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Search Results for " ar-v7 "

13

Compounds

Cat No. Product Name Synonyms Targets
T36841 IPI-9119 Fatty Acid Synthase
IPI-9119 is an orally active, selective and irreversible FASN inhibitor (IC50 = 0.3 nM).
T61820 Ar-V7-IN-1
Ar-V7-IN-1 is a highly potent inhibitor specifically targeting Ar-V7, a splice variant of the androgen receptor that exhibits hormone-independent behavior. Its development shows promise for researching various indication...
T74410 PROTAC AR-V7 degrader-1
PROTAC AR-V7 degrader-1 (Compound 6) is an orally bioavailable, potent, and selective degrader targeting the androgen receptor (AR) variant V7, achieving degradation with a DC50 of 0.32 µM by directing the VHL E3 ligase ...
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...
T36375 Ralaniten triacetate
Ralaniten triacetate (EPI-506) is a novel pro-drug of Ralaniten, functioning as an orally active inhibitor of the androgen receptor (AR) N-terminal domain (NTD). Its remarkable first-in-class status signifies its unique ...
T9005 VPC-80051 racemate Others
VPC-80051 is the first small molecule inhibitor of hnRNP A1 splicing activity by using a computer-aided drug discovery approach.
T79465 Anticancer agent 135 Androgen Receptor
Anticancer agent 135 (compound 26h) acts as a potent androgen receptor (AR) antagonist, effectively blocking AR nuclear translocation and inhibiting AR/AR-V7 heterodimerization to suppress downstream gene transcription. ...
T78811 PROTAC AR-NTD degrader 1 Androgen Receptor
PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal domain (AR-NTD) of the Androgen Receptor variant AR-V7. By antago...
T74744 MTX-23
MTX-23, an AR-targeted Proteolysis Targeting Chimera (PROTAC), effectively degrades both AR-V7 and AR-FL, inhibiting the proliferation of CaP cells and inducing apoptosis [1].
T79156 (R)-SKBG-1 Androgen Receptor
(R)-SKBG-1 is an inhibitor of the RNA-binding protein NONO, effectively downregulating androgen receptor expression by targeting both AR-FL mRNA and AR-V7 mRNA, with inhibition concentration (IC50) values of 3.1 μM and 5...
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...
T39071 Thailanstatin D
Thailanstatin D, an analogue of Thailanstatin A, inhibits AR-V7 gene splicing by disrupting the interaction between U2AF65 and SAP155, hindering their binding to the polypyrimidine tract situated between the branch point...
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