Search Result
Results for "
LNCaP cells
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-70002
-
Enzalutamide
Maximum Cited Publications
152 Publications Verification
MDV3100
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Androgen Receptor
Autophagy
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Cancer
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Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
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-
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- HY-70002S1
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MDV3100-d6
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Androgen Receptor
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Cancer
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Enzalutamide-d6 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
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-
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- HY-70002S
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Enzalutamide-d3; MDV3100-d3
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Androgen Receptor
Autophagy
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Cancer
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Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
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-
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- HY-149862
-
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PROTACs
Androgen Receptor
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Cancer
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ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer .
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-
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- HY-N2908
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Methyl atrarate
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Androgen Receptor
NO Synthase
p38 MAPK
NF-κB
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Inflammation/Immunology
Cancer
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Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
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-
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- HY-70002R
-
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Androgen Receptor
Autophagy
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Cancer
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Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator .
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-
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- HY-N10265
-
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Endogenous Metabolite
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Cancer
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Stephacidin B is a fungal metabolite. Stephacidin B shows in vitro cytotoxicity against a panel of human tumor cell lines. Stephacidin B shows the strongest cytotoxicity against testosterone-dependent prostate LNCaP cancer cells .
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-
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- HY-N2733
-
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Others
|
Others
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7,2',4'-Trihydroxy-5-methoxy-3-arylcoumarin is a coumarin, that can be isolated from campylotropis hirtella (FRANCH.) SCHINDL. 7,2',4'-Trihydroxy-5-methoxy-3-arylcoumarin inhibits PSA secretion in LNCaP cells, with an IC50 of 24.2 μg/mL .
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-
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- HY-144755
-
|
Histone Demethylase
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Cancer
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MC2652 (compound 1a) is a potent LSD1 inhibitor. MC2652 displays high inhibiting effects in MV4-11 and NB4 leukaemia cells. MC2652 shows antiproliferative activity against prostate cancer LNCaP cells .
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-
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- HY-N3816
-
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Others
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Others
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ent-17-Hydroxykaur-15-en-19-oic acid is a ent-kaurene
diterpene that can be isolated from the leaves of Laetia thamnia L..
ent-17-Hydroxykaur-15-en-19-oic acid was cytotoxic to human prostate LNCaP2
cells with IC50 17.63
mg/mL .
|
-
-
- HY-144756
-
|
Histone Demethylase
Monoamine Oxidase
|
Cancer
|
LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor. LSD1-IN-15 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 9.9 μM .
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-
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- HY-144757
-
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Histone Demethylase
Monoamine Oxidase
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Cancer
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LSD1-IN-16 (compound 4b) is a potent LSD1 inhibitor. LSD1-IN-16 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 15.2 μM .
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-
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- HY-144758
-
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Histone Demethylase
Monoamine Oxidase
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Cancer
|
LSD1-IN-17 (compound 5b) is a potent LSD1 inhibitor. LSD1-IN-17 can inhibit LSD1-CoREST, MAO-A and MAO-B, with IC50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 displays cell growth arrest in prostate cancer LNCaP cells, with an IC50 of 17.2 μM .
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- HY-121619
-
|
Apoptosis
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Inflammation/Immunology
Cancer
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Jacaric acid is a conjugated linolenic acid, which inhibits viability in cells PC-3 (IC50 is 11.8 μM), LNCaP (IC50 is 2.2 μM) and DLD-1, induces apoptosis and necrosis . Jacaric acid exhibits anticaner activity against prostate cancer and adenocarcinoma . Jacaric acid exhibits immunomodulating activity in murine peritoneal macrophages as an immunopotentiator . Jacaric acid is orally active.
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-
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- HY-N1342
-
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Apoptosis
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Cancer
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Rocaglaol induces apoptosis and cell cycle arrest in LNCaP cells .
