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30

抑制剂 & 化合物

2

天然产物

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Cat. No. Product Name Target Signaling Pathways
T6906 Tamoxifen

ICI 46474,他莫昔芬,Z-Tamoxifen,trans-Tamoxifen,ICI47699

Apoptosis; Estrogen Receptor/ERR; HSP; Estrogen/progestogen Receptor; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; Endocrinology/Hormones; Metabolism
Tamoxifen (ICI47699) 是一种雌激素受体调节剂 (SERM),具有选择性和口服有效性。Tamoxifen 对雌激素具有抑制活性 (如乳腺细胞) 和激活活性 (如骨、肝和子宫细胞)。
T13076 Tamoxifen-​d5

ICI 47699-​d5,(Z)-Tamoxifen-​d5,trans-Tamoxifen-​d5

HSP Cytoskeletal Signaling; Metabolism
Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen is a selective modulator of estrogen receptor (SERM). Tamoxifen is a potent activator of Hsp90 and enhances the Hsp90 molecular chaperone ATPase activity.
T28919 Tamoxifen analog II

Tamoxifen analog III

Tamoxifen analog II is a potent growth inhibitor. Tamoxifen analog II displays activity against various cancer cell lines.
T0835 Tamoxifen Citrate

Tamoxifen Z-isomer citrate,ICI 46474,ICI 46474 Citrate,枸橼酸他莫昔芬,他莫昔芬柠檬酸盐

Apoptosis; Estrogen Receptor/ERR; HSP; Estrogen/progestogen Receptor; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; Endocrinology/Hormones; Metabolism
Tamoxifen Citrate 是一种口服有效的,选择性雌激素受体调节剂,可阻断乳腺细胞中的雌激素作用,并可激活如骨骼、肝脏和子宫细胞中的雌激素活性。它是 Hsp90激活剂,可增强 Hsp90 分子伴侣 ATPase 的活性,可激活自噬和诱导凋亡。
T22512 4’-hydroxy Tamoxifen

Others Others
It is a metabolite of tamoxifen and an estrogen receptor modulator.
T4281 Endoxifen

(E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen

Estrogen Receptor/ERR; Aromatase; Estrogen/progestogen Receptor; Parasite; Drug Metabolite Endocrinology/Hormones; Metabolism; Microbiology/Virology
Endoxifen ((E/Z)-Endoxifen) 是 Tamoxifen 的关键活性代谢物,能抑制芳香酶的活性,与雌激素受体有较高的亲和力和特异性。它有潜力研究乳腺癌。
T4420 4-Hydroxytamoxifen

ICI 79280,(Z)-4-hydroxy Tamoxifen,4-羟基他莫昔芬,trans-4-Hydroxytamoxifen

Estrogen Receptor/ERR; Estrogen/progestogen Receptor Endocrinology/Hormones
4-Hydroxytamoxifen (ICI 79280) 是 Tamoxifen 的活性代谢产物,是一种雌激素受体调节剂 (SERM),具有选择性和口服有效性。4-Hydroxytamoxifen 具有抗肿瘤活性,可用于乳腺癌的研究。
T31262 Deamino-hydroxytamoxifen

Tamoxifen-ol,Tamoxifen metabolite Y

Tamoxifen is a medication that is used to prevent breast cancer patients.
T19192 α-Hydroxytamoxifen

α-OHTAM,(E)-α-Hydroxy tamoxifen

Others Others
α-Hydroxytamoxifen is a metabolite of tamoxifen. It reacts with DNA and causes the formation of DNA adducts.
T8984 FLTX1

Estrogen Receptor/ERR; Estrogen/progestogen Receptor Endocrinology/Hormones
FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.
T12148 N-Desmethyltamoxifen hydrochloride

Estrogen Receptor/ERR; Endogenous Metabolite; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Endocrinology/Hormones; Metabolism
N-Desmethyltamoxifen hydrochloride 是 Tamoxifen 在人体内主要的三苯氧胺代谢物。它是蛋白激酶 C 抑制剂,也是人体 AML 细胞神经酰胺代谢的有效调节因子,可限制神经酰胺糖基化、水解和鞘氨醇磷酸化。
T6743 (E/Z)-4-Hydroxytamoxifen

