33
5
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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3955 |
AR7
|
Retinoid Receptor | Metabolism |
AR7 是一种非典型的 RARA/RARα(视黄酸受体 α) 拮抗剂,能够特异性激活伴侣介导的自噬活性,对自噬无影响。 | |||
T17209 |
UVI 3003
|
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
UVI 3003 是一种高度选择性的类视黄醇 X 受体拮抗剂。在 Cos7 细胞中,它抑制非洲爪蟾蜍和人RXRα的活性,IC50值分别为 0.22 和 0.24 μM。 | |||
T22843 |
HX 531
|
Retinoid Receptor | Metabolism |
HX 531 是的RXR 拮抗剂 (IC50:18 nM) 。它能减少高脂饮食小鼠的骨骼肌、白色脂肪组织和肝脏中的甘油三酯含量。 | |||
T5341 |
WYC-209
WYC209 |
Apoptosis; Retinoid Receptor; Autophagy | Apoptosis; Autophagy; Metabolism |
WYC-209 是一种合成类视黄醇,是维甲酸受体激动剂。它主要通过 caspase 3途径抑制恶性鼠黑色素瘤肿瘤再生细胞的增殖,IC50值为 0.19 μM。 | |||
T15811 |
LY2955303
|
Others; Retinoid Receptor | Metabolism; Others |
LY2955303 是一种有效的特异性视黄酸受体 γ 拮抗剂(RARγ,Ki = 1.09 nM)。 | |||
TQ0097 |
AGN 193109
|
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
AGN 193109 是一种类视黄醇类似物,是一种有效的特异性 RAR 拮抗剂,可抑制 RARα、RARβ和 RARγ的活性,Kd 值分别为 2 nM、2 nM 和 3 nM。 | |||
T7370 |
Talarozole
R115866,他拉罗唑 |
Others; P450; Retinoid Receptor; Autophagy | Autophagy; Metabolism; Others |
Talarozole (R115866) 是一种口服性全反式维甲酸代谢阻断剂,可抑制 CYP26A1 和 CYP26B1,IC50 分别为 5.4 和 0.46 nM。它用于治疗痤疮、牛皮癣和其他角化疾病。 | |||
T7586 |
trifarotene
CD5789,曲法罗汀 |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
Trifarotene (CD5789) 是一种有效的选择性 RARγ 激动剂,对 RARγ 的选择性是 RARα 和 RARβ 的 65 倍和 16 倍,EC50分别为7.7、500和125 nM。 | |||
TQ0064 |
Peretinoin
NIK333 |
HCV Protease; Retinoid Receptor; S1P Receptor; Autophagy | Autophagy; GPCR/G Protein; Metabolism; Microbiology/Virology; Proteases/Proteasome |
Peretinoin (NIK333) 是口服非环状类视黄醇,靶向类视黄醇核受体,结构类维生素 A 。 | |||
T1093 |
Adapalene
CD271,阿达帕林 |
Apoptosis; Retinoid Receptor; Autophagy | Apoptosis; Autophagy; Metabolism |
Adapalene (CD271) 是一种合成类视黄醇,局部应用于痤疮。它以非竞争性方式抑制 GOT1的酶活性,具有抗肿瘤活性。它是一种 RAR 激动剂,对 RARβ、RARγ、RARα的AC50值分别为 2.3 nM、9.3 nM 和 22 nM。 | |||
T23383 |
SR11237
SR 11237 |
Others; RAR/RXR | Metabolism; Others |
SR11237 是一种泛视黄醇 X 受体 (RXR) 激动剂。 SR11237 导致 RXR/RXR 同源二聚体形成并反式激活包含 RXR 反应元件的报告基因。 | |||
T6696 |
Tazarotene
他扎罗汀,Tazorac,AGN 190168,Zorac |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
Tazarotene (Zorac) 是一种选择性视黄酸受体激动剂,用于研究寻常痤疮和斑块状银屑病。 | |||
T4538 |
palovarotene
Ro 3300074,R 667,帕罗伐汀 |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
Palovarotene (Ro 3300074) 是核视网膜酸受体γ 的激动剂。 | |||
T21314 |
Amsilarotene
TAC-101,TAC 101,TAC101 |
CDK | Cell Cycle/Checkpoint |
Amsilarotene (TAC101) 是口服有活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki=为 2.4 nM 和 400 nM。它可造成人胃癌、卵巢癌细胞及肝细胞癌的凋亡,可用于研究癌症。 | |||
T6694 |
Tamibarotene
NSC 608000,Am 80,Amnolake,他米巴罗汀 |
Apoptosis; Retinoid Receptor; Autophagy | Apoptosis; Autophagy; Metabolism |
Tamibarotene (Amnolake) 是一种具有口服活性的合成维甲酸,旨在克服全反式维甲酸耐药性,具有潜在的抗肿瘤活性。它也是视黄酸受体α/β 的激动剂,比RARγ的选择性高。 | |||