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-
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- HY-126464
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EoM
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Androgen Receptor
|
Cancer
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Estromustine (EoM) is the active metabolite of Estramustine phosphate (HY-13627A). Estromustine binds to mutant androgen receptor (m-AR) with EC50 of 2.6 μM in LNCaP, exhibits cytotoxicity in human prostate cells LNCaP with IC50 of 9.73 μM .
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-
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- HY-113332
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-
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- HY-N3999
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ESK246
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Others
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Cancer
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Venuloside A is a potent inhibitor of LAT3. Venuloside A inhibits the leucine uptake in LNCaP prostate cancer cells with an IC50 of 8.12 μM .
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-
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- HY-120581
-
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PGE synthase
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Cancer
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ML388 is a potent and selective hydroxyprostaglandin dehydrogenase (HPGD) inhibitor with an IC50 of 34 nM. ML388 induces PGE2 production in A549 cells and LNCaP prostate cancer cells .
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-
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- HY-N8856
-
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Others
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Others
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Angelol M,isolated from the roots of Angelica gigas Nakai, shows activity in inhibiting prostate specific antigen (PSA) secreted from androgen dependent prostate cancer cell line, LNCaP cells .
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-
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- HY-163641
-
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Androgen Receptor
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Cancer
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AR Degrader-1 is an androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR without obvious cytotoxicity in LNCaP prostate cancer cells .
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-
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- HY-N1338
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NSC 122417
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mTOR
Akt
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Cancer
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Royleanone, a diterpenoid isolated from plants, inhibits the proliferation of cancer cells by inducing cell cycle arrest and mitochondria-mediated apoptosis, also inhibits cell migration potential, inhibits mTOR/PI3/AKT signaling pathway in LNCaP prostate cancer cells .
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-
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- HY-131953
-
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Androgen Receptor
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Cancer
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Androgen receptor-IN-3 (Compound 22) is an androgen receptor inhibitor. Androgen receptor-IN-3 inhibits AR-driven transcriptional activity in LNCaP cells, with an IC50 of 5.04 μM .
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-
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- HY-13626
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ES-285
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PKC
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Cancer
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Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKCζ activation .
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-
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- HY-N12124
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Monascinol
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Akt
mTOR
AMPK
Androgen Receptor
Apoptosis
Autophagy
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Cancer
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Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
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-
-
- HY-150268
-
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Epigenetic Reader Domain
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Cancer
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BET-IN-16 (Comp I) is a BET inhibitor. BET-IN-16 shows anticancer activity. BET-IN-16 inhibits prostate cancer cell growth, with IC50 values of 0.043 and 0.034 μM against LNCaP and 22Rv1 cells, respectively .
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-
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- HY-13626S
-
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Isotope-Labeled Compounds
PKC
|
Cancer
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Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
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- HY-149433
-
|
Androgen Receptor
Apoptosis
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Cancer
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BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .
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-
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- HY-118091A
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LY300502
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Others
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Cancer
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Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer .
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-
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- HY-153772
-
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Androgen Receptor
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Cancer
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Androgen receptor antagonist 8 (Example 13) is an androgen receptor antagonist. Androgen receptor antagonist 8 inhibits prostate specific antigen secretion in LNcap cell (IC50: 88 nM). Androgen receptor antagonist 8 can be used for prostate cancer research .
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-
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- HY-156778
-
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Others
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Cancer
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Antitumor agent-120 (compound 1) is a flavonoid compound isolated from Kudzu root.Antitumor agent-120 has no significant inhibitory activity against LNCaP and PC3 cancer cells, with IC50s >50 μM .
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-
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- HY-17548
-
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Caspase
Apoptosis
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Cancer
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VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. VMY-1-103 reduces mitochondrial membrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP .
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-
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- HY-142772
-
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Epigenetic Reader Domain
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Cancer
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Y08284 is a potent, selective, oral active CBP bromodomain inhibitor with an IC50 of 4.21 nM. Y08284 suppresses the proliferation of prostate cancer cell lines LNCaP, C4-2B, and 22Rv1. Antitumor activity .
