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20

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8395	Nomegestrol acetate	Others; Progesterone Receptor	Others
	Nomegestrol acetate 是一种孕酮受体的完全激动剂，是一种高选择性孕激素。
T28362	PF-02413873 PF02413873	Progesterone Receptor	Others
	PF-02413873 是一种非甾体孕酮受体的竞争性拮抗剂，Ki 为 2.6 nM。 PF-02413873 可用于治疗子宫内膜异位症等妇科疾病的研究。
T2567	Etonogestrel 3-Oxodesogestrel,3-keto-Desogestrel,依托孕烯,Nexplanon,Implanon	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Progesterone Receptor; Endogenous Metabolite	Endocrinology/Hormones; Metabolism; Others
	Etonogestrel (Implanon) 是孕激素去氧孕烯的生物活性代谢物，与靶器官中的孕酮受体和雌激素受体高亲和力地结合，可诱导FKBP51mRNA 和蛋白表达。它是一种甾体孕激素，用作激素避孕药。
T13703	Gestonorone Capronate	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Gestonorone Capronate 是一种孕激素，在良性前列腺肥大和子宫内膜癌领域有研究价值。
T1916	Apitolisib RG 7422,GNE 390,GDC-0980	Apoptosis; PI3K; mTOR	Apoptosis; PI3K/Akt/mTOR signaling
	Apitolisib (RG 7422) 是一种口服有效的 PI3K 和 mTOR(TORC1/2) 激酶抑制剂，抑制 PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ的活性，IC50值为 5 nM/27 nM/7 nM/14 nM，抑制 mTOR，Ki 为 17 nM。它用于乳腺癌、前列腺癌、肾细胞癌和子宫内膜癌等实体癌的试验研究。
T2357	GSK1059615 GSK 1059615,GSK-1059615	Apoptosis; PI3K; mTOR	Apoptosis; PI3K/Akt/mTOR signaling
	GSK1059615 是一种 PI3Kα/β/δ/γ可逆的抑制剂，同时也抑制 mTOR，IC50值分别为 0.4 nM/0.6 nM/2 nM/5 nM 和 12 nM，已用于研究淋巴瘤、实体瘤、子宫内膜癌、实体瘤癌和转移性乳腺癌治疗的试验。
T61864	Melengestrol acetate	Progesterone Receptor	Others
	Melengestrol acetate 是孕酮的衍生物，充当皮质类固醇激素。 Melengestrol acetate 可以促进月经活动和妊娠维持的子宫内膜增殖延迟。
T76749	Zilovertamab Cirmtuzumab,UC-961	Others	Others
	Zilovertamab (UC-961) 是一种人源化抗 ROR1 单克隆抗体，可切断 Wnt5a 诱导的 ROR1 信号通路，在卵巢癌和子宫内膜癌细胞中显示出抗增殖活性。可用于研究淋巴癌。
T11146	EC359 EC-359	Apoptosis; Others	Apoptosis; Others
	EC359 是一种具有高效性和选择性的白血病抑制因子受体 (LIFR) 抑制剂，是一种有效的具有抗癌活性，阻断 LIF/LIFR 相互作用，可用于研究白血病和子宫内膜癌。
T2527	Ulipristal acetate Ulipristal,醋酸乌利司他,CDB-2914	Estrogen/progestogen Receptor; Progesterone Receptor; Autophagy	Autophagy; Endocrinology/Hormones; Others
	Ulipristal acetate (CDB-2914) 是一种具有抗孕酮活性的选择性孕酮受体调节剂。它可抑制子宫平滑肌瘤病的生长。它通过抑制或延迟排卵和影响子宫内膜组织，可用作紧急避孕药。
T20755	Trimegestone RU27987,RU-27987,RU 27987
	Trimegestone, a highly effective oral progestogen, is used for endometrial protection, all doses inducing secretory endometrial transformation.
T61212	Steroid sulfatase-IN-2
	Steroid sulfatase-IN-2 is an active inhibitor of steroid sulfatase (STS), demonstrating an IC50 value of 109.5 nM. Its potential application lies in hormone-dependent cancer research, specifically estrogen-dependent breast and endometrial cancer [1].
T5317L	Cridanimod sodium XBIO-101,XBIO 101,Cycloferon,Sodium Cridanimod,Cridanimod Na,XBIO101
	Cridanimod can increase progesterone receptor (PR) expression, with potential antineoplastic adjuvant activity. Cridanimod is able to induce the expression of PR in endometrial cancer. In combination with a progestin, cancer cells could be eradicated thro
T36968	ARN-21934	Topoisomerase	DNA Damage/DNA Repair
	ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T72390	Estradiol hemihydrate 17β-Oestradiol hemihydrate,β-Estradiol hemihydrate ; 17β-Estradiol hemihydrate ; 17β-Oestradiol hemihydrate,17β-Estradiol hemihydrate,β-Estradiol hemihydrate
	Estradiol (β-Estradiol) hemihydrate 是主要女性性激素的类固醇激素。它能上调人类子宫内膜干细胞 (hEnSCs) 的神经标志物表达，促进神经分化，适用于癌症、神经退行性疾病和神经组织工程研究。
T71218	AEZS-112
	AEZS-112, also known as ZEN012, is an orally active small mol. anti-cancer drug which inhibits the polymn. of tubulin at low micromolar concns. AEZS 112 dose-dependently increased non-vital hypodiploid cells and the cytotoxic effect was least pronounced in G2 phase of the cell cycle, indicating cell death during mitosis, as detd. by FACS anal. AEZS 112 showed anti-tumor activity in human ovarian and endometrial cancer cell lines at low micromolar concns., which could not be abrogated by caspase ...
T74415	Imlunestrant tosylate
	Imlunestrant (LY-3484356) tosylate 是口服有效且选择性的雌激素受体(estrogen receptor, ER)降解剂(SERD)，具纯拮抗性。该化合物能持续抑制ER依赖的基因转录与细胞生长，适用于研究ER阳性(ER+)晚期乳腺癌(aBC)与子宫内膜样癌(EEC)。
T70775	Zoptarelin doxorubicin
	Zoptarelin doxorubicin, also known as AEZS-108, is an LHRH agonist. Zoptarelin doxorubicin is a peptide agonist of the gonadotropin releasing hormone-1 receptor (GnRH-1R) that is conjugated to the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Zoptarelin doxorubicin binds to GnRH-1Rs, which may be highly expressed on endometrial and ovarian tumor cell membrane surfaces, and is internalized. Once inside the cell, the doxorubicin moiety of this agent intercalates in...
T60854	ENMD-1068 hydrochloride
	ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride 可通过抑制TGF-β1/Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 hydrochloride 还能抑制子宫内膜细胞的增殖，并诱导病灶中上皮细胞的凋亡。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。
T36913	17-Epiestriol
	17-Epiestriol is a metabolite of estrone .1It is formed from estroneviaa 16α-hydroxy estrone intermediate by reduction of the C-17 ketone. 17-Epiestriol binds to estrogen receptor α (ERα) and ERβ with relative binding affinities of 29 and 80 compared with 17β-estradiol .2 1.Brinton, L.A., Trabert, B., Anderson, G.L., et al.Serum estrogens and estrogen metabolites and endometrial cancer risk among postmenopausal womenCancer Epidemiol. Biomarkers Prev.25(7)1081-1089(2016) 2.Kuiper, G.G.J.M., Lemme...

