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T36841 |
IPI-9119
|
|
Fatty Acid Synthase
|
|
IPI-9119 is an orally active, selective and irreversible FASN inhibitor (IC50 = 0.3 nM). |
|
T2430 |
HPOB
|
|
Apoptosis
,
HDAC
|
|
|
|
T12928 |
SK33
|
|
Androgen Receptor
|
|
SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity. |
|
T6002 |
Enzalutamide
|
MDV3100 |
Androgen Receptor
,
Autophagy
|
|
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate canc... |
|
T21740 |
RD162
|
|
Androgen Receptor
|
|
RD162 is a non-steroidal antiandrogen (NSAA) specifically binding to the androgen receptor (AR). |
|
T9246 |
JNJ-63576253
|
|
Androgen Receptor
|
|
JNJ-63576253 is a Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). |
|
T6400 |
AZD3514
|
|
Androgen Receptor
|
|
AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1. |
|
T4697 |
ABBV-744
|
ABBV744 |
Epigenetic Reader Domain
,
HIV Protease
|
|
ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2/3/4. It is used in the research on inflammatory diseases, cancer, and AIDS. |
|
T1267 |
Abacavir
|
Epzicom,Ziagen,Abacavir sulfate |
Apoptosis
,
HIV Protease
,
Reverse Transcriptase
|
|
Abacavir (Ziagen) is a nucleoside reverse transcriptase inhibitor analog of guanosine. This agent decreases HIV viral loads, retards or prevents the damage to the immune system, and reduces the risk of developing AIDS. |
|
T9179 |
CLP-3094
|
2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE |
Androgen Receptor
|
|
CLP-3094 (2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE) is a potent androgen receptor BF3 (binding function 3) inhibitor. BF3-IN-1 inhibits AR transcriptional activity with IC50 of 4 μM. CLP-3094 is a selective and potent GP... |
|
T10359 |
AR antagonist 1
|
|
Androgen Receptor
,
Ligand for E3 Ligase
,
Ligands for Target Protein for PROTAC
|
|
AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266. |
|
T6367 |
Abacavir sulfate
|
Abacavir Hemisulfate,1592U89,ABC sulfate,Ziagen |
Apoptosis
,
HIV Protease
,
Reverse Transcriptase
|
|
Abacavir sulfate (Ziagen) , a nucleoside analogue, effectively utilize its antiviral activity |
|
T60019 |
VPC-70063
|
Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)- |
Apoptosis
,
PARP
,
c-Myc
|
|
VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX. VPC-70063 exhibits Myc-Max transcriptional activity inhibition of 106% with an IC50 of 8.9 μM and Myc-Max/UBE2C do... |
|
T6909 |
NSC348884
|
|
Apoptosis
,
p53
|
|
NSC348884 is a nucleophosmin inhibitor disrupts oligomer formation and induces apoptosis, inhibits cell proliferation at an IC50 of 1.7-4.0 μM in distinct cancer cell lines. |
|
T8933 |
JNJ-63576253 free base
|
TRC253,JNJ-63576253 |
Androgen Receptor
|
|
JNJ-63576253 free base (TRC253) 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 re... |
|
T29110 |
VPC-13163
|
2,3-dihydro-2,3'-Bi-1H-indole,VPC13163,NSC52361,NSC 52361,VPC 13163 |
Others
|
|
VPC-13163 (NSC-52361) has strong anti-proliferative activity against LNCaP and Enzalutamide-resistant prostate cancer cell lines (MR49F) whereas it did not affect the growth of AR independent PC3 cell line. It also inhib... |
|
T67705 |
MTOR inhibitor 9a
|
|
|
|
mTOR inhibitor 9a inhibited the growth of human LNCap cells with an ic50 of 80 nm. 1-methyl-3 -{4-[4-(8-oxa-3-azabicyclo[3.2.1]oct-3-yl)thieno[3,2-d]pyrimidin-2-yl]phenyl}urea may have antitumor activity. |
|
T39695 |
ARD-2128
|
|
Androgen Receptor
|
|
ARD-2128 is a highly potent, orally bioavailable PROTAC (proteolysis-targeting chimera) degrader of the androgen receptor (AR), effectively diminishing AR protein levels, suppressing AR-regulated gene expression in tumor... |