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-
-
- HY-118375
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ISC-4
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Apoptosis
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Cancer
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Phenylbutyl isoselenocyanate (ISC-4) is a selective apoptosis inducer that increases reactive oxygen species levels to inhibit androgen receptor (AR) and activate p53 pathway. Phenylbutyl isoselenocyanate induces apoptosis in LNCaP prostate cancer cells and has anti-prostate cancer properties.
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-
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- HY-149914
-
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Androgen Receptor
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Cancer
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WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell) .
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-
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- HY-161741
-
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Androgen Receptor
|
Cancer
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VinclozolinM2-2204 is a androgen receptor (AR) degrader, with an DC50 of 200 nM in LNCaP prostate cancer cells. VinclozolinM2-2204 induces the formation of AR +LC3 + autophagic membranes. VinclozolinM2-2204 can be used for the research of cancer .
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-
-
- HY-164662
-
|
mTOR
PI3K
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Cancer
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mTOR inhibitor-24 (comounp 9d) is a mTOR inhibitor, with IC50s of 0.34 nM (mTOR) and 324 nM (PI3K-α) respectively. mTOR inhibitor-24 inhibtis LNCaP cell proliferation (IC50: 180 nM) .
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- HY-139970
-
|
Androgen Receptor
|
Endocrinology
Cancer
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VPC-13789 is a potent, selective, and orally bioavailable antiandrogen. VPC-13789 can be used for the research of castration-resistant prostate cancer (CRPC) therapeutics. VPC-13789 inhibits androgen receptor (AR) transcriptional activity in LNCaP cells (IC50=0.19 μM) .
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-
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- HY-130992
-
|
Androgen Receptor
Ligands for Target Protein for PROTAC
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Cancer
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Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM . Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively .
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-
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- HY-115282A
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TRC-253
|
Androgen Receptor
|
Cancer
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JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
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-
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- HY-129672
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25-Dihydrostichorrenoside E
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Others
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Cancer
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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 .
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-
-
- HY-169282
-
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Others
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Cancer
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RGS2–Galpha-q interaction-IN-1 (Compound AJ-3) is an inhibitor of the RGS2-Galpha-q interaction. RGS2–Galpha-q interaction-IN-1 can inhibit the growth of cancer cell lines expressing RGS2 and exhibits anti-cell migration properties .
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-
-
- HY-162794
-
|
Apoptosis
Deubiquitinase
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Cancer
|
YCH3124 (compound Z33) is a USP7 inhibitor (IC50=41.9 nM) with antitumor activity. YCH3124 has good in vitro antiproliferative activity against various tumor cells including LNCaP (IC50=3.6 nM) and CHP-212 (IC50=9.9 nM). In addition, YCH3124 disrupts cell cycle progression by restricting G1 phase and induces apoptosis in CHP-212 cells .
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-
-
- HY-115282
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TRC-253 free base
|
Androgen Receptor
|
Cancer
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JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
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-
-
- HY-144127
-
|
Androgen Receptor
|
Cancer
|
AR antagonist 3 is a potent and selective androgen receptor (AR) antagonist with an IC50 of 0.47 µM. AR antagonist 3 exhibits a dose-dependent decrease of the FRET signal (IC50= 18.05 μM). AR antagonist 3 shows effective inhibition on tumor growth when administered intratumorally .
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-
-
- HY-152520
-
|
Androgen Receptor
|
Cancer
|
RLA-5331 is an iron activator containing anti-androgen. RLA-5331 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
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-
-
- HY-121094
-
|
Estrogen Receptor/ERR
|
Cancer
|
Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
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-
-
- HY-156003
-
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HDAC
|
Cancer
|
HDAC-IN-64 (Compound 13) is a HDAC inhibitor. HDAC-IN-64 inhibits HDAC4/5/6/7/9 with IC50s of 24, 45, 85, 31, 37 nM. HDAC-IN-64 has anti-proliferative activity and anti-migration properties on prostate cancer (PCA) cells. HDAC-IN-64 inhibits LNCaP and RWPE-1 cell growth with GI50 of 0.32 and 1.1 μM respectively .