4-羟基他莫昔芬,(E/Z)-4-羟基他莫昔芬,Afimoxifene,4-Hydroxytamoxifen

Estrogen Receptor/ERR; Estrogen/progestogen Receptor Endocrinology/Hormones
(E/Z)-4-Hydroxytamoxifen (Afimoxifene) 是 tamoxifen 的活性代谢物和选择性雌激素受体(ER)调节剂,广泛用于乳腺癌的治疗和化学预防治疗。
T12148L N-Desmethyltamoxifen

Others Others
N-Desmethyltamoxifen, the principal metabolite of tamoxifen in humans, serves as an efficacious modulator of ceramide metabolism within human AML cells by inhibiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. Although it demonstrates weak antiestrogenic properties, it acts as a protein kinase C (PKC) inhibitor with a potency ten times greater than that of tamoxifen.
T15186 (E)-4-Hydroxytamoxifen

Others Others
(E)-4-Hydroxytamoxifen is a less active isomer of (Z)-4-hydroxytamoxifen and also is an estrogen receptor modulator.
T2280 Endoxifen (Z-isomer)

Z-因多昔芬,Endoxifen Z-isomer,4-[(1E)-1-{4-[2-(甲基氨基)乙氧基]苯基}-2-苯基-1-丁烯-1-基]苯酚

Estrogen Receptor/ERR; EGFR; Potassium Channel; Estrogen/progestogen Receptor; HER Angiogenesis; Endocrinology/Hormones; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors
Endoxifen Z-isomer (EDX)是 Tamoxifen 重要的代谢产物,在表达 ERα的乳腺癌细胞中发挥抗雌激素作用。它以浓度依赖的方式抑制 hERG, IC50值为1.6μM。
T15249 Estrogen receptor modulator 1

Estrogen Receptor/ERR Endocrinology/Hormones
Estrogen receptor modulator 1 是一种有效的、具有口服活性的、选择性雌激素受体(estrogen receptor)调节剂 (SERM),其 pIC50为 0.46。它能够诱导 Tamoxifen 耐药、激素非依赖性异种移植瘤的消退。
T35973 Cholesterol-5α,6α-epoxide

Epoxycholesterol,5α,6α-epoxy Cholestanol,NSC 18176

Others Others
Cholesterol-5α,6α-epoxide (Epoxycholesterol) 是胆固醇氧化产生的代谢产物。 在应用他莫昔芬和 PBPE 后,5α,6α-环氧胆甾烷醇通过与 LXRβ 结合诱导三酰甘油生物合成。
T6827L Endoxifen hydrochloride

Endoxifen hydrochloride,Tamoxifen的主要活性代谢产物,具备较高的对雌激素受体(estrogen receptor)的亲和力和特异性,并能抑制芳香酶活性。它在乳腺癌研究中表现出潜在应用价值。
T11098 Droloxifene

3-Hydroxytamoxifen

Estrogen Receptor/ERR Endocrinology/Hormones
Droloxifene (3-Hydroxytamoxifen),Tamoxifen 衍生物,是一种具有口服活性和选择性的雌激素受体 (estrogen receptor) 调节剂。Droloxifene 具有抗雌激素和抗植入作用。Droloxifene 诱导 MCF-7 细胞 p53 表达及凋亡。Droloxifene 预防去卵巢大鼠骨丢失。
T29179 YM-01 Tosylate

YM-01 Tosylate, a potent antitumor agent, selectively targets cancer cells and overcoming tamoxifen resistance.
T34326 Ridaifen-B

RidaifenB

Ridaifen-B, a tamoxifen derivative, works by inducing independent autophagy of Bcl-2, without estrogen receptor involvement.
T33876 panomifene

GYKI13504,GYKI 13504,EGIS5650,EGIS-5650,EGIS 5650,GYKI-13504

Panomiphene (Gyki-13504, EGIS-5650) is an anti-estrogen drug that is a tamoxifen (TMX) analogue.
T6827 Endoxifen Z-isomer hydrochloride

