Cancer
|
|
EGFR/HER2/TS-IN-1 (Compound 4d) is an EGFR, HER2 and TS (Thymidylate synthase) inhibitor with IC50 values of 0.203, 0.088 and 0.168 μM against EGFR, HER2 and TS, respectively. EGFR/HER2/TS-IN-1 induces MCF7 cell apoptosis .
|
-
- HY-W179181
-
MSNBA
1 Publications Verification
|
GLUT
|
Metabolic Disease
Cancer
|
|
MSNBA is a potent and selective GLUT5 fructose transport inhibitor with an IC50 of 0.10 mM. MSNBA does not affect the transport activity of human GLUT1, GLUT2, GLUT3, GLUT4 or bacterial GlcPSe. MSNBA competitively inhibits GLUT5 fructose uptake with a Ki of 3.2 μM in MCF7 cells. MSNBA can be used for the study of cancer or diabetes .
|
-
- HY-149376
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 38 (compound 14) is a tetrazole-based Tubulin inhibitor with antiproliferative potencies. Tubulin inhibitor 38 (100 nM，24 h) mediates mitotic arrest，blocks cell cycle at G2/M phase and induces apoptosis. Tubulin inhibitor 38 exhibits high cytotoxicity with high selectivity index among HeLa，MCF7，and U87 MG cells .
|
-
- HY-181880
-
|
|
PROTACs
NAMPT
|
Cancer
|
|
PROTAC NAMPT Degrader-28 is a NAMPT PROTAC degrader with DC50 values of 45 nM and 55 nM in MCF7 and 4T1cl5 cells, respectively. PROTAC NAMPT Degrader-28 retains nicotinamide phosphoribosyltransferase inhibitory activity and does not induce degradation of this enzyme. PROTAC NAMPT Degrader-28 can be used in breast cancer-related research .
|
-
- HY-175171
-
|
|
Topoisomerase
VEGFR
c-Met/HGFR
EGFR
Estrogen Receptor/ERR
|
Cancer
|
|
Anticancer agent 276 (Compound 5) is a multi-target anticancer agent. Anticancer agent 276 has a potent anticancer activity against human tumor cells with IC50s of 6.90 and 4.48 μM for HEPG2 and MCF7 cells, respectively. Anticancer agent 276 shows strong and stable interactions across multiple targets, including Topoisomerase II, VEGFR2, c-Met, EGFR and ERα .
|
-
- HY-15668
-
|
|
MMP
Bcl-2 Family
Caspase
Apoptosis
Drug Derivative
|
Cancer
|
|
ST09 is an efficient and low toxicity Curcumin (HY-N0005) derivative. ST09 significantly inhibits cell migration and downregulates the expression of MMP1, MMP2, and Vimentin. ST09 has strong cytotoxicity to breast cancer cells, such as MDA-MB-231, MCF7 and T47D cells. ST09 induces cell apoptosis by upregulating Bax and cleaved caspase-3/9. ST09 can be used in the research of cancer such as breast cancer .
|
-
- HY-Z12208
-
|
|
Drug Derivative
|
Cancer
|
|
N1-Phenylsuberamide is an organic amide compound, and its structure can be regarded as a simplified analogue of Vorinostat (HY-10221). N1-Phenylsuberamide exhibits moderate anti-proliferative activity against MDA-MB-231 and MCF-7 cells. N1-Phenylsuberamide does not show significant HDAC inhibitory activity and can only weakly induce the expression of the p21 gene. N1-Phenylsuberamide has extremely low relative binding affinity of estrogen receptor. N1-Phenylsuberamide can be used as a control compound .
|
-
- HY-N9848
-
|
|
Others
|
Cancer
|
|
2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid is a triterpenoid with anticancer effects. 2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid inhibits HepG2, A549, MCF-7, SK-OV-3, and HeLa cells with IC50 values of 19.62 μM, 18.86 μM, 45.94 μM, 62.41 μM, and 28.74 μM, respectively .
|
-
- HY-170603
-
|
|
Fluorescent Dye
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
PRMT5-targeted fluorescent ligand-1 (Compound 7) is a PRMT5-targeted fluorescent ligand, that inhibits PRMT5 with an IC50 of 29.39 nM. PRMT5-targeted fluorescent ligand-1 exhibits cell imaging activity, that exhibits good fluorescence signal in MCF-7 with an IC50 of 29 nM. PRMT5-targeted fluorescent ligand-1 induces apoptosis. PRMT5-targeted fluorescent ligand-1 exhibits a maximal excitation wavelength of 438 nm and a maximal emission wavelength of 550 nm .
|
-
- HY-121149B
-
|
(E/Z)-3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
(E/Z)-Droloxifene is a mixture of (E)-droloxifene (a selective estrogen receptor modulator) and (Z)-droloxifene. (E)-Droloxifene binds to the estrogen receptor (ER) with an IC50 value of 24 nM in rabbit uterine homogenates. (E)-Droloxifene increases uterine weight in immature rats, and reduces estradiol-induced increases in uterine weight in juvenile rats. (E)-Droloxifene also inhibits 17β-estradiol-stimulated growth of MCF-7, ZR-75-1, and T47D human breast cancer cells. (Z)-Droloxifene binds weakly to ER and has no estrogenic or antiestrogenic activity .
|
-
- HY-P10790
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
|
-
- HY-178441
-
|
|
Pyruvate Kinase
Reactive Oxygen Species (ROS)
Apoptosis
Microtubule/Tubulin
|
Metabolic Disease
Cancer
|
|
PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer .
|
-
- HY-135453
-
|
|
Bacterial
|
Infection
|
|
(-)-Pinocembrin exhibits anti-mycobacterium activity against mycobacteriuum tuberculosis H37Ra with an IC50 value of 1.11 mg/mL in dormant phase and 1.21 mg/mL in active phase, respectively. (-)-Pinocembrin has potent antiproliferative activity with IC50 values of 1.88-11.00 mg/mL against THP-1, A549, Panc-1, HeLa and MCF7 cell lines .
|
-
- HY-168435
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-63 (Compound 12b) is the inhibitor for VEGFR2 that inhibits 87.2% VEGFR-2 at 10 μM. VEGFR-2-IN-63 exhibits antiproliferative activity in multiple cancer cell, IC50s for HCT116, MCF7 and PaCa2 is 6.5 μM, 2.1 μM and 4.1 μM, respectively .
|
-
- HY-174232
-
|
|
EGFR
Carbonic Anhydrase
Caspase
|
Cancer
|
|
EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor against epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) with IC50 values of 5.92 nM and 63 nM, respectively. EGFR/CA-IX-IN-1 shows strong cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM, respectively. EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, up-regulates BAX/Bcl-2, activates caspases, and arrests the cell cycle at the G1 phase. EGFR/CA-IX-IN-1 is promising for research of breast cancer .
|
-
- HY-173365
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-67 (Compound 6b) is an inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2). Its IC50 values for MDA-231 and MCF-7 cell lines are 5.91 µM and 7.16 µM respectively, and its inhibitory effect on VEGFR-2 is comparable to that of Sorafenib (HY-10201) (IC50 is 53.63 nM). VEGFR-2-IN-67 exerts significant anti-cancer activity through mechanisms such as inducing Apoptosis (the early apoptosis rate reaches 57.20%), arresting the cell cycle at the G1 phase, upregulating pro-apoptotic markers and downregulating Bcl-2. VEGFR-2-IN-67 can be used for research in the field of cancer .
|
-
- HY-169382
-
|
|
Melatonin Receptor
|
Cancer
|
|
Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively.
|
-
- HY-178065
-
|
|
PROTACs
Histone Methyltransferase
GLP Receptor
|
Cancer
|
|
PROTAC G9a/GLP degrader 1 is a G9a/GLP PROTAC degrader with DC50s of 336 nM (G9a) and 988 nM (GLP). PROTAC G9a/GLP degrader 1 exhibits inhibitory activity against G9a with an IC50 of 98 nM. PROTAC G9a/GLP degrader 1 effectively inhibits the migration of breast cancer MCF-7 cells without inhibiting cell proliferation. PROTAC G9a/GLP degrader 1 can be used for the study of breast cancer (Pink: G9a/GLP ligand (HY-152775); Blue: VHL ligand (HY-125845); Black: Linker (HY-140468)) .
|
-
- HY-121255
-
|
(R)-Cryptopleurine; NSC 19912
|
TMV
|
Cancer
|
|
(–)-Cryptopleurine is an alkaloid that has been found in Lauraceae and has diverse biological activities. It inhibits the growth of human A375 melanoma, A431 epidermoid carcinoma, A549 lung, MES-SA uterine sarcoma, and MCF-7 breast cancer cells (IC50=3 nM for all).2 (–)-Cryptopleurine inhibits hypoxia-induced gene expression in a hypoxia response element (HRE) reporter assay (IC50=8.7 nM).3 (–)-Cryptopleurine (500 μg/mL) prevents lesion formation in tobacco (N. tabacum) plants infected with tobacco mosaic virus (TMV). It also inhibits protein synthesis by yeast and mammalian ribosomes.
|
-
- HY-N12887
-
|
|
Mitochondrial Metabolism
|
Others
Cancer
|
|
Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans .
|
-
- HY-171895
-
|
12-Nitro-9-cis,12-cis-octadecadienoic acid
|
PPAR
Interleukin Related
NF-κB
TNF Receptor
|
Inflammation/Immunology
|
|
12-Nitrolinoleate (12-Nitro-9-cis,12-cis-octadecadienoic acid) is an activator for peroxisome proliferator-activated receptor γ (PPARγ). 12-Nitrolinoleate is a nitrated form of linoleic acid. 12-Nitrolinoleate can be formed upon exposure to acidified nitrate and found in human red blood cells and plasma. 12-Nitrolinoleate can activate PPARγ-dependent gene expression in MCF-7 cells expressing PPARγ with an EC50 = 0.045 μM. 12-Nitrolinoleate is able to inhibit LPS (HY-D1056)-induced NF-κB transcription in RAW 264.7 cells. 12-Nitrolinoleate can inhibit IL-6, TNF-α and CCL2 induced by LPS .
|
-
- HY-181769
-
|
|
MMP
Polo-like Kinase (PLK)
CDK
PAK
Bcl-2 Family
Caspase
Apoptosis
|
Cancer
|
|
Anticancer agent 306 is a spiro tetramic acid derivative and a inhibitor of MMP1, MMP7 and PLK1. Anticancer agent 306 exerts antiproliferative activity against H1299, RKO and MCF-7 cells with IC50 values of 19.25 μM, 3.29 μM and 102.36 μM, respectively. Anticancer agent 306 can up-regulate p21 protein and down-regulate CCND1 and CCNB1 proteins to induce cell cycle arrest, regulate the expression of Bcl-2 and Bax to induce cell apoptosis. Anticancer agent 306 can down-regulate MMP1 and MMP7 proteins to inhibit tumor invasion and metastasis. Anticancer agent 306 can be used for the research of lung cancer, colorectal cancer, breast cancer .
|
-
- HY-N8146
-
|
|
STAT
Bcl-2 Family
Ser/Thr Kinase
Survivin
c-Myc
Apoptosis
Necroptosis
CDK
|
Infection
Cancer
|
|
Bruceantinol is a quassinoid that can be isolated from Brucea javanica, inhibits pepper mottle virus (PepMoV) in pepper. Bruceantinol is a STAT3 inhibitor demonstrating potent antitumor activity in in vitro and in vivo human colorectal cancer (CRC) models. Bruceantinol has potent anti-leukemic activity. Bruceantinol strongly inhibits STAT3 DNA-binding ability (IC50 = 2.4 pM), blocks the constitutive and IL-6-induced STAT3 activation, and suppresses transcription of MCL-1, PTTG1, survivin and c-Myc. Bruceantinol binds with CDK2/4/6 to facilitate protein degradation through proteasome pathway. Bruceantinol can dose- and time-dependently reduces the cell growth, impede cell proliferation, disrupts the cell cycle, and induces necrosis in MCF-7 cells and apoptosis in MDA-MB-231 cells .
|
-
- HY-180961
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer .
|
-
- HY-172167
-
|
|
PD-1/PD-L1
HDAC
|
Inflammation/Immunology
Cancer
|
|
PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC50 of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC50=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME .
|
-
- HY-164619
-
|
|
CDK
SARS-CoV
|
Infection
Cancer
|
|
CDK9-IN-34 (Compound 1b) is an inhibitor for CDK9 with an IC50 of 0.25 μM. CDK9-IN-34 exhibits cytotoxicity to cancer cell HCT116, MCF7 and K652 with IC50s of 1.43, 3.01 and 50.27 μM, respectively. CDK9-IN-34 exhibits antiviral activity against coronavirus 229E with an IC50 of 145.92 μM .
|
-
- HY-N15636
-
|
(-)-Coccinine
|
Serotonin Transporter
P-glycoprotein
|
Neurological Disease
Cancer
|
|
Coccinine ((-)-Coccinine) is a weak inhibitor of SERT (IC50: 196.3 μM; Ki: 106.8 μM) and P-gp (IC50: 0.96 mM). Coccinine exhibits significant anti-tumor activity against various cancer cell lines, such as breast cancer (MCF7, Hs578T, MDA-MB-231), colon cancer (HCT-15), and lung cancer (A549). Coccinine can be used in the research of tumors and neurological diseases .
|
-
- HY-178176
-
|
|
PROTACs
Cannabinoid Receptor
Akt
ERK
Bcl-2 Family
Apoptosis
|
Cancer
|
|
PROTAC CB1R Degrader-1 is a potent and selective CB1R PROTAC degrader that exploits the ubiquitin-proteasome system (UPS) achieving a DC50 of 3.37 μM in MCF-7 cells and showing no impact on CB2R. PROTAC CB1R Degrader-1 reduces CB1R-associated downstream signaling (p-AKT, p-ERK, BCL2, and MCM5), thereby inhibiting breast cancer cell proliferation and inducing apoptosis. PROTAC CB1R Degrader-1 can be used for breast cancer research. (Blue: CRBN ligand (HY-41547); Black: linker (HY-178198); Pink: CB1R ligand (HY-134497)) .
|
-
- HY-123715
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 255 is a monocarbonylated curcumin-1,2,3-oxazole conjugate with significant anticancer activity. The IC50 values of Anticancer agent 255 in prostate cancer cells PC-3 and DU-145 are 8.8μM and 9.5μM respectively. The IC50 values of Anticancer agent 255 against breast cancer cells MCF-7, MDA-MB-231 and 4T1 are 6μM, 10μM and 6.4μM, showing good anti-cancer activity Effect. Anticancer agent 255 can induce mitochondria-mediated apoptosis in cancer cells and prevent cell cycle progression. Anticancer agent 255 down-regulated the cell proliferation marker PCNA and inhibited the activation of cell survival proteins. Anticancer agent 255 up-regulated the pro-apoptotic protein Bax and down-regulated the anti-apoptotic protein Bcl-2 .
|
-
- HY-173222
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 28 (Compound 4h) is an inhibitor targeting P-glycoprotein (P-gp). It can inhibit the proliferation of cancer cells, and its IC50 value for MCF-7/ADR cells is between 15.88 and 21.96 μM. P-gp inhibitor 28 can increase the accumulation of Rho123 in MCF-7/ADR cells and can be used in research related to cancer and overcoming multidrug resistance in tumors .
|
-
- HY-141877B
-
|
YS43-22 (isomer)
|
PROTACs
Histone Methyltransferase
|
Cancer
|
MS4322 (YS43-22) isomer is an isomer of MS4322. MS4322 is a specific PRMT5 PROTAC degrader. MS4322 reduces the PRMT5 protein level with a DC50 of 1.1 μM in MCF-7 cells. MS4322 inhibits the methyltransferase activity of PRMT5 with an IC50 of 18 nM. MS4322 promotes ubiquitination and degradation of PRMT5. MS4322 can be used for the research of breast cancer, lung cancer, and hepatocellular cancer. (Pink: PRMT5 ligand (HY-173092); Blue: E3 ligase ligand HY-112078); Black: linker (HY-124780); E3+linker (HY-173093 )) .
|
-
- HY-N10778
-
|
|
Others
|
Others
|
|
(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol is a cucurbitane-type triterpenoid. (19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol has been tested to no effect against 5 cancer cell lines, MCF-7, HepG2, Du145, Colon205 and HL-60 by MTT assay .
|
-
- HY-147825
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-149633
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
Apoptosis
|
Cancer
|
|
EGFR/HER2/DHFR-IN-3 (compound 4c) is a potent dual inhibitor of EGFR/HER2, with IC50s of 0.138 and 0.092 μM, respectively. EGFR/HER2/DHFR-IN-3 also inhibits DHFR, with an IC50 of 0.193 M. EGFR/HER2/DHFR-IN-3 causes arrest at the S phase of the cell cycle and induces apoptosis in MCF7 breast cancer cells .
|
-
- HY-175297
-
|
|
VEGFR
EGFR
|
Cancer
|
|
EGFR T790M/VEGFR-2-IN-1 (Compound 6) is a dual EGFR T790M mutant (IC50=0.26 μM) and VEGFR-2 (IC50=0.95 μM) inhibitor. EGFR T790M/VEGFR-2-IN-1 blocks tumor cell proliferation and angiogenesis signaling pathways. EGFR T790M/VEGFR-2-IN-1 exhibits potent cytotoxicity against multiple cancer cell lines (HCT116, MCF-7, HepG2, A549; IC50=5.35-9.90 μM). EGFR T790M/VEGFR-2-IN-1 is promising for research of non-small cell lung cancer and solid tumors .
|
-
- HY-P10785
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Iturin A-2 is a cyclic lipopeptide discovered in B. subtilis and exhibits inhibitory activity against the plant pathogenic fungus P. expansum (MIC = 8 µg/disk). Iturin A-2 is cytotoxic to MCF-7 and BT474 breast cancer cells, as well as HeLa cervical cancer cells, with IC50 values of 66.81, 95.04, and 77.5 µg/mL, respectively. In greenhouse studies, Iturin A-2 at concentrations of 100 and 300 mg/kg Iturin A-2 reduces the lesion area of southern corn leaf blight caused by B. maydis, and in field studies, concentrations of 300 and 500 mg/kg Iturin A-2 reduce the incidence of the disease. Iturin A-2 (12.5 µg/mL) inhibits cell division, but not nuclear division, in isolated fertilized starfish eggs .
|
-
- HY-159122
-
|
|
Carbonic Anhydrase
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
CA IX-IN-2 (Compound 9o) is an inhibitor for carbonic anhydrase (CA), that inhibits CA IX, CA XII and CA II with an IC50 of 5.6, 7.4 and 430 nM, respectively. CA IX-IN-2 inhibits the proliferation of cancer cell HCT-116, SW480, MDA-MB 231 and MCF-7, with IC50s of 14.63-29.33 μM. CA IX-IN-2 intercalates DNA, arrests cell cycle at G1/S phase, and induces apoptosis in MDA-MB-231. CA IX-IN-2 affects the mitochondrial membrane potential (MMP), increases the intracellular ROS levels, causes mitochondrial damage, and inhibits the cell migration of MDA-MB-231. CA IX-IN-2 exhibits antitumor efficacy in mouse models .
|
-
- HY-154978
-
|
|
Drug Derivative
|
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) .
|
-
- HY-178822
-
|
|
Drug Derivative
|
Cancer
|
|
AQ-13 (Compound 7) is a Chloroquine (HY-17589A) analogue with anti-breast cancer property. AQ-13 shows antiproliferative activities against MDA-MB231 and MCF7 with GI50 of 27.81 and 17.85 μM. AQ-13 shows low cytotoxicity against non-cancerous breast epithelial cells MCF10A (GI50 = 65.26 μM). AQ-13 can be used for the research of breast cancer .
|
-
- HY-169409
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property .
|
-
- HY-161687
-
|
|
Src
|
Cancer
|
|
Cisplatin/Dasatinib prodrug-1 (Compound 3) is a prodrug of Cisplatin (HY-17394) and Dasatinib (HY-10181). Cisplatin/Dasatinib prodrug-1 exhibits antiproliferative activity against A2780, MDA-MB-231, MCF7, HCT116, RD, Thp1 and HL60 cancer cells with IC50s of 0.1, 0.1, 0.36, 2.0, 0.4, 0.3 and 0.25 μM, respectively .
|
-
- HY-170336
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-10 (Compound 160a) is an orally active degrader for ERα with DC50 of 0.37-1.1 nM, in cells MCF7, T47D and CAMA-1. PROTAC ERα Degrader-10 exhibits antitumor efficacy in mouse model . (Pink: ligand for target protein (HY-170339); Black: linker (HY-30105); Blue: ligand for E3 ligase Cereblon (HY-168055))
|
-
- HY-103455
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.
|
-
- HY-110193
-
SPP-86
2 Publications Verification
|
RET
|
Cancer
|
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-179485
-
|
|
EGFR
VEGFR
COX
Caspase
Apoptosis
Bcl-2 Family
|
Cancer
|
|
EGFR/VEGFR2-IN-10 is a selective EGFR, VEGFR2 and COX2 inhibitor with IC50s of 8.5, 68 and 158 nM, respectively. EGFR/VEGFR2-IN-10 induces G1-phase cell cycle arrest in MCF-7 cells. EGFR/VEGFR2-IN-10 increases the Bax/Bcl-2 ratio, upregulates caspase-8, and elevates caspase-9 protein levels, confirming activation of the intrinsic apoptotic pathway. EGFR/VEGFR2-IN-10 demonstrates exceptional therapeutic potential by simultaneously inhibiting tumor proliferation, angiogenesis, and inflammation pathways while maintaining a favorable selectivity profile. EGFR/VEGFR2-IN-10 can be used as a research tool for cervical, liver, colon, and breast cancer studies .
|
-
- HY-111640
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-P11102
-
|
|
Bacterial
Fungal
HIV
Parasite
|
Infection
Cancer
|
|
Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
|
-
- HY-161995
-
|
|
Apoptosis
Necroptosis
FGFR
VEGFR
PDGFR
|
Cancer
|
|
FGFR1/VEGFR2-IN-2 (compound 6l) is a VEGFR2/FGFR1 dual inhibitor. The IC50 values for VEGFR2 and FGFR1 are 0.025 µM and 0.026 µM respectively, and for EGFR and PDGFR-β, the IC50 values are 0.106 µM and 0.077 µM. FGFR1/VEGFR2-IN-2 showes significant anti-cancer activity (GI=60.38%) on NCI-60 cell line, with an IC50 of 8.51 µM in T-47D cell line and anti-migration. FGFR1/VEGFR2-IN-2 acts to arrest cells in the G1 phase and promote apoptosis and necrosis; the IC50 for MCF-7 cell line exceeds 100 µM, and the IC50 for MDA-MB-231 is 69.17 µM, non-toxic to normal cells .
|
-
- HY-N7012
-
|
5-Hydroxy-3',4',7-trimethoxyflavone
|
Lipoxygenase
TNF Receptor
Interleukin Related
COX
Fungal
Parasite
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activities sup>[4]sup>[5].
|
-
- HY-N16377
-
|
|
Others
|
Cancer
|
|
1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione (Compound 2) is an anthraquinone analog. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione can be isolated from soil Actinomycete Streptomyces. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has potent cytotoxicity against HepG2, A875, BGC-823 and MCF-7 cells with IC50s of 2.29, 4.90, 0.99 and 1.66 μg/mL, respectively. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has an antitumor activity .
|
-
- HY-179433
-
|
|
PROTACs
Androgen Receptor
Estrogen Receptor/ERR
Src
|
Cancer
|
|
PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
|
-
- HY-151459
-
|
|
VEGFR
Bacterial
Dihydrofolate reductase (DHFR)
Fungal
|
Infection
Cancer
|
|
VEGFR-2/DHFR-IN-2 (compound 5b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.623 and 9.085 μM, respectively. VEGFR-2/DHFR-IN-2 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 3.59-8.38 μM. VEGFR-2/DHFR-IN-2 can be used for the research of cancer .
|
-
- HY-169096
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
|
-
- HY-178034
-
|
|
PROTACs
Oxysterol-binding Protein-related Protein (ORP)
|
Cancer
|
|
PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells . Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
|
-
- HY-172964
-
|
|
PI3K
Akt
mTOR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
KIM-161 is a PIK3CA inhibitor. KIM-161 has significant antiproliferative activity with IC50 values of 1.428 and 1.562 µM against PI3KCA mutant breast cancer MCF7 and T47D cells, respectively. KIM-161 induces apoptosis and cell cycle arrest by inhibiting the PI3K/AKT/mTOR signaling pathway and inducing ROS production. KIM-161 can be used to study breast cancer and its PI3KCA mutant subtypes .
|
-
- HY-174403
-
|
|
Bcl-2 Family
c-Myc
Apoptosis
Caspase
|
Cancer
|
|
c-MYC/BCL2 ligand 1 iodide is a dual-targeting c-MYC/Bcl-2 G4 ligand with Kd values of 0.90 μM (c-MYC G4) and 0.56 μM (Bcl-2 G4). c-MYC/BCL2 ligand 1 iodide inhibits c-MYC and Bcl-2 gene transcription by binding to G4-forming sequences and downregulates their protein expression. c-MYC/BCL2 ligand 1 iodide inhibits suppresses migration, induces caspase-dependent apoptosis, and triggers cell cycle G1 arrest in MCF-7 cells. c-MYC/BCL2 ligand 1 iodide significantly suppresses tumor growth in a 4T1 syngeneic model with no observable toxicity. c-MYC/BCL2 ligand 1 iodide can be used for the research of breast cancer.
