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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T36841 |
IPI-9119
|
Fatty Acid Synthase | Metabolism |
IPI-9119 是一种具有口服活性、选择性和不可逆的 FASN 抑制剂 (IC50 = 0.3 nM)。 | |||
T60019 |
VPC-70063
Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)- |
Apoptosis; PARP; c-Myc | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; DNA Damage/DNA Repair |
VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) 是 c-Myc-MAX 的抑制剂。 VPC-70063 的 Myc-Max 转录活性抑制率为 106%,IC50 为 8.9 μM,Myc-Max/UBE2C 下游通路抑制率为 94%。 VPC-70063 可用于抗癌研究。 | |||
T74410 | PROTAC AR-V7 degrader-1 | ||
PROTACAR-V7 degrader-1 (Compound 6)为一种口服有效的,选择性针对AR-V7的降解剂,DC50值为0.32 µM,其作用机制主要是通过VHL E3连接酶将其招募至雄激素受体DNA结合域(AR DBD)。此外,PROTACAR-V7 degrader-1在表达AR-V7的22Rv1细胞系中展现出了活性,EC50值为0.88 µM。 | |||
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 indications, notably cancers such as prostate cancer[1]. | |||
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 nature within the field. This compound exhibits significant efficacy against various AR species, including AR-v7, which are associated with resistance. Notably, Ralaniten triacetate's activity encompasses full-length AR as well [1][2]. | |||
T9005 |
VPC-80051 racemate
|
Others | Others |
VPC-80051 是一种有效的 hnRNP A1 剪接活性抑制剂,靶向 hnRNP A1 RBD 并降低 22Rv1 CRPC 细胞系中的 AR-V7 信使水平。 | |||
T78811 |
PROTAC AR-NTD degrader 1
|
Androgen Receptor | Endocrinology/Hormones |
PROTACAR-NTD antagonist 1 (compound 18) 是一款针对雄激素受体AR-V7变体的PROTACs,它特异性地拮抗AR的N末端结构域 (AR-NTD),能有效诱导前列腺癌细胞凋亡,并在VCaP细胞中以1 μM 和 5 μM的浓度分别实现了62.2%和71.1%的AR-V7蛋白降解率。 | |||
T78810 |
BWA-522
|
Androgen Receptor | Endocrinology/Hormones |
BWA-522是一种口服有效的小分子PROTACs,针对AR-FL和AR-V7显示出显著的降解活性。该化合物通过对Androgen Receptor的AR-NTD进行拮抗,诱发PC细胞的apoptosis。在LNCaP异种移植模型中,BWA-522以每日60 mg/kg的剂量口服给药,实现了76%的肿瘤生长抑制(TGI=76%)。在VCaP和LNCaP细胞系中对AR-V7和AR-FL的降解效率分别达到77.3%(1 μM)和72.0%(5 μM)。 | |||
T74744 |
MTX-23
|
||
MTX-23为基于AR的PROTAC, 通过降解AR-V7与AR-FL,抑制CaP细胞增殖,并诱导细胞凋亡(apoptosis)。 | |||
T79465 |
Anticancer agent 135
|
Androgen Receptor | Endocrinology/Hormones |
Anticanceragent 135(compound 26h)为一有效的雄激素受体(AR)拮抗剂,能够阻断AR核转位并抑制AR/AR-V7异二聚化,以抑制下游基因转录。该化合物在前列腺癌异种移植模型中展现出显著疗效。 | |||
T79156 |
(R)-SKBG-1
|
Androgen Receptor | Endocrinology/Hormones |
(R)-SKBG-1为RNA结合蛋白NONO的抑制剂,能够抑制雄激素受体表达,并对AR-FL mRNA及AR-V7 mRNA具有IC50。 | |||
T78945 |
WCA-814
|
Androgen Receptor | Endocrinology/Hormones |
WCA-814是雄激素受体(AR)拮抗剂与Hsp90抑制剂的融合化合物,能够诱导全长AR及AR-V7降解,并展现出对前列腺癌细胞的细胞毒性(IC50: LNCaP细胞为171.2 nM,22Rv1细胞为26.5 nM)。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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 and the 3' splice site. This compound displays potent tumor inhibitory properties in human castration-resistant prostate cancer (CRPC) xenografts, resulting in cellular apoptosis. |