化合物

Nomegestrol acetate

Cat.No: T8395

Target: Others, Progesterone Receptor

Cat.No: T28362

Synonym: PF02413873

Target: Progesterone Receptor

Cat.No: T2567

Synonym: 3-Oxodesogestrel,3-keto-Desogestrel,依托孕烯,Nexplanon,Implanon

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Progesterone Receptor, Endogenous Metabolite

Gestonorone Capronate

Cat.No: T13703

Target: Prostaglandin Receptor

Cat.No: T1916

Synonym: RG 7422,GNE 390,GDC-0980

Target: Apoptosis, PI3K, mTOR

Cat.No: T2357

Synonym: GSK 1059615,GSK-1059615

Target: Apoptosis, PI3K, mTOR

Melengestrol acetate

Cat.No: T61864

Target: Progesterone Receptor

Cat.No: T76749

Synonym: Cirmtuzumab,UC-961

Target: Others

Cat.No: T11146

Synonym: EC-359

Target: Apoptosis, Others

Ulipristal acetate

Cat.No: T2527

Synonym: Ulipristal,醋酸乌利司他,CDB-2914

Target: Estrogen/progestogen Receptor, Progesterone Receptor, Autophagy

Cat.No: T20755

Synonym: RU27987,RU-27987,RU 27987

Steroid sulfatase-IN-2

Cat.No: T61212

Cridanimod sodium

Cat.No: T5317L

Synonym: XBIO-101,XBIO 101,Cycloferon,Sodium Cridanimod,Cridanimod Na,XBIO101

Cat.No: T36968

Target: Topoisomerase

Estradiol hemihydrate

Cat.No: T72390

Synonym: 17β-Oestradiol hemihydrate,β-Estradiol hemihydrate ; 17β-Estradiol hemihydrate ; 17β-Oestradiol hemihydrate,17β-Estradiol hemihydrate,β-Estradiol hemihydrate

