The nuclear retinoic acid receptors (RARs) are transcriptional transregulators, which control the expression of specific gene subsets subsequently to ligand binding and to strictly controlled phosphorylation processes. RARs consist of three subtypes, α (NR1B1), β (NR1B2) and γ (NR1B3), encoded by separate genes. RARs function as ligand-dependent transcriptional regulators, heterodimerized with retinoid X receptors (RXRs), which also consist of three types, α NR2B1, β (NR2B2) and γ (NR2B3). RARs play critical roles in a variety of biological processes, including development, reproduction, immunity, organogenesis and homeostasis, as assessed by vitamin A-deficiency (VAD), pharmacological and genetic studies conducted in the mouse.
Retinoid X receptor (RXR) belongs to a family of ligand-activated transcription factors that regulate many aspects of metazoan life. A class of nuclear receptors requires RXR as heterodimerization partner for their function.
货号 | 产品名 | Cas | 产品描述 |
---|---|---|---|
PC15252 | AC 261066 | 870773-76-5 | 有效的RARβ2激动剂,AC-261066 是一种高效、口服有效的、亚型选择性的 RARbeta2 受体激动剂,其 pEC50 为 8.0 。 |
PC15197 | AC 55649 | 59662-49-6 | RARβ2的强效选择性激动剂,AC-55649 是有效的,高度具有亚型特异性的人视黄酸β2 (RARβ2) 受体的激动剂,其pEC50 值为6.9。 |
PC14753 | Adarotene | 496868-77-0 | 细胞凋亡诱导剂/DNA损伤,Adarotene 是一种有效的 apoptosis 诱导剂,通过产生 DNA 损伤,来阻止人类肿瘤细胞的增殖。 |
PC15238 | BMS 195614 | 253310-42-8 | RARα选择性拮抗剂 |
PC15226 | BMS 453 | 166977-43-1 | RARβ激动剂,RARα和RARγ拮抗剂。BMS-189453 (BMS189453, BMS453) is a synthetic retinoid that acts as an agonist of RARβ and an antagonist of RARα and RARγ. |
PC15231 | BMS 493 | 215030-90-3 | Pan-RAR反相激动剂,BMS493 是一种反向泛视黄酸受体 (RARs) 激动剂。BMS493 增加了 RARs 与核共抑制因子的相互作用,还可阻止视黄酸诱导的分化。 |
PC15063 | BMS 753 | 215307-86-1 | RARα激动剂,A potent, specific RARα agonist with Ki of 2 nM, displays no significant effects on RARγ in reporter based assays.. |
PC15227 | BMS 961 | 185629-22-5 | RARγ选择性激动剂 |
PC15200 | CD 1530 | 107430-66-0 | RAR受体激动剂,A potent and selective RARγ receptor agonist with Ki of 150 nM. |
PC15070 | CD 2314 | 170355-37-0 | RARβ激动剂 |
PC15243 | CD 2665 | 170355-78-9 | RARβ/γ选择性拮抗剂,CD2665 是一种选择性的 RAR-beta/gamma 拮抗剂,对 RARγ 和 RARβ 作用的 Ki 值分别为 110 nM、306 nM。 |
PC15183 | CD 437 | 125316-60-1 | RARγ激动剂,CD437 是一个选择性视黄酸受体 (Retinoic Acid Receptor γ (RARγ)) 激动剂。 |
PC15193 | Ch 55 | 110368-33-7 | RAR激动剂,Ch55 是一种有效的合成类维生素 A。Ch55 与 RAR-α 和 RAR-β 受体具有高亲和力。Ch55 对细胞视黄酸结合蛋白 (CRABP) 的亲和力较低。Ch55 是 HL60 细胞分化的有效诱导物,EC50 为 200 nM,可用于癌症的研究。 |
PC15245 | ER 50891 | 187400-85-7 | RARα受体拮抗剂 |
PC15194 | LE 135 | 155877-83-1 | RARβ拮抗剂,An effective retinoic acid receptor (RAR) antagonist with Ki of 0.22 uM for RARβ. |
PC15384 | Luffariellolide | 111149-87-2 | RA受体RARα、β和γ的激动剂 |
PC15244 | MM 11253 | 345952-44-5 | RARγ拮抗剂,MM 11253 is a selective RARγ antagonist. MM 11253 blocks the growth inhibitory ability of RARγ-selective agonists in squamous cell carcinoma (SCC)-25 cells. |
PC14799 | Talarozole | 201410-53-9 | 细胞色素P450酶抑制剂,Talarozole是有效的 CYP26A1 和 CYP26B1 抑制剂,IC50 分别为5.4和0.46 nM。 |
PC14800 | Tamibarotene | 94497-51-5 | RARα激动剂,Tamibarotene是视黄酸受体α/β (RARα/β)的激动剂,比RARγ的选择性高。 |
PC14879 | Tretinoin (Aberela). | 302-79-4 | 视黄酸,用于治疗痤疮和毛发角化病.Retinoic acid是维生素A的代谢产物,在细胞生长,分化和器官发生中起重要作用。 Retinoic acid是RAR 核受体的天然激动剂,对RARα/β/γ的 IC50 为14 nM。 Retinoic acid与 PPARβ/δ 结合的 Kd 值为17 nM。 |