|
-
- HY-155180
-
|
|
PI3K
|
Cancer
|
|
FD2056 is a potent and orally active PI3K inhibitor. FD2056 inhibits PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ with IC50s of 0.30, 0.80, 1.10, 0.42 nM. FD2056 also inhibits CDK2-CyclinA2 and CDK4-CyclinD3 with IC50 of 115.95 and 2782.15 nM. FD2056 inhibits breast cancer cell proliferation with IC50s of 1.06, 0.04, 1.40 μM for MDA-MB-231, MDA-MB-468, MCF-7 cells. FD2056 also induces cancer apoptosis and inhibits tumor growth .
|
-
- HY-138074
-
|
5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
|
Parasite
|
Infection
|
|
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-N0534
-
|
|
DNA/RNA Synthesis
Apoptosis
PI3K
Akt
Caspase
SOD
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases .
|
-
- HY-114803
-
-
- HY-113062
-
|
20-OH-P
|
Endogenous Metabolite
Cytochrome P450
|
Endocrinology
Cancer
|
|
20α-Dihydroprogesterone is the metabolite of Progesterone (HY-N0437). 20α-Dihydroprogesterone inhibits cell proliferation and migration in breast tissue. 20α-Dihydroprogesterone inhibits aromatase in cell MCF-7aro with IC50 about 5 μM .
|
-
- HY-139090
-
|
28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin
|
Bacterial
HIV
Drug Derivative
|
Cancer
|
|
3-Oxobetulin acetate (28-O-Acetyl-3-Oxobetulin; 3-oxo-28-O-Acetylbetulin) is a derivative of betulin (HY-N0083), a cholesterol biosynthesis inhibitor. 3-Oxobetulin acetate inhibits the growth of P388 murine lymphocytic leukemia cells (EC50=0.12 μg/mL) and human MCF-7 breast cancer, SF-268 CNS cancer, H460 lung cancer, and KM20L2 colon cancer cells (GI50s=8, 10.6, 5.2, and 12.7 μg/mL), but not BxPC-3 pancreatic cancer cells or DU145 prostate cancer cells (GI50s=>10 μg/mL for both). 3-Oxobetulin acetate inhibits the replication of X4-tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblastoid cells (IC50=13.4 μM). 3-Oxobetulin acetate is also effective against Listeria donovani amastigotes.
|
-
- HY-149632
-
|
|
EGFR
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
|
-
- HY-162447
-
|
|
P-glycoprotein
Apoptosis
|
Cancer
|
|
P-gp inhibitor 22 is a P-glycoprotein (P-gp) inhibitor that effectively inhibits P-pg and efflux function. P-gp inhibitor 22 induces apoptosis and accumulation of MCF-7/ADR cells processed in the S phase .
|
-
- HY-N12135
-
|
|
Others
|
Cancer
|
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
|
-
- HY-178353
-
|
|
EGFR
TNF Receptor
Interleukin Related
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR/Cytokine-IN-1 is an EGFR (IC50 = 0.03 μM) and Cytokine inhibitor (TNF-α, IC50 = 3.1 μM; IL-6, IC50 = 1.6 μM). EGFR/Cytokine-IN-1 shows potent anticancer activity on A549 and MCF7, respectively. EGFR/Cytokine-IN-1 significantly reduces IL-6 and TNF-α levels in A549 cells, and also shows promising ADMET profiles. EGFR/Cytokine-IN-1 can induce apoptosis in a dose-dependent manner. compound 5h can be used for the study of breast cancer and lung cancer .
|
-
- HY-170932
-
|
|
EGFR
COX
Apoptosis
|
Cancer
|
|
EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
|
-
- HY-N0534R
-
|
|
Reference Standards
DNA/RNA Synthesis
Apoptosis
PI3K
Akt
Caspase
SOD
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Vitexin-2"-O-rhamnoside (Standard) is the analytical standard of Vitexin-2"-O-rhamnoside (HY-N0534). This product is intended for research and analytical applications. Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases .
|
-
- HY-W010713
-
|
Fimaporfin free base
|
Photosensitizer
|
Cancer
|
|
Meso-tetraphenylchlorin (TPCS2a) is a photosensitizer with poor water solubility, which limits its use in the blood circulation. However, TPCS2a@NPs nanoparticles can be prepared based on polylactic-co-polyethylene glycol acid (PLGA) polymer core loaded with TPCS2. Such nanoparticles can be coated with mesenchymal stem cell-derived plasma membranes (mMSCs) to form mMSC-TPCS2a@NPs, which prolongs blood circulation time and improves tumor targeting ability. Compared with uncoated TPCS2a@NPs, mMSC-TPCS2a@NPs can reduce macrophage uptake by 54% to 70% under different conditions. Both nanoparticle forms are effectively accumulated in MCF7 and MDA-MB-231 breast cancer cells, while uptake in normal breast epithelial cells MCF10A is significantly lower .
|
-
- HY-151458
-
|
|
VEGFR
Bacterial
Dihydrofolate reductase (DHFR)
Fungal
|
Infection
Cancer
|
|
VEGFR-2/DHFR-IN-1 (compound 8b) is an inhibitor of VEGFR-2 and DHFR with IC50s of 0.384 and 7.881 μM, respectively. VEGFR-2/DHFR-IN-1 shows good antibacterial activities against Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA and MRSA with MIC values of 16, 16, 16, 8, and 16 μg/mL, respectively. VEGFR-2/DHFR-IN-1 exhibits good cytotoxic activities against C26, HepG2, and MCF7 cancer cell lines with IC50 values of 2.97-7.12 μM. VEGFR-2/DHFR-IN-1 can be used for the research of cancer .
|
-
- HY-180546
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-53 (compound 9) is a CDK2 inhibitor with anticancer activity. CDK2-IN-53 selectively inhibits the proliferation of HCT-116 and MCF-7cells with IC50 values of 13.89 and 7.65 μM, respectively, while showing lower cytotoxicity toward normal lung fibroblast (WI-38) cells (IC50 = 71.24 μM). CDK2-IN-53 can be used for cancer research, such as colon and breast cancer .
|
-
- HY-161260
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 20 (compound H27) is a low cytotoxicity P-glycoprotein (P-gp) inhibitor. P-gp inhibitor 20 inhibits the efflux function of P-gp in a dose-dependent manner (without affecting the expression of P-gp), thereby reversing the multidrug resistance (MDR) of MCF-7/ADR cells, with an IC50 value of 46.6 nM. P-gp inhibitor 20 can be used for cancer research .
|
-
- HY-161171
-
|
|
Parasite
Ephrin Receptor
|
Cancer
|
|
Antimalarial agent 37 (compound 33) is a selective inhibitor against Type Ⅱ kinase with antiplasmodial activity. Antimalarial agent 37 exhibited cytotoxicity and selectivity towards cancer cells HepG2 and MCF 7 .
|
-
- HY-144666
-
|
|
Glutaminase
|
Cancer
|
|
GLS-1-IN-1 (compound 1d) is a GLS-1 inhibitor. GLS-1-IN-1 shows inhibitory effect against Hep G2, MCF 7, and MCF 10A cells .
|
-
- HY-149360
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells .
|
-
- HY-163981
-
|
|
P-glycoprotein
|
Cancer
|
|
ABCB1-IN-2 (compound 16q) is a functional inhibitor that can directly bind to the ABCB1 protein and stabilize its structure without affecting the expression and subcellular localization of ABCB1. ABCB1-IN-2 can increase the sensitivity of MCF-7/ADR cells to paclitaxel (PTX), increase the accumulation of PTX, and prevent the accumulation and excretion of luciferin Rh123 mediated by ABCB1. ABCB1-IN-2, as an ABCB1-mediated multidrug resistance (MDR) reversal agent, shows a strong ability to reverse MDR .
|
-
- HY-173044
-
|
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM .
|
-
- HY-176719
-
|
|
Aldose Reductase
STAT
Amino acid Transporter
Apoptosis
|
Cancer
|
|
AKR1B1/STAT3/SLC7A11-regulator-1 (5a) is an AKR1B1/STAT3/SLC7A11 regulator that reverses DOX resistance in MCF-7/ADR cells by enhancing ferroptosis activity. AKR1B1/STAT3/SLC7A11-regulator-1 can be used in breast cancer research .
|
-
- HY-178351
-
|
|
HDAC
Microtubule/Tubulin
Apoptosis
Caspase
Bcl-2 Family
|
Cancer
|
|
HDAC6-IN-67 is a selective HDAC6 inhibitor (IC50 = 17.15 nM) that exhibits 19-fold selectivity over HDAC1. HDAC6-IN-67 selectively inhibits HDAC6 by interacting with Ser531 and His614. HDAC6-IN-67 induces apoptosis by inducing the cleavage of caspases 9, 8, 3, and PARP, upregulating Bax expression, and downregulating Bcl-2 expression. HDAC6-IN-67 effectively induces the acetylation of α-tubulin, without affecting histone H3 acetylation in MCF-7/ADR cells. HDAC6-IN-67 can be used for the study of breast cancer .
|
-
- HY-N12606
-
|
|
Fungal
|
Infection
|
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
|
-
- HY-P10843
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
|
-
- HY-164726
-
|
|
Estrogen Receptor/ERR
|
Others
|
|
Estrogen receptor modulator 11 (Compound 27) is a tetrahydroisoquinoline derivative. Estrogen receptor modulator 11 has a certain affinity for estrogen receptors (ER), with IC50 values of 285 nM and 421 nM for ERα and ERβ, respectively. Estrogen receptor modulator 11 lacks antagonist activity in the MCF-7 cellular assay .
|
-
- HY-169367
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-1233 is a potent and orally active estrogen receptor PROTAC degrader, with the DC50 of 0.9 nM. ERD-1233 plays an important role in ER + breast cancer research (Pink: ligand for target protein (HY-201580); Black: linker (HY-W889109); Blue: E3 ligase ligand (HY-W1009348)) .
|
-
- HY-173132
-
|
|
Aldose Reductase
|
Cancer
|
|
AKR1Cs-IN-1 (Compound 29) is a potent and broad-spectrum inhibitor targeting members of the Aldo-Keto Reductase 1C family (AKR1C1-1C4). By simultaneously occupying the SP2 and SP3 pockets, it effectively inhibits multiple isoforms and disrupts metabolic pathways associated with drug resistance. In enzymatic activity assays, AKR1Cs-IN-1 exhibited significant inhibitory potency, with IC50 values of 0.09, 0.28, 0.05, and 0.51 µM against AKR1C1, AKR1C2, AKR1C3, and AKR1C4, respectively. In the doxorubicin (DOX)-resistant breast cancer cell line MCF-7/ADR, AKR1Cs-IN-1 showed remarkable resensitization effects and significantly enhanced the cytotoxicity of DOX. AKR1Cs-IN-1 holds promise for research on overcoming drug resistance in breast cancer .
|
-
- HY-162752
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 250 (compound 104) has antitumor activity, inducing apoptosis, slowing proliferation, and degrading key oncogenic proteins (such as aRaf, CDK4 ) without inducing a heat shock response .
|
-
- HY-N10353
-
-
- HY-161861
-
|
|
VEGFR
Akt
|
Cancer
|
|
VEGFR-2/AKT-IN-1 (compound 17) is a dual inhibitor of VEGFR-2 and AKT, with the IC50s of 0.164 μM and 0.452 μM, respectively. VEGFR-2/AKT-IN-1 has antitumor activity .
|
-
- HY-19625A
-
|
|
Reactive Oxygen Species (ROS)
Paraptosis
|
Cancer
|
|
(E/Z)-MCB-613 is a pan-Steroid Receptor Coactivator (SRC) stimulator. (E/Z)-MCB-613 overstimulates SRC activity in cancer cells resulting in excessive generation of reactive oxygen species (ROS), leading to cell stress and death by a process called paraptosis. (E/Z)-MCB-613 is a cytotoxic molecule that plays an important role in cancer .
|
-
- HY-N2331R
-
|
|
Reference Standards
Topoisomerase
|
Cancer
|
|
Proscillaridin A (Standard) is the analytical standard of Proscillaridin A. This product is intended for research and analytical applications. Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively .
|
-
- HY-146810
-
-
- HY-N2331
-
|
|
Topoisomerase
|
Cancer
|
|
Proscillaridin A is a potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively .
|
-
- HY-19148
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
7U85 is a potent DNA synthesis inhibitor. 7U85 inhibits DNA synthesis. 7U85 can be used in the research of breast cancer .
|
-
- HY-116543
-
|
|
Apoptosis
|
Cancer
|
|
ST362 is a anti-cancer agent. ST362 induces cell apoptosis and inhibits cancer cell growth .
|
-
- HY-172582
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-38 (compound 14) is a CDK9 inhibitor with IC50 values of 1.2 nM and 3.3 nM for CDK9 wild-type and L156F mutant, respectively. CDK9-IN-38 inhibits tumor growth in vivo and in vitro .
|
-
- HY-N7083
-
-
- HY-N7083R
-
|
|
Reference Standards
Apoptosis
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
Cancer
|
|
Citral (Standard) is the analytical standard of Citral. This product is intended for research and analytical applications. Citral is an orally active monoterpene compound in lemon grass essential oil and a natural ALDH1A inhibitor, which can induce apoptosis and cycle arrest in breast cancer cell lines, and has analgesic, anti-injurious and anti-inflammatory effects .
|
-
- HY-145867
-
|
|
Topoisomerase
EGFR
CDK
Apoptosis
|
Cancer
|
|
EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, with IC50s of 0.4 µM and 1.6 µM for EGFR and CDK2, respectively. EGFR-IN-45 also inhibit Topo I and Topo II. EGFR-IN-45 arrests cancer cells in the pre-G1 phase and induces apoptosis .
|
-
- HY-168095
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research .
|
-
- HY-N15054
-
|
|
Drug Derivative
|
Cancer
|
|
17-O-Demethylgeldanamycin is a secondary metabolite that can be isolated from Streptomyces. 17-O-Demethylgeldanamycin exhibits cytotoxicity against a variety of tumor cells and has anti-tumor activity .
|
-
- HY-79576
-
|
Oestrone methyl ether; 3-O-Methylestrone
|
Drug Intermediate
|
Cancer
|
|
Estrone 3-methyl ether (Oestrone methyl ether; 3-O-Methylestrone) is a synthetic intermediate useful for synthesis of estrogen receptor modulator .
|
-
- HY-126423
-
|
Isorhamnetin 3-O-glucuronide
|
Apoptosis
|
Cancer
|
|
Isorhamnetin 3-glucuronide is a potent anticancer agent. Isorhamnetin 3-glucuronide shows anti-proliferative activity. Isorhamnetin 3-glucuronide induces Apoptosis and cell cycle arrest at S-phase .
|
-
- HY-100706
-
|
|
DNA-PK
|
Cancer
|
|
AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively .
|
-
- HY-100706R
-
|
|
DNA-PK
Reference Standards
|
Cancer
|
|
AMA-37 (Standard) is the analytical standard of AMA-37 (HY-100706). This product is intended for research and analytical applications. AMA-37, an Arylmorpholine analog, is ATP-competitive DNA-PK inhibitor, with IC50 values of 0.27 μM (DNA-PK), 32 μM (p110α), 3.7 μM (p110β), and 22 μM (p110γ), respectively .
|
-
- HY-N10229
-
|
|
Fungal
|
Infection
|
|
Harzianum A is a trichothecene compound. Harzianum A has no antibacterial activity against Gram-negative and Gram-positive bacteria, but has antifungal activity. In addition, Harzianum A is cytotoxic to tumor cells .
|
-
- HY-149024
-
|
|
VEGFR
Apoptosis
MDM-2/p53
|
Cancer
|
|
VEGFR-2-IN-23 (compound 11b) is a potent and selective VEGFR-2 inhibitor with an IC50 value of 0.34 nM. VEGFR-2-IN-23 shows antitumor activity. VEGFR-2-IN-23 induces apoptosis and cell cycle arrest at G1 phase .
|
-
- HY-174867
-
|
|
PROTACs
Ferroptosis
|
Cancer
|
|
AY-4 (Compound AY-4) is an efficient PROTAC degrader targeting FTH1 (Kd = 3.17 nM). AY-4 effectively upregulates the levels of ferrous (Fe 2+) and ferric (Fe 3+) ions in cells. AY-4 is a potential anticancer candidate compound that regulates iron homeostasis through ferritin degradation and enhances the efficacy of existing drugs. AY-4 can effectively reduce the level of FTH1 in breast cancer cells (Pink: FTH1 ligand AY-2 (HY-174871); Blue: E3 ligand Pomalidomide (HY-10984); Black: Linker, Pomalidomide-PEG3-acid (HY-174872)) .
|
-
- HY-N1268
-
|
|
Others
|
Others
|
|
Scutebata E is a new neoclerodane diterpenoid isolated from Scutellaria barbata with weak cytotoxic activity .
|
-
- HY-N1267
-
|
|
Others
|
Others
|
|
Scutebata C is a neoclerodane diterpenoid isolated from Scutellaria barbata with weak cytotoxic activity .
|
-
- HY-157137
-
|
|
PARP
Caspase
Apoptosis
|
Cancer
|
|
PARP1-IN-17 is a PARP-1 inhibitor (IC50 = 19.24 nM for PARP-1 and = 32.58 nM for PARP-2) and induce apoptosis. PARP1-IN-17 shows excellent anti-proliferative activity .
|
-
- HY-174854
-
|
|
HDAC
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
PySAHA is a multifunctional HDAC inhibitor. PySAHA can degrade intracellular HDAC via a hydrophobic tagging mechanism. PySAHA also possesses photodynamic therapeutic activity and can generate reactive oxygen species under light irradiation. PySAHA can inhibit the proliferation, migration and induce cell apoptosis of breast cancer cells. PySAHA has antitumor activity and can be used in breast cancer research .
|
-
- HY-124611
-
|
|
HSP
Apoptosis
|
Cancer
|
|
JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a Ki of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity .
|
-
- HY-175253
-
|
|
STAT
Apoptosis
|
Cancer
|
|
YZ-35 is a STAT3 inhibitor, with a Ki value of 0.38 μM. YZ-35 binds directly to STAT3 with high
affinity, exhibiting a dissociation constant (Kd) of 190 nM. YZ-35 directly attenuates the dual phosphorylation of STAT3 (Tyr705 and Ser727). YZ-35 suppresses colony formation, cellular migration, and induces apoptosis in breast cancer cell lines (BCSC). YZ-35 selectively suppresses BCSC self-renewal. YZ-35 inhibits tumor growth in the BCSC xenograft models. YZ-35 can be used for the study of breast cancer .
|
-
- HY-D0190
-
|
HTTA; TTA; TTFA
|
Mitochondrial Metabolism
|
Infection
Others
Cancer
|
|
2-Theoyltrifluoroacetone is a chelating agent and mitochondrial electron transfer chain inhibitor, with a IC50 value of 51.5 μM. 2-Thermoyltrifluoroacetone can chelate with various metal ions and has cytotoxicity and anti-tumor activity, which is expected to play an important role in the treatment of mitochondrial dysfunction related diseases .
|
-
- HY-N12792
-
|
|
Others
|
Cancer
|
|
5,8-Dihydroxy-3',4',6,7-tetramethoxyflavone (Compound 8) is a flavonoid with anticancer activity. 5,8-Dihydroxy-3',4',6,7-tetramethoxyflavone can be isolated from Euryops arabicus .
|
-
- HY-D0190R
-
|
HTTA (Standard); TTA (Standard); TTFA (Standard)
|
Mitochondrial Metabolism
Reference Standards
|
Infection
Others
Cancer
|
|
2-Thenoyltrifluoroacetone (Standard) is the analytical standard of 2-Thenoyltrifluoroacetone. This product is intended for research and analytical applications. 2-Theoyltrifluoroacetone is a chelating agent and mitochondrial electron transfer chain inhibitor, with a IC50 value of 51.5 μM. 2-Thermoyltrifluoroacetone can chelate with various metal ions and has cytotoxicity and anti-tumor activity, which is expected to play an important role in the treatment of mitochondrial dysfunction related diseases .
|
-
- HY-163524
-
|
|
Apoptosis
|
Cancer
|
|
NAE-IN-2 (compound III-26) is N2–(1-benzylpiperidin-4-yl)quinazoline-2,4-diamine derivative, and inhibits Cullin1 and Cullin3. NAE-IN-2 inhibits migration and induces cell apoptosis of gastric cancer cells .
|
-
- HY-157765
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-6 (compound A2) is a potent PROTAC degrader of ERα, with IC50 of 0.11 μM in MCE-7 cells. PROTAC ERα Degrader-6 has anti-tumor effect. PROTAC ERα Degrader-6 is a fluorescent probes with Em of 582 nm that enable real-time visualization of ERα protein degradation .
|
-
- HY-14526
-
|
543U76; 5,11-Methenyltetrahydrohomofolate
|
DNA/RNA Synthesis
|
Cancer
|
|
5-DACTHF (543U76) is an inhibitor of purine de novo biosynthesis. 5-DACTHF is a GAR-TFase and AICAR-TFase inhibitor (IC50: 3 and 94 μM). 5-DACTHF is a potent antitumor agent .
|
-
- HY-175209
-
|
|
Keap1-Nrf2
Ferroptosis
Reactive Oxygen Species (ROS)
Atg8/LC3
|
Cancer
|
|
Nrf2-IN-4 is a Nrf2 inhibitor. Nrf2-IN-4 induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor efficacy. Nrf2-IN-4 can be used for the study of breast cancer .
|
-
- HY-137422
-
-
- HY-118672
-
|
|
HDAC
MMP
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HNHA is a potent HDAC inhibitor with an IC50 of 100 nM. HNHA arrests the cell cycle at the G1/S phase via p21 induction. HNHA inhibits tumor growth and tumor neovascularization. HNHA may be a potent anti-cancer agent against breast cancer .
|
-
- HY-154986
-
|
|
MARK
AMPK
|
Cancer
|
|
MARK4 inhibitor 2 is an inhibitor of microtubule affinity-regulating kinase 4 (MARK4) with an Km of 6.3×10 7 and an IC50 of 0.82 μM. MARK4 inhibitor 2 inhibits the growth of human cells and can be used for cancer research .
|
-
- HY-178118
-
|
|
PROTACs
PDI
|
Cancer
|
|
PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation . Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
|
-
- HY-181251
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-195 is a EGFR inhibitor with an IC50 of 0.89 nM. EGFR-IN-195 inhibits the viability of breast cancer cells. EGFR-IN-195 can be used in breast cancer-related research .
|
-
- HY-175815
-
|
|
Apoptosis
Bcl-2 Family
Caspase
MMP
Cadherin
|
Cancer
|
|
Apoptosis inducer 44 is an apoptosis inducer. Apoptosis inducer 44 triggers apoptosis in MDA-MB-231 cells by increasing the levels of Bax and Cyt C, reducing Bcl-2, and initiating caspase-3 cleavage. Apoptosis inducer 44 suppresses the invasion and migration of MDA-MB-231 cells by down-regulating MMP-2 and MMP-9 expression and up-regulating E-cadherin protein levels. Apoptosis inducer 44 can be used for the study of breast cancer .
|
-
- HY-N17453
-
|
|
Others
|
Cancer
|
|
(+)-Mornaphthoate E is a growth inhibitor that suppresses cancer cell proliferation. It can be used in research on cancers such as lung cancer and breast cancer .
|
-
- HY-162654
-
|
|
Factor VIII
|
Cardiovascular Disease
|
|
FXIIIa-IN-1 (Compound 16) is a potent and selective FXIIIa (Factor XIIIa) inhibitor with an IC50 value of 2.4 μM. FXIIIa-IN-1 inhibits FXIIIa by competing with the Gln-donor protein substrate (dimethylcasein). FXIIIa-IN-1 holds promise for the development of effective and safe novel anticoagulants .
|
-
- HY-152159
-
|
|
Cytochrome P450
|
Cancer
|
|
CYP4Z1-IN-1 (compound 7c) is a potent CYP4Z1 inhibitor, with an IC50 of 41.8 nM. CYP4Z1-IN-1 decreases the expression of breast CSCs stemness markers, spheroid formation, and metastatic ability as well as tumor-initiation capability in a concentration-dependent manner in vitro and in vivo .
|
-
- HY-B0111
-
|
Dihydrospirorenone
|
Progesterone Receptor
Androgen Receptor
|
Endocrinology
Cancer
|
|
Drospirenone (Dihydrospirorenone) is an orally active fourth-generation progestin that interacts with the progesterone receptor (PR) and androgen receptor (AR). Drospirenone significantly decreases both plasminogen activator inhibitor-1 (PAI-1) and tissue plasminogen activator (tPA) via the AR. Drospirenone can produce DNA damage in bone marrow cells of female mice. .
|
-
- HY-163402
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-108 chloride (Compound Ru3S) is an EGFR inhibitor with an IC50 value of 5.8 nM for hEGFR. EGFR-IN-108 chloride induces apoptosis and has anti-proliferative activity against cancer cells. EGFR-IN-108 chloride also has anti-angiogenic effects .
