MicroRNAs (miRNAs) are a naturally occurring class of small (approximately 22 nucleotides long) non-coding RNAs that regulate post-transcriptional gene expression to control cellular processes, development, cell differentiation, and homeostasis. MicroRNAs are essential for embryo, cell, and tissue development, regulating cell differentiation, proliferation, and apoptosis, hence their importance in human reproduction. Meanwhile, abnormal expression or function of miRNAs are found to be closely associated with the occurrence or development of various human diseases, including cancers. In light of their significant roles in physiology and pathology, miRNAs are emerging as novel biomolecular targets for chemical-biological studies, including regulation and detection.
Multiple steps are involved in the generation of miRNAs. Most miRNAs are produced by the canonical biogenesis pathway, which involves transcription by RNA polymerase II to make a primary transcript (pri-miRNA) and cleