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12

抑制剂 & 化合物

7

天然产物

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Cat. No. Product Name Target Signaling Pathways
T0380 Bicalutamide

比卡鲁胺,ICI-176334

Androgen Receptor; Autophagy Autophagy; Endocrinology/Hormones
Bicalutamide (ICI-176334) 是一种具有口服活性的非甾体雄激素受体拮抗剂,可研究前列腺癌。
T6400 AZD3514

Androgen Receptor Endocrinology/Hormones
AZD3514 是一种口服雄激素受体下调剂(Ki :2.2 μM),能够减少 AR 蛋白表达。
T6829 EPI-001

EPI001,EPI 001

Apoptosis; Androgen Receptor; PPAR Apoptosis; DNA Damage/DNA Repair; Endocrinology/Hormones; Metabolism
EPI-001 是一种选择性雄激素受体 (AR) 的抑制剂,靶向 AR 的反式激活单元 5,可抑制 AR 氨基末端结构域的反式激活,IC50值约为 6 μM。它也是一种选择性的PPARγ调节剂,对去势抵抗性前列腺癌具有活性。
T12928 SK33

Androgen Receptor Endocrinology/Hormones
SK33 是一种有效的组织选择性抗雄激素药物,是一种肌醇类似物,能够降低雄激素受体 (AR) 的转录活性。
T2236 RU 58841

4-[3-(4-羟基丁基)-4,4-二甲基-2,5-二氧代-1-咪唑烷基]-2-(三氟甲基)苯腈,RU58841,PSK-3841,HMR-3841

Androgen Receptor Endocrinology/Hormones
RU 58841 (PSK-3841) 是一种雄激素受体拮抗剂,能够促进头发再生。
T0272 Nilutamide

尼鲁米特,RU23908

Androgen Receptor Endocrinology/Hormones
Nilutamide (RU23908) 是一种非甾体抗雄激素药物,有用于转移性前列腺癌的潜力。
T13273 UT-34

Androgen Receptor Endocrinology/Hormones
UT-34 是选择性的、具有口服活性的泛雄激素受体拮抗剂和降解剂,能够作用于野生型 AR (IC50:211.7 nM)、F876L-AR (IC50:262.4 nM)、W741L-AR (IC50:215.7 nM)。它与配体结合结构域和功能 1结构域结合,并需要泛素蛋白酶体途径来降解AR。它有抗前列腺癌的能力。
T21016 Cyproterone

BAY 94-8367,Ciproterone,Androcur,SH 80881

Cyproterone, an anti-androgen, is used in combination with estrogen for the therapy of hirsutism and severe acne in females and as a palliative in prostatic carcinoma.
T75058 RLA-5331

RLA-5331,一种含有抗雄激素的铁活化剂,针对(mCRPC)细胞系显示出抗增殖活性。
T75057 RLA-4842

RLA-4842,含有抗雄激素性质的铁活化剂,表现出对于转移性去势抵抗性前列腺癌(mCRPC)细胞系的抗增殖活性。
T68406 A-849519

A-849519 is a reversible inhibitor of MetAP2 that has demonstrated anti-angiogenesis and anticancer activity in a number of in vitro and in vivo models. In this study, we evaluated the anticancer activity of A-849519 in a modified Dunning model of androgen-independent prostate cancer and compared its efficacy with TNP-470, an established MetAP2 inhibitor.
T81662 N-Nitrosodicyclohexylamine

NDCHA

Androgen Receptor Endocrinology/Hormones
N-Nitrosodicyclohexylamine (NDCHA) 是一种N-亚硝基化合物,具有抗雄激素活性。它通过与雄激素受体 (AR) 竞争性结合来抑制 5α-二氢睾酮的作用,并能降低 AR 蛋白水平。