Endoxifen HCl,Z-因多昔芬盐酸盐

Estrogen Receptor/ERR; Potassium Channel; Estrogen/progestogen Receptor; HER Angiogenesis; Endocrinology/Hormones; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors
Endoxifen Z-isomer hydrochloride (Endoxifen HCl) 是Tamoxifen 最重要的代谢产物, 在表达ERα的乳腺癌细胞中发挥抗雌激素作用, Endoxifen HCl 以浓度依赖的方式抑制hERG, IC50值为1.6μM。
T3645 Endoxifen E-isomer hydrochloride

E-Endoxifen hydrochloride

Estrogen Receptor/ERR; Estrogen/progestogen Receptor Endocrinology/Hormones
Endoxifen E-isomer hydrochloride (E-Endoxifen hydrochloride) 是 Endoxifen 的 E-异构体,是 Endoxifen Z-isomer 原料中主要的杂质,具有抗雌激素作用。
T71578 Endoxifen mesylate

Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromat...
T70013 Pipendoxifene

Pipendoxifene, also known as ERA-923, is a new antiestrogen with potential anticancer activity. ERA-923 potently inhibits estrogen binding to ER-alpha (IC50 = 14 nM). In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth (IC50 = 0.2 nM) associated with cytostasis. In vitro, a MCF-7 variant with inherent resistance to tamoxifen (10-fold) or 4-OH tamoxifen (>1000-fold) retains complete sensitivity to ERA-923 . In preclinical models, ERA-923 has an imp...
T71010 Norendoxifen

Norendoxifen, also known as 4-hydroxy-N, N-didesmethyltamoxifen, is a nonsteroidal aromatase inhibitor of the triphenylethylene group that was never marketed. It is an active metabolite of the selective estrogen receptor modulator tamoxifen.
T25888 NSC-670224

NSC 670224

NSC-670224 is an inhibitor of histone deacetylases-6 (HDAC6) and nuclear factor-κB (NF-κB) activation blocker. It has been shown to be toxic to Saccharomyces cerevisiae at low micromolar concentrations, potentially acts via a mechanism of action related t
T74457 EGFR-IN-42

EGFR-IN-42 (Compound 17b) 是一种有效的 EGFR 抑制剂,具有单位数纳摩尔活性。EGFR-IN-42 通过共价键将他莫昔芬或安多昔芬与 EGFR 抑制剂吉非替尼连接起来。EGFR-IN-42 保留 ER 拮抗剂活性和 EGFR 抑制作用。EGFR-IN-42 具有优越的抗癌活性。
T74458 EGFR-IN-43

EGFR-IN-43 (Compound 17c) 是一种有效的EGFR 抑制剂,具有单位数纳摩尔活性。EGFR-IN-43 通过共价键将他莫昔芬或安多昔芬与EGFR 抑制剂吉非替尼连接起来。EGFR-IN-43 保留 ER 拮抗剂活性和EGFR 抑制作用。EGFR-IN-43 具有优越的抗癌活性。