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-
-
- HY-16079
-
AZD3514
3 Publications Verification
|
Androgen Receptor
|
Cancer
|
AZD3514 is an orally activie and selective androgen receptor (AR) inhibitor. AZD3514 androgen-dependently and -independently inhibits AR signal. AZD351 down-regulates nuclear AR levels in human LNCaP prostate cancer cells in the absence of androgen with an pIC50 value of 5.75. AZD3514 can be used for the research of prostate cancer .
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-
-
- HY-N7510
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12-Methoxycarnosic acid
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5 alpha Reductase
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Infection
Cancer
|
12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity .
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-
- HY-W748509
-
|
Caspase
Apoptosis
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Cancer
|
Pipernonaline is a piperine derivative with antiprostate cancer activity. Pipernonaline inhibits the proliferation of androgen-dependent/independent LNCaP/PC-3 prostate cells. Pipernonaline activates caspase-3 and promotes procaspase-3/PARP cleavage. Pipernonaline also mediates reactive oxygen species (ROS) production, increased intracellular Ca(2+), and mitochondrial membrane depolarization .
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-
- HY-152512
-
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Androgen Receptor
|
Cancer
|
RLA-4842 is an iron activator containing anti-androgen. RLA-4842 has anti-proliferative activity on metastatic castration-resistant prostate cancer (mCRPC) cell line .
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-
- HY-W012088
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Myristoleic acid methyl ester; Methyl myristoleate; cis-9-Tetradecenoate methyl ester
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Others
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Infection
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(Z)-Methyl tetradec-9-enoate (Myristoleic acid methyl ester; Methyl myristoleate) is a cytotoxic component extracted from S. repens fruit extract. It induces apoptosis and necrosis in human prostate cancer LNCaP cells. In addition, (Z)-Methyl tetradec-9-enoate found in cheese-making byproducts inhibits Candida albicans germination with a minimum inhibitory concentration (MIC) of 9 μM in vivo.
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- HY-133045
-
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Ligands for E3 Ligase
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Cancer
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VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM .
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-
- HY-162702
-
|
Androgen Receptor
PROTACs
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Cancer
|
AZ‘3137 (Compound 22) is an orally active PROTAC-type androgen receptor (AR) degrader, with a DC50 value of 22 nM. AZ'3137 can inhibit cell proliferation of LNCaP, with a GI50 value of 74 nM. AZ'3137 can inhibit AR signaling and tumor growth in prostate cancer mice (Red: AR antagonists; Blue: CRBN ligand (HY-A0003); Black: linker) .
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- HY-151533
-
|
Epigenetic Reader Domain
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Cancer
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PBRM1-BD2-IN-6 is a potent PBRM1 bromodomain inhibitor with an IC50 value of 0.22 μM. PBRM1-BD2-IN-6 shows antiproliferation activity. PBRM1-BD2-IN-6 has the potential for the research of PBRM1-dependent cancer .
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-
- HY-169078
-
|
Histone Methyltransferase
|
Cancer
|
ML234 is a dual inhibitor against EZH2/LSD1 with IC50 values of 0.09 and 0.12 μM, respectively. ML234 displays an excellent antiproliferative capacity against prostate cancer cell lines LNCAP, PC3 and 22RV1. ML234 suppresses the tumor growth in the 22RV1 xenograft mouse model. ML234 is promising for research of anticancer agents in prostate cancer .
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-
- HY-156111
-
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PROTACs
Androgen Receptor
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Cancer
|
ARD-1676 is an orally available androgen receptor (AR) PROTAC degrader, consisting of AR ligand and cereblon ligand. ARD-1676 has AR-degrading activity in vitro and in vivo and inhibits VCaP tumor growth in mouse xenograft tumor models .