T11844 |
LG-100064
4-[(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)羰基]苯甲酸 |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
LG-100064 是一种类视黄醇 X 受体激动剂,对 RXRα、RXRβ 和 RXRγ 的 EC50值分别为 330、200 和 260 nM,可用于癌症研究。 | |||
T5843 |
Tarenflurbil
MPC7869,(R)-Flurbiprofen,R-flurbiprofen,氟比洛芬,R-氟比洛芬 |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
Tarenflurbil ((R)-Flurbiprofen) 是 Flurbiprofen 的 R 型对映体,可抑制 [3H]9-cis-RA 结合到 RXRαLBD,IC50为 75 μM。它可研究阿尔兹海默症。 | |||
T11847L |
Liarozole
R75251 dihydrochloride,利阿唑 |
P450; Retinoid Receptor | Metabolism |
Liarozole (R75251 dihydrochloride) 是一种咪唑衍生物,是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA),具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM),导致组织维甲酸水平增加。 | |||
T21714 |
BMS453
BMS 453,BMS-189453 |
Retinoid Receptor | Metabolism |
BMS453 (BMS-189453) 是一种合成类维生素 A,是一种 RARβ激动剂,也是一种 RARα/RARγ拮抗剂。它主要通过诱导活性 TGFβ 来抑制乳腺细胞生长。 | |||
T1872 |
Fenretinide
4-HPR,MK-4016,芬维A胺,4-hydroxy(phenyl)retinamide |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
Fenretinide (4-HPR) 是一种可口服的合成类维生素 A 衍生物,具有潜在的抗肿瘤和化学预防活性。 | |||
T1288 |
TTNPB
AGN191183,Arotinoid acid,Ro 13-7410,AGN-191183,Ro 13-7410 |
Apoptosis; Retinoid Receptor; Autophagy | Apoptosis; Autophagy; Metabolism |
TTNPB (Ro 13-7410,AGN-191183) 是一种RAR 激动剂。在使用人RARs 进行竞争性结合实验中,作用于RARα,RARβ和RARγ,IC50分别为 5.1 nM,4.5 nM 和 9.3 nM。 | |||
T5854 |
AM580
NSC608001,CD336,Ro 40-6055 |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
AM580 (CD336) 是一种视黄酸受体激动剂,对 RARα 具有选择性,IC50和EC50分别为 8 和 0.36 nM。 | |||
T6410 |
Bexarotene
Ro 26-4455,Targretin,蓓萨罗丁,贝沙罗汀,LGD1069 |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
Bexarotene (LGD1069) 是一种高亲和力的选择性类视黄醇 X 受体 (RXR) 激动剂,对 RXRα、RXRβ和 RXRγ的 EC50分别为 33、24和25 nM。它是一种类视黄醇类似物,用于治疗皮肤 T 细胞淋巴瘤的皮肤表现。 | |||
T4371 |
CD437
AHPN,O-Desmethyl Adapalene,6-[3-(1-金刚烷基)-4-羟基苯基]-2-萘甲酸,Apoptosis Activator VI |
Retinoid Receptor; Autophagy | Autophagy; Metabolism |
CD437 (AHPN) 是一种特异性视黄酸受体激动剂。 | |||
T0499 |
Oxybenzone
二苯酮-3,KAHSCREEN BZ-3,Benzophenone 3,Eusolex 4360,紫外线吸收剂UV-9,Escalol 567 |
Apoptosis; Retinoid Receptor; Autophagy | Apoptosis; Autophagy; Metabolism |
Oxybenzone 是晒黑和皮肤保护剂中常用的紫外线过滤剂。它是二苯甲酮的衍生物,用作破坏内分泌的化学物质,可穿透胎盘和血脑屏障。它损害自噬,改变表观遗传状态并破坏凋亡神经元细胞中的类维生素 X 受体信号传导。 | |||
T68104 |
Mofarotene
Ro-40-8757,Ro 40-8757 |
Retinoid Receptor | Metabolism |
Mofarotene (Ro-40-8757) 是一种小分子化合物,在许多癌细胞系中显示出相当大的抗肿瘤活性,可用于治疗肿瘤和呼吸系统疾病。Mofarotene 是一种维甲酸类似物,可结合并激活维甲酸受体(RARs),从而改变某些基因的表达,导致易感细胞的细胞分化和细胞增殖降低。 | |||
T12516 |
Polyinosinic-polycytidylic acid sodium
双链聚肌胞,Poly(I:C) sodium |
Apoptosis; Others; TLR | Apoptosis; Immunology/Inflammation; Others |
Polyinosinic-polycytidylic acid sodium (Poly(I:C) sodium) 是双链 RNA 的合成类似物,是TLR3和视黄酸诱导型基因 I 受体激动剂。它可以用作疫苗佐剂,直接触发癌细胞发生凋亡,还增强先天性和适应性免疫反应,并改变肿瘤的微环境。 | |||
T37414 |
CAY10771
|
Others | Others |
CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Ch... | |||
T85297 |
6-hydroxy Bexarotene
|
Others | Others |
6-Hydroxy Bexarotene, an oxidative metabolite of bexarotene, serves as a high-affinity ligand for retinoid X receptors (RXRs), specifically binding to RXRα, RXRβ, and RXRγ, as well as to the retinoic acid receptor α (RARα) with dissociation constants (Kds) of 3.46, 4.21, 4.83, and 8.17 μM, respectively. It demonstrates selective activation of RXRα, RXRβ, and RXRγ over RARα, RARβ, and RARγ in vitro, with half-maximal effective concentrations (EC50s) of 398, 356, 420, 4,414, 2,121, and 2,043 nM, r... | |||
T71933 |
GNE-3500
|
Others | Others |
GNE-3500 is a Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C (RORc or RORγ) Inverse Agonist. Retinoic acid receptor-related orphan receptor C (RORc, RORγ, or NR1F3) is a nuclear receptor that plays a major role in the production of interleukin (IL)-17. Considerable efforts have been directed toward the discovery of selective RORc inverse agonists as potential treatments of inflammatory diseases such as psoriasis and rheumatoid arthritis. GNE-3500 poss... | |||
T36998 |
7β,27-dihydroxy Cholesterol
7β,27-DHC,7β,27-dihydroxy Cholesterol |
Others | Others |
7β,27-dihydroxy Cholesterol is an oxysterol and agonist of retinoic acid receptor-related orphan receptor γ (RORγ) and RORγt. [1] It activates RORγ- or RORγt-dependent signaling with EC50 values of 691 and 1,045 nM, respectively, in reporter assays using HEK293T cells expressing the recombinant human receptors. 7β,27-dihydroxy Cholesterol is selective for RORγ and RORγt over a panel of eight additional nuclear receptors at 30 µM. It increases IL-17A production in Th17-polarized isolated hum... | |||
T74052 |
Polyinosinic-polycytidylic acid potassium
|
Others | Others |
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) 是双链 RNA 的合成类似物,是一种TLR3和视黄酸诱导型基因 I 受体 (RIG-I 和MDA5) 的激动剂。Polyinosinic-polycytidylic acid potassium 可以用作疫苗佐剂,以增强先天性和适应性免疫反应,并改变肿瘤的微环境,还可以直接触发癌细胞发生凋亡 (Apoptosis)。 | |||
T85283 |
AGN 193109 sodium
CD3106 |
Others | Others |
AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar exc... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T1051 |
Retinoic acid
维生素A酸,Vitamin A acid,ATRA,all-trans-Retinoic acid,Tretinoin |
Retinoid Receptor; Endogenous Metabolite; PPAR; Autophagy | Autophagy; DNA Damage/DNA Repair; Metabolism |
Retinoic acid (Tretinoin) 是维生素 A 的代谢产物,是一种视黄酸受体 RAR 的天然激动剂,激动 RARα/β/γ (IC50=14 nM)。Retinoic acid 可以诱导细胞分化、减少细胞增殖和抑制肿瘤发生。 | |||
T1611 |
Isotretinoin
13-cis-Retinoic acid,异维A酸 |
Retinoid Receptor; Endogenous Metabolite; Autophagy | Autophagy; Metabolism |
Isotretinoin (13-cis-Retinoic acid) 是一种天然存在的维甲酸,具有潜在的抗肿瘤活性。 它结合并激活核视黄酸受体 (RAR), 活化的 RARs 作为促进细胞分化和凋亡的转录因子。它是一种类维生素A 和维生素A 衍生物,用于治疗严重的痤疮和某些形式的皮肤、头颈癌。 | |||