|
-
- HY-18976
-
-
- HY-175635
-
|
|
EGFR
VEGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-6 (Compound 3k) is a dual-functional inhibitor of EGFR and VEGFR2 with IC50s of 10.53 and 3.37 μM for EGFR and VEGFR2, respectively. EGFR/VEGFR2-IN-6 has significant anti-proliferation activity against breast cancer cells, and induces G0/G1 cell cycle arrest and cell apoptosis, especially early apoptosis. EGFR/VEGFR2-IN-6 can be used for cancers research .
|
-
- HY-155090
-
|
|
ATM/ATR
|
Cancer
|
|
ATM Inhibitor-8 (Compound 10r) is a highly potent, selective and orally active ATM inhibitor,with an IC50 of 1.15 nM. ATM Inhibitor-8 exhibits anti-tumor activity .
|
-
- HY-146277
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity .
|
-
- HY-151635
-
|
|
PI3K
VEGFR
Apoptosis
|
Cancer
|
|
PI3K/VEGFR2-IN-1 is a potent dual PI3K/VEGFR2 inhibitor with IC50 values of 2.21 and 68 μM for PI3K and VEGFR2, respectively. PI3K/VEGFR2-IN-1 induces apoptosis. PI3K/VEGFR2-IN-1 can be used in research of cancer .
|
-
- HY-146277A
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity .
|
-
- HY-120139
-
KMH-233
1 Publications Verification
|
Amino acid Transporter
|
Cancer
|
|
KMH-233, a potent, reversible and selective inhibitor of l-type amino acid transporter LAT1/SLC7A5, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-N0595R
-
|
Genistine (Standard); Genistoside (Standard); Genistein 7-O-β-D-glucopyranoside (Standard)
|
Reference Standards
Estrogen Receptor/ERR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Genistin (Standard) is the analytical standard of Genistin. This product is intended for research and analytical applications. Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway .
|
-
- HY-P4210
-
|
ALRN-6924; MP-4897
|
MDM-2/p53
|
Cancer
|
|
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .
|
-
- HY-181164
-
|
|
PROTACs
Epigenetic Reader Domain
HIV
|
Infection
|
|
PROTAC BRD4 Degrader-43 is a BRD4 PROTAC degrader. PROTAC BRD4 Degrader-43 recruits the DCAF1-DDB1-Cul4A E3 ligase complex via a Vpr-derived peptide moiety to induce BRD4 ubiquitination and degradation through the ubiquitin-proteasome system. PROTAC BRD4 Degrader-43 exhibits potent HIV latency-reversing activity. PROTAC BRD4 Degrader-43 can be used for the research of HIV-1 latent infection . (Pink: BRD4 ligand (HY-13030); Blue: Cul4A-DDB1-DCAF1 ligand (HY-P11640); Black: conjugate of PEG linker + cell-penetrating peptide (HY-P2483))
|
-
- HY-168655
-
|
|
Apoptosis
EGFR
VEGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-3 (compound 9) is a potent EGFR and VEGFR-2 inhibitor with IC50 values of 0.129, 0.142, 3.428 µM for EGFR, VEGFR-2, COX-2, respectively. EGFR/VEGFR2-IN-3 shows cytotoxicity. EGFR/VEGFR2-IN-3 induces apoptosis and cell cycle arrest at G2/M phase .
|
-
- HY-N0595
-
|
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway .
|
-
- HY-120139A
-
|
|
ASCT
|
Cancer
|
|
(R)-KMH-233 is the isomer of KMH-233 (HY-120139), and can be used as an experimental control. KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-N12997
-
|
|
Others
|
Others
|
|
Torachrysone 8-O-β-D-glucoside is a phenolic glycoside that can be isolated from the seeds of Senna tora. Torachrysone 8-O-β-D-glucoside shows cytotoxicity .
|
-
- HY-132135
-
|
|
Polo-like Kinase (PLK)
|
Cancer
|
|
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). (1E)-CFI-400437 dihydrochloride inhibits Aurora A, Aurora B, KDR and FLT-3 with IC50s of 0.37, 0.21, 0.48, and 0.18 μM, respectively. Antiproliferative activity .
|
-
- HY-N12231
-
|
|
Antibiotic
Bacterial
Lipoxygenase
|
Infection
Cancer
|
|
Carbazomycin B is a bacterial metabolite and can be isolated from Streptomyces. Carbazomycin B is an antifungal and antibacterial agent. Carbazomycin B inhibits 5-lipoxygenase (5-LO) activity in extract from RBL-1 cell with the IC50 Of 1.5 µM sup>[2]sup>[3]sup>[4].
|
-
- HY-170366
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with an IC50 of 42.5 nM. VEGFR-2-IN-58 displays selective cytotoxicity against cancer cells. VEGFR-2-IN-58 shows cellular growth arrest at the G2/M phase in cancer cells. VEGFR-2-IN-58 induces cancer cells Apoptosis, increasing BAX expression and reducing Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells .
|
-
- HY-173482
-
|
|
Wnt
β-catenin
|
Cancer
|
|
TFAP4/Wnt/β-catenin-IN-1 (Compound A61) is an orally active TFAP4/Wnt/β-catenin inhibitor. TFAP4/Wnt/β-catenin-IN-1 has significant anticancer activity against a variety of cancer cells (such as gastric cancer, lung cancer, breast cancer, etc.), and has the strongest anticancer activity against MGC-803 gastric cancer cells (IC50: 3.92 μM). TFAP4/Wnt/β-catenin-IN-1 induces apoptosis and cell cycle arrest (S phase) in cancer cells by inhibiting the TFAP4/Wnt/β-catenin signaling pathway. TFAP4/Wnt/β-catenin-IN-1 can be used in the study of gastric cancer .
|
-
- HY-185344
-
|
TRX01
|
NF-κB
|
Cancer
|
|
Ratutrelvir is a NF-κB p65 inhibitor. Ratutrelvir blocks the translocation of NF-κB p65 from the cytoplasm to the nucleus, reduces the phosphorylation levels of NF-κB p65 and IκBα, and inhibits the DNA-binding activity of NF-κB p65. Ratutrelvir inhibits the migration and invasion abilities of breast cancer cells, and reduces their viability and colony-forming capacity. Ratutrelvir can be used for the research of luminal A breast cancer .
|
-
- HY-146548
-
|
|
Apoptosis
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
Anticancer Agent 43 is a potent anticancer agent. Anticancer Agent 43 induces apoptosis by caspase 3, PARP1, and Bax dependent mechanisms. Anticancer Agent 43 induces DNA damage .
|
-
- HY-146010
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 13 (compound 7) is a potent carbonic anhydrase (CA) inhibitor, which features 3-methylthiazolo[3,2-a]benzimidazole moiety (as a tail) connected to the zinc anchoring benzenesulfonamide moiety via ureido linker .
|
-
- HY-N0404
-
-
- HY-N2423
-
-
- HY-176143
-
-
- HY-175785
-
|
|
Estrogen Receptor/ERR
Aryl Hydrocarbon Receptor
Apoptosis
MDM-2/p53
|
Cancer
|
|
X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer .
|
-
- HY-183697
-
|
|
FAK
|
Cancer
|
|
FAK-IN-30 is a focal adhesion kinase (FAK) inhibitor with moderate cytotoxicity against breast cancer cells. FAK-IN-30 can be used for the research of triple-negative breast cancer .
|
-
- HY-150695
-
|
|
Carbonic Anhydrase
Apoptosis
|
Cancer
|
|
hCAIX/XII-IN-5 (Coumarin 9a) a carbonic anhydrase (CA) inhibitor, and exhibits excellent hCA IX/XII selectivity (Ki=93.9 and 85.7 nM, respectively) over hCA I and hCA II. hCAIX/XII-IN-5 shows anti-proliferative activities to cancer cells. hCAIX/XII-IN-5 can delay cell cycle and induce apoptosis .
|
-
- HY-182617
-
|
|
SHP2
|
Cancer
|
|
NSC-13030 is a SHP2 inhibitor with an IC50 value of 3.2 μM. NSC-13030 reduces the proliferation and viability of breast cancer cells. NSC-13030 is applicable to breast cancer-related research .
|
-
- HY-161366
-
|
|
PI3K
|
Cancer
|
|
OMS14 is exhibits inhibitory activity for phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, which inhibits 19% PI3Kγ and 65% PIK3CD/PIK3R1 activity at 100 μM. OMS14 exhibits anticancer efficacy in various cancer cells .
|
-
- HY-124337
-
|
|
HDAC
|
Cancer
|
|
BG48 is a potent HDAC inhibitor. BG48 inhibits the enzymatic activity of HDAC1 and HDAC2 .
|
-
- HY-19992
-
|
Bromopyruvic acid; 3-BrPA; Hexokinase II Inhibitor II, 3-BP
|
Hexokinase
Apoptosis
Autophagy
|
Cancer
|
|
3-Bromopyruvate (Bromopyruvic acid) is an analogue of pyruvate and a potent hexokinase (HK)-II inhibitor with high tumor selectivity. 3-Bromopyruvate inhibits cell growth and induces apoptosis through interfering with glycolysis. 3-Bromopyruvate induces autophagy by stimulating ROS formation in breast cancer cells. Antimicrobial activities .
|
-
- HY-145143
-
|
|
Apoptosis
|
Cancer
|
|
anti-TNBC agent-1 is a potent anti-triple-negative breast cancer (TNBC) agent. anti-TNBC agent-1 exhibits potent activity against different breast cancer cells with IC50 values ranging from 0.20 μM to 0.27 μM. anti-TNBC agent-1 induces apoptosis of SUM-159 cells through mitochondria pathway and causes G1 phase arrest of SUM-159 cells .
|
-
- HY-168205
-
|
|
HSP
Apoptosis
|
Cancer
|
|
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
|
-
- HY-145556
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic .
|
-
- HY-168850
-
|
|
Apoptosis
|
Cancer
|
|
MTDH-SND1 blocker 2 (compound C19) is a potent MTDH-SND1 blocker with an IC50 value of 487 nM. MTDH-SND1 blocker 2 binds to the SND1 protein with a Kd value of 279 nM. MTDH-SND1 blocker 2 degrades SND1 protein. MTDH-SND1 blocker 2 shows antiproliferative activity and induces apoptosis. MTDH-SND1 blocker 2 has the potential for the research of breast cancer .
|
-
- HY-161153
-
|
|
Apoptosis
|
Cancer
|
|
Microtubule inhibitor 9 (Compound O-7) is a 2-Aryl-1H-benzo [d] imidazole derivative with in vitro anticancer activity. Microtubule inhibitor 9 can induce cell cycle arrest at the G2/M phase and early apoptosis. Microtubule inhibitor 9 inhibits cancer cell migration by inhibiting wound healing and colony formation .
|
-
- HY-P5834A
-
|
|
Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Boc-AEVD-CHO TFA is a Caspase 8 inhibitor. Boc-AEVD-CHO TFA significantly increases the frequencies of Nocodazole (HY-13520) or methyl methane sulfonate (MMS) induced micronuclei (MN) and micronucleated binucleates (MNCB) in PBMC by inhibiting cell apoptosis. Boc-AEVD-CHO TFA can be used for immune and inflammatory diseases research .
|
-
- HY-147854
-
|
|
Raf
Apoptosis
|
Cancer
|
|
B-Raf IN 9 (compound 8b) is a potent B-Raf inhibitor, with an IC50 of 24.79 nM. B-Raf IN 9 induces apoptosis and shows cell cycle arrest at G2/M phase. B-Raf IN 9 exhibits potent antitumor activity against human prostate cancer PC-3 cell line, with an IC50 of 7.83 µM .
|
-
- HY-13502
-
Mitoxantrone
Maximum Cited Publications
46 Publications Verification
Mitozantrone; NSC 301739
|
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity . Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502AS
-
|
Mitozantrone-d8dihydrochloride; NSC 301739-d8 dihydrochloride
|
Endogenous Metabolite
PKC
Apoptosis
Topoisomerase
Orthopoxvirus
Isotope-Labeled Compounds
|
Infection
Cancer
|
|
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502AR
-
|
Mitozantrone dihydrochloride (Standard); NSC 301739 dihydrochloride (Standard)
|
Reference Standards
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone (dihydrochloride) (Standard) is the analytical standard of Mitoxantrone (dihydrochloride). This product is intended for research and analytical applications. Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-170311
-
|
|
YAP
|
Cancer
|
|
YAP/TEAD-IN-1 (compound 4) is a potent YAP and TEAD inhibitor. YAP/TEAD-IN-1 shows antioxidant activity. YAP/TEAD-IN-1 shows antiproliferation activity for tumor cells. YAP/TEAD-IN-1 shows little cytotoxic activity for human normal cells .
|
-
- HY-13502R
-
|
Mitozantrone (Standard); NSC 301739 (Standard)
|
Reference Standards
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone (Standard) is the analytical standard of Mitoxantrone. This product is intended for research and analytical applications. Mitoxantrone is a potent topoisomerase II inhibitor. Mitoxantrone also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone shows antitumor activity . Mitoxantrone also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502A
-
|
Mitozantrone dihydrochloride; NSC 301739 dihydrochloride
|
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
Infection
Cancer
|
|
Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-146087
-
|
|
Autophagy
|
Cancer
|
|
Autophagy inducer 4 is a Magnolol-based Mannich base derivatives, which can be used as an anticancer agent. Autophagy inducer 4 suppresses cancer cells via inducing autophagy. Autophagy inducer 4 has 76-fold improvement in cytotoxicity against T47D cells compared with Magnolol. Autophagy inducer 4 also possesses suppressive effects on migration of T47D and Hela cancer cells .
|
-
- HY-125273
-
|
|
Fluorescent Dye
Phosphoglycerate Dehydrogenase (PHGDH)
|
Others
|
|
DNS-pE is a 3-phosphoglycerate dehydrogenase (PHGDH) inhibitor with a Ki of 7.4 μM. DNS-pE selectively and irreversibly covalently modifies endogenous PHGDH in live mammalian cells, its vinyl sulfone moiety acts as a fluorescence quencher that becomes highly fluorescent upon covalent modification of PHGDH. DNS-pE can be used as a fluorescent dye for live-cell imaging .
|
-
- HY-161857
-
|
|
Akt
mTOR
Caspase
CDK
|
Cancer
|
|
Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC) .
|
-
- HY-176288
-
|
|
Eukaryotic Initiation Factor (eIF)
Bcl-2 Family
Apoptosis
Ras
PERK
|
Cancer
|
|
eIF4E/eIF4G PPI-IN-1 is an eIF4E/eIF4G interaction inhibitor with a KD of 20.2 μM for eIF4E protein. eIF4E/eIF4G PPI-IN-1 plays an antitumor role in multiple modes of action including regulating the activity of eIF4E by inhibiting the Ras/MAPK/eIF4E signaling pathway, apoptosis and cell migration. eIF4E/eIF4G PPI-IN-1 suppresses the growth of HepG2 xenografts in nude mice and was relatively nontoxic to mice .
|
-
- HY-N5208
-
|
|
Others
|
Cancer
|
|
YM-216391 is an antitumor cyclic peptide that can be isolated from the cultured mycelium of Streptomyces nobilis JCM 4274. YM-216391 exhibits potent cytotoxic activity against a variety of human cancer cell lines and can be used in anticancer research .
|
-
- HY-N6607
-
-
- HY-N17570
-
|
|
Drug Derivative
|
Others
|
|
23α-Hydroxy-olean-12-en-3-one (Compound 15) is a pentacyclic triterpenoid, which is a natural derivative of the oleanane skeleton .
|
-
- HY-105414
-
|
|
Drug Derivative
|
Cancer
|
|
Esterbut-3 is a potent anticancer agent. Esterbut-3 inhibits cell proliferation. Esterbut-3 decreases the antigen expression of 115D8, 140C1 and increases the antigen expression of 123C3. Esterbut-3 induces cell cycle arrest at G0/G1 phase .
|
-
- HY-126437
-
|
|
Apoptosis
Bcl-2 Family
MDM-2/p53
VEGFR
|
Cardiovascular Disease
Cancer
|
|
Poly-L-lysine hydrobromide (MW 30000-70000) is a water-soluble synthetic polypeptide. Poly-L-lysine hydrobromide (MW 30000-70000) downregulates Bcl-2 and upregulates Bax and p53 proteins. Poly-L-lysine hydrobromide (MW 30000-70000) promotes Apoptosis and reduces VEGF expression. Poly-L-lysine hydrobromide (MW 30000-70000) shows anticancer activity against a variety of tumors. Poly-L-lysine hydrobromide (MW 30000-70000) can also be used as a coating material .
|
-
- HY-178004
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-73 is a potent and selective VEGFR-2 inhibitor, showing selectively inhibition of VEGFR-2 (IC50 = 0.0787 μM) over EGFR (IC50 = 1.31 μM). VEGFR-2-IN-73 demonstrates potent antiproliferative activity across multiple cancer cell lines. VEGFR-2-IN-73 induces G2/M and Pre-G1 phase arrest and significantly enhances apoptosis. VEGFR-2-IN-73 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-176560
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Raloxifene alkene (Compound 101) is a serum cholesterol clearance agent. Raloxifene alkene has significant anti-proliferation activity against breast adenocarcinoma cells. Raloxifene alkene effectively reduces serum cholesterol level without significant uterine weight and increase of number oieosinoohils in the stromallaver of ovarleclomized rat models. Raloxifene alkene can be used for post-menopausasyndrome, particularly osteoporosis, estrogen-dependent breast and uterine carcinoma research .
|
-
- HY-163808
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 237 (compound 13) is a potent anticancer agent. Anticancer agent 237 shows cytotoxicity. Anticancer agent 237 induces apoptosis and cell cycle arrest at the S and G2/M phases .
|
-
- HY-N15201
-
|
|
STAT
|
Cancer
|
|
Betavulgarin is an anticancer agent. Betavulgarin can be isolated from Sugar Beet (Beta vulgaris). Betavulgarin suppresses the proliferation, migration, colony formation, and mammosphere formation of breast cancer cells, and reduces the size of the CD44 +/CD24 − subpopulation and the expression of the self-renewal- related genes C-Myc, Nanog and Oct4. Betavulgarin promotes BCSCs death through the regulation of Stat3/Sox2 signaling .
|
-
- HY-143272
-
|
|
FGFR
|
Cancer
|
|
FGFR1 inhibitor-6 is a potent FGFR1 inhibitor with an IC50 value of 16.31 nM. FGFR1 inhibitor-6 shows cytotoxic activities. FGFR1 inhibitor-6 induces apoptosis and cell cycle arrest at pre-G1 and G2/M phase .
|
-
- HY-N6607R
-
|
|
Reference Standards
Leukotriene Receptor
NO Synthase
NF-κB
COX
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Tryptanthrin (Standard) is the analytical standard of Tryptanthrin. This product is intended for research and analytical applications. Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α .
|
-
- HY-146063
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 54 is a potent anticancer agent. Anticancer agent 54 shows antiproliferative activity. Anticancer agent 54 induces apoptosis and cell cycle arrest at G0/G1 phases. Anticancer agent 54 shows anticancer activity depends on DNA intercalation and ROS generation .
|
-
- HY-151172
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MDM2-p53-IN-15 is a MDM2-p53 inhibitor with an IC50 value of 26.1 nM. MDM2-p53-IN-15 inhibits the proliferation of various cancer cells and induces cell apoptosis. MDM2-p53-IN-15 can be used for the research of cancer .
|
-
- HY-N17294
-
|
|
Amylases
|
Cancer
|
|
Dendromoniliside D is a sesquiterpene glycoside. Dendromoniliside D can be isolated from D. nobile. Dendromoniliside D inhibits α-amylase. Dendromoniliside D can be used in the research of liver cancer, lung cancer, and breast cancer .
|
-
- HY-124798
-
|
|
mTOR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity .
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
|
-
- HY-N18047
-
|
|
Others
|
Cancer
|
|
Quinquefoloside Lc is a dammarane-type saponin that can be isolated from the leaves of Panax quinquefolium. Quinquefoloside Lc exhibits no significant inhibitory activity against human breast cancer cells. Quinquefoloside Lc can be used in studies related to human breast cancer .
|
-
- HY-N12999
-
|
|
Apoptosis
Bcl-2 Family
Caspase
MDM-2/p53
PARP
Amylases
|
Metabolic Disease
Endocrinology
Cancer
|
|
Stigmast-5-en-3-ol induces cancer cell apoptosis and inhibits proliferation by increasing the production of Bax, Caspase-9, p53, and PARP cleavage and reducing Bcl-xl expression. Stigmast-5-en-3-ol exhibits potent inhibitory activity against glucoamylase and α-amylase and possesses high antioxidant activity. Stigmast-5-en-3-ol can be used in the research of diseases such as leukemia, breast cancer, type 2 diabetes, and obesity .
|
-
- HY-130713
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-C2-amido-C2-COOH contains a CRBN ligand and a linker for recruiting E3 ubiquitin ligases. Thalidomide-C2-amido-C2-COOH can be used to design and synthesize PROTAC CDK2/9 Degrader-1 (HY-130709). PROTAC CDK2/9 Degrader-1 is applicable to prostate cancer-related research .
|
-
- HY-N0353R
-
|
(+)-Curdione (Standard)
|
Reference Standards
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
Heme Oxygenase (HO)
TGF-β Receptor
Indoleamine 2,3-Dioxygenase (IDO)
|
Others
|
|
Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression .
|
-
- HY-183549
-
|
|
Apoptosis
Ferroptosis
|
Cancer
|
|
Ferroptosis/apoptosis inducer-4 is a pyridine-hydrazone-derived Cu (II) complex and a synergistic inducer of ferroptosis and apoptosis. Ferroptosis/apoptosis inducer-4 exerts anti-tumor proliferation and anti-metastasis effects with extremely low systemic toxicity. Ferroptosis/apoptosis inducer-4 disrupts cellular redox homeostasis by depleting glutathione and generating hydroxyl radicals through the Cu 2+/Cu + redox cycle. Ferroptosis/apoptosis inducer-4 also triggers mitochondrial dysfunction and endoplasmic reticulum stress, which in turn lead to Ca 2+ release, mitochondrial Ca 2+ overload, and the formation of a ROS−Ca 2+ self-amplifying feedback loop. Ferroptosis/apoptosis inducer-4 can be used in studies related to cervical cancer .
|
-
- HY-N0353
-
|
(+)-Curdione
|
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
Heme Oxygenase (HO)
TGF-β Receptor
Indoleamine 2,3-Dioxygenase (IDO)
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression .
|
-
- HY-N19311
-
|
|
Bacterial
|
Cancer
|
|
3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone is an alkylated 2(1H)-pyrazinone derivative and cytotoxic agent found in the tunicate-derived actinomycete Streptomyces sp. Did-27.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone exhibits cytotoxic activity against cancer cells.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone can be used for the research of colorectal carcinoma, hepatocellular carcinoma, breast cancer .
|
-
- HY-178005
-
|
|
EGFR
VEGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-174 is a potent EGFR inhibitor (IC50 = 0.17 μM) and also displays VEGFR-2 inhibition (IC50 = 0.2007 μM). EGFR-IN-174 exhibits potent anticancer effects with low cytotoxicity to normal cells. EGFR-IN-174 induces G2/M and Pre-G1 phase arrest and significantly triggers apoptosis. EGFR-IN-174 can be used in cancer research, such as colorectal carcinoma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-162557
-
|
|
VEGFR
|
Cancer
|
|
VEGFR-2-IN-45 (compound 3j) is a potent inhibitor of VEGFR-2, with the IC50 of 0.2 μM. VEGFR-2-IN-45 plays an important role in cancer research .
|
-
- HY-N1506
-
|
|
Epigenetic Reader Domain
p38 MAPK
|
Cancer
|
|
Ganodermanontriol, a sterol isolated from Ganoderma lucidum, induces anti-inflammatory activity in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells through the expression of HO-1. Ganodermanontriol exhibits hepatoprotective activity .
|
-
- HY-N1506R
-
-
- HY-173164
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAF V600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity .
|
-
- HY-108999A
-
|
BWA770U
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-108999
-
|
BWA770U mesylate
|
DNA/RNA Synthesis
|
Cancer
|
|
Crisnatol (BWA770U) mesylate is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol mesylate shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-108999AR
-
|
BWA770U (Standard)
|
DNA/RNA Synthesis
Reference Standards
|
Cancer
|
|
Crisnatol (Standard) is the analytical standard of Crisnatol. This product is intended for research and analytical applications. Crisnatol (BWA770U) is an orally active and anticancer agent, and a member of the arylmethylaminopropanediol class of DNA intercalators. Crisnatol shows in vitro cytotoxicity against human breast cancer cells, but not normal human skin fibroblasts .
|
-
- HY-N17410
-
|
|
Drug Derivative
|
Others
|
|
Umbellatolide A is an 11-noriridoid found in the aerial parts of Morinda umbellata. Umbellatolide A shows no significant cytotoxic activity against human cancer cells .
|
-
- HY-D3215
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
Lyso-Cu (II) is a lysosome-targeted divalent copper ion probe. Lyso-Cu (II) is applicable to the research of Wilson's disease, Menkes disease and Alzheimer's disease .