|
T26323 |
VPC-3033
|
|
|
|
VPC-3033 is an antagonist of the androgen receptor. It acts by inhibiting the LNCaP cell line as well as cell lines with the wild-type androgen receptor. |
|
T24407 |
LG190119
|
LG-190119,LG 190119 |
|
|
LG190119 is a nonsecosteroidal vitamin D receptor modulator. It effectively inhibited LNCaP xenograft tumor growth without increased serum calcium levels or any other apparent side effects. It also inhibits the growth of... |
|
T78989 |
BET-IN-16
|
|
Epigenetic Reader Domain
|
|
BET-IN-16 (Comp I), a bromodomain and extra-terminal (BET) inhibitor, demonstrates anticancer activity by impeding the growth of prostate cancer cells. It exhibits potent inhibitory effects with half-maximal inhibitory c... |
|
T63324 |
Androgen receptor antagonist 5
|
|
|
|
Androgen receptor antagonist 5 is a potent antagonist of the androgen receptor (AR) (IC50: 6.17 μM). Androgen receptor antagonist 5 inhibited the proliferation of prostate cancer cells LNCaP and showed antitumor effect i... |
|
T67702 |
MTOR inhibitor 9d
|
|
PI3K
,
mTOR
|
|
mTOR inhibitor 9d is a dual inhibitor of the protein kinases mTOR and PI3K with an mTOR IC50 value of 0.31 nm, and can be used for the treatment of leukemia, skin cancer, breast cancer, lung cancer and colon cancer. |
|
T11208 |
Enzalutamide-d3
|
MDV3100 D3 |
Others
|
|
Enzalutamide D3 is a deuterium labeled Enzalutamide . Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. |
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T60942 |
MC2652
|
|
|
|
MC2652 (compound 1a) is a potent LSD1 inhibitor that shows high inhibitory effects in leukaemia cells MV4-11 and NB4. MC2652 has antiproliferative activity against LNCaP cells of prostate cancer [1]. |
|
T83007 |
Antitumor agent-120
|
|
|
|
Antitumor agent-120 (compound 1), a flavonoid derived from Kudzu root, exhibits negligible inhibitory effects on LNCaP and PC3 cancer cells, with IC50 values exceeding 50 μM [1]. |
|
T24411 |
Y08060
|
Y 08060,Y-08060 |
|
|
Y08060 is an effective and selective BET Inhibitor for the Treatment of Prostate Cancer. Y08060 effectively suppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC ... |
|
T83853 |
L-K6L9 TFA
|
|
|
|
L-K6L9, a cytolytic peptide comprised of L-isomer leucine and lysine, demonstrates cytotoxicity against both androgen-independent (LNCaP-CL1) and androgen-dependent (22Rv1 and LNCaP) human prostate cancer cells, with LC5... |
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T10320 |
Androgen receptor antagonist 1
|
|
Others
|
|
Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP... |
|
T63109 |
Y08284
|
|
|
|
Y08284 is a selective, potent, orally active inhibitor of CBP bromodomain (IC50: 4.21 nM). y08284 inhibits the proliferation of the prostate cancer cell lines LNCaP, C4-2B and 22Rv1 and has anti-tumour effects. |
|
T70962 |
MHY219
|
|
|
|
MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) whe... |
|
T69438 |
MT477
|
|
|
|
MT477 is PKC-α inhibitor. MT477 interfered with PKC activity as well as phosphorylation of Ras and ERK1/2 in H226 human lung carcinoma cells. It also induced poly-caspase-dependent apoptosis. MT477 had a dose-dependent (... |
|
T78922 |
ARD-2051
|
|
PROTACs
|
|
ARD-2051 is a potent, orally active proteolysis-targeting chimera degrader of the androgen receptor (AR), exhibiting DC50 values of 0.6 nM in degrading AR protein within LNCaP and VCaP prostate cancer cell lines. It hold... |
|
T61653 |
VPC-13789
|
|
|
|
VPC-13789 is a highly potent, selective, and orally bioavailable antiandrogen compound that shows promise for studying and developing therapeutics for castration-resistant prostate cancer (CRPC). In LNCaP cells, VPC-1378... |
|
T78810 |
BWA-522
|
|
Androgen Receptor
|
|
BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL) and the AR-V7 splice variant. It specifically antagonizes the... |
|
T78945 |
WCA-814
|
|
Androgen Receptor
|
|
WCA-814, an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate, induces degradation of both full-length and AR-V7, exhibiting cytotoxic effects in prostatic cancer cells with half maximal inhibitory concentratio... |
|
T9660 |
Bexlosteride
|
|
|
|
Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP huma... |
|
T13552 |
ARD-266
|
|
Others
|
|
ARD-266 is a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces the degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines (DC50s... |
|
T61022 |
LSD1-IN-17
|
|
|
|
LSD1-IN-17 (compound 5b) is a potent inhibitor of LSD1 that inhibits LSD1-CoREST, MAO-A and MAO-B, with IC 50 values of 0.005, 0.028, and 0.820 μM, respectively. LSD1-IN-17 exhibits cell growth arrest in prostate cancer ... |
|
T61021 |
LSD1-IN-16
|
|
|
|
LSD1-IN-16 (compound 4b) is a potent inhibitor of LSD1 that inhibits LSD1-CoREST, MAO-A and MAO-B with IC50 values of 0.015, 0.024, and 0.366 μM, respectively. LSD1-IN-16 exhibits cell growth arrest in prostate cancer LN... |
|
T60941 |
LSD1-IN-15
|
|
|
|
LSD1-IN-15 (compound 1b) is a potent LSD1 inhibitor that inhibit LSD1-CoREST, MAO-A and MAO-B with IC 50 values of 0.149, 0.028, and 0.327 μM, respectively. LSD1-IN-15 shows cell growth arrest in LNCaP cells of prostate ... |
|
T13958 |
VHL Ligand 8
|
|
Others
|
|
VHL Ligand 8, a VHL ligand essential for synthesizing ARD-266, acts as a highly potent VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. It efficiently facilitates the degradation of AR protein in AR-positive p... |
|
T63200 |
NTQ1062
|
|
|
|
NTQ1062 (compound 22b) is an orally active and potent Akt inhibitor that acts on Akt1 (IC50: 0.4 nM), Akt2 (IC50: 6.3 nM) and Akt3 (IC50: 0.1 nM). NTQ1062 showed significant anti-tumor effects in the LNCap xenograft tumo... |
|
T17689 |
Boc-Pip-alkyne-Ph-COOH
|
|
Others
|
|
Boc-Pip-alkyne-Ph-COOH, a PROTAC linker characterized by its alkyl/ether composition, plays a crucial role in synthesizing PROTACs including ARD-266. This compound demonstrates significant efficacy in promoting the degra... |
|
T35668 |
Neoaureothin
|
|
|
|
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 exp... |
|
T79674 |
HDAC-IN-64
|
|
HDAC
|
|
HDAC-IN-64 (Compound 13), an HDAC inhibitor, demonstrates potent inhibition of HDAC4/5/6/7/9 with IC50 values of 24, 45, 85, 31, and 37 nM, respectively. It exhibits anti-proliferative and anti-migration effects on prost... |
|
T38107 |
JJH260
|
JJH260 |
|
|
JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value... |
|
T36457 |
CAY10416
|
|
|
|
Dual cyclooxygenase-2 (COX-2)/5-lipoxygenase (5-LO) inhibitors are potential therapeutic agents for inflammatory diseases and for prostate cancer. CAY10416 is a dual COX-2/5-LO inhibitor with IC50 values of 50 and 3 nM, ... |
|
T69758 |
Flutamide-d7
|
|
|
|
Flutamide-d7 is intended for use as an internal standard for the quantification of flutamide by GC- or LC-MS. Flutamide is an androgen receptor antagonist and prodrug form of 2-hydroxy flutamide. Flutamide is converted ... |
|
T69618 |
XR3054
|
|
|
|
XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.... |