TN6735 |
Bigelovin
|
Apoptosis; Reactive Oxygen Species; Retinoid Receptor; Autophagy; RAR/RXR | Apoptosis; Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Bigelovin 是从海百合中分离得到的一种倍半萜内酯,是选择性视黄素 X 受体 α 激动剂。它通过抑制ROS 的生成来调节 mTOR 信号通路。它诱导凋亡和自噬,有抗肿瘤活性。 | |||
T1330 |
Acitretin
阿曲汀,Ro 10-1670,Etretin |
Apoptosis; Retinoid Receptor; Autophagy | Apoptosis; Autophagy; Metabolism |
Acitretin (Ro 10-1670) 是一种维甲酸,可用于银屑病和阿尔兹海默症的研究。 | |||
T3000 |
Magnolol
NSC 293099,厚朴酚,5,5'-Diallyl-2,2'-biphenyldiol |
NF-κB; Retinoid Receptor; Antibacterial; PPAR; p53; Autophagy | Apoptosis; Autophagy; DNA Damage/DNA Repair; Metabolism; Microbiology/Virology; NF-κB |
Magnolol (5,5'-Diallyl-2,2'-biphenyldiol) 是RXRα和PPARγ的激动剂,EC50值分别为 10.4 µM 和 17.7 µM。他是从厚朴的树皮中分离得到的一种木脂素。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPH-01650 |
PRAME Protein, Human, Recombinant (E. coli, His)
Opa-interacting protein 4,Preferentially expressed antigen o... |
Human | E. coli |
Substrate-recognition component of a Cul2-RING (CRL2) E3 ubiquitin-protein ligase complex, which mediates ubiquitination of target proteins, leading to their degradation. The CRL2(PRAME) complex mediates ubiquitination and degradation of truncated MSRB1/SEPX1 selenoproteins produced by failed UGA/Sec decoding. In the nucleus, the CRL2(PRAME) complex is recruited to epigenetically and transcriptionally active promoter regions bound by nuclear transcription factor Y (NFY) and probably plays a role... | |||
TMPH-02221 |
TRIM24 Protein, Human, Recombinant (His & SUMO)
Transcription intermediary factor 1-alpha,E3 ubiquitin-prote... |
Human | E. coli |
Transcriptional coactivator that interacts with numerous nuclear receptors and coactivators and modulates the transcription of target genes. Interacts with chromatin depending on histone H3 modifications, having the highest affinity for histone H3 that is both unmodified at 'Lys-4' (H3K4me0) and acetylated at 'Lys-23' (H3K23ac). Has E3 protein-ubiquitin ligase activity. Promotes ubiquitination and proteasomal degradation of p53/TP53. Plays a role in the regulation of cell proliferation and apopt... | |||
TMPJ-01213 |
ASXL1 Protein, Human, Recombinant (GST)
Putative Polycomb group protein ASXL1,Additional sex combs-l... |
Human | E. coli |
Putative Polycomb group protein ASXL1 involved in transcriptional regulation mediated by ligand-bound nuclear hormone receptors, such as retinoic acid receptors (RARs) and peroxisome proliferator-activated receptor gamma (PPARG). It acts as coactivator of RARA and RXRA through association with NCOA1. ASXL1 also acts as corepressor through recruitment of KDM1A and CBX5 to target genes in a cell-type specific manner; the function seems to involve differential recruitment of methylated histone H3 t... |