|
-
- HY-N8210
-
|
|
Drug Metabolite
Autophagy
Apoptosis
Reactive Oxygen Species (ROS)
Keap1-Nrf2
MMP
Caspase
PARP
MDM-2/p53
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo .
|
-
- HY-176220
-
|
|
AUTACs
Autophagy
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
GPX4-AUTAC is a GPX4-targeting autophagy-mediated degrader (AUTAC). GPX4-AUTAC consists of an inhibitor ML162-yne (HY-153748), a degradation tag FBnG (HY-W073762) and a glycol linker (HY-W021401). GPX4-AUTAC promotes the ubiquitination of GPX4 by E3 ligase TRAF6, and enhances the binding with GPX4 and p62, leading to the selective autophagy-dependent degradation of GPX4. GPX4-AUTAC significantly induces ferroptosis and shows a potent anti-cancer activity in breast cancer cells, breast cancer-derived organoids (PDOs) and MDA-MB-231 tumor xenograft mice model, with potent synergistic effects when combined with Sulfasalazine (SAS) (HY-14655) or chemotherapy drugs (Paclitaxel (HY-B0015) or Cisplatin (HY-17394)) .
|
-
- HY-P991646
-
|
heMab
|
Transmembrane Glycoprotein
|
Cancer
|
|
ING-1 (heMab) is a high-affinity humanized monoclonal antibody against epithelial cell adhesion molecule (Ep-CAM). ING-1 is a transmembrane glycoprotein mediating Ca 2+. ING-1 binds to Ep-CAM on tumor cells and exhibits potent in vitro activity, targeting and inhibiting tumor growth and metastasis in mouse cancer models. ING-1 is useful in the research of breast, colorectal, and lung cancers, among other cancers .
|
-
- HY-W035150
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Chloro[1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene]copper(I) (Compound 1) is a NHC copper complex and anticancer agent. Chloro[1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene]copper(I) exhibits cytotoxic activity against breast cancer, lung cancer, melanoma, and glioma cells .
|
-
![Chloro[1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene]copper(I)](//file.medchemexpress.com/product_pic/hy-w035150.gif)
- HY-P992386
-
|
|
CD22
|
Cancer
|
|
IMM47 is a humanized monoclonal antibody targeting CD24, which acts as a competitive inhibitor of the CD24/Siglec-10 interaction and exhibits potent anti-tumor activity. The EC50 value of IMM47 for CD24 is 0.289 nM, and its Ka is 0.876 nM. IMM47 selectively binds to CD24-positive tumor cells and human granulocytes. By competitively blocking CD24/Siglec-10 binding, IMM47 abrogates the immunosuppressive signals of tumor cells, clears tumor cells through multiple effector pathways including ADCC, ADCP, ADCT and CDC, upregulates the levels of M1 and M2 macrophages in the spleen, promotes macrophage antigen presentation and induces tumor-specific memory immunity. IMM47 can be used in cancer-related research .
|
-
- HY-181558
-
|
|
Others
|
Cancer
|
|
Anticancer agent 303 is a selective, orally active anticancer agent belonging to the pyrazolopyridine derivatives. Anticancer agent 303 exhibits low cytotoxicity to healthy cells, with a selective window of approximately 2-fold between cancer cells and healthy cells. Anticancer agent 303 produces detectable systemic exposure in mice following intraperitoneal or oral administration. Anticancer agent 303 effectively inhibits the proliferation of prostate cancer and breast cancer cells .
|
-
- HY-185208
-
|
|
Antibody-Drug Conjugates (ADCs)
VEGFR
Apoptosis
|
Cancer
|
|
Bevacizumab vedotin is an antibody-drug conjugate (ADC). Bevacizumab vedotin blocks the VEGF/VEGFR pathway to exert anti-angiogenic effects. Bevacizumab vedotin exhibits anti-proliferative effects on cancer cells, promotes cancer cell apoptosis (Apoptosis), induces cancer cell cycle arrest, and possesses anti-migratory activity against breast cancer cells. Bevacizumab vedotin can be used in research related to glioma, hepatocellular carcinoma, and breast cancer .
|
-
- HY-N18195
-
|
|
Others
|
Cancer
|
|
Trichilin B is a limonoid compound found in the twigs and leaves of Trichilia connaroides. Trichilin B exhibits no in vitro cytotoxic activity against tumor cell lines .
|
-
- HY-N19873
-
|
|
Others
|
Cancer
|
|
Mukurozioside IIa is a sesquiterpene glycoside found in S. mukorossi. Mukurozioside IIa can be used for the research of breast cancer .
|
-
- HY-148483
-
|
|
IKK
|
Cancer
|
|
SR8185 is a potent and selective TBK1/IKKi dual inhibitor with IC50s of 3 nM and < 10 nM against IKKi and TBK1, respectively. SR8185 exhibits potent and broad spectrum antiproliferative effects on human cancer cells. SR8185 can be used for cancer research .
|
-
- HY-N10670
-
|
Methylpluviatolide
|
Apoptosis
|
Cancer
|
|
Bursehernin (Methylpluviatolide) is an antitumor agent. Bursehernin induces Apoptosis and cell cycle arrest at G2/M phase. Bursehernin shows anti-proliferative activity .
|
-
- HY-145849
-
|
|
VEGFR
|
Cancer
|
|
VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition .
|
-
- HY-169170
-
|
|
Apoptosis
DNA/RNA Synthesis
Epigenetic Reader Domain
PARP
|
Cancer
|
|
PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC50 values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .
|
-
- HY-N15612
-
|
|
Others
|
Cancer
|
|
5-Hydroxy-7-methoxycoumarin is a coumarin compound present in the whole plant of Euphorbia kansuensis, with an IC50 > 40 μM against five human cancer cell lines .
|
-
- HY-173166
-
|
|
PPAR
|
Cancer
|
|
PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier .
|
-
- HY-182260
-
|
|
Apoptosis
|
Cancer
|
|
Apoptotic agent-5 is an apoptosis inducer that releases large amounts of nitric oxide to induce cell apoptosis. Apoptotic agent-5 can be used in research related to triple-negative breast cancer .
|
-
- HY-175397
-
|
DFHBI-thalidomide
|
PROTACs
NF-κB
Early 2 Factor (E2F)
Bcl-2 Family
VEGFR
|
Cancer
|
|
Dth (DFHBI-thalidomide) is an RNA aptamer-based PROTAC degrader. Dth can degrade a variety of endogenous proteins (such as mCherry, p50, p65 and E2F1) by replacing the 3′ module on the RNA scaffold with the RNA aptamer corresponding to the target protein. Dth upregulates IκB-α and Bax, and downregulates Bcl-2 and VEGF. Dth generates green fluorescence upon binding to the Broccoli RNA aptamer, enabling the tracing of RNA scaffolds. Dth can be used in cancer-related research .
|
-
- HY-147785
-
|
|
Pim
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
|
Pim-1 kinase inhibitor 2 is a PIM-1 kinase inhibitor with a human IC50 of 0.63 μM. Pim-1 kinase inhibitor 2 exhibits high selectivity for cancer cells over normal cells. Pim-1 kinase inhibitor 2 induces apoptosis, increases active caspase-3 levels, upregulates BAX, downregulates Bcl-2, and elevates the Bax/Bcl-2 ratio. Pim-1 kinase inhibitor 2 suppresses cancer cell proliferation and induces cell cycle arrest. Pim-1 kinase inhibitor 2 can be used for the research of prostate carcinoma, hepatocellular carcinoma, and breast adenocarcinoma .
|
-
- HY-172470
-
|
|
Liposome
EGFR
|
Cancer
|
|
DSPE-PEG2000-GE11 is a nanocarrier component composed of DSPE and the EGFR-targeting peptide (GE11). DSPE-PEG2000-GE11 specifically binds to EGFR and mediates receptor-mediated endocytosis of micellar drug carriers. DSPE-PEG2000-GE11 can be used for drug delivery .
|
-
- HY-181893
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 60 (Compound 4a) is an Apoptosis inducer. Apoptosis inducer 60 induces concentration-dependent apoptosis in cells. Apoptosis inducer 60 exhibits moderate cytotoxicity against breast cancer cell lines .
|
-
- HY-172209
-
|
|
p38 MAPK
Apoptosis
Reactive Oxygen Species (ROS)
Caspase
Bcl-2 Family
|
Cancer
|
|
PPIA-IN-1 is a PPIA inhibitor with a Kd value of 0.52 μM. PPIA-IN-1 inhibits the PPIA/MAPK signaling pathway to exert antiproliferative activity. PPIA-IN-1 induces G0/G1 cell cycle arrest in cancer cells. PPIA-IN-1 upregulates the expression of Bax and caspase-3, downregulates Bcl-2 expression, and induces apoptosis in cancer cells. PPIA-IN-1 induces increased ROS levels, DNA damage, endoplasmic reticulum stress, and mitochondrial dysfunction in cancer cells. PPIA-IN-1 exhibits antitumor activity in a mouse colon cancer xenograft model. PPIA-IN-1 can be used for the research of colorectal cancer .
|
-
- HY-N0204
-
|
Anemoside A3
|
NF-κB
p38 MAPK
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Pulchinenoside A (Anemoside A3) is an orally active triterpenoid glycoside found in the root of Pulsatilla chinensis. Pulchinenoside A has amti-inflammation, antitumor, antidepressant, immunoregulatory and neuroprotective efrects. Pulchinenoside A activates NF-κB/MAPK signaling pathway. Pulchinenoside A can induce relaxing effect in rat renal arteries. Pulchinenoside A can be used for the researches of experimental autoimmune encephalomyelitis, breast cancer, depression and renovascular hypertension .
|
-
- HY-168565
-
|
|
Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
|
-
- HY-183801
-
|
|
Phosphatase
Apoptosis
|
Cancer
|
|
Cu2LCl2(H2O) acts as a proteasome inhibitor and protein tyrosine phosphatase inhibitor, with antiproliferative and apoptosis-inducing effects. Cu2LCl2(H2O) exhibits low cytotoxicity against normal cells and remarkable in vivo antitumor efficacy. Cu2LCl2(H2O) inhibits proteasome activity in colon cancer cells, and suppresses PTP1B and TCPTP activities in breast cancer cells. Cu2LCl2(H2O) can be used in the research of colon cancer, breast cancer and liver cancer .
|
-
- HY-N18247
-
|
|
Others
|
Cancer
|
|
12-Ethoxynimbolinin F is a nimbolinin-type limonoid found in the fruits of Melia toosendan. 12-Ethoxynimbolinin F shows low cytotoxic activity against cancer cells .
|
-
- HY-121706
-
|
|
HSP
|
Cancer
|
|
PU-20F (compound 59) is a Hsp90 inhibitor with an EC50 of 6.8 μM. PU-20F competes with Geldanamycin (HY-15230) for binding to Hsp90 and regulates the function of this molecular chaperone. PU-20F induces the degradation of oncogenic Her2 tyrosine kinase. PU-20F blocks the growth of breast cancer cells. PU-20F can be used in breast cancer-related research .
|
-
- HY-N19872
-
|
|
Drug Derivative
|
Cancer
|
Mukurozioside IIb is a sesquiterpene glycoside found in S. mukorossi and Sapindus rarak. Mukurozioside IIb can be used for the research of breast cancer .
|
-
- HY-157977
-
|
|
Biochemical Assay Reagents
Radionuclide-Drug Conjugates (RDCs)
MMP
|
Cancer
|
|
DOTA-GA-maleimide is a bifunctional chelator with protein conjugation and radiometal chelation capabilities. DOTA-GA-maleimide forms stable complexes with 111In and conjugates with proteins via maleimide chemistry. DOTA-GA-maleimide conjugates with LFn, enabling 111In radiolabeling of LFn through direct or pre-labeling strategies. Radiolabeled LFn is applicable to MMP activity imaging studies. DOTA-GA-maleimide is used in cancer research .
|
-
- HY-P5423D
-
|
|
Exosomes
|
Others
|
|
Ahx-GALA-Cys is a GALA peptide (HY-P5423) derivative with an N-terminal 6-aminohexanoic acid (Ahx) linker and a C-terminal cysteine residue. Ahx-GALA-Cys possesses strong covalent coupling capacity, which can be used to conjugate fluorophores and targeting ligands for investigating the surface functionalization of small extracellular vesicles (sEV) and lysosomal escape .
|
-
- HY-185565
-
|
|
PD-1/PD-L1
CXCR
|
Cancer
|
|
PD-1/PD-L1-IN-63 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 9.1 nM. PD-1/PD-L1-IN-63 blocks the PD-1/PD-L1 interaction, induces cancer cell death and inhibits tumor growth. PD-1/PD-L1-IN-63 can be used in the research of melanoma .
|
-
- HY-159059
-
|
|
c-Myc
Bcl-2 Family
Eukaryotic Initiation Factor (eIF)
Survivin
β-catenin
MMP
Interleukin Related
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Ganoderma Lucidum/Reishi Extract is a Ganoderma lucidum extract. Ganoderma Lucidum/Reishi Extract reduces the expression of c-Myc, BCL-2, BCL-XL, TERT, PDGFB, eIF4G, Survivin, β-catenin, and eIF4E. Ganoderma Lucidum/Reishi Extract downregulates the gene expression of MMP-9. Ganoderma Lucidum/Reishi Extract upregulates the expression of IL8. Ganoderma Lucidum/Reishi Extract is applicable to the research of inflammatory breast cancer. Ganoderma Lucidum is used in the research of various diseases, such as allergy, arthritis, hypertension, neurasthenia, inflammation, and cancer .
|
-
- HY-153789
-
|
|
PI5P4K
mTOR
|
Cancer
|
|
PI5P4Kγ-IN-1 is an ATP-competitive, highly selective chemical probe for PI5P4Kγ, with a Kd of 19 nM and an IC50 of 67 nM. PI5P4Kγ-IN-1 effectively inhibits PI5P4Kγ function and activates the mTORC1 signaling pathway in cells. PI5P4Kγ-IN-1 can be used in studies related to diseases such as breast cancer .
|
-
- HY-N12717
-
|
|
PAK
FASTK
HSP
p38 MAPK
NF-κB
NO Synthase
COX
HSV
Caspase
TNF Receptor
Fungal
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
Casuarinin is an orally active antiproliferative, anti-inflammatory, antifungal, virucidal and gastroprotective agent. Casuarinin upregulates the expression of p21/WAF1, Fas/APO‑1, mFasL, sFasL and HSP‑70, arrests cell cycle, induces apoptosis and inhibits cancer cell proliferation. Casuarinin inhibits TNF‑α-induced phosphorylation of MAPK and activation of NF‑κB, downregulates the expression of iNOS, NF‑κB, COX‑2 and ICAM‑1, and reduces the production of proinflammatory mediators. Casuarinin attenuates ethanol-induced activation of caspase‑3 and elevation of TNF‑α, inhibits the growth of Candida albicans, and inhibits HSV‑2. Casuarinin can be used in research related to mammary adenocarcinoma, inflammatory skin diseases, gastric ulcers, candidiasis and herpes simplex virus infections .
|
-
- HY-182780
-
|
|
Drug Derivative
|
Cancer
|
|
LSPN925 is an anticancer agent. LSPN925 exhibits cytotoxic and antiproliferative activities against tumor cells. LSPN925 has predicted oral bioavailability, low risks of hepatotoxicity and acute toxicity, and no risk of cardiotoxicity. LSPN925 can be used for the research of ovarian cancer, melanoma and breast cancer .
|
-
- HY-N11060A
-
|
(±)-PBI 344
|
Others
|
Cancer
|
|
(±)-Dehydrovomifoliol ((±)-PBI 344) is a norisoprenoid found in the rhizomes of Sinomenium acutum. (±)-Dehydrovomifoliolshows no significant cytotoxic activity against cancer cells .
|
-
- HY-146021
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .
|
-
- HY-183139
-
|
|
RAR/RXR
AP-1
|
Cancer
|
|
CD666 is a selective retinoic acid receptor-γ (RAR-γ) agonist with a Kd of 68 nM. CD666 inhibits proliferation of cancer cells and shows synergistical effects and anti-AP-1 activity with IFN-γ. CD666 can be used for the research of breast cancer .
|
-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
|
-
- HY-P11829
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer .
|
-
- HY-125351
-
|
|
Ceramidase
|
Metabolic Disease
|
|
SPT-IN-1 (compound 1) is an orally active and potent SPT (serine palmitoyl transferase) inhibitor, with an IC50 of 5.19 nM for hSPT1. SPT-IN-1 can be used for type 2 diabetes and dyslipidemia research .
|
-
- HY-146020
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines .
|
-
- HY-N17244
-
|
|
Others
|
Cancer
|
|
Polysimiaric acid B is a C31 triterpene found in Polyalthia simiarum and shows no activity against tumor cells .
|
-
- HY-143491
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells) .
|
-
- HY-182602
-
|
|
Microtubule/Tubulin
Cytochrome P450
|
Cancer
|
|
KOSN 1724 is an anticancer agent. KOSN 1724 disrupts tubulin activity, stabilizes microtubules, and inhibits cancer cells proliferation. KOSN 1724 inhibits cytochrome P450 3A4, CYP2C9, and CYP2C19 activity. KOSN 1724 can be used for the research of cancer .
|
-
- HY-172609
-
|
|
Phosphatase
Apoptosis
MDM-2/p53
Caspase
|
Metabolic Disease
Cancer
|
|
SL-176 is a PPM1D (Wip1) inhibitor. SL-176 inhibits lipid droplet formation, downregulates the mRNA and protein expression of PPARγ and C/EBPα, and blocks adipocyte differentiation. SL-176 induces G2/M cell cycle arrest, apoptosis and inhibits cell proliferation in breast cancer cells overexpressing PPM1D, and activates components of the p53 pathway. SL-176 suppresses tumor growth in a zebrafish model of neuroblastoma. SL-176 is applicable to research related to obesity, breast cancer and neuroblastoma .
|
-
- HY-P6292
-
|
|
PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
|
Neurological Disease
Cancer
|
|
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
|
-
- HY-176225
-
|
|
PROTACs
Src
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
BY13 is a SRC-3 PROTAC degrader with a DC50 of 0.031 μM. BY13 selectively blocks the ER signaling pathway over that of androgen receptor (AR)) through down-regulating ERα level. BY13 potently overcomes endocrine resistance in breast cancer by inducing cell cycle arrest in G1 phase and apoptosis, with superior effect over Fulvestrant (HY-13636). BY13 significantly inhibits the growth of drug-resistant breast tumors without obvious toxicity in LCC2 xenograft mice model . Pink: SRC-3 ligand (SI-2) (HY-101447); Blue: CRBN ligase ligand (HY-41547); Black: linker (HY-176226)
|
-
- HY-181660
-
|
|
PROTACs
IKK
Apoptosis
|
Cancer
|
|
PROTAC IKKβ degrader-1 is a IKKβ PROTAC degrader (DC50 = 7.15 μM). PROTAC IKKβ degrader-1 induces apoptosis (Apoptosis) in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 induces G1 phase cell cycle arrest in triple-negative breast cancer cells. PROTAC IKKβ degrader-1 exhibits antiproliferative activity against a variety of cells. PROTAC IKKβ degrader-1 is applicable for research related to cancers such as triple-negative breast cancer, colon cancer, liver cancer, pancreatic cancer .
|
-
- HY-W001520
-
|
|
EGFR
|
|
|
1-Methyl-1H-pyrrolopyridine is a 7-azaindole derivative that binds to the EGFR kinase domain. It inhibits the growth of breast cancer cells but shows no activity against lung cancer and liver cancer cells. 1-Methyl-1H-pyrrolopyridine can be used in breast cancer research .
|
-
![1-Methyl-1H-pyrrolo[2,3-b]pyridine](//file.medchemexpress.com/product_pic/hy-w001520.gif)
- HY-151980
-
|
|
Mps1
Apoptosis
|
Cancer
|
|
Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage .
|
-
- HY-136244
-
|
|
TGF-β Receptor
|
Cancer
|
|
PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer .
|
-
- HY-146433
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer .
|
-
- HY-N16866
-
-
- HY-150287A
-
|
ITS-X
|
Biochemical Assay Reagents
|
Others
|
|
Insulin-Transferrin-Selenium-Ethanolamine (ITS-X) is a cell culture supplement as well as a cell growth and adhesion promoter. Insulin-Transferrin-Selenium-Ethanolamine supports adhesion, pseudopodium formation, pseudopodium elongation and proliferation of adherent cancer cells in serum-free culture systems .
|
-
- HY-176404
-
|
|
HSP
|
Cancer
|
|
DDO-6691 is a heat shock protein 90 (HSP90) inhibitor. DDO-6691 has antiproliferative effects on a variety of tumor cells, with HCT-116 colon cancer cells being the most sensitive (IC50: 1.08 μM). DDO-6691 exhibits potent tumor growth inhibition in the HCT-116 xenograft mouse model .
|
-
- HY-125727
-
|
|
Fungal
|
Infection
Cancer
|
|
Globosuxanthone A is a dihydroxanthenone with obvious antifungal activity towards Fusarium graminearum, Fusarium solani, and Botrytis cinerea with MIC values of 4, 8, and 16 μg/mL, respectively. Anticancer activity .
|
-
- HY-172086
-
|
|
TrxR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
TrxR-IN-7 is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 3.5 μM. TrxR-IN-7 induces reactive oxygen species (ROS) generation and apoptosis in tumor cells. TrxR-IN-7 can be used for the research of liver cancer and breast cancer .
|
-
- HY-164548
-
|
|
HSP
Apoptosis
PI3K
Akt
NF-κB
|
Inflammation/Immunology
Cancer
|
|
WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases .
|
-
- HY-183108
-
|
|
Thymidylate Synthase
|
Cancer
|
|
Anticancer agent 315 is an antitumor agent. Anticancer agent 315 binds to the active pocket of thymidylate synthase via forming strong hydrogen bonds with Lys487 and Ala498, stabilizing the arrangement of the ligand within the pocket. Anticancer agent 315 inhibits the proliferation of tumor cells. Anticancer agent 315 can be used for the research of liver cancer and breast cancer .
|
-
- HY-181553A
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-45 (Compound 2b) is a PROTAC degrader targeting BRD4. PROTAC BRD4 Degrader-45 exhibits enhanced passive membrane permeability, stability in cell culture medium supplemented with 10% FBS, and higher intracellular concentrations in cancer cells .
|
-
- HY-183771
-
|
|
CDK
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Bcl-2 Family
Caspase
|
Cancer
|
|
CDK4/6-IN-28 is a potent, orally active, and selective CDK4/6 inhibitor IC50 values of 14.02 and 10.03 nM, respectively. CDK4/6-IN-28 inhibits breast cancer cell colony formation, migration, and proliferation. CDK4/6-IN-28 induces G1-phase cell cycle arrest and apoptosis in breast cancer cells. CDK4/6-IN-28 exhibits tumor inhibitory activity in breast cancer xenograft mouse models. CDK4/6-IN-28 can be used for the research of breast cancer .
|
-
- HY-135312
-
|
|
Estrogen Receptor/ERR
PROTACs
|
Cancer
|
|
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer .
|
-
- HY-176166
-
|
|
mTOR
PROTACs
Autophagy
|
Cancer
|
|
PD-M6 is a mTOR PROTAC degrader (DC50: 4.8 μM). PD-M6 promotes ubiquitination and degradation of mTOR. PD-M6 downregulates MAPKAP1 and CASTOR1, and induces Autophagy. PD-M6 inhibits the proliferation of cervical cancer, breast cancer and liver cancer cell lines. PD-M6 can be used for the research of cervical cancer, breast cancer and liver cancer .
|
-
- HY-181252
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp-IN-35 is a P-glycoprotein (P-gp) inhibitor. P-gp-IN-35 exhibits cytotoxicity against sensitive breast cancer and colorectal cancer cells, and can reverse multidrug resistance in breast cancer cells with P-gp overexpression. P-gp-IN-35 can be used in research related to multidrug-resistant breast cancer and colon cancer .
|
-
- HY-114354
-
|
BOD FL alkyne
|
Fluorescent Dye
|
Inflammation/Immunology
|
|
BODIPY (BOD) FL alkyne is an alkyne-containing BODIPY fluorophore derivative. BODIPY FL alkyne is a bioorthogonal labeling reagent with low toxicity and extremely low non-specific reactivity, and it is widely used in fluorescent bioimaging. BODIPY FL alkyne specifically labels azide groups on intracellular glycoconjugates mainly via strain-promoted azide-alkyne cycloaddition (SPAAC), or mediates site-specific conjugation with proteins such as IL-33, and supports positive cross-linking with other probes (e.g., DBCO-SCy5) for dual labeling. With the advantages of high specificity and low background interference, BODIPY FL alkyne can be used in the research of related diseases such as asthma, atopic dermatitis and inflammatory bowel disease .
|
-
- HY-160062
-
|
|
Mucin
|
Cancer
|
|
S2.2 aptamer sodium is a nucleic acid-based MUC1-binding aptamer with high affinity and low toxicity. Upon binding to its target, S2.2 aptamer sodium undergoes a conformational switch and restores fluorescence signal, serving as a targeted imaging agent for MUC1-positive cancer cells. S2.2 aptamer sodium enables targeted delivery to breast cancer cells with overexpressed MUC1. When formulated as the S2.2-PEG-MZF molecular probe, S2.2 aptamer sodium possesses the functions of T2 signal inhibition, magnetic field-induced hyperthermia and targeted magnetic resonance molecular imaging. In the S2.2-PEG-MZF/DOX nanoliposome, S2.2 aptamer sodium supports targeted thermochemotherapy, effectively inhibiting cancer cell proliferation and invasion as well as inducing apoptosis, and is widely used in studies related to breast cancer .
