アンドロゲン受容体

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S2840 Apalutamide (ARN-509) <1 mg/mL 18 mg/mL 5 mg/mL
S6885 Ailanthone -1 mg/mL 100 mg/mL '-1 mg/mL
S0097 (S,R,S)-AHPC (MDK7526) 10 mg/mL 86 mg/mL '''86 mg/mL
S1304 Megestrol Acetate <1 mg/mL 33 mg/mL '15 mg/mL
S7040 AZD3514 <1 mg/mL 100 mg/mL 100 mg/mL
S1250 Enzalutamide (MDV3100) <1 mg/mL 92 mg/mL '<1 mg/mL
S1190 Bicalutamide <1 mg/mL 86 mg/mL ''5 mg/mL
S6896 Clascoterone <1 mg/mL 80 mg/mL '''80 mg/mL
S8885 UT-34 <1 mg/mL 71 mg/mL ''71 mg/mL
S2803 Galeterone <1 mg/mL 24 mg/mL 40 mg/mL
S1908 Flutamide <1 mg/mL 55 mg/mL '55 mg/mL
S2604 Dehydroepiandrosterone (DHEA) <1 mg/mL 57 mg/mL 57 mg/mL
S2042 Cyproterone Acetate <1 mg/mL 83 mg/mL 10 mg/mL
S4054 Spironolactone <1 mg/mL 83 mg/mL 20 mg/mL
S4836 Nilutamide <1 mg/mL 63 mg/mL 63 mg/mL
S4593 Chlormadinone acetate <1 mg/mL 27 mg/mL '1 mg/mL
S7559 Darolutamide (ODM-201) <1 mg/mL 80 mg/mL 38 mg/mL
S5285 RU58841 <1 mg/mL 73 mg/mL 73 mg/mL
S7955 EPI-001 <1 mg/mL 79 mg/mL '79 mg/mL
S9045 Triptophenolide -1 mg/mL 62 mg/mL -1 mg/mL
S4728 3,3'-Diindolylmethane <1 mg/mL 49 mg/mL 18 mg/mL
S1140 Andarine <1 mg/mL 88 mg/mL '88 mg/mL
S2832 Epiandrosterone <1 mg/mL 29 mg/mL '58 mg/mL
S6352 Androsterone -1 mg/mL 29 mg/mL -1 mg/mL
S5508 Dehydroepiandrosterone acetate -1 mg/mL 12 mg/mL -1 mg/mL
S3946 Mesterolone -1 mg/mL 13 mg/mL -1 mg/mL
S6407 Tulobuterol hydrochloride 53 mg/mL 53 mg/mL 10 mg/mL
S4794 Drostanolone Propionate -1 mg/mL 18 mg/mL -1 mg/mL
S4795 Trenbolone acetate -1 mg/mL 62 mg/mL '-1 mg/mL
S3717 Testosterone Enanthate 9 mg/mL 80 mg/mL 80 mg/mL
S4757 Dihydrotestosterone(DHT) <1 mg/mL 58 mg/mL 58 mg/mL
S1174 Ostarine (GTx-024) <1 mg/mL 78 mg/mL '78 mg/mL
S6630 Dimethylcurcumin (ASC-J9) <1 mg/mL 79 mg/mL ''<1 mg/mL
S0276 GSK-2881078 ˂1 mg/mL 66 mg/mL 50 mg/mL
S5275 Testolone (RAD140) -1 mg/mL 78 mg/mL ''-1 mg/mL
S8822 Ligandrol (LGD-4033) <1 mg/mL 68 mg/mL 68 mg/mL

Androgen Receptor製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2840

Apalutamide (ARN-509)

Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.

S6885

Ailanthone

Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.

S0097

(S,R,S)-AHPC (MDK7526)

(S,R,S)-AHPC (MDK7526) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.

S1304

Megestrol Acetate

Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.

S7040

AZD3514

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

S1250

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

S1190

Bicalutamide

Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

S6896

Clascoterone

Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) is a topical and peripherally selective antagonist of androgen receptor (AR).

S8885

UT-34

UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

S1908

Flutamide

Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

S2042

Cyproterone Acetate

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

S4054

Spironolactone

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

S4836

Nilutamide

Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.