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- HY-163510
-
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Androgen Receptor
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Cancer
|
AR/AR-V7-IN-1 (Compound 20i) is an AR/ARV7 inhibitor (IC50 = 172.85 nM). AR/AR-V7-IN-1 potently inhibits cell growth with IC50 values of 4.87 and 2.07 μM in the LNCaP and 22RV1 cell lines, respectively. AR/AR-V7-IN-1 exhibits effective tumor growth inhibition in the 22RV1 xenograft study. AR/AR-V7-IN-1 can be used for the research of prostate cancer .
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-
- HY-N7510R
-
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5 alpha Reductase
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Infection
Cancer
|
12-O-Methylcarnosic acid (Standard) is the analytical standard of 12-O-Methylcarnosic acid. This product is intended for research and analytical applications. 12-O-Methylcarnosic acid (12-Methoxycarnosic acid), a diterpene carnosic acid isolated from the acetone extract of Salvia microphylla, is an active constituent of 5α-reductase inhibition with an IC50 value of 61.7 μM. 12-O-Methylcarnosic acid inhibits proliferation in LNCaP cells. 12-O-Methylcarnosic acid has antioxidant, anti-cancer and antimicrobial activity .
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-
- HY-109015S
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Chidamide-d4; HBI-8000-d4; CS 055-d4
|
Isotope-Labeled Compounds
HDAC
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Cancer
|
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
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- HY-146396
-
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Others
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Cancer
|
Anticancer agent 51 (compound 3d) is a potent anticancer agent with an Ki of 731.62 nM. Anticancer agent 51 shows anticancer activity. Anticancer agent 51 has the potential for the research of prostate cancer .
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-
- HY-116895
-
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Androgen Receptor
MAGL
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Metabolic Disease
|
JJH260 is AIG1inhibitor, and inhibit the fluorophosphonate reactivity and fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1in HEK293T cells, with IC50 values of 0.50 μM and 0.57 μM, respectively .
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-
- HY-133020
-
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PROTACs
Androgen Receptor
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Cancer
|
ARD-266 is a highly potent and von Hippel-Lindau E3 ligase-based Androgen Receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . ARD-266 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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-
- HY-158113
-
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Histone Acetyltransferase
PROTACs
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Cancer
|
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC50 of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC50s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .
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- HY-N8504
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NSC 260179; Spectinabilin
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Bacterial
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Infection
|
Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50=13 μM) and inhibits DHT-induced expression of prostate-specific antigen in LNCaP cells (IC50=1.75 nM). Neoaureothin is cytotoxic to A549, HCT116, and HepG2 cells (IC50s=34.3, 47, and 37.2 μg/mL, respectively). It also has nematocidal activity against the pine wood nematode B. xylophilus (LC50=0.84 μg/mL) and increases survival of P. densiflora trees inoculated with B. xylophilus.
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-
- HY-19747
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HPOB
3 Publications Verification
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HDAC
Apoptosis
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Cancer
|
HPOB is a highly potent and selective inhibitor of HDAC6 with an IC50 of 56 nM. HPOB displays >30 fold less potent against other HDACs. HPOB enhances the effectiveness of DNA-damaging anticancer agents in transformed cells but not normal cells. HPOB does not block the ubiquitin-binding activity of HDAC6 .
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- HY-135732
-
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Androgen Receptor
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Cancer
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SK33, a trifluoromethylated enobosarm analog, is a potent, and tissue selective anti-androgen. SK33reduces androgen receptor (AR) transcriptional activity .
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- HY-161369
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PROTACs
Histone Acetyltransferase
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Cancer
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CBPD-268 is a potent and orally active CBP/p300 PROTAC degrader with an DC50 value of ≤ 0.03 nM. CBPD-268 induces CBP/p300 degradation and inhibits cell growth. CBPD-268 shows antitumor activity. CBPD-268 has the potential for the research of AR-positive prostate cancer (Srtucture Note: Red, Androgen receptor degrader (HY-W248665A); Blue, CBP/p300 ligand (HY-161483); Black, Linker) .