|
-
- HY-W585917
-
|
BFDGE·2HCl
|
Androgen Receptor
|
Metabolic Disease
|
|
Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) is an androgen receptor antagonist with a human IC50 of 18 μM. Bisphenol F bis(2-chloro-1-propanol) ether binds to the androgen receptor. Bisphenol F bis(2-chloro-1-propanol) ether (BFDGE·2HCl) can be used for research on hormonal activity .
|
-
- HY-P11792
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
CP2-CPP is a conjugate of p27 Analogue CP2 (HY-P11020) and Antennapedia Peptide (HY-P0307). CP2-CPP crosses cell membranes and localizes to live cell cytosol. CP2-CPP blocks SCF Skp2/Cks1-p27 interaction to inhibit p27 ubiquitination and degradation, restoring p27 levels and inhibiting cell proliferation. CP2-CPP can be used for the research of cancer, such as breast cancer .
|
-
- HY-181886
-
|
|
IRE1
PDGFR
c-Kit
|
Others
|
|
AK177 is an allosteric activator of IRE1α ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively. AK177 promotes IRE1α-mediated cleavage of XBP1 mRNA probe in a concentration-dependent manner and binds stably to its kinase domain. However, AK177 shows poor kinase selectivity, and due to poor membrane permeability at the cellular level, it induces no significant downstream pathway activation or antiproliferative activity .
|
-
- HY-183756
-
|
|
Cytochrome P450
Apoptosis
|
Cancer
|
|
CYP4Z1-IN-3 is a selective CYP4Z1 inhibitor with a human IC50 of 55.3 nM. CYP4Z1-IN-3 inhibits breast cancer cell migration and induces apoptosis. CYP4Z1-IN-3 can be used for the research of breast cancer .
|
-
- HY-P991922
-
|
|
Fc Receptor (FcR)
Complement System
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
AKIR001 is a high-affinity human IgG1 antibody targeting CD44v6. AKIR001 carries LALA-silencing mutations in its FcγR-binding domain to reduce FcγR and C1q interactions, minimizing tissue interactions and limiting CDC and ADCC risks. [ 177Lu] radiolabeled AKIR001, namely [ 177Lu]Lu-AKIR001, has anticancer activity against epidermoid carcinoma .
|
-
- HY-182054
-
|
|
Topoisomerase
Beclin1
Autophagy
Apoptosis
|
Cancer
|
|
Topoisomerase ll/ME-1-IN-1 (Compound 7a) is a Topoisomerase ll and ME-1 inhibitor with an IC50 of 5.03 μM against Topoisomerase ll. Topoisomerase ll/ME-1-IN-1 functionally inhibits the activity of Topoisomerase II and functionally blocks the activity of ME-1. Topoisomerase ll/ME-1-IN-1 induces Autophagy by upregulating the expression of Beclin-1 and LC3-II. Topoisomerase ll/ME-1-IN-1 promotes Apoptosis. Topoisomerase ll/ME-1-IN-1 exhibits antiproliferative activity against breast cancer cells and shows no toxicity to normal mammary epithelial cells. Topoisomerase ll/ME-1-IN-1 can be used in studies related to breast cancer (including triple-negative breast cancer) .
|
-
- HY-173156
-
|
|
Histone Methyltransferase
|
Cancer
|
|
UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research .
|
-
- HY-N13833
-
-
- HY-110329
-
|
|
Nuclear Hormone Receptor 4A/NR4A
|
Cancer
|
|
ML179 (SR-1309) is a inverse LRH1/NR5A2 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
|
-
- HY-N6651
-
|
|
STAT
Phosphatase
Apoptosis
Autophagy
p38 MAPK
EGFR
JAK
Bcl-2 Family
Survivin
Akt
mTOR
PARP
Caspase
Atg8/LC3
CDK
|
Cancer
|
|
Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation [1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC .
|
-
- HY-163468
-
|
|
Src
|
Cancer
|
|
SRC-3-IN-1 (compound SI-10) is a steroid receptor coactivator 3 (SRC-3) inhibitor (IC50=3.3 μM). SRC-3-IN-1 has good water solubility, oral bioavailability, and improved selectivity profile. SRC-3-IN-1 can be used in prostate cancer research .
|
-
- HY-P99605
-
|
PRS 343
|
EGFR
TNF Receptor
|
Cancer
|
|
Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
|
-
- HY-183060
-
|
|
|
Cancer
|
|
Antitumor agent-215 is an antitumor agent. Antitumor agent-215 occupies the binding pocket of thymidylate synthase and interacts with key catalytic residues. Antitumor agent-215 induces cancer cell apoptosis and cell cycle arrest, and inhibits cell proliferation. Antitumor agent-215 can be used in the research of breast cancer and colorectal cancer .
|
-
- HY-182896
-
|
|
TRP Channel
Calcium Channel
|
Neurological Disease
Cancer
|
|
HKC54 is a selective TRPV2 antagonist with an IC50 of 0.4 μM. HKC54 binds directly to TRPV2 and inhibits TRPV2-mediated calcium influx. HKC54 inhibits glioblastoma cell migration in vitro and breast cancer metastasis in vivo. HKC54 can be used for the research of breast cancer lung metastasis .
|
-
- HY-182307
-
|
|
Apoptosis
Caspase
TNF Receptor
|
Cancer
|
|
OH14 is a cellular FLICE-like inhibitory protein (cFLIP) inhibitor and TNF-related apoptosis-inducing ligand (TRAIL) sensitizer. OH14 selectively binds to the DED1 pocket of cFLIP, disrupting its recruitment to the TRAIL-death inducing signalling complex without affecting procaspase-8 recruitment to FADD, allowing procaspase-8 activation. OH14 promotes TRAIL-mediated apoptosis and impairs cell viability in breast cancer systems when combined with TRAIL. OH14 can be used for the research of breast cancer .
|
-
- HY-156228
-
|
|
Ras
|
Cancer
|
|
RGB-1 selectively binds to and stabilizes RNA G-quadruplex structures, and reduces the expression of the NRAS proto-oncogene in breast cancer cells. RGB-1 can serve as a tool for investigating the cellular functions of RNA G-quadruplex structures and identifying novel mRNA G-quadruplex-forming sequences. RGB-1 is applicable for breast cancer research .
|
-
- HY-182383
-
|
|
CDK
Apoptosis
|
Cancer
|
|
VMY-1-101 is a fluorescent cyclin-dependent kinase (CDK) inhibitor, with an excitation of 410 nm and emission of 512 nm. VMY-1-101 competitively inhibits ATP binding to CDKs. VMY-1-101 induces G2/M cell cycle arrest in human breast cancer cells. VMY-1-101 induces modest apoptosis in human breast cancer cells. VMY-1-101 blocks proliferation of human breast cancer cells, including multidrug resistance-positive cells, and is not a substrate for p-glycoprotein. VMY-1-101 localizes to the cytoplasm of human breast cancer cells. VMY-1-101 shows increased binding to human breast cancer tissue compared to fluorophore alone. VMY-1-101 can be used for the research of breast cancer .
|
-
- HY-N0554
-
|
|
HIV Protease
Monoamine Oxidase
|
Infection
Inflammation/Immunology
Cancer
|
|
Escin IA is an oral LOXL2 inhibitor and EMT inhibitor, with selectivity for LOXL2-expressing cells. Escin IA suppresses invasion, migration, and metastasis of breast cancer cells, and acts as the primary anti-TNBC metastasis constituent of Aesculus chinensis Bunge fruit saponin fraction. Escin IA can be used for the research of triple-negative breast cancer, acute inflammation, and ethanol-induced gastric mucosal lesions .
|
-
- HY-181657
-
|
|
EGFR
TNF Receptor
Interleukin Related
Apoptosis
|
Cancer
|
|
EGFR-IN-200 is an inhibitor targeting EGFR, TNF-α, and the IL-6/GP130 complex, which potently targets human EGFR (IC50=0.03 μM), TNF-α (IC50=3.1 μM), and the IL-6/GP130 complex (IC50=1.6 μM). EGFR-IN-200 binds to the ATP pocket of EGFR, the trimer interface of TNF-α, and the cytokine-receptor interface of IL-6/GP130, induces G2/M cell cycle arrest, apoptosis, and antiproliferative activity. EGFR-IN-200 exhibits high gastrointestinal absorbability, low BBB permeability, and complies with the Lipinski's rule. EGFR-IN-200 can be used for the research of lung cancer and breast adenocarcinoma .
|
-
- HY-183568
-
|
|
Methionine Adenosyltransferase (MAT)
|
Cancer
|
|
MAT2A-IN-26 is an orally active MAT2A inhibitor with a human IC50 of 17.53 nM. MAT2A-IN-26 inhibits the enzymatic activity of MAT2A, thereby reducing the levels of S-adenosylmethionine (SAM) and symmetric dimethylarginine (sDMA). MAT2A-IN-26 inhibits the proliferation of MTAP-deficient cancer cells and induces anti-tumor efficacy in xenograft models. MAT2A-IN-26 can be used in non-small cell lung cancer research .
|
-
- HY-N7712
-
-
- HY-P11640
-
|
|
Ligands for E3 Ligase
HIV
|
Infection
|
|
Vpr (1-14) is a viral protein R and acts as an accessory protein of HIV-1. Vpr (1-14) can binds to Cul4A-DDB1-DCAF1 E3 ligase complex and can be used as an E3 ligase-binding component in PROTACs. Vpr (1-14) can be used to synthesize PROTAC BRD4 Degrader-43 (HY-181164) .
|
-
- HY-172615
-
|
|
Molecular Glues
Epigenetic Reader Domain
|
Cancer
|
|
AMPTX-1 is a selective, orally active, covalent reversible BRD9 molecular glue degrader with a DC50 of 0.05 nM. AMPTX-1 selectively recruits BRD9 to the E3 ligase DCAF16. AMPTX-1 forms a ternary complex with BRD9 and a reversible covalent adduct with Cys58 on the surface of DCAF16. AMPTX-1 mediates BRD9 degradation via the proteasome and Cullin RING E3 ligase pathways. AMPTX-1 can be used in the research of solid tumors and hematological malignancies .
|
-
- HY-N7317
-
-
- HY-181232
-
|
|
ERK
|
Cancer
|
|
Anticancer agent 301 is an anticancer agent. Anticancer agent 301 selectively downregulates the phosphorylation level of ERK1/2 without affecting the NF-κB p65 subunit. Anticancer agent 301 exhibits antiproliferative activity against breast cancer cells and can be used in breast cancer-related research .
|
-
- HY-N1983
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
- HY-P991966
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse EGFR Antibody (7A7) ia an anti-mouse EGFR monoclonal antibody proposed to be the mouse equivalent of cetuximab. Anti-Human/Mouse EGFR Antibody (7A7) fails to induce tumor regression in the HPV38 tumor model where EGFR is not expressed in mice. Anti-Human/Mouse EGFR Antibody (7A7) can be used in EGFR-expressing HPV38 tumor-related studies .
|
-
- HY-181553
-
|
|
PROTACs
Epigenetic Reader Domain
|
Cancer
|
|
PROTAC BRD4 Degrader-44 (compound 2a) is a PROTAC degrader targeting BRD4 with passive membrane permeability. PROTAC BRD4 Degrader-44 maintains stability within 6 hours in medium supplemented with 10% FBS. PROTAC BRD4 Degrader-44 shows a trend of increasing intracellular accumulation within 6 hours, indicating reduced efflux .
|
-
- HY-182946
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-31 is an orally active and selective PI3Kα inhibitor. PI3Kα-IN-31 shows potent preference for mutant PI3Kα over wild-type PI3Kα. PI3Kα-IN-31 exerts antiproliferative effects in PI3Kα-mutant cancer cells. PI3Kα-IN-31 suppresses tumor growth in xenograft models. PI3Kα-IN-31 can be used for the research of breast cancer .
|
-
- HY-D3234
-
|
|
Fluorescent Dye
|
Others
|
|
Cy-AP is a hypoxia-sensitive near-infrared Fluorescent probe (emission wavelength: 725 nm). Cy-AP exhibits no fluorescence under normoxic microenvironments, while under hypoxic microenvironments, its azo group is reduced, releasing strong near-infrared fluorescence with an emission at 725 nm. Cy-AP enables visualization of intracellular hypoxic status through multiple imaging modalities .
|
-
- HY-181150
-
|
|
PI3K
|
Cancer
|
|
Hit20 is a PI3Kα selective inhibitor, inhibits PI3Kα kinase activity, suppresses PI3Kα phosphorylation. Hit20 suppresses proliferation, colony formation, migration, and invasion of colon cancer cells. Hit20 can be used for the research of colon cancer .
|
-
- HY-D3419
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
Neuro-DiO 4-chlorobenzenesulfonate is a hydrophobic C18 alkyl chain carbocyanine dye with green fluorescence, commonly used as a vascular marker, cell internalizer and deposition agent. Neuro-DiO 4-chlorobenzenesulfonate inserts its alkyl chain into the endothelial plasma membrane via liposome-mediated perfusion to achieve vascular labeling. Neuro-DiO chlorobenzenesulfonate can also stain the cell membrane and cytoplasm of cancer cells to assist in confocal microscopy observations. Neuro-DiO chlorobenzenesulfonate can be released from nanosponges and accumulate on the surface of mouse retina, then internalize into retinal ganglion cells, which is applicable to researches related to glaucoma and other diseases. It should be noted that during liposome-mediated vascular staining in mice, Neuro-DiO 4-chlorobenzenesulfonate may cause leakage of airway lavage fluid .
|
-
- HY-182695
-
|
|
5-HT Receptor
|
Neurological Disease
Cancer
|
|
AS2030680 is a blood-brain barrier-permeable, orally active 5-HT5A receptor antagonist. AS2030680 regulates 5-HT5A-related downstream signaling pathways, reduces the frequency of tumorsphere-initiating cells in breast cancer cells, and exerts procognitive activity in animal models. AS2030680 can be used to study cognitive impairments associated with dementia and schizophrenia, as well as breast cancer .
|
-
- HY-113293A
-
|
|
Endogenous Metabolite
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Estrone sulfate potassium is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate potassium is also a substrate of the OATP1B3 transporter. Estrone sulfate potassium can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate potassium stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate potassium is applicable to breast cancer-related research .
|
-
- HY-N0699
-
|
Dephnoretin; Thymelol
|
PKC
Influenza Virus
NOD-like Receptor (NLR)
Apoptosis
HBV
JNK
PI3K
Akt
CDK
Caspase
Bcl-2 Family
|
Infection
Inflammation/Immunology
Cancer
|
|
Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection .
|
-
- HY-163034
-
|
|
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
Antitumor photosensitizer-5 (Ru2) is a photosensitizer which effectively target tumor mitochondria with an IC50 of 0.3 μM for phototoxicity to A549 cells. Under 460 nm light irradiation, antitumor photosensitizer-5 induces the generation of reactive oxygen species and NADH depletion, causes mitochondrial damage and activation of caspase-3, inducing apoptosis and suppressing cell migration. Antitumor photosensitizer-5 has the potential to prevent the growth of malignant tumors, therefore, shows the potential to be applied to photodynamic therapy .
|
-
- HY-N18186
-
|
|
Others
|
Cancer
|
|
Neojiangyouaconitine is a diterpenoid alkaloid cytotoxin isolated from Aconitum soongaricum var. pubescens. Neojiangyouaconitine exhibits cytotoxic activity against human breast cancer, prostate cancer and lung cancer cells, with weak inhibitory effect on HeLa cells. Neojiangyouaconitine has the ability to kill specific tumor cell lines and can be applied to the research on the mechanisms of related cancers such as breast cancer, prostate cancer and lung cancer .
|
-
- HY-183716
-
|
|
Drug Derivative
|
Cancer
|
|
Mito-TP-2 is a triptolide (HY-32735) derivative. Mito-TP-2 exhibits concentration-dependent cytotoxicity in cancer cells. Mito-TP-2 is selectively driven and accumulated into the mitochondria of tumor cells by mitochondrial transmembrane potential and exerts specific mitochondrial toxicity. Mito-TP-2 can be used for the research of liver cancer, breast cancer, and non-small cell lung cancer .
|
-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
Bacterial
Apoptosis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
PARP
MMP
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
NF-κB
mTOR
Lactate Dehydrogenase
CDK
Glutathione Peroxidase
SOD
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
- HY-181940
-
|
|
Proteasome
|
Cancer
|
|
Berberine-amide-m-PhBA chloride (Compound 8b) is a selective anti-breast cancer agent. Berberine-amide-m-PhBA chloride may inhibit the proteasome by interacting with the 20S proteasome β5 subunit. Berberine-amide-m-PhBA chloride can be used in the research of breast cancer .
|
-
- HY-N18272
-
|
|
Others
|
Cancer
|
|
1α-Benzoyloxy-3α-acetoxyl-7α-hydroxy-12β-ethoxynimbolinin is a nimbolinin-type limonoid and cytotoxin, found in the fruits of Melia toosendan. 1α-Benzoyloxy-3α-acetoxyl-7α-hydroxy-12β-ethoxynimbolinin exhibits in vitro cytotoxicity against human hepatocellular carcinoma, human lung cancer, and human breast cancer cells. 1α-Benzoyloxy-3α-acetoxyl-7α-hydroxy-12β-ethoxynimbolinin can be used for the research of hepatocellular carcinoma, lung cancer, breast cancer .
|
-
- HY-182988
-
|
|
Liposome
|
Cancer
|
|
L-Arg-DSPE is an arginine-functionalized DSPE lipid containing free guanidine groups. L-Arg-DSPE serves as a component of NO-responsive degradable drug-loaded liposomal nanomotors (L-Arg@Lip-DOX), promoting drug deep tumor tissue penetration and cellular internalization. L-Arg-DSPE can be used for the research of drug delivery .
|
-
- HY-124627
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor ERα degrader (SERD) (IC50=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer .
|
-
- HY-W020955
-
|
Chloro(triphenylphosphine)gold(I)
|
Biochemical Assay Reagents
Apoptosis
DNA Alkylator/Crosslinker
Lipoxygenase
|
Cancer
|
|
Triphenylphosphinechlorogold (Chloro(triphenylphosphine)gold(I)) is a gold complex, Apoptosis inducer, and catalyst. Triphenylphosphinechlorogold exhibits high LOX inhibitory activity. Triphenylphosphinechlorogold induces cell cycle arrest and apoptosis. Triphenylphosphinechlorogold catalyzes the peroxidation of linoleic acid. A weak interaction exists between Triphenylphosphinechlorogold and DNA. Triphenylphosphinechlorogold displays antiproliferative activity against breast cancer cells .
|
-
- HY-108638
-
|
XI-011 hydrochloride
|
MDM-2/p53
Apoptosis
PARP
|
Cancer
|
|
NSC 146109 hydrochloride (XI-011 hydrochloride) is a p53 activator and MDMX inhibitor. NSC 146109 hydrochloride inhibits MDMX gene transcription, downregulates MDMX mRNA and protein levels, stabilizes p53 and activates the transcriptional activity of p53. NSC 146109 hydrochloride induces cancer cell apoptosis (apoptosis) and inhibits the growth of transformed cells. NSC 146109 hydrochloride inhibits the growth of xenograft tumors. NSC 146109 hydrochloride can be used in research related to breast cancer and cervical cancer .
|
-
- HY-183252
-
|
|
PKC
Apoptosis
Caspase
PARP
p38 MAPK
JNK
|
Cancer
|
|
ICA-1S is a specific PKC-ι inhibitor. ICA-1S can inhibit MAPK/JNK signaling pathway and downregulate the levels of c-Jun and TNF-α. ICA-1S inhibits the proliferation of breast cancer cells. ICA-1S induces apoptosis of breast cancer cells. ICA-1S can be used in breast cancer-related research .
|
-
- HY-N19464
-
|
|
PDI
|
Inflammation/Immunology
Cancer
|
|
Dicentrinone is an orally active PDI inhibitor with an IC50 value of 43.95 μM. Dicentrinone directly binds to PDI and suppresses cell proliferation and reduces cancer cell viability. Dicentrinone elicits anti-inflammatory and antioxidant effects by suppressing leukocyte migration, plasma leakage and paw edema, and scavenging free radicals. Dicentrinone can be used in the research of hepatoma, rheumatism and arthritis .
|
-
- HY-151424
-
|
|
Proteasome
Mitosis
|
Cancer
|
|
Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1 .
|
-
- HY-181093
-
|
|
Akt
EGFR
Apoptosis
Necroptosis
Caspase
Bcl-2 Family
MDM-2/p53
|
Cancer
|
|
EGFR-IN-191 is an anti-tumor agent targeting both EGFR and AKT. EGFR-IN-191 exerts its anti-tumor activity by inducing DNA damage, apoptosis, cell cycle arrest, and inhibition of the PI3K/AKT-EGFR signaling pathway in tumor cells. EGFR-IN-191 can be used in the study of tumors such as triple-negative breast cancer .
|
-
- HY-N3000A
-
|
|
JNK
IRE1
Akt
mTOR
YAP
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Fungal
Caspase
DNA/RNA Synthesis
|
Infection
Inflammation/Immunology
Cancer
|
|
6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .
|
-
- HY-183600
-
-
- HY-185373
-
|
Liposomal paclitaxel
|
Liposome
Microtubule/Tubulin
|
Cancer
|
|
Paclitaxel liposome is a liposome-encapsulated form of Paclitaxel (HY-B0015). Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel liposome is characterized by reduced acute toxicity, prolonged circulating half-life of paclitaxel, and enhanced accumulation at tumor sites. Paclitaxel liposome can be used in research related to breast cancer and locally advanced esophageal squamous cell carcinoma .
|
-
- HY-N19297
-
|
Prieurianin
|
Elastase
|
Inflammation/Immunology
Cancer
|
|
Endosidin1 (Prieurianin) is a Prieurianin with cleaved A and B rings. Endosidin1 is isolated from the roots of Aphanamixis polystachya. Endosidin1 inhibits superoxide anion production and Elastase release in neutrophils, with an IC50 >10 μg/mL. Endosidin1 exhibits mild cytotoxic activity against laryngeal cancer cells in vitro. Endosidin1 shows anti-inflammatory activity. Endosidin1 can be used in studies related to laryngeal cancer .\n
|
-
- HY-N9672
-
-
- HY-181060
-
|
|
Apoptosis
DNA/RNA Synthesis
Caspase
Bcl-2 Family
MDM-2/p53
|
Cancer
|
|
Apoptosis inducer 56 is an apoptosis inducer. Apoptosis inducer 56 induces DNA damage (upregulation of γH2AX and p-ATM expression) by minor groove binding. Apoptosis inducer 56 induces intrinsic apoptosis (upregulation of p53 and Bax/Bcl-2 ratio, cleaved caspase-7) via S-phase cell cycle arrest. Apoptosis inducer 56 shows selectivity for cancer cells over normal breast epithelial cells. Apoptosis inducer 56 can be used for the research of breast cancer .
|
-
- HY-182032
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species (ROS)
|
Cancer
|
|
VEGFR-2-IN-83 is a VEGFR-2 kinase inhibitor with an IC50 of 0.037 μM. VEGFR-2-IN-83 induces G0/G1 cell cycle arrest and apoptosis in breast cancer cells, and increases the production of reactive oxygen species (ROS). VEGFR-2-IN-83 is applicable to relevant research on breast cancer .
|
-
- HY-183779
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Antiangiogenic agent 10 is a potent orally active antiangiogenic agent with antiproliferative activity against breast cancer cells. Antiangiogenic agent 10 induces apoptosis via caspase-3 activation in breast cancer cells. Antiangiogenic agent 10 can be used for the research of breast cancer .
|
-
- HY-P11828
-
|
|
Survivin
Caspase
Apoptosis
|
Cancer
|
|
Anticancer agent 324 is a Survivin inhibitor. Anticancer agent 324 competitively binds to Survivin’s linker region and triggers proteasomal IAP degradation. Anticancer agent 324 blocks Borealin binding and chromosomal passenger complex formation, and inhibits Survivin-CRM1 nuclear-cytoplasmic transport. Anticancer agent 324 activates extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, activates executioner caspases-3 and caspases-7, and arrests cell cycle. Anticancer agent 324 can be used for the research of breast cancer .
|
-
- HY-N19821
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Gangaleoidin is a FOXM1 inhibitor with an IC50 of 2.8 μM. Gangaleoidin inhibits interaction between FOXM1’s DNA-binding domain and target DNA sequence, downregulates FOXM1 and downstream target gene CCNB1 at the transcriptional level. Gangaleoidin suppresses proliferation of FOXM1-overexpressing breast cancer cells. Gangaleoidin can be used for the research of breast cancer .