S4593

Chlormadinone acetate

Chlormadinone acetate (Gestafortin) is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S7559

Darolutamide (ODM-201)

Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

S5285

RU58841

RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.

S7955

EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

S9045

Triptophenolide

Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.

S4728

3,3'-Diindolylmethane

3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.

S1140

Andarine

Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.

S2832

Epiandrosterone

Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.

S3830

Protodioscin

Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.

S6352

Androsterone

Androsterone is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.

S5508

Dehydroepiandrosterone acetate

Dehydroepiandrosterone acetate (DHEA acetate) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.

S3946

Mesterolone

Mesterolone is a synthetic steroid with anabolic and androgenic activities.

S6407

Tulobuterol hydrochloride

Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.

S4794

Drostanolone Propionate

Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.

S4795

Trenbolone acetate

Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.

S3717

Testosterone Enanthate

Testosterone Enanthate is an androgen and anabolic steroid used in androgen replacement therapy.

S3715

Boldenone Undecylenate

Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.

S4757

Dihydrotestosterone(DHT)

Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.

S1174

Ostarine (GTx-024)

Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

S6630

Dimethylcurcumin (ASC-J9)

Dimethylcurcumin (ASC-J9) is an androgen receptor (AR) degradation enhancer that suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.

S0276

GSK-2881078

GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.

S5275

Testolone (RAD140)

Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

S8822

Ligandrol (LGD-4033)

Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S2840

Apalutamide (ARN-509)

Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.

S6885

Ailanthone

Ailanthone (AIL, Δ13-Dehydrochaparrinone), a natural anti-hepatocellular carcinoma (HCC) component in Ailanthus altissima, induces G0/G1-phase cell cycle arrest by decreasing expression of cyclins and CDKs and increases expression of p21 and p27. Ailanthone triggers DNA damage characterized by activation of the ATM/ATR pathway. Ailanthone induces apoptosis which is mitochondrion-mediated and involves the PI3K/AKT signaling pathway in Huh7 cells. Ailanthone is also a potent inhibitor of both full-length Androgen Receptor (AR-FL) and constitutively active truncated AR splice variants (AR-Vs, AR1-651) with IC50 of 69 nM and 309 nM, respectively.

S0097

(S,R,S)-AHPC (MDK7526)

(S,R,S)-AHPC (MDK7526) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC is potential useful for the targeted degradation of the androgen receptor. (S,R,S)-AHPC can be connected to the ligand for protein such as BCR-ABL1 by a linker to form PROTACs such as GMB-475. GMB-475 induces the degradation of BCR-ABL1 with IC50 of 1.11 μM in Ba/F3 cells.

S1304

Megestrol Acetate

Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.

S7040

AZD3514

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1250

Enzalutamide (MDV3100)

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.

2020, 29;11(1):2089

2020, 19;11(1):2508

2020, 23

S1190

Bicalutamide

Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

2020, 10(8):3366-3381

2020, 10(1):3836

2020, 10.1007/s10637-020-00901-w

S6896

Clascoterone

Clascoterone (Winlevi, Cortexolone 17 alpha-propionate, Cortexolone 17α-propionate, CB-03-01) is a topical and peripherally selective antagonist of androgen receptor (AR).

S8885

UT-34

UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.

S2803

Galeterone

Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

2020, 153:108534

2018, 138:82-90

2016, 477(4):1005-10

S1908

Flutamide

Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

2020, 19;20:58

2018, 17(10):2091-2099

2018, 234:846-854

S2604

Dehydroepiandrosterone (DHEA)

Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

2020, 10.1038/s41416-020-1007-3

, 382(2):195-202

S2042

Cyproterone Acetate

Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

2017, 1863(9):2319-2332

S4054

Spironolactone

Spironolactone is a potent antagonist of the androgen receptor with IC50 of 77 nM.

2020, 55(2):91-102

2018, 242(Pt A):12-18

2018, 234:846-854

S4836

Nilutamide

Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.

S4593

Chlormadinone acetate

Chlormadinone acetate (Gestafortin) is a steroidal progestin with additional antiandrogen and antigonadotropic effects, used often in combinations as an oral contraceptive. Its half-life is about 34-38 hours.

S7559

Darolutamide (ODM-201)

Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

2020, 19;molcanther00152020

2020, 10.1007/s12672-020-00391-5

2019, 29(8):2355-2370

S5285

RU58841

RU58841, also known as PSK-3841 or HMR-3841, is a non-steroidal anti-androgen.

S7955

EPI-001

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ∼6 μM and a selective PPAR-gamma modulator.

2019, 79(2):206-214

S9045

Triptophenolide

Triptophenolide, derived from Tripterygium wilfordii, is a pan-antagonist for wild-type and mutant androgen receptors with the IC50 values of 260 nM for AR-WT, 480 nM for AR-F876L, 388 nM for AR-T877A, and 437 nM for W741C+T877A.

S4728

3,3'-Diindolylmethane

3,3'-Diindolylmethane(DIM) is a major digestive product of indole-3-carbinol, a potential anticancer component of cruciferous vegetables. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.

2019, 10(2):38

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1140

Andarine

Andarine (GTx-007, S-4) is a selective non-steroidal androgen receptor (AR) agonist with Ki of 4 nM, tissue-selective for anabolic organs. Phase 3.

2018, 158:189-203

2017, 1490:89-101

2013, 30(9):1517-26

S2832

Epiandrosterone

Epiandrosterone (3β-androsterone, EpiA) is a steroid hormone with weak androgenic activity, is a natural metabolite of DHEA.

S3830

Protodioscin

Protodioscin (Furostanol I), a steroidal saponin compound found in a number of plant species, is able to stimulate testosterone production and it also has an androgen-mimetic action, binding and activating the testosterone receptors.

S6352

Androsterone

Androsterone is a steroid metabolite derived from sex hormones, which displays weak androgenic properties.

2019, 2019:7162976

S5508

Dehydroepiandrosterone acetate

Dehydroepiandrosterone acetate (DHEA acetate) is a kind of dehydroepiandrosterone derivatives. DHEA is an endogenous steroid hormone, which is considered to be a natural product/dietary supplement with many proposed benefits to humans.

2020, 10.1038/s41416-020-1007-3

S3946

Mesterolone

Mesterolone is a synthetic steroid with anabolic and androgenic activities.

S6407

Tulobuterol hydrochloride

Tulobuterol is a long-acting β2-adrenergic receptor agonist that has bronchodilatory, anti-inflammatory, and antiviral activities.

S4794

Drostanolone Propionate

Drostanolone Propionate is an anabolic androgenic steroid with strong anti-estrogenic properties.

S4795

Trenbolone acetate

Trenbolone acetate (RU-1697, Trenbolone 17β), a synthetic anabolic steroid, is an androgen ester and a long-acting prodrug of trenbolone.

S3717

Testosterone Enanthate

Testosterone Enanthate is an androgen and anabolic steroid used in androgen replacement therapy.

2020, 8;13:2987-2995

S3715

Boldenone Undecylenate

Boldenone is an agonist of the androgen receptor (AR). Boldenone Undecylenate is a derivative of testosterone, which has strong anabolic effect and only moderately androgenic.

S4757

Dihydrotestosterone(DHT)

Dihydrotestosterone is an endogenous androgen sex steroid and hormone and a potent agonist of the androgen receptor with 2-3-fold greater androgen receptor affinity than testosterone and 10-fold higher potency of inducing androgen receptor signaling.

2020, 6 pii: deaa077

2020, 80(9):674-686

2020, 21;526(1):267-272

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S1174

Ostarine (GTx-024)

Ostarine (GTx-024, MK-2866) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

2018, 128(12):5531-5548

2013, 84:278-84

2011, 3(5):331-6

S6630

Dimethylcurcumin (ASC-J9)

Dimethylcurcumin (ASC-J9) is an androgen receptor (AR) degradation enhancer that suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors.

S0276

GSK-2881078

GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.

S5275

Testolone (RAD140)

Testolone (RAD140) is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator with Ki value of 7 nM as well as good selectivity over other steroid hormone nuclear receptors.

S8822

Ligandrol (LGD-4033)

Ligandrol (LGD-4033, VK-5211) is a novel nonsteroidal, oral selective androgen receptor modulator with high affinity (Ki of ∼1 nM) and selectivity.