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)。 | |||
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。 | |||
T61327 |
BRD4 Inhibitor-15
|
||
BRD4 Inhibitor-15 (compound 13) is a highly potent and specific inhibitor of BRD4, effectively inhibiting it with an IC50 of 18 nM. By regulating the Bcl-2/Bax proteins and activating the caspase-3 signaling pathway, BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells. Additionally, it effectively down-regulates the c-Myc level in 22RV1 cells. Due to its properties, BRD4 Inhibitor-15 is a valuable compound for research related to prostate cancer [1]. | |||
T78837 |
CP-07
|
CDK | Cell Cycle/Checkpoint |
CP-07为高效的PROTAC CDK9选择性降解剂(DC50:43 nM),能显著抑制22RV1细胞增殖(IC50:62 nM)及集落形成,其作用机制为通过下调Mcl-1与c-Myc。此外,CP-07有效抑制22RV1异种移植肿瘤的生长,有望成为研究前列腺癌的重要化合物。 | |||
T63109 |
Y08284
|
||
Y08284 是一种选择性的、高效的、口服具有活力的 CBP bromodomain 抑制剂 (IC50: 4.21 nM)。Y08284 能够抑制前列腺癌细胞系 LNCaP、C4-2B 和 22Rv1 的增殖,并具有抗肿瘤效果。 | |||
T78989 | BET-IN-16 | Epigenetic Reader Domain | Chromatin/Epigenetic |
BET-IN-16 (Comp I) 是一种BET抑制剂,展现出抗癌活性。BET-IN-16抑制前列腺癌细胞的生长,其对LNCaP和22Rv1细胞的IC50值分别为0.043 μM和0.034 μM。 | |||
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)。 | |||
T13552 |
ARD-266
|
Others | 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: 0.2-1 nM). | |||
T13958 | VHL Ligand 8 | Others | Others |
VHL Ligand 8 是一种 von Hippel-Lindau (VHL) 蛋白配体,可用于合成 ARD-266 。ARD-266 是一种基于 VHL E3 连接酶的高效雄激素受体 (AR) PROTAC 降解剂。ARD-266 在 AR 阳性 LNCaP,VCaP 和 22Rv1 前列腺癌细胞系中有效诱导 AR 蛋白降解,DC50值为 0.2-1 nM。 | |||
T17689 |
Boc-Pip-alkyne-Ph-COOH
|
Others | 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 degradation of androgen receptor (AR) protein across AR-positive prostate cancer cell lines such as LNCaP, VCaP, and 22Rv1, showcasing DC50 values ranging from 0.2-1 nM[1]. | |||
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。 | |||
T83853 |
L-K6L9 TFA
|
||
L-K6L9 是由 L-亮氨酸和 L-赖氨酸的L-异构体组成的溶细胞肽。对LNCaP-CL1 雄激素独立型和22Rv1以及LNCaP雄激素依赖型人类前列腺癌细胞具有细胞毒性(LC50分别为4、4和6 µM),同时也对非癌性NIH3T3小鼠成纤维细胞和OL人类包皮成纤维细胞具有细胞毒性(LC50分别为7和5 µM)。在100 µM的浓度下,引起分离的人类红细胞溶血。 | |||
T83936 |
LL-K9-3
|
||
LL-K9-3是一种基于选择性疏水标记技术(HyT)的CDK9-cyclin T1复合物降解剂(DC50值分别为cyclin T1的589 nM和CDK9的662 nM)。它由CDK9抑制剂SNS 032和一个糖基连接器连接到疏水标记组成。LL-K9-3不会降解其他CDKs(CDK1、2、4、5、6和7)。在22RV1细胞中,LL-K9-3通过诱导CDK9和cyclin T1的选择性和同步降解,降低雄激素受体(AR)和cMyc的表达。 | |||
T30123 |
ARD-69
|
||
ARD-69 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent mann | |||
T15205 |
EL-102
EL102 |
Microtubule Associated; HIF | Angiogenesis; Chromatin/Epigenetic; Cytoskeletal Signaling |
EL-102 是一种 HIF1α 抑制剂,具有抗癌活性,可抑制微管蛋白聚合,可用于研究前列腺癌。 |