|
-
- HY-N19791
-
|
|
NF-κB
Fungal
Interleukin Related
|
Infection
Cancer
|
|
6-Methoxymellein, a phytoalexin, is a NF-κB inhibitor. 6-Methoxymellein reduces nuclear localization and DNA binding activity of NF-κB p65 and p50 subunits. 6-Methoxymellein decreases mRNA transcription and secretion of IL-6 and IL-8. 6-Methoxymellein reduces the proportion of CD44 +/CD24 − breast cancer cells, decreases expression of c-Myc, Sox-2 and Oct4, inhibits proliferation and migration of breast cancer cells, and reduces mammosphere growth. 6-Methoxymellein inhibits fungal growth of Trichophyton rubrum and Botrytis cinerea, and inhibits Trichophyton rubrum biofilm formation via hyphal disintegration. 6-Methoxymellein can be used for the research of breast cancer, tinea corporis, and carrot post-harvest storage rot .
|
-
- HY-P11766
-
|
GALA-cholesterol
|
Biochemical Assay Reagents
|
Cancer
|
|
GALA-chol is a cholesterol-conjugated pH-responsive fusion peptide that can serve as a delivery adjuvant. GALA-chol enhances the endocytosis of siRNA RET/PTC1-SQ nanoparticles, inhibits cell viability, and undergoes pH-responsive charge conversion in the acidic lysosomal environment, thereby promoting lysosomal escape of small extracellular vesicle (sEV) cargo. GALA-chol anchors to the sEV membrane and maintains the structural integrity and intrinsic homing activity of sEVs. GALA-chol can be used in studies related to adjuvant delivery .
|
-
- HY-D3233
-
|
|
Fluorescent Dye
|
Others
|
|
Ctrl-BDPS1 is a BODIPY-based control probe that shows no response to copper ions (exhibiting two emission peaks at 575 nm and 708 nm; the maximum excitation wavelength is at 627 nm). Ctrl-BDPS1 has no fluorescent response to Cu + .
|
-
- HY-B1095
-
|
|
Progesterone Receptor
Androgen Receptor
Glucocorticoid Receptor
GABA Receptor
|
Neurological Disease
Metabolic Disease
|
|
Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABAA receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders .
|
-
- HY-P11020
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the Cks1-Skp2-Skp1 complex (Kd = 32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer .
|
-
- HY-181687
-
|
|
HSP
CDK
|
Cancer
|
|
Hsp90-IN-46 is a Hsp90 inhibitor. Hsp90-IN-46 exhibits broad-spectrum antiproliferative activity against tumor cell lines. Hsp90-IN-46 inhibits breast cancer cell proliferation by reducing colony formation and downregulating the proliferation marker Ki-67. Hsp90-IN-46 inhibits Hsp90 and its ATPase activity, downregulates the downstream substrate oncoproteins HER2 and CDK4, and moderately induces the heat shock response. Hsp90-IN-46 shows significant antitumor activity in a mouse model of triple-negative breast cancer tumor xenografts. Hsp90-IN-46 can be used for research on various cancers including triple-negative breast cancer, leukemia, non-small cell lung cancer, colon cancer, ovarian cancer, renal cancer, prostate cancer .
|
-
- HY-183784
-
|
|
P2X Receptor
FAK
MMP
|
Cancer
|
|
P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research .
|
-
- HY-W743094
-
|
|
Drug Derivative
|
Inflammation/Immunology
Cancer
|
|
Methylstenbolone is a steroid and an anti-inflammatory agent. Methylstenbolone inhibits nitric oxide production in macrophages and exhibits cytotoxicity against breast cancer cells and normal fibroblasts. Methylstenbolone can be used for the research of inflammation and breast cancer .
|
-
- HY-B1309
-
|
AMAP
|
Drug Derivative
Mitochondrial Metabolism
|
Infection
Cancer
|
|
Metacetamol (AMAP) is an analog of Acetaminophen (HY-66005). Metacetamol induces dose-dependent necrosis in primary hepatocytes via glutathione depletion, mitochondrial damage, and formation of mitochondrial protein adducts. Metacetamol derivatives act as anticancer and antibacterial agents. Metacetamol can be used in studies related to breast cancer, bacterial infections, and fungal infections (candidiasis) .
|
-
- HY-183327
-
|
|
PI3K
mTOR
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Bcl-2 Family
Caspase
|
Cancer
|
|
PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC50 values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models .
|
-
- HY-176761
-
|
|
Apoptosis
Autophagy
Caspase
mTOR
|
Cancer
|
|
NSC647889 is an apoptosis and autophagy inducer. NSC647889 induces apoptosis, inhibits mTOR pathway and abrogates DNA synthesis. NSC647889 triggers LC3-positive vesicle formation, modulates AKT and 4EBP1 phosphorylation and shows heightened caspase-3 activation in multicellular spheroids. NSC647889 can be used for the research of solid cancer tumour, head-neck carcinoma, and colorectal cancer .
|
-
- HY-W778423
-
|
Dihydroxy Oxaliplatin-Pt(IV)
|
Drug Intermediate
|
Cancer
|
|
[Pt(DACH)(OH)2(ox)] is a Pt(IV) derivative of Oxaliplatin (HY-17371) with two axial hydroxido ligands, used as a precursor for synthesizing Pt(IV)-HDAC inhibitor prodrugs. [Pt(DACH)(OH)2(ox)] exerts cytotoxic activity against human cancer cells and accumulates in cancer cells for nuclear internalization and nuclear DNA platination. [Pt(DACH)(OH)2(ox)] can be used for the research of lung carcinoma, breast carcinoma, pancreatic carcinoma, colon carcinoma .
|
-
![[Pt(DACH)(OH)2(ox)]](//file.medchemexpress.com/product_pic/hy-w778423.gif)
- HY-N19938
-
|
|
Reactive Oxygen Species (ROS)
|
Others
|
|
Roseopurpurin B is a polyketide compound found in Aspergillus aculeatus DL1011 and Penicillium roseopurpureum (CMB-MF038), with DPPH scavenging activity. Roseopurpurin B shows no cytotoxicity against human cancer cells, and exhibits no growth inhibitory activity against Gram-positive or Gram-negative bacteria .
|
-
- HY-181832
-
|
|
AMPK
Apoptosis
|
Cancer
|
|
ASS1 activator 1 (Compound 10f) is a ASS1 activator with an EC50 of 1.90 μM. ASS1 activator 1 enhances the activity of ASS1 and promotes AMPK phosphorylation. ASS1 activator 1 induces cell Apoptosis. ASS1 activator 1 exhibits anticancer activity against triple-negative breast cancer, colorectal cancer and liver cancer .
|
-
- HY-183090
-
|
|
VEGFR
Apoptosis
Topoisomerase
EGFR
|
Cancer
|
|
EGFR/VEGFR2-IN-13 is a multi-target inhibitor, with an IC50 of 0.98 µM against VEGFR-2, 1.01 µM against EGFR, and 1.94 µM against topoisomerase II. EGFR/VEGFR2-IN-13 induces cell cycle arrest and apoptosis in tumor cells. As an anticancer agent, EGFR/VEGFR2-IN-13 exhibits cytotoxicity against cancer cells. EGFR/VEGFR2-IN-13 can be used in research related to breast cancer, colon cancer, and liver cancer .
|
-
- HY-W420454
-
|
|
Others
|
Inflammation/Immunology
Cancer
|
|
Danshenspiroketallactone is a lactone found in the roots of Salvia miltiorrhiza. Danshenspiroketallactone shows no anti-inflammatory and anticancer activity .
|
-
- HY-106021
-
|
ILX651 free base
|
Microtubule/Tubulin
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Tasidotin (ILX651 free base) is a tubulin inhibitor and competitive Prolyl Endopeptidase (PREP) inhibitor, with an IC50 of 10 μM against bovine tubulin. Tasidotin exhibits high cerebrospinal fluid penetration in non-human primates. Tasidotin antagonizes microtubule assembly and induces an extended assembly lag phase, thereby inhibiting mitosis and cell proliferation, and exerts cytotoxic and oncolytic effects on cancer cells. Tasidotin is metabolized into polypeptides and proline inside cells, and its in vivo metabolism is mediated by prolyl endopeptidase. Tasidotin can be applied in research related to Burkitt's lymphoma, breast cancer, leukemia, melanoma, central nervous system malignancies and various solid tumors .
|
-
- HY-N19113
-
|
|
Endogenous Metabolite
|
Infection
Cancer
|
|
Emindole SB is an anticancer agent. Emindole SB can be isolated from Penicillium species. Emindole SB exerts anticancer effects against ovarian cancer, breast cancer and lymphoma. Emindole SB shows no toxicity to Caenorhabditis elegans. Emindole SB can be used in studies related to ovarian cancer, lymphoma and breast cancer .
|
-
- HY-N10342
-
|
|
Apoptosis
Bcl-2 Family
Caspase
PARP
Reactive Oxygen Species (ROS)
Bacterial
PI3K
Akt
NF-κB
P-glycoprotein
|
Infection
Cancer
|
|
Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp. . Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections .
|
-
- HY-181493
-
|
|
VEGFR
Reactive Oxygen Species (ROS)
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-81 is a thiazole-based isoquinolin-1(2H)-one derivative and an VEGFR-2 inhibitor with IC50 of 1.94 μM. VEGFR-2-IN-81 exhibits significant selective cytotoxicity against colorectal cancer cells (IC50 = 7.75 μM). VEGFR-2-IN-81 exerts anti-colorectal cancer effects by inducing apoptosis, elevating intracellular ROS levels and reducing mitochondrial transmembrane potential. VEGFR-2-IN-81 can be used for the research of colorectal cancer, lung cancer, breast cancer, liver cancer .
|
-
- HY-W778375
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Hesperetin triacetate is an active compound with anti-inflammatory and anti-tumor activities. Hesperetin triacetate inhibits bovine serum albumin denaturation in vitro. Hesperetin triacetate inhibits carrageenan-induced paw swelling in mice in vivo. Hesperetin triacetate exhibits anti-proliferative activity against breast cancer cells. Hesperetin triacetate induces DNA degradation and apoptosis in breast cancer cells. Hesperetin triacetate can be used in studies related to breast cancer and inflammation .
|
-
- HY-107835
-
|
FCR 2769
|
Environmental Pollutants
Apoptosis
Bcl-2 Family
Parasite
Insecticide
|
Infection
Cancer
|
|
Flumethrin (FCR 2769) is a pyrethroid insecticide and acaricide . Flumethrin targets voltage-gated sodium channels and estrogen receptor α (ERα). Flumethrin induces cytotoxicity, apoptosis, genotoxicity and DNA damage in breast cancer cells by regulating the expression of BCL2, BAX, TP53 and P21 genes. Flumethrin is applicable to relevant studies on ectoparasite infections (tick and flea burdens) in dogs and cats, as well as breast cancer .
|
-
- HY-181720
-
|
|
Caspase
PARP
Apoptosis
|
Cancer
|
|
Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer .
|
-
- HY-183804
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-16 is an orally active ERα PROTAC degrader with a DC50 of 1.4 nM and an IC50 of 1.9 nM. PROTAC ER Degrader-16 inhibits ER-dependent breast cancer cell proliferation and exerts anti-tumor effects in mouse models. PROTAC ER Degrader-16 can be used for breast cancer research .
|
-
- HY-N0660
-
|
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
|
-
- HY-126756
-
|
|
Phosphorylase
|
Metabolic Disease
Cancer
|
|
Amorphin is a phosphorylase b with glycogen metabolism activity. Amorphin binds directly to alpha-actinin, with alpha-actinin mediating its binding to actin filaments. Amorphin can be used for the research of McArdle’s disease and breast cancer .
|
-
- HY-108964
-
-
- HY-N12586
-
|
|
ERK
Reactive Oxygen Species (ROS)
COX
PGE synthase
STAT
HCV
HCV Protease
|
Infection
Neurological Disease
Cancer
|
|
Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC50=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease .
|
-
- HY-133668
-
|
|
Drug Metabolite
Cytochrome P450
PPAR
|
Endocrinology
Cancer
|
|
Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms .
|
-
- HY-182245
-
|
|
Microtubule/Tubulin
Carbonic Anhydrase
Apoptosis
MDM-2/p53
|
Cancer
|
|
Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
|
-
- HY-161618
-
|
|
JAK
EGFR
PI3K
IGF-1R
GSK-3
|
Inflammation/Immunology
Endocrinology
|
|
MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
|
-
- HY-N6005
-
|
|
Bacterial
Fungal
Apoptosis
Bcl-2 Family
|
Infection
Metabolic Disease
Cancer
|
|
Methyl caffeate is a phenylpropanoid, antibacterial agent, and Apoptosis-inducing agent. Methyl caffeate can be isolated from the flowers of peach Prunus persica (L.). Methyl caffeate upregulates the expression of pro-apoptotic proteins Bid, Bax and p53, and downregulates the expression of anti-apoptotic protein BCL-2. Methyl caffeate downregulates SASP factors. Methyl caffeate enhances glucose-stimulated insulin secretion. Methyl caffeate inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, fungi, and Mycobacterium tuberculosis strains. Methyl caffeate can be used in studies related to breast cancer, type 2 diabetes, and tuberculosis .
|
-
- HY-N8250
-
|
|
Topoisomerase
PEPCK
|
Metabolic Disease
|
|
cis-THSG is a selective and orally active DNA topoisomerase II inhibitor with no activity against DNA topoisomerase I. cis-THSG suppresses transcription of PEPCK. cis-THSG reduces blood glucose levels, ameliorates glucose intolerance, and alleviates insulin resistance in high fat diet-induced diabetic male CF-1 mice. cis-THSG can be used for the research of type 2 diabetes mellitus .
|
-
- HY-153468
-
|
TEQ103; Sera2
|
Sodium Channel
TRP Channel
|
Cancer
|
|
ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer .
|
-
- HY-75625
-
|
4-Methoxysalicylic Acid
|
Monocarboxylate Transporter
Apoptosis
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
2-Hydroxy-4-methoxybenzoic acid is an orally active inhibitor of MCT-1 and MCT-4, as well as a plant biomarker. 2-Hydroxy-4-methoxybenzoic acid can be isolated from roots. 2-Hydroxy-4-methoxybenzoic acid induces Apoptosis and loss of mitochondrial membrane potential. 2-Hydroxy-4-methoxybenzoic acid exhibits anticancer activity against breast cancer. 2-Hydroxy-4-methoxybenzoic acid normalizes lactic acid levels. 2-Hydroxy-4-methoxybenzoic acid neutralizes viper venom and attenuates its lethal, hemorrhagic, coagulant and anticoagulant activities in male albino mice. 2-Hydroxy-4-methoxybenzoic acid possesses antihyperlipidemic, antidiabetic and hepatoprotective activities .
|
-
- HY-N13838
-
|
|
Bacterial
|
Infection
|
|
8,9-Dehydro-7,9-diisobutyryloxythymol is a Thymol (HY-N6810) derivative, as well as an antibacterial agent. 8,9-Dehydro-7,9-diisobutyryloxythymol can be found in the aerial parts of Ageratina adenophora, with selective activity against Gram-positive bacterial strains including Bacillus cereus. 8,9-Dehydro-7,9-diisobutyryloxythymol does not exhibit detectable in vitro cytotoxic activity against human cancer cell lines. 8,9-Dehydro-7,9-diisobutyryloxythymol can be used for the research of bacterial infection .
|
-
- HY-180416
-
|
|
Antibiotic
|
Cancer
|
|
TMC-169 is a potent antibiotic of the Aspochalasin group that can be isolated from Aspergillus flavipes. TMC-169 exhibits anti-tumor activity against multiple cancer cells. TMC-169 can be used for the research of cancer, such as hematologic malignancies, non-small cell lung cancer, breast cancer, and glioma .
|
-
- HY-182264
-
|
Nordihydroguaiaretic acid tetrapivalate
|
IGF-1R
EGFR
Drug Metabolite
|
Cancer
|
|
Masoprocol tetrapivalate (Nordihydroguaiaretic acid tetrapivalate) is a catecholic butane metabolite and also a tyrosine kinase activity inhibitor of IGF-1R and EGFR. Masoprocol tetrapivalate regulates tyrosine kinase signaling pathways associated with cell proliferation. Masoprocol tetrapivalate can be used in the research of proliferative diseases, including malignant, precancerous or benign cancers, and solid tumors .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-114354
-
|
BOD FL alkyne
|
Fluorescent Dye
|
|
BODIPY (BOD) FL alkyne is an alkyne-containing BODIPY fluorophore derivative. BODIPY FL alkyne is a bioorthogonal labeling reagent with low toxicity and extremely low non-specific reactivity, and it is widely used in fluorescent bioimaging. BODIPY FL alkyne specifically labels azide groups on intracellular glycoconjugates mainly via strain-promoted azide-alkyne cycloaddition (SPAAC), or mediates site-specific conjugation with proteins such as IL-33, and supports positive cross-linking with other probes (e.g., DBCO-SCy5) for dual labeling. With the advantages of high specificity and low background interference, BODIPY FL alkyne can be used in the research of related diseases such as asthma, atopic dermatitis and inflammatory bowel disease .
|
-
- HY-D3215
-
|
|
Fluorescent Dye
|
|
Lyso-Cu (II) is a lysosome-targeted divalent copper ion probe. Lyso-Cu (II) is applicable to the research of Wilson's disease, Menkes disease and Alzheimer's disease .
|
-
- HY-D3234
-
|
|
Fluorescent Dye
|
|
Cy-AP is a hypoxia-sensitive near-infrared Fluorescent probe (emission wavelength: 725 nm). Cy-AP exhibits no fluorescence under normoxic microenvironments, while under hypoxic microenvironments, its azo group is reduced, releasing strong near-infrared fluorescence with an emission at 725 nm. Cy-AP enables visualization of intracellular hypoxic status through multiple imaging modalities .
|
-
- HY-D3419
-
|
|
Fluorescent Dye
|
|
Neuro-DiO 4-chlorobenzenesulfonate is a hydrophobic C18 alkyl chain carbocyanine dye with green fluorescence, commonly used as a vascular marker, cell internalizer and deposition agent. Neuro-DiO 4-chlorobenzenesulfonate inserts its alkyl chain into the endothelial plasma membrane via liposome-mediated perfusion to achieve vascular labeling. Neuro-DiO chlorobenzenesulfonate can also stain the cell membrane and cytoplasm of cancer cells to assist in confocal microscopy observations. Neuro-DiO chlorobenzenesulfonate can be released from nanosponges and accumulate on the surface of mouse retina, then internalize into retinal ganglion cells, which is applicable to researches related to glaucoma and other diseases. It should be noted that during liposome-mediated vascular staining in mice, Neuro-DiO 4-chlorobenzenesulfonate may cause leakage of airway lavage fluid .
|
-
- HY-D3233
-
|
|
Fluorescent Dye
|
|
Ctrl-BDPS1 is a BODIPY-based control probe that shows no response to copper ions (exhibiting two emission peaks at 575 nm and 708 nm; the maximum excitation wavelength is at 627 nm). Ctrl-BDPS1 has no fluorescent response to Cu + .
|
| Cat. No. |
Product Name |
Type |
-
- HY-126437
-
|
|
Biochemical Assay Reagents
|
|
Poly-L-lysine hydrobromide (MW 30000-70000) is a water-soluble synthetic polypeptide. Poly-L-lysine hydrobromide (MW 30000-70000) downregulates Bcl-2 and upregulates Bax and p53 proteins. Poly-L-lysine hydrobromide (MW 30000-70000) promotes Apoptosis and reduces VEGF expression. Poly-L-lysine hydrobromide (MW 30000-70000) shows anticancer activity against a variety of tumors. Poly-L-lysine hydrobromide (MW 30000-70000) can also be used as a coating material .
|
-
- HY-B0812
-
|
SSA dihydrate
|
Biochemical Assay Reagents
|
|
5-Sulfosalicylic acid dihydrate is a sulfonated salicylic acid derivative. 5-Sulfosalicylic acid dihydrate is effective against the breast cancer cell line, MCF-7, with less toxicity . 5-Sulfosalicylic acid dihydrate has antioxidant activities .
|
-
- HY-172470
-
|
|
Biochemical Assay Reagents
|
|
DSPE-PEG2000-GE11 is a nanocarrier component composed of DSPE and the EGFR-targeting peptide (GE11). DSPE-PEG2000-GE11 specifically binds to EGFR and mediates receptor-mediated endocytosis of micellar drug carriers. DSPE-PEG2000-GE11 can be used for drug delivery .
|
-
- HY-113319
-
|
|
Biochemical Assay Reagents
|
|
β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
-
- HY-150287A
-
|
ITS-X
|
Biochemical Assay Reagents
|
|
Insulin-Transferrin-Selenium-Ethanolamine (ITS-X) is a cell culture supplement as well as a cell growth and adhesion promoter. Insulin-Transferrin-Selenium-Ethanolamine supports adhesion, pseudopodium formation, pseudopodium elongation and proliferation of adherent cancer cells in serum-free culture systems .
|
-
- HY-W020955
-
|
Chloro(triphenylphosphine)gold(I)
|
Biochemical Assay Reagents
|
|
Triphenylphosphinechlorogold (Chloro(triphenylphosphine)gold(I)) is a gold complex, Apoptosis inducer, and catalyst. Triphenylphosphinechlorogold exhibits high LOX inhibitory activity. Triphenylphosphinechlorogold induces cell cycle arrest and apoptosis. Triphenylphosphinechlorogold catalyzes the peroxidation of linoleic acid. A weak interaction exists between Triphenylphosphinechlorogold and DNA. Triphenylphosphinechlorogold displays antiproliferative activity against breast cancer cells .
|
-
- HY-159059
-
|
|
Biochemical Assay Reagents
|
|
Ganoderma Lucidum/Reishi Extract is a Ganoderma lucidum extract. Ganoderma Lucidum/Reishi Extract reduces the expression of c-Myc, BCL-2, BCL-XL, TERT, PDGFB, eIF4G, Survivin, β-catenin, and eIF4E. Ganoderma Lucidum/Reishi Extract downregulates the gene expression of MMP-9. Ganoderma Lucidum/Reishi Extract upregulates the expression of IL8. Ganoderma Lucidum/Reishi Extract is applicable to the research of inflammatory breast cancer. Ganoderma Lucidum is used in the research of various diseases, such as allergy, arthritis, hypertension, neurasthenia, inflammation, and cancer .
|
-
- HY-113319R
-
|
|
Biochemical Assay Reagents
|
|
β-D-Fructose, (Standard) is the analytical standard of β-D-Fructose (HY-113319R). This product is intended for research and analytical applications. β-D-Fructose is a monosaccharide. Derivatives synthesized using β-D-Fructose as the sugar backbone exhibit potent and selective antiproliferative activity against breast cancer MCF-7 cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W016887
-
|
H-Gly-Pro-OH; Gly-Pro
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
Cancer
|
|
Glycyl-L-proline (H-Gly-Pro-OH) is a dipeptide. Glycyl-L-proline can induce MCF-7 cells apoptosis. Glycyl-L-proline can enhance the inhibitory effect of the PRODH/POX knockout on collagen and DNA biosynthesis. Glycyl-L-proline can inhibit Gly-Sar and L-proline transport. Glycyl-L-proline can be used for the researches of cancer and metabolic disease, such as breast cancer .
|
-
- HY-P4210
-
|
ALRN-6924; MP-4897
|
MDM-2/p53
|
Cancer
|
|
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .
|
-
- HY-P6292
-
|
|
PACAP Receptor
PKA
ERK
PI3K
Akt
GSK-3
|
Neurological Disease
Cancer
|
|
KS-133 is a bicyclic peptide with VIPR2 antagonistic activity that can cross the blood-brain barrier. KS-133 selectively blocks VIPR2-mediated Gq/Ca, Gs/cAMP, cAMP/PKA/ERK and PI3K/AKT/GSK3β signaling pathways. KS-133 inhibits VIPR2 agonist-induced CREB phosphorylation in the prefrontal cortex of mice. KS-133 shifts the polarization direction of macrophages toward M1. KS-133 attenuates cancer cell proliferation and reduces the cell cycle distribution level at the S-M phase. KS-133 exerts antitumor effects in a mouse model of colorectal cancer. KS-133 reverses cognitive decline in mouse models of psychiatric disorders. KS-133 can be used for research related to schizophrenia, colorectal cancer and breast cancer .
|
-
- HY-P5755
-
|
|
Peptides
|
Cancer
|
|
SWELYYPLRANL-NH2 is an E-cadherin and N-cadherin antagonist. SWELYYPLRANL-NH2 inhibits phage clone binding to E- or N-cad/Fc chimeric protein (IC50: 0.7 and 0.09 μM respectively). SWELYYPLRANL-NH2 inhibits cell aggregation. SWELYYPLRANL-NH2 can be used to promote drug delivery through epithelial and endothelial permeability barriers .
|
-
- HY-120234
-
|
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia .
|
-
- HY-P11020
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the Cks1-Skp2-Skp1 complex (Kd = 32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer .
|
-
- HY-P5033
-
|
|
Bacterial
|
Cancer
|
Cyclo(Gly-His) is a liposome-encapsulated cyclic dipeptide with antimicrobial and anticancer activity. Cyclo(Gly-His) has cytotoxicity for HeLa and MCF-7 cell with IC50 values of 1.699 mM and 0.358 mM, respectively. Cyclo(Gly-His) can be used for the research of drug delivery systems .