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- HY-151576
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Others
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Cancer
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PRMT5:MEP50 PPI is a novel PRMT5:MEP50 protein-protein interaction (PRMT5:MEP50 PPI) inhibitor, shows anti-tumor activity and anti-proliferative activity of lung and prostate cancer cells .
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- HY-164477
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Androgen Receptor
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Cancer
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FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
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- HY-133044
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PROTAC Linkers
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Cancer
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Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM . Boc-Pip-alkyne-Ph-COOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-108250
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Androgen Receptor
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Cancer
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(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer .
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- HY-144636
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Atg4
Cathepsin
Phospholipase
Autophagy
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Cancer
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Atg4B-IN-2 is a potent competitive Atg4B inhibitor with Ki value of 3.1 μM, also possesses declining PLA2 inhibitory potency, IC50s of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. Atg4B-IN-2 enhances the anticancer activity of anti-castration-resistant prostate cancer agents via autophagy inhibition .
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- HY-151172
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MDM-2/p53
Apoptosis
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Cancer
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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 .
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- HY-160777
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Galeterone 3β-imidazole
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Androgen Receptor
MNK
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Cancer
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VNPP433-3β is a molecular glue degrader, which degrades androgen receptor (AR) and its splice variants (AR-Vs) and MAP kinase-interacting serine/threonine protein kinase Mnk1/2. VNPP433-3β inhibits proliferation of cancer cell LNCaP, C4-2B and CWR22Rv1 with GI50 of 0.2, 0.3 and 0.31 μM. VNPP433-3β exhibits good pharmacokinetic characters in CD-1 mouse and inhibits tumor growth in the CWR22Rv1 xenograft mouse model .
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- HY-162706
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CDK
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Cancer
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BSJ-5-63 is a potent CDK12, CDK7, CDK9 degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer .
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- HY-115747
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Histone Demethylase
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Cancer
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Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research .
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- HY-149091
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Others
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Cancer
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KDM5B-IN-4 (compound 11ad) is a lysine demethylase 5B (KDM5B) inhibitor with an IC50 of 0.025 μM KDM5B-IN-4 increases substrate H3K4me1/2/3 level by inhibiting KDM5B in PC-3 cells. KDM5B-IN-4 downregulates PI3K/AKT. KDM5B-IN-4 reduces tumor volume in mice and shows less toxic to organs .
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- HY-13915
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Apoptosis
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Cancer
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NSC348884 is a nucleophosmin (NPM) inhibitor, it disrupts oligomer formation and induces apoptosis, inhibits cell proliferation with IC50s of 1.7-4.0 μM in distinct cancer cell lines. NSC348884 can be used for the research of cancer .
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- HY-125727
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Fungal
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Infection
Cancer
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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 .
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- HY-124089
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Cannabinoid Receptor
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Metabolic Disease
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Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
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- HY-163468
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Src
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Cancer
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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 .
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- HY-12325
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Fatty Acid Synthase (FASN)
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Cancer
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GSK2194069 is a potent inhibitor of β-ketoyl reductase (KR) of fatty acid synthase (FASN), with an IC50 value of 7.7 nM. GSK2194069 shows specifically inhibitory effect on FAS expressing cancer cells, by acting potent efficacy on acetoacetyl-CoA, NADPH with IC50 or Ki values of 4.8 nM and 5.6 nM, respectively .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-70002S1
-
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Enzalutamide-d6 is a deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells[1].
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- HY-70002S
-
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Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells .
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- HY-13626S
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Spisulosine-d3 is deuterium labeled Spisulosine. Spisulosine (ES-285) is an antiproliferative (antitumoral) compound of marine origin. Spisulosine inhibits the growth of the prostate PC-3 and LNCaP cells through intracellular ceramide accumulation and PKC
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- HY-109015S
-
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Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
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