化合物

Tamoxifen
Cat.No: T6906
Synonym: ICI 46474,他莫昔芬,Z-Tamoxifen,trans-Tamoxifen,ICI47699
Target: Apoptosis, Estrogen Receptor/ERR, HSP, Estrogen/progestogen Receptor, Autophagy
Tamoxifen-​d5
Cat.No: T13076
Synonym: ICI 47699-​d5,(Z)-Tamoxifen-​d5,trans-Tamoxifen-​d5
Target: HSP
Tamoxifen analog II
Cat.No: T28919
Synonym: Tamoxifen analog III
Target:
Tamoxifen Citrate
Cat.No: T0835
Synonym: Tamoxifen Z-isomer citrate,ICI 46474,ICI 46474 Citrate,枸橼酸他莫昔芬,他莫昔芬柠檬酸盐
Target: Apoptosis, Estrogen Receptor/ERR, HSP, Estrogen/progestogen Receptor, Autophagy
4’-hydroxy Tamoxifen
Cat.No: T22512
Synonym:
Target: Others
Endoxifen
Cat.No: T4281
Synonym: (E/Z)-N-desmethyl-4-hydroxy Tamoxifen,N-去甲基-4-羟基-,(E/Z)-Endoxifen
Target: Estrogen Receptor/ERR, Aromatase, Estrogen/progestogen Receptor, Parasite, Drug Metabolite
4-Hydroxytamoxifen
Cat.No: T4420
Synonym: ICI 79280,(Z)-4-hydroxy Tamoxifen,4-羟基他莫昔芬,trans-4-Hydroxytamoxifen
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor
Deamino-hydroxytamoxifen
Cat.No: T31262
Synonym: Tamoxifen-ol,Tamoxifen metabolite Y
Target:
α-Hydroxytamoxifen
Cat.No: T19192
Synonym: α-OHTAM,(E)-α-Hydroxy tamoxifen
Target: Others
FLTX1
Cat.No: T8984
Synonym:
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor
N-Desmethyltamoxifen hydrochloride
Cat.No: T12148
Synonym:
Target: Estrogen Receptor/ERR, Endogenous Metabolite, PKC
(E/Z)-4-Hydroxytamoxifen
Cat.No: T6743
Synonym: 4-羟基他莫昔芬,(E/Z)-4-羟基他莫昔芬,Afimoxifene,4-Hydroxytamoxifen
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor
N-Desmethyltamoxifen
Cat.No: T12148L
Synonym:
Target: Others
(E)-4-Hydroxytamoxifen
Cat.No: T15186
Synonym:
Target: Others
Endoxifen (Z-isomer)
Cat.No: T2280
Synonym: Z-因多昔芬,Endoxifen Z-isomer,4-[(1E)-1-{4-[2-(甲基氨基)乙氧基]苯基}-2-苯基-1-丁烯-1-基]苯酚
Target: Estrogen Receptor/ERR, EGFR, Potassium Channel, Estrogen/progestogen Receptor, HER
Estrogen receptor modulator 1
Cat.No: T15249
Synonym:
Target: Estrogen Receptor/ERR
Cholesterol-5α,6α-epoxide
Cat.No: T35973
Synonym: Epoxycholesterol,5α,6α-epoxy Cholestanol,NSC 18176
Target: Others
Endoxifen hydrochloride
Cat.No: T6827L
Synonym:
Target:
Droloxifene
Cat.No: T11098
Synonym: 3-Hydroxytamoxifen
Target: Estrogen Receptor/ERR
YM-01 Tosylate
Cat.No: T29179
Synonym:
Target:
Ridaifen-B
Cat.No: T34326
Synonym: RidaifenB
Target:
panomifene
Cat.No: T33876
Synonym: GYKI13504,GYKI 13504,EGIS5650,EGIS-5650,EGIS 5650,GYKI-13504
Target:
Endoxifen Z-isomer hydrochloride
Cat.No: T6827
Synonym: Endoxifen HCl,Z-因多昔芬盐酸盐
Target: Estrogen Receptor/ERR, Potassium Channel, Estrogen/progestogen Receptor, HER
Endoxifen E-isomer hydrochloride
Cat.No: T3645
Synonym: E-Endoxifen hydrochloride
Target: Estrogen Receptor/ERR, Estrogen/progestogen Receptor
Endoxifen mesylate
Cat.No: T71578
Synonym:
Target:
Pipendoxifene
Cat.No: T70013
Synonym:
Target:
Norendoxifen
Cat.No: T71010
Synonym:
Target:
NSC-670224
Cat.No: T25888
Synonym: NSC 670224
Target:
EGFR-IN-42
Cat.No: T74457
Synonym:
Target:
EGFR-IN-43
Cat.No: T74458
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3855 Tracheloside

Estrogen Receptor/ERR; Phosphorylase Endocrinology/Hormones; Metabolism
Tracheloside 是抗雌激素木质素,利用 ERK1/2 刺激促进角质形成细胞增殖,是一种良好的促进伤口愈合的药物。
TN4731 Pachyaximine A

Antifection Microbiology/Virology
Pachyaximine A possesses significant antibacterial activity against Escherichia coli, Staphylococcus aureus, Corynebacterium diphtheriae and Corynebacterium pyrogenes. (-)-Pachyaximine A demonstrates significant activity as antiestrogen binding site (AEBS

天然产物

Tracheloside
Cat.No: T3855
Synonym:
Target: Estrogen Receptor/ERR, Phosphorylase
Pachyaximine A
Cat.No: TN4731
Synonym:
Target: Antifection
TargetMol Loading
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