|
-
- HY-P10790
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Breast cancer targeting peptide 18–4 is a KRT1 receptor-targeting peptide, with a Kd of 0.98 μM. The amino acid sequence of Breast cancer targeting peptide 18–4 is WxEAAYQrFL, and it is an analogue of P160 peptide (HY-P10789). When covalently conjugated with the anticancer peptide MccJ25, Breast cancer targeting peptide 18–4 significantly increases the cellular uptake of MccJ25 in breast cancer cells and enhances its anticancer activity. The covalent conjugate exhibits IC50 values of 14.2, 20, and 25 μM against MCF-7, MDA-MB-435, and MDA-MB-435-MDR cells, respectively .
|
-
- HY-P10785
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Iturin A-2 is a cyclic lipopeptide discovered in B. subtilis and exhibits inhibitory activity against the plant pathogenic fungus P. expansum (MIC = 8 µg/disk). Iturin A-2 is cytotoxic to MCF-7 and BT474 breast cancer cells, as well as HeLa cervical cancer cells, with IC50 values of 66.81, 95.04, and 77.5 µg/mL, respectively. In greenhouse studies, Iturin A-2 at concentrations of 100 and 300 mg/kg Iturin A-2 reduces the lesion area of southern corn leaf blight caused by B. maydis, and in field studies, concentrations of 300 and 500 mg/kg Iturin A-2 reduce the incidence of the disease. Iturin A-2 (12.5 µg/mL) inhibits cell division, but not nuclear division, in isolated fertilized starfish eggs .
|
-
- HY-P11102
-
|
|
Bacterial
Fungal
HIV
Parasite
|
Infection
Cancer
|
|
Temporin-Sha is an antibacterial peptide with extensive biological activity. Temporin-Sha exhibits broad-spectrum antibacterial activity (e.g., against L. ivanovii, MIC = 6.25 μM), and is effective against Gram-negative bacteria (such as Escherichia coli, MIC = 10 μM), including drug-resistant strains (such as Methicillin (HY-121544)-resistant Staphylococcus aureus). Temporin-Sha also has inhibitory effects on Candida albicans (MIC = 25 μM), Saccharomyces cerevisiae (MIC = 12 μM), the pre-flagellated and non-flagellated forms of Leishmania infantum (IC50 = 5-20 μM), and Trypanosoma cruzi (IC50 = 17 μM). Temporin-Sha exhibits antiviral activity against HSV-1 and has anti-cancer effects (cytotoxicity against breast cancer cells MCF-7 and lung cancer cells H460, etc.) .
|
-
- HY-168095
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 10 (compound 21) is a potent antagonist of CXCR4, with the IC50 of 7.8 nM. CXCR4 antagonist 10 plays an important role in cancer research .
|
-
- HY-P5956
-
|
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-LEHD-CHO is an inhibitor of caspases 4, 5 and 9. Ac-AAVALLPAVLLALLAP-LEHD-CHO shows protective effects upon Neocarzinostatin (HY-111183)-treated MCF-7 cells .
|
-
- HY-P4523
-
|
|
Endogenous Metabolite
|
Endocrinology
|
|
FA-Ala-Arg is a dipeptide with furylacryloyl group. FA-Ala-Arg breaks down to produce arginine. While cell-surface Carboxypeptidase-D (CPD) also increases intracellular Arg, which is converted to nitric oxide (NO). FA-Ala-Arg enhances NO production in MCF-7 cells. FA-Ala-Arg also increases the cell survival of prolactin (PRL)-treated cells, PRL regulates CPD mRNA levels in cells .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-P10873
-
|
|
Nuclear Hormone Receptor 4A/NR4A
Mitochondrial Metabolism
|
Cancer
|
|
ST-CY14 is an inhibitor for Nur77-PPARγ interaction with an EC50 of 3.15 μM, that binds to Nur77 (Kd=32 nM), blocks Nur77 from being ubiquitinated and degraded by PPARγ, reduces fatty acid uptake and mitochondrial respiration, and inhibits the transcription of CD36 and FABP4. ST-CY14 inhibits the proliferation and migration of cancer cell MCF7 and MDA-MB-231. ST-CY14 inhibits tumor growth and bone metastasis in mouse models .
|
-
- HY-P10843
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
R4K1 is a cell-permeable stapled peptide. R4K1 binds to the estrogen receptor (ER) α with high affinity and inhibits its interaction with coactivators. R4K1 can enter breast cancer cells to regulate gene transcription and inhibit cell proliferation. R4K1 can be used in the study of cancer .
|
-
- HY-P5755A
-
|
|
Peptides
|
Cancer
|
|
SWELYYPLRANL-NH2 TFA is an E-cadherin and N-cadherin antagonist. SWELYYPLRANL-NH2 TFA inhibits phage clone binding to E- or N-cad/Fc chimeric protein (IC50: 0.7 and 0.09 μM respectively). SWELYYPLRANL-NH2 TFA inhibits cell aggregation. SWELYYPLRANL-NH2 can be used to promote drug delivery through epithelial and endothelial permeability barriers .
|
-
- HY-P5834A
-
|
|
Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Boc-AEVD-CHO TFA is a Caspase 8 inhibitor. Boc-AEVD-CHO TFA significantly increases the frequencies of Nocodazole (HY-13520) or methyl methane sulfonate (MMS) induced micronuclei (MN) and micronucleated binucleates (MNCB) in PBMC by inhibiting cell apoptosis. Boc-AEVD-CHO TFA can be used for immune and inflammatory diseases research .
|
-
- HY-P5423D
-
|
|
Exosomes
|
Others
|
|
Ahx-GALA-Cys is a GALA peptide (HY-P5423) derivative with an N-terminal 6-aminohexanoic acid (Ahx) linker and a C-terminal cysteine residue. Ahx-GALA-Cys possesses strong covalent coupling capacity, which can be used to conjugate fluorophores and targeting ligands for investigating the surface functionalization of small extracellular vesicles (sEV) and lysosomal escape .
|
-
- HY-P11829
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer .
|
-
- HY-P11792
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
CP2-CPP is a conjugate of p27 Analogue CP2 (HY-P11020) and Antennapedia Peptide (HY-P0307). CP2-CPP crosses cell membranes and localizes to live cell cytosol. CP2-CPP blocks SCF Skp2/Cks1-p27 interaction to inhibit p27 ubiquitination and degradation, restoring p27 levels and inhibiting cell proliferation. CP2-CPP can be used for the research of cancer, such as breast cancer .
|
-
- HY-P11640
-
|
|
Ligands for E3 Ligase
HIV
|
Infection
|
|
Vpr (1-14) is a viral protein R and acts as an accessory protein of HIV-1. Vpr (1-14) can binds to Cul4A-DDB1-DCAF1 E3 ligase complex and can be used as an E3 ligase-binding component in PROTACs. Vpr (1-14) can be used to synthesize PROTAC BRD4 Degrader-43 (HY-181164) .
|
-
- HY-P11658
-
|
Peptoid 1
|
Peptides
|
Cancer
|
|
Anticancer peptoid 1 (Peptoid 1) is a peptoid with antitumor activity. Anticancer peptoid 1 exerts cytotoxicity primarily via plasma membrane damage. Anticancer peptoid 1 exerts cytotoxicity against a broad range of cancer cell lines, including those with multidrug resistance. Anticancer peptoid 1 inhibits tumor growth in a human breast cancer xenotransplantation mouse model without noticeable acute adverse effects. Anticancer peptoid 1 can be used for the research of cancer, such as breast cancer, and prostate cancer .
|
-
- HY-P11828
-
|
|
Survivin
Caspase
Apoptosis
|
Cancer
|
|
Anticancer agent 324 is a Survivin inhibitor. Anticancer agent 324 competitively binds to Survivin’s linker region and triggers proteasomal IAP degradation. Anticancer agent 324 blocks Borealin binding and chromosomal passenger complex formation, and inhibits Survivin-CRM1 nuclear-cytoplasmic transport. Anticancer agent 324 activates extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, activates executioner caspases-3 and caspases-7, and arrests cell cycle. Anticancer agent 324 can be used for the research of breast cancer .
|
-
- HY-P11766
-
|
GALA-cholesterol
|
Biochemical Assay Reagents
|
Cancer
|
|
GALA-chol is a cholesterol-conjugated pH-responsive fusion peptide that can serve as a delivery adjuvant. GALA-chol enhances the endocytosis of siRNA RET/PTC1-SQ nanoparticles, inhibits cell viability, and undergoes pH-responsive charge conversion in the acidic lysosomal environment, thereby promoting lysosomal escape of small extracellular vesicle (sEV) cargo. GALA-chol anchors to the sEV membrane and maintains the structural integrity and intrinsic homing activity of sEVs. GALA-chol can be used in studies related to adjuvant delivery .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P99605
-
|
PRS 343
|
EGFR
TNF Receptor
|
Cancer
|
|
Cinrebafusp alfa (PRS 343) is a high affinity CD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
|
-
(5)
-
- HY-P991646
-
|
heMab
|
Transmembrane Glycoprotein
|
Cancer
|
|
ING-1 (heMab) is a high-affinity humanized monoclonal antibody against epithelial cell adhesion molecule (Ep-CAM). ING-1 is a transmembrane glycoprotein mediating Ca 2+. ING-1 binds to Ep-CAM on tumor cells and exhibits potent in vitro activity, targeting and inhibiting tumor growth and metastasis in mouse cancer models. ING-1 is useful in the research of breast, colorectal, and lung cancers, among other cancers .
|
-
(5)
-
- HY-P992386
-
|
|
CD22
|
Cancer
|
|
IMM47 is a humanized monoclonal antibody targeting CD24, which acts as a competitive inhibitor of the CD24/Siglec-10 interaction and exhibits potent anti-tumor activity. The EC50 value of IMM47 for CD24 is 0.289 nM, and its Ka is 0.876 nM. IMM47 selectively binds to CD24-positive tumor cells and human granulocytes. By competitively blocking CD24/Siglec-10 binding, IMM47 abrogates the immunosuppressive signals of tumor cells, clears tumor cells through multiple effector pathways including ADCC, ADCP, ADCT and CDC, upregulates the levels of M1 and M2 macrophages in the spleen, promotes macrophage antigen presentation and induces tumor-specific memory immunity. IMM47 can be used in cancer-related research .
|
-
(5)
-
- HY-P991922
-
|
|
Fc Receptor (FcR)
Complement System
Radionuclide-Drug Conjugates (RDCs)
|
Cancer
|
|
AKIR001 is a high-affinity human IgG1 antibody targeting CD44v6. AKIR001 carries LALA-silencing mutations in its FcγR-binding domain to reduce FcγR and C1q interactions, minimizing tissue interactions and limiting CDC and ADCC risks. [ 177Lu] radiolabeled AKIR001, namely [ 177Lu]Lu-AKIR001, has anticancer activity against epidermoid carcinoma .
|
-
(5)
-
- HY-P991966
-
|
|
EGFR
|
Cancer
|
|
Anti-Human/Mouse EGFR Antibody (7A7) ia an anti-mouse EGFR monoclonal antibody proposed to be the mouse equivalent of cetuximab. Anti-Human/Mouse EGFR Antibody (7A7) fails to induce tumor regression in the HPV38 tumor model where EGFR is not expressed in mice. Anti-Human/Mouse EGFR Antibody (7A7) can be used in EGFR-expressing HPV38 tumor-related studies .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-119358
-
-
-
- HY-W016887
-
-
-
- HY-N1366
-
-
-
- HY-113319
-
-
-
- HY-Y0598
-
-
-
- HY-N2198
-
-
-
- HY-N5052
-
-
-
- HY-N0435
-
-
-
- HY-N2887
-
-
-
- HY-N8146
-
-
-
- HY-N6990
-
-
-
- HY-149132
-
|
DDA
|
Triterpenes
Terpenoids
Endogenous metabolite
Source Classification
|
LXR
|
|
Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase .
|
-
-
- HY-N4010
-
-
-
- HY-N7654
-
-
-
- HY-W587738
-
-
-
- HY-119358R
-
-
-
- HY-N8679
-
-
-
- HY-N10846
-
-
-
- HY-N3316
-
-
-
- HY-N10871
-
-
-
- HY-N11928
-
-
-
- HY-N13772
-
|
(+)-Dihydroisorhamnetin
|
Flavanonols
Flavonoids
Pulicaria jaubertii E.Gamal-Eldin
Asteraceae
Plants
Source Classification
|
Apoptosis
|
|
3'-O-Methyltaxifolin ((+)-Dihydroisorhamnetin) is a dihydroflavanol found in Pulicaria jaubertii. A mixture of these alcohol compounds including 3'-O-Methyltaxifolin found in Pulicaria jaubertii exhibits antitumor activity with IC50 values of 19.1 μg, 20.0 μg, and 24.1 μg against prostate cancer (PC-3), breast cancer (MCF-7), and hepatocellular carcinoma (HepG-2) cell lines, respectively. Furthermore, 3'-O-Methyltaxifolin can induce cell apoptosis, making it a promising candidate for anticancer research. .
|
-
-
- HY-Z12208
-
|
|
Structural Classification
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
Drug Derivative
|
|
N1-Phenylsuberamide is an organic amide compound, and its structure can be regarded as a simplified analogue of Vorinostat (HY-10221). N1-Phenylsuberamide exhibits moderate anti-proliferative activity against MDA-MB-231 and MCF-7 cells. N1-Phenylsuberamide does not show significant HDAC inhibitory activity and can only weakly induce the expression of the p21 gene. N1-Phenylsuberamide has extremely low relative binding affinity of estrogen receptor. N1-Phenylsuberamide can be used as a control compound .
|
-
-
- HY-N5103
-
-
-
- HY-W747516
-
-
-
- HY-N2298
-
-
-
- HY-N10777
-
-
-
- HY-N1833
-
-
-
- HY-N10023
-
-
-
- HY-N15577
-
|
|
Flavonols
Platanus acerifolia Aiton) Willd.
Flavonoids
Platanaceae
Plants
Source Classification
|
Drug Derivative
|
|
Antiproliferative agent-69 (Compound 1) is a prenylated kaempferol derivative found in the fresh bud’s fur of Platanus acerifolia. Antiproliferative agent-69 shows significant antiproliferative effects against human breast cancer cells (MCF-7) and human hepatocellular carcinoma cells (Hep-G2) with IC50 values of 38.2 μM and 39.5 μM, respectively. Antiproliferative agent-69 is promising for research of breast cancer and liver cancer .
|
-
-
- HY-N4010R
-
-
-
- HY-N15584
-
-
-
- HY-N10959
-
-
-
- HY-N11973
-
-
-
- HY-N3042
-
-
-
- HY-N14603
-
-
-
- HY-N10305
-
-
-
- HY-N7464
-
-
-
- HY-N2863
-
-
-
- HY-N9391
-
-
-
- HY-N3443
-
-
-
- HY-N8859
-
-
-
- HY-113796
-
-
-
- HY-N16642
-
-
-
- HY-N11438
-
-
-
- HY-N3261
-
-
-
- HY-N11919
-
-
-
- HY-N4227
-
-
-
- HY-N10351
-
-
-
- HY-N1252
-
-
- HY-126803
-
-
- HY-N6885
-
-
- HY-N3615
-
-
- HY-N16645
-
-
- HY-N12299
-
-
- HY-N14378
-
-
- HY-N14255
-
-
- HY-138098
-
-
- HY-145379
-
-
- HY-117872
-
|
20-O-Acetylsartorypyrone D
|
Microorganisms
Terpenoids
Diterpenoids
Source Classification
|
Fungal
|
|
Sartorypyrone A (20-O-Acetylsartorypyrone D) is a monocyclic terpenoid isolated from the soil fungus Neosartorya fischeri. Sartorypyrone A exhibits in vitro growth inhibitory activity against MCF-7, NCI-H460, and A375-C5 cell lines, and has potential anticancer properties.
|
-
- HY-N1107
-
|
NSC 119993; NSC 277290; Odorigeni
|
Apocynaceae
Cardiacglycosides
Plants
Steroids
Source Classification
|
Others
|
|
Uzarigenin (NSC 119993; NSC 277290; Odorigeni) is a carnolide can be isolated from Pergularia tomentosa and exhibits antiproliferative activity. Uzarigenin resists the proliferation of PC3 cells, HeLa cells, Calu-1 cells, MCF-7 cells and U251MG cells, with IC50 values of 0.3 μM, 3.0 μM, 8.0 μM, 6.0 μM and 6.0 μM respectively .
|
-
- HY-N14280
-
-
- HY-126618
-
-
- HY-N13162
-
|
|
Triterpenes
Terpenoids
Cucurbitaceae
Plants
Hemsleya pengxianensis W. J. Chang
Source Classification
|
Others
|
|
Hemsleyadin D is a triterpenoid compound derived from Hemsleya penxianensis with antitumor activity. Its IC50 values against K562, MGC-803, U118, HepG2, A549, and MCF-7 cells are 93.9, 47.1, 25.9, 56.1, 66.3, and 67.6 μM, respectively .
|
-
- HY-N1366R
-
|
Methylumbelliferone (Standard)
|
Structural Classification
other families
Coumarins
Phenylpropanoids
Plants
Source Classification
|
Reference Standards
Apoptosis
Bacterial
|
|
Herniarin (Standard) (Methylumbelliferone (Standard)) is the analytical standard of Herniarin (HY-N1366). This product is intended for research and analytical applications. Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer.
|
-
- HY-N3210
-
-
- HY-N2741
-
-
- HY-N15652
-
-
- HY-N12232
-
-
- HY-138210
-
|
|
Natural Products
Microorganisms
Source Classification
|
Fungal
|
|
N,O-Diacetyltyramine is a compound with antibacterial activity and cytotoxicity that can be isolated from the actinomycete Pseudonocardia endophytica VUK-10. N,O-Diacetyltyramine has antibacterial activity against Gram-positive and Gram-negative bacteria and fungi. N,O-Diacetyltyramine is cytotoxic to MDA-MB-231, HeLa, MCF-7 and OAW-42 cells .
|
-
- HY-N14892
-
-
- HY-113319R
-
-
- HY-N14056
-
|
|
Natural Products
Microorganisms
Source Classification
|
Bacterial
|
|
Chrolactomycin is found in the strain of Streptomyces sp. 569N-3. The IC50 of Chrolactomycin for ACHN, A431, McF-7 and T24 cells are 1.2 μM, 1.6 μM, 0.69 μM and 0.45 μM, respectively. Chrolactomycin has only anti-Gram-positive bacteria activity with the MIC of 5.2-10.4 μg/mL .
|
-
- HY-119539
-
-
- HY-N12208
-
-
- HY-N12209
-
-
- HY-N8508
-
|
|
Natural Products
Microorganisms
Source Classification
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-N13115A
-
|
(E)-21-Angeloyl-protoaescigenin
|
Aesculus chinensis Bunge
Triterpenes
Terpenoids
Hippocastanaceae
Plants
Source Classification
|
Others
|
|
Protoescigenin 21-tiglate (compound 10) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. However, the antitumor activity of Protoescigenin 21-tiglate is relatively weak, with IC50 values of >80 μM and 80 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-N13115
-
|
(Z)-Protoescigenin 21-tiglate
|
Aesculus chinensis Bunge
Triterpenes
Terpenoids
Hippocastanaceae
Plants
Source Classification
|
Others
|
|
21-Angeloyl-protoaescigenin (compound 11) is a glycosidic oleanane-type triterpenoid (BAT) that can be isolated from the acid hydrolysis product (AHP) of the crude extract of Aesculus chinensis seeds. Aesculus-derived triterpenoids (BAT) generally exhibit good antitumor, anti-inflammatory, and anti-Alzheimer's activities. Protoescigenin 21-tiglate has antitumor activity, with IC50 values of 38.2 μM and 33 μM against MCF-7 and HeLa cells, respectively .
|
-
- HY-N15392
-
-
- HY-129672
-
|
25-Dihydrostichorrenoside E
|
Other Terpenoids
Animals
Terpenoids
Source Classification
|
Drug Derivative
|
|
Thelenotoside B (25-Dihydrostichorrenoside E) shows strong cytotoxicities against five cancer cell lines as HepG2, KB, LNCaP, MCF7 and SK-Mel2 with the IC50 values from 0.95 ± 0.08 to 1.90 ± 0.13 μM. Thelenotoside B is a triterpene tetraglycoside .
|
-
- HY-N12230
-
|
|
Microorganisms
Ketones, Aldehydes, Acids
Source Classification
|
Bacterial
Parasite
Fungal
|
|
Penicolinate B is a picolinic acid derivative that can be isolated from Penicillium sp. Penicolinate B exhibits antimalarial activity (IC50: 1.40 μg/mL), antitubercular activity (MIC: 25.0 μg/mL), activity against Bacillus cereus (IC50: 25.0 μg/mL), and activity against Candida albicans (IC50: 1.45 μg/mL). Penicolinate B also has certain cytotoxicity against cancer cells such as MCF-7, KB, and NCI-H187. Penicolinate B can be used in research on malaria, tuberculosis, bacterial/fungal infections and tumors .
|
-
- HY-N9174
-
|
|
Flavonoids
Flavones
Plants
Moraceae
Broussonetia papyrifera (Linnaeus) L'Heritier ex Ventenat
Source Classification
|
Others
|
|
5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone is a natural product that can be extracted from B. papyrifera. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone has potent anti-proliferation effects on ER-positive breast cancer cells, with an IC50 value of 4.41 μM for MCF-7 cells. 5,7,3',4'-Tetrahydroxy-3-methoxy-8,5'-diprenylflavone also reduces the tumor growth in the BCAP-37 xenograft .
|
-
- HY-125620
-
|
|
Quinones
Microorganisms
Anthraquinones
Source Classification
|
Antibiotic
Bacterial
|
|
Rubiginone D2 is an antibiotic, which exhibits antimicrobial activities against Bacillus subtilis, Staphylococcus aureus and Escherichia coli. Rubiginone D2 exhibits antitumor efficacy, inhibits proliferations of cancer cells HM02, Kato III, HepG2 and MCF7, with GI50s of 0.1, 0.7, <0.1 and 7.5 μM, respectively .
|
-
- HY-135453
-
-
- HY-N12887
-
|
|
Natural Products
Marine natural products
Sponge
Source Classification
|
Mitochondrial Metabolism
|
|
Mycothiazole is an inhibitor for mitochondrial electron transport chain (ETC) complex I. Mycothiazole exhibits cytotoxicity in cancer cells Huh7 (IC50 is 55.8 μM), U87 and MCF7. Mycothiazole induces apoptosis in Huh7. Mycothiazole utilizes the unfolded protein response (UPR) and heat shock response (HSR) pathway involved transcription factors ATFS-1 and HSF1, to extend the lifespan of C. elegans .
|
-
- HY-N15636
-
-
- HY-N14604
-
-
- HY-N15306
-
|
|
Microorganisms
Ketones, Aldehydes, Acids
Phenols
Source Classification
|
Apoptosis
|
|
Boerelasin E is the first cytochalasan possessing a cis-configured Δ21(22) double bond that can be isolated from endophytic fungus Boeremia exigua. Boerelasin E exhibits antiproliferative activity against MCF-7 cells (IC50=20.52 μM) more potent than cisplatin (HY-17394). Boerelasin E inhibits the complete cell division of MCF-7 cells by arresting them in the G2/M phase and inducing apoptosis[1].
|
-
- HY-N16759
-
-
- HY-N3318
-
-
- HY-N7302
-
-
- HY-N14893
-
-
- HY-N10949
-
-
- HY-N13709
-
-
- HY-N15479
-
|
|
Microorganisms
Terpenoids
Sesquiterpenes
Source Classification
|
Bacterial
|
|
Nanangenine F is a drimane sesquiterpenoid with weak antibacterial and anticancer activities. Nanangenine F inhibits Bacillus subtilis (ATCC 6633) with an IC50 of 78 µg/mL. Nanangenine F inhibits NS-1, DU-145, MCF-7 and human fibroblast NFF cells with IC50s of 49 µg/mL, 95 µg/mL, 49 µg/mL, and 84 µg/mL, respectively .
|
-
- HY-N7340
-
-
- HY-Y0598R
-
-
- HY-N10621
-
|
|
Combretaceae
Phenols
Polyphenols
Plants
Quisqualis indica Linn.
|
Others
|
|
3,5-Dimethoxy-2,7-phenanthrenediol (compound 2) is a phenanthrene compound isolated from the roots of Combretum laxum. 3,5-Dimethoxy-2,7-phenanthrenediol is cytotoxic to human cancer cell lines 786-0, MCF-7 and NCI/ADR-RES, with IC50s of 73.26 μM, 118.40 μM and 83.99 μM respectively. 3,5-Dimethoxy-2,7-phenanthrenediol also has free radical scavenging activity with an IC50 of 20.4 μM .
|
-
- HY-N9848
-
|
|
Triterpenes
Senegalia pennata (L.) Maslin
Terpenoids
Labiatae
Plants
Source Classification
|
Others
|
|
2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid is a triterpenoid with anticancer effects. 2α,3α,24-Trihydroxyursa-12,20(30)-dien-28-oic acid inhibits HepG2, A549, MCF-7, SK-OV-3, and HeLa cells with IC50 values of 19.62 μM, 18.86 μM, 45.94 μM, 62.41 μM, and 28.74 μM, respectively .
|
-
- HY-N10778
-
|
|
Triterpenes
Terpenoids
Cucurbitaceae
Plants
Source Classification
Momordica charantia Linn.
|
Others
|
|
(19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol is a cucurbitane-type triterpenoid. (19R,23E)-5b,19-Epoxy19-ethoxycucurbita-6,23-diene-3b,25-diol has been tested to no effect against 5 cancer cell lines, MCF-7, HepG2, Du145, Colon205 and HL-60 by MTT assay .
|
-
- HY-N7012
-
|
5-Hydroxy-3',4',7-trimethoxyflavone
|
Monophenols
Flavonoids
Classification of Application Fields
Flavones
Labiatae
Phenols
Plants
Swartzia polyphylla DC.