Cat.No: T71218

Imlunestrant tosylate

Cat.No: T74415

Zoptarelin doxorubicin

Cat.No: T70775

ENMD-1068 hydrochloride

Cat.No: T60854

Cat.No: T36913

Cat. No.	Product Name	Target	Signaling Pathways
T1048	Estradiol 雌二醇,E2,17β-Estradiol,17β-Oestradiol,β-Estradiol	Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Endogenous Metabolite	Endocrinology/Hormones; Metabolism
	Estradiol (E2) 是一种天然的类固醇性激素，对于女性生育能力和第二性征的维持至关重要。Estradiol 通过雌激素受体 β (ERβ) 上调 IL-6 表达。
T1261	Medroxyprogesterone Acetate Medroxyprogesterone 17-acetate,Provera,Metigestrona,NSC-26386,醋酸甲羟孕酮,Farlutin,安宫黄体酮,Medroxyprogesterone (acetate)	Glucocorticoid Receptor; Estrogen/progestogen Receptor; Progesterone Receptor; Androgen Receptor; Endogenous Metabolite	Endocrinology/Hormones; Metabolism; Others
	Medroxyprogesterone Acetate (Farlutin) 是广泛使用的合成类固醇，与雄激素，孕酮及糖皮质激素受体均有作用。
T1284	Megestrol acetate SC10363,醋酸甲地孕酮,BDH1298	Glucocorticoid Receptor; Estrogen/progestogen Receptor; Progesterone Receptor; HIV Protease; Autophagy	Autophagy; Endocrinology/Hormones; Microbiology/Virology; Others; Proteases/Proteasome
	Megestrol acetate (BDH1298) 是具有口服活性的合成孕激素。它还具有抗雄激素特性，可用于治疗厌食症和恶病质。
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。
TN2400	alpha-Terthienylmethanol	Others	Others
	Alpha-terthienylmethanol possesses potent cytotoxic activity against human endometrial cancer cells; it inhibits growth mediated by the induction of apoptosis, as shown by the accumulation of sub-G1 and apoptotic cells.
TN6524	Irilone
	Irilone has immunomodulatory, and α-amylase inhibitory activities, it exhibits the selective inhibition toward CYP3 A4 rather than other major human CYPs. Irilone exhibited prominent antioxidant activities with the IC50 value of 10.46μM. Irilone potentiat
T79971	Asparanin A	Apoptosis	Apoptosis
	Asparanin A 是一种具有抗癌活性的凋亡 (apoptosis) 诱导剂。它能够通过线粒体和 PI3K/AKT 信号通路使细胞周期在 G0/G1 期停滞，并有效抑制癌细胞生长。此外，Asparanin A 在小鼠Ishikawa子宫内膜癌异种移植模型中显示出显著的体内抑制肿瘤生长效力。

天然产物

Cat.No: T1048

Synonym: 雌二醇,E2,17β-Estradiol,17β-Oestradiol,β-Estradiol

Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor, Endogenous Metabolite

Medroxyprogesterone Acetate

Cat.No: T1261

Synonym: Medroxyprogesterone 17-acetate,Provera,Metigestrona,NSC-26386,醋酸甲羟孕酮,Farlutin,安宫黄体酮,Medroxyprogesterone (acetate)

Target: Glucocorticoid Receptor, Estrogen/progestogen Receptor, Progesterone Receptor, Androgen Receptor, Endogenous Metabolite

Megestrol acetate

Cat.No: T1284

Synonym: SC10363,醋酸甲地孕酮,BDH1298

Target: Glucocorticoid Receptor, Estrogen/progestogen Receptor, Progesterone Receptor, HIV Protease, Autophagy

Cat.No: T3824

Target: Apoptosis, BCL, COX, UGT

alpha-Terthienylmethanol

Cat.No: TN2400

Target: Others

Cat.No: TN6524

Cat.No: T79971

Target: Apoptosis

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