化合物

Bicalutamide
Cat.No: T0380
Synonym: 比卡鲁胺,ICI-176334
Target: Androgen Receptor, Autophagy
AZD3514
Cat.No: T6400
Synonym:
Target: Androgen Receptor
EPI-001
Cat.No: T6829
Synonym: EPI001,EPI 001
Target: Apoptosis, Androgen Receptor, PPAR
SK33
Cat.No: T12928
Synonym:
Target: Androgen Receptor
RU 58841
Cat.No: T2236
Synonym: 4-[3-(4-羟基丁基)-4,4-二甲基-2,5-二氧代-1-咪唑烷基]-2-(三氟甲基)苯腈,RU58841,PSK-3841,HMR-3841
Target: Androgen Receptor
Nilutamide
Cat.No: T0272
Synonym: 尼鲁米特,RU23908
Target: Androgen Receptor
UT-34
Cat.No: T13273
Synonym:
Target: Androgen Receptor
Cyproterone
Cat.No: T21016
Synonym: BAY 94-8367,Ciproterone,Androcur,SH 80881
Target:
RLA-5331
Cat.No: T75058
Synonym:
Target:
RLA-4842
Cat.No: T75057
Synonym:
Target:
A-849519
Cat.No: T68406
Synonym:
Target:
N-Nitrosodicyclohexylamine
Cat.No: T81662
Synonym: NDCHA
Target: Androgen Receptor
Cat. No. Product Name Target Signaling Pathways
T2895 Lupeol

Fagarasterol,羽扇豆醇,Monogynol B,Clerodol,(3β,13ξ)-Lup-20(29)-en-3-ol,Farganasterol

Apoptosis; Androgen Receptor; Akt Apoptosis; Cytoskeletal Signaling; Endocrinology/Hormones; PI3K/Akt/mTOR signaling
Lupeol (Monogynol B) 是一个活跃的五环三萜,具有抗氧化剂、抗肿瘤和抗炎活性。它是一种雄激素受体抑制剂,可研究癌症,特别是雄激素依赖表型和去势抵抗表型的前列腺癌。
T14008 2,2,5,7,8-Pentamethyl-6-Chromanol

PMC

Androgen Receptor Endocrinology/Hormones
2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) 是维生素 E (α-tocopherol) 的抗氧化部分,能够有效的调节雄激素受体 (androgen receptor) 信号,及抗前列腺癌细胞系的抗癌活性。
TN1805 Isosilybin B

Apoptosis; Androgen Receptor Apoptosis; Endocrinology/Hormones
Isosilybin B 是一种从水飞蓟中提取的黄酮木脂素,具有抗前列腺癌 (PCA) 活性,对癌细胞增殖有抑制作用,促使 G1 期阻滞和凋亡。Isosilybin B 诱导雄激素受体降解。
T3851 Vicenin 2

Vicenin -2,维采宁 2,新西兰牡荆苷

RAAS Endocrinology/Hormones
Vicenin 2 来源于广金钱草 (Desmodium styracifolium) 的地上部分。Vicenin 2 是一种血管紧张素转换酶 (ACE) 抑制剂,IC50=43.83 μM。
TN6638 (E)-6-O-(p-coumaroyl)scandoside methyl ester

(E)-6-O-(p-coumaroyl)scandoside methyl ester shows moderate anti-proliferation effect on PC3 human androgen-independent prostate cancer cells.
T75702 Galloylalbiflorin

Galloylalbiflorin (6′-O-Galloylalbiflorin) 为芍药根部提取的雄性激素受体 (AR) 拮抗剂,具IC50值为53.3 μM,展现抗雄激素活性。
TN4774 Physalin A

ERK; BCL; p38 MAPK; NF-κB; Androgen Receptor; ROS; JAK; JNK; STAT; p53; Autophagy Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Endocrinology/Hormones; Immunology/Inflammation; JAK/STAT signaling; MAPK; NF-κB; Stem Cells
Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth through activation of cell apoptosis and downregulation of androgen receptor ex

天然产物

Lupeol
Cat.No: T2895
Synonym: Fagarasterol,羽扇豆醇,Monogynol B,Clerodol,(3β,13ξ)-Lup-20(29)-en-3-ol,Farganasterol
Target: Apoptosis, Androgen Receptor, Akt
2,2,5,7,8-Pentamethyl-6-Chromanol
Cat.No: T14008
Synonym: PMC
Target: Androgen Receptor
Isosilybin B
Cat.No: TN1805
Synonym:
Target: Apoptosis, Androgen Receptor
Vicenin 2
Cat.No: T3851
Synonym: Vicenin -2,维采宁 2,新西兰牡荆苷
Target: RAAS
(E)-6-O-(p-coumaroyl)scandoside methyl ester
Cat.No: TN6638
Synonym:
Target:
Galloylalbiflorin
Cat.No: T75702
Synonym:
Target:
Physalin A
Cat.No: TN4774
Synonym:
Target: ERK, BCL, p38 MAPK, NF-κB, Androgen Receptor, ROS, JAK, JNK, STAT, p53, Autophagy
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