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Lipoxygenase
TNF Receptor
Interleukin Related
COX
Fungal
Parasite
Apoptosis
|
|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid with multiple biological activities. 7,3',4'-Tri-O-methylluteolin inhibits soybean lipoxygenase (LOX), with an IC50 value of 23.97 µg/mL. 7,3',4'-Tri-O-methylluteolin possesses anti-inflammatory effects in Lipopolysaccharides (HY-D1056) (LPS)-induced RAW 264.7 macrophages. 7,3',4'-Tri-O-methylluteolin inhibits the binding of MDM2 with p53 and induces apoptosis in MCF-7 breast cancer cells. 7,3',4'-Tri-O-methylluteolin also has antioxidant, antifungal and antitrypanosomal activities sup>[4]sup>[5].
|
-
- HY-N16377
-
|
|
Quinones
Microorganisms
Anthraquinones
Source Classification
|
Others
|
|
1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione (Compound 2) is an anthraquinone analog. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione can be isolated from soil Actinomycete Streptomyces. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has potent cytotoxicity against HepG2, A875, BGC-823 and MCF-7 cells with IC50s of 2.29, 4.90, 0.99 and 1.66 μg/mL, respectively. 1-Butyl-3,5,8-trihydroxy-9,10-anthracenedione has an antitumor activity .
|
-
- HY-N0534
-
-
- HY-114803
-
-
- HY-113062
-
-
- HY-N12135
-
|
|
Senegalia pennata (L.) Maslin
Terpenoids
Labiatae
Diterpenoids
Plants
Source Classification
|
Others
|
|
15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide (compound 2) is an enantio-kaurene diterpenoid (ent -kaurene diterpenoid), which can be isolated from Rubescens rubescens. 15α-Hydroxy-20-oxo-6,7-seco-ent-kaur-16-en-1,7α(6,11α)-diolide has cellular activity against EC-1, U87, A549, MCF-7 and HeLa cell lines Toxicity, IC50s are 37.69 μM, 79.362 μM, 80.07 μM, 197.35 μM, 462.13 μM, and 180.09 μM respectively .
|
-
- HY-N0534R
-
|
|
Structural Classification
Flavonoids
other families
Flavones
Phenols
Polyphenols
Plants
Source Classification
|
Reference Standards
DNA/RNA Synthesis
Apoptosis
PI3K
Akt
Caspase
SOD
Interleukin Related
|
|
Vitexin-2"-O-rhamnoside (Standard) is the analytical standard of Vitexin-2"-O-rhamnoside (HY-N0534). This product is intended for research and analytical applications. Vitexin-2"-O-rhamnoside is an orally active flavonoid glycoside. Vitexin-2"-O-rhamnoside inhibits Apoptosis, increases the phosphorylation levels of PI3K/Akt, inhibits caspase-3, SOD activity, and promotes cytokine (IL-2, IL-6, and IL-12) secretion. Vitexin-2"-O-rhamnoside strongly inhibits DNA synthesis in MCF-7 cells with an IC50 of 17.5 μM. Vitexin-2"-O-rhamnoside enhances immune function and improves the absorption of active compounds. Vitexin-2"-O-rhamnoside has antioxidant activity. Vitexin-2"-O-rhamnoside is used in the study of cardiovascular disease and immune-related diseases .
|
-
- HY-N12606
-
|
|
Microorganisms
Saccharides
Monosaccharides
Source Classification
|
Fungal
|
|
Neodidymelliosides A (compound 1)It is a secondary metabolite of fungi and has a significant inhibitory effect on Staphylococcus aureus and Candida albicans biofilms. Neodidymelliosides AIt also has anti-cancer activity and can inhibit KB3.1 (cervix),PC-3 (prostate),MCF-7(breast),SKOV-3 (ovary),A431 (skin )and A549 (lung )Cell viability of cell lines .
|
-
- HY-N10353
-
-
- HY-N2331R
-
-
- HY-N2331
-
-
- HY-N7083
-
-
- HY-N7083R
-
-
- HY-N15054
-
-
- HY-126423
-
-
- HY-N10229
-
-
- HY-N1268
-
-
- HY-N1267
-
-
- HY-N12792
-
-
- HY-N17453
-
-
- HY-N0595R
-
-
- HY-N0595
-
-
- HY-N12997
-
-
- HY-N12231
-
-
- HY-N0404
-
-
- HY-N2423
-
-
- HY-13502
-
-
- HY-13502AR
-
|
Mitozantrone dihydrochloride (Standard); NSC 301739 dihydrochloride (Standard)
|
Quinones
Structural Classification
Anthraquinones
Endogenous metabolite
Source Classification
|
Reference Standards
Topoisomerase
PKC
Orthopoxvirus
Apoptosis
Endogenous Metabolite
|
|
Mitoxantrone (dihydrochloride) (Standard) is the analytical standard of Mitoxantrone (dihydrochloride). This product is intended for research and analytical applications. Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
- HY-13502R
-
-
- HY-13502A
-
-
- HY-N5208
-
|
|
Natural Products
Microorganisms
Source Classification
|
Others
|
|
YM-216391 is an antitumor cyclic peptide that can be isolated from the cultured mycelium of Streptomyces nobilis JCM 4274. YM-216391 exhibits potent cytotoxic activity against a variety of human cancer cell lines and can be used in anticancer research .
|
-
- HY-N6607
-
-
- HY-N17570
-
-
- HY-N15201
-
|
|
Structural Classification
Flavonoids
Beta vulgaris Linn.
Plants
Isoflavones
Chenopodiaceae
Source Classification
|
STAT
|
|
Betavulgarin is an anticancer agent. Betavulgarin can be isolated from Sugar Beet (Beta vulgaris). Betavulgarin suppresses the proliferation, migration, colony formation, and mammosphere formation of breast cancer cells, and reduces the size of the CD44 +/CD24 − subpopulation and the expression of the self-renewal- related genes C-Myc, Nanog and Oct4. Betavulgarin promotes BCSCs death through the regulation of Stat3/Sox2 signaling .
|
-
- HY-N6607R
-
-
- HY-N17294
-
-
- HY-N18047
-
-
- HY-N12999
-
-
- HY-N0353R
-
|
(+)-Curdione (Standard)
|
Structural Classification
Terpenoids
Sesquiterpenes
Curcuma phaeocaulis Valeton
Plants
Source Classification
Zingiberaceae
|
Reference Standards
Ferroptosis
Apoptosis
Reactive Oxygen Species (ROS)
Autophagy
Glutathione Peroxidase
Keap1-Nrf2
Heme Oxygenase (HO)
TGF-β Receptor
Indoleamine 2,3-Dioxygenase (IDO)
|
|
Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression .
|
-
- HY-N0353
-
-
- HY-N19311
-
|
|
Structural Classification
Alkaloids
Microorganisms
Other Alkaloids
Source Classification
|
Bacterial
|
|
3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone is an alkylated 2(1H)-pyrazinone derivative and cytotoxic agent found in the tunicate-derived actinomycete Streptomyces sp. Did-27.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone exhibits cytotoxic activity against cancer cells.3,6-Bis(1-methylpropyl)-2(1H)-pyrazinone can be used for the research of colorectal carcinoma, hepatocellular carcinoma, breast cancer .
|
-
- HY-N1506
-
-
- HY-N1506R
-
-
- HY-N17410
-
-
- HY-N8210
-
-
- HY-N18195
-
-
- HY-N19873
-
-
- HY-N10670
-
-
- HY-N15612
-
-
- HY-N0204
-
-
- HY-N18247
-
-
- HY-N19872
-
-
- HY-N12717
-
|
|
Terminalia arjuna (Roxb. ex DC.) Wight & Arn.
Structural Classification
Combretaceae
Phenols
Polyphenols
Plants
Source Classification
|
PAK
FASTK
HSP
p38 MAPK
NF-κB
NO Synthase
COX
HSV
Caspase
TNF Receptor
Fungal
Apoptosis
|
|
Casuarinin is an orally active antiproliferative, anti-inflammatory, antifungal, virucidal and gastroprotective agent. Casuarinin upregulates the expression of p21/WAF1, Fas/APO‑1, mFasL, sFasL and HSP‑70, arrests cell cycle, induces apoptosis and inhibits cancer cell proliferation. Casuarinin inhibits TNF‑α-induced phosphorylation of MAPK and activation of NF‑κB, downregulates the expression of iNOS, NF‑κB, COX‑2 and ICAM‑1, and reduces the production of proinflammatory mediators. Casuarinin attenuates ethanol-induced activation of caspase‑3 and elevation of TNF‑α, inhibits the growth of Candida albicans, and inhibits HSV‑2. Casuarinin can be used in research related to mammary adenocarcinoma, inflammatory skin diseases, gastric ulcers, candidiasis and herpes simplex virus infections .
|
-
- HY-N11060A
-
-
- HY-N17244
-
-
- HY-N16866
-
-
- HY-125727
-
-
- HY-W585917
-
-
- HY-N13833
-
-
- HY-N6651
-
-
- HY-N0554
-
-
- HY-N7712
-
-
- HY-N7317
-
-
- HY-N1983
-
|
|
Structural Classification
Classification of Application Fields
Asclepiadaceae
Cynanchum otophyllum Schneid．
Cynanchum auriculatum Royle ex Wight
Plants
Disease Research Fields
Steroids
Source Classification
Cancer
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
|
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
- HY-113293A
-
-
- HY-N0699
-
-
- HY-N18186
-
-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
Cardiovascular Disease
Structural Classification
Classification of Application Fields
Leguminosae
Glycine max (L.) merr
Plants
Inflammation/Immunology
Disease Research Fields
Steroids
Source Classification
|
Bacterial
Apoptosis
Reactive Oxygen Species (ROS)
MDM-2/p53
Caspase
PARP
MMP
Bcl-2 Family
HIF/HIF Prolyl-Hydroxylase
TNF Receptor
Interleukin Related
NF-κB
mTOR
Lactate Dehydrogenase
CDK
Glutathione Peroxidase
SOD
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
- HY-N18272
-
|
|
Structural Classification
Natural Products
Melia azedarach Linn.
Plants
Meliaceae
Source Classification
|
Others
|
|
1α-Benzoyloxy-3α-acetoxyl-7α-hydroxy-12β-ethoxynimbolinin is a nimbolinin-type limonoid and cytotoxin, found in the fruits of Melia toosendan. 1α-Benzoyloxy-3α-acetoxyl-7α-hydroxy-12β-ethoxynimbolinin exhibits in vitro cytotoxicity against human hepatocellular carcinoma, human lung cancer, and human breast cancer cells. 1α-Benzoyloxy-3α-acetoxyl-7α-hydroxy-12β-ethoxynimbolinin can be used for the research of hepatocellular carcinoma, lung cancer, breast cancer .
|
-
- HY-N19464
-
-
- HY-N3000A
-
|
|
Structural Classification
Alkaloids
Meconopsis simplicifolia (D. Don) Walp.
Quinoline Alkaloids
Plants
Papaveraceae
Source Classification
|
JNK
IRE1
Akt
mTOR
YAP
Reactive Oxygen Species (ROS)
Autophagy
Apoptosis
Ferroptosis
Fungal
Caspase
DNA/RNA Synthesis
|
|
6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer .
|
-
- HY-N19297
-
-
- HY-N9672
-
-
- HY-N19821
-
|
|
Structural Classification
Monophenols
Microorganisms
Phenols
Source Classification
|
DNA/RNA Synthesis
|
|
Gangaleoidin is a FOXM1 inhibitor with an IC50 of 2.8 μM. Gangaleoidin inhibits interaction between FOXM1’s DNA-binding domain and target DNA sequence, downregulates FOXM1 and downstream target gene CCNB1 at the transcriptional level. Gangaleoidin suppresses proliferation of FOXM1-overexpressing breast cancer cells. Gangaleoidin can be used for the research of breast cancer .
|
-
- HY-N19791
-
|
|
Structural Classification
Monophenols
Coumarins
Phenols
Phenylpropanoids
Decachaeta ovatifolia (DC.) R.M.King & H.Rob.
Umbelliferae
Plants
Source Classification
|
NF-κB
Fungal
Interleukin Related
|
|
6-Methoxymellein, a phytoalexin, is a NF-κB inhibitor. 6-Methoxymellein reduces nuclear localization and DNA binding activity of NF-κB p65 and p50 subunits. 6-Methoxymellein decreases mRNA transcription and secretion of IL-6 and IL-8. 6-Methoxymellein reduces the proportion of CD44 +/CD24 − breast cancer cells, decreases expression of c-Myc, Sox-2 and Oct4, inhibits proliferation and migration of breast cancer cells, and reduces mammosphere growth. 6-Methoxymellein inhibits fungal growth of Trichophyton rubrum and Botrytis cinerea, and inhibits Trichophyton rubrum biofilm formation via hyphal disintegration. 6-Methoxymellein can be used for the research of breast cancer, tinea corporis, and carrot post-harvest storage rot .
|
-
- HY-B1309
-
-
- HY-N19938
-
-
- HY-W420454
-
-
- HY-N19113
-
-
- HY-N10342
-
|
|
Structural Classification
Flavonoids
Leguminosae
Phenols
Polyphenols
Plants
Isoflavones
Cajanus cajan (L.) Millsp.
Source Classification
|
Apoptosis
Bcl-2 Family
Caspase
PARP
Reactive Oxygen Species (ROS)
Bacterial
PI3K
Akt
NF-κB
P-glycoprotein
|
|
Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp. . Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections .
|
-
- HY-N0660
-
|
|
Cardiovascular Disease
Triterpenes
Structural Classification
other families
Classification of Application Fields
Terpenoids
Plants
Disease Research Fields
Source Classification
|
Apoptosis
PARP
Caspase
AMPK
Autophagy
VEGFR
Keap1-Nrf2
STING
11β-HSD
Ferroptosis
PI3K
Akt
p38 MAPK
ERK
|
|
Jujuboside B is a bioactive saponin component isolated from Ziziphi Spinosae Semen (sour jujube seed), with oral efficacy and blood-brain barrier permeability. Jujuboside B induces acute leukemia cell death and drives necroptosis apoptosis by activating the RIPK1/RIPK3/MLKL pathway. Jujuboside B upregulates the expression of NOXA, PARP and caspase-3, activates AMPK, inhibits the proliferation of breast cancer cells, and induces cell apoptosis and autophagy. Jujuboside B inhibits angiogenesis and tumor growth by blocking the VEGFR-2 signaling pathway. Jujuboside B alleviates liver injury in mice by regulating the Nrf2-STING signaling pathway . Jujuboside B alleviates liver injury by regulating anti-inflammatory responses and downregulating the expression of 11β-HSD2. Jujuboside B induces ferroptosis and overcomes radioresistance in non-small cell lung cancer via the PPARγ-ATF3-Gpx4 signaling pathway. Jujuboside B exerts inhibitory effects on platelet aggregation. Jujuboside B inhibits febrile seizures by suppressing the activity of AMPA receptors. Jujuboside B reverses chronic unpredictable mild stress-promoted tumor progression by blocking the PI3K/Akt and MAPK/ERK pathways and dephosphorylating CREB signaling. Jujuboside B is applicable to related studies on acute leukemia, breast cancer, PM2.5-induced lung injury, hepatotoxicity, liver injury, colorectal cancer, non-small cell lung cancer, thromboembolic diseases, cardiovascular diseases associated with high platelet aggregation, febrile seizures, and depressive-like phenotypes .
|
-
- HY-126756
-
-
- HY-108964
-
-
- HY-N12586
-
|
|
Suaeda vermiculata Forssk. ex J.F.Gmel.
Structural Classification
Alkaloids
Other Alkaloids
Amaranthaceae
Plants
Source Classification
|
ERK
Reactive Oxygen Species (ROS)
COX
PGE synthase
STAT
HCV
HCV Protease
|
|
Pheophytin a is a multi-target inhibitor, anticancer agent, antioxidant and antiviral agent. Pheophytin a directly binds to and inhibits HCV-NS3/4A protease (IC50=0.89 μM) to block viral replication. Pheophytin a also scavenges free radicals, reduces ferric ions, and exhibits cytotoxic activity against breast cancer cells. Pheophytin a effectively inhibits LPS-induced production of nitric oxide, prostaglandin E2, NOS2 and COX-2, as well as various pro-inflammatory cytokines, by downregulating the transcription levels of inflammatory mediators and blocking the ERK1/2 and STAT-1 pathways. In a low nerve growth factor environment, Pheophytin a also enhances ERK1/2 phosphorylation and synergistically promotes neurite outgrowth through MAPK pathway. Pheophytin a can be used to investigate the pathogenic mechanisms of diseases including chronic hepatitis C, sepsis, breast cancer and Alzheimer's disease .
|
-
- HY-133668
-
|
|
Other disease
Disease markers
Endogenous metabolite
|
Drug Metabolite
Cytochrome P450
PPAR
|
|
Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms .
|
-
- HY-N6005
-
-
- HY-N8250
-
-
- HY-75625
-
-
- HY-N13838
-
|
|
Triterpenes
Structural Classification
Pongamia pinnata (L.) Pierre
Terpenoids
Plants
Compositae
Source Classification
|
Bacterial
|
|
8,9-Dehydro-7,9-diisobutyryloxythymol is a Thymol (HY-N6810) derivative, as well as an antibacterial agent. 8,9-Dehydro-7,9-diisobutyryloxythymol can be found in the aerial parts of Ageratina adenophora, with selective activity against Gram-positive bacterial strains including Bacillus cereus. 8,9-Dehydro-7,9-diisobutyryloxythymol does not exhibit detectable in vitro cytotoxic activity against human cancer cell lines. 8,9-Dehydro-7,9-diisobutyryloxythymol can be used for the research of bacterial infection .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13636S
-
|
|
|
Fulvestrant-d3 is the deuterium labeled Fulvestrant. Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy .
|
-
-
- HY-13636S1
-
|
|
|
Fulvestrant-d5 (ICI 182780-d5) is a isotope of Fulvestrant (HY-13636) . Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.
|
-
-
- HY-50936S
-
|
|
|
Trabectedin D3 (Ecteinascidin 743 D3) is deuterium labeled Trabectedin. Trabectedin is a tetrahydroisoquinoline alkaloid with potent antitumor activity. Trabectedin binds to the minor groove of DNA, blocks transcription of stress-induced proteins, induces DNA backbone cleavage and cancer cells apoptosis, and increases the generation of ROS in MCF-7 and MDA-MB-453 cells. Trabectedin has tje potential for soft tissue sarcoma and ovarian cancer treatment .
|
-
-
- HY-N1366S
-
|
|
|
Herniarin-d3 is the deuterium labeled Herniarin (HY-N1366). Herniarin is a natural coumarin occurs in some flowering plants with anticancer effects. Herniarin results in a significant decrease in cell viability by inducing apoptosis in MCF-7 cells. Herniarin also has anti-dermatophytic activity. Herniarin can be used for the study of bladder cancer and breast cancer .
|
-
-
- HY-13762S
-
|
|
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
-
- HY-13502AS
-
|
|
|
Mitoxantrone-d8 dihydrochloride is deuterated labeled Mitoxantrone dihydrochloride (HY-13502A). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity . Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC50s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively .
|
-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-B1029
-
Danazol
4 Publications Verification
|
|
Alkynes
|
|
Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
|
-
- HY-115997
-
|
|
|
PROTAC Synthesis
|
|
PROTAC HSP90 degrader BP3 is a potent and selective degradation of HSP90 in a CRBN-dependent fashion. PROTAC HSP90 degrader BP3 has a certain degradation effect on HSP90 protein in MCF-7 cells (DC50=0.99 μM). PROTAC HSP90 degrader BP3 inhibits the growth of breast cancer cell . PROTAC HSP90 degrader BP3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-111640
-
|
|
|
Azide
|
|
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells . 3'-Azido-3'-deoxy-5-methylcytidine is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-178118
-
|
|
|
Alkynes
|
|
PROTAC PDIA1 degrader 1 (Compound H4) is a PDIA1 PROTAC degrader with a DC50 of 29.71 μM. PROTAC PDIA1 degrader 1 has potent anticancer activity and significantly inhibits cancer cell proliferation . Pink: PDIA1 ligand (HY-100433); Blue: CRBN ligase ligand (HY-10984); Black: linker (HY-W015088)
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-N0171A
-
|
β-Sitosterol (purity>98%); 22,23-Dihydrostigmasterol (purity>98%)
|
|
Cholesterol
|
|
Beta-Sitosterol (purity>98%) is orally active. Beta-Sitosterol exhibits multiple activities, including anti-inflammatory, anticancer, antioxidant, antimicrobial, antidiabetic, antioxidant enzyme, and analgesic. Beta-Sitosterol inhibits inflammation and impaired adipogenesis in bovine mammary epithelial cells by reducing levels of ROS, TNF-α, IL-1β, and NF-κB p65 and restoring the activity of the HIF-1α/mTOR signaling pathway. Beta-Sitosterol induces apoptosis in cancer cells through ROS-mediated mitochondrial dysregulation and p53 activation. Beta-Sitosterol exerts its anticancer effects in cancer cells by activating caspase-3, caspase-8, and caspase-9, mediating PARP inactivation, MMP loss, altered Bcl-2-Bax ratio, and cytochrome c release. Beta-Sitosterol modulates macrophage polarization and reduces rheumatoid inflammation in mice. Beta-Sitosterol inhibits tumor growth in multiple mouse cancer models. Beta-Sitosterol can be used in the research of arthritis, lung cancer, breast cancer and other cancers, diabetes, etc .
|
-
- HY-147081
-
AS 1411
2 Publications Verification
AGRO-100
|
|
Aptamers
|
|
AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity .
|
-
- HY-126437
-
|
|
|
Polymers
|
|
Poly-L-lysine hydrobromide (MW 30000-70000) is a water-soluble synthetic polypeptide. Poly-L-lysine hydrobromide (MW 30000-70000) downregulates Bcl-2 and upregulates Bax and p53 proteins. Poly-L-lysine hydrobromide (MW 30000-70000) promotes Apoptosis and reduces VEGF expression. Poly-L-lysine hydrobromide (MW 30000-70000) shows anticancer activity against a variety of tumors. Poly-L-lysine hydrobromide (MW 30000-70000) can also be used as a coating material .
|
-
- HY-172470
-
|
|
|
Pegylated Lipids
|
|
DSPE-PEG2000-GE11 is a nanocarrier component composed of DSPE and the EGFR-targeting peptide (GE11). DSPE-PEG2000-GE11 specifically binds to EGFR and mediates receptor-mediated endocytosis of micellar drug carriers. DSPE-PEG2000-GE11 can be used for drug delivery .
|
-
- HY-147081A
-
|
AGRO-100 sodium
|
|
Aptamers
|
|
AS 1411 (AGRO-100) sodium is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 sodium inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 sodium reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. S 1411 sodium works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. S 1411 sodium-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity
|
-
- HY-160062
-
|
|
|
Aptamers
|
|
S2.2 aptamer sodium is a nucleic acid-based MUC1-binding aptamer with high affinity and low toxicity. Upon binding to its target, S2.2 aptamer sodium undergoes a conformational switch and restores fluorescence signal, serving as a targeted imaging agent for MUC1-positive cancer cells. S2.2 aptamer sodium enables targeted delivery to breast cancer cells with overexpressed MUC1. When formulated as the S2.2-PEG-MZF molecular probe, S2.2 aptamer sodium possesses the functions of T2 signal inhibition, magnetic field-induced hyperthermia and targeted magnetic resonance molecular imaging. In the S2.2-PEG-MZF/DOX nanoliposome, S2.2 aptamer sodium supports targeted thermochemotherapy, effectively inhibiting cancer cell proliferation and invasion as well as inducing apoptosis, and is widely used in studies related to breast cancer .
|
-
- HY-185373
-
|
Liposomal paclitaxel
|
|
Liposome
|
|
Paclitaxel liposome is a liposome-encapsulated form of Paclitaxel (HY-B0015). Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel liposome is characterized by reduced acute toxicity, prolonged circulating half-life of paclitaxel, and enhanced accumulation at tumor sites. Paclitaxel liposome can be used in research related to breast cancer and locally advanced esophageal squamous cell carcinoma .
|
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent:
![Chloro[1,3-bis(2,6-diisopropylphenyl)imidazol-2-ylidene]copper(I)](http://file.medchemexpress.com/product_pic/hy-w035150.gif)
![1-Methyl-1H-pyrrolo[2,3-b]pyridine](http://file.medchemexpress.com/product_pic/hy-w001520.gif)
![[Pt(DACH)(OH)2(ox)]](http://file.medchemexpress.com/product_pic/hy-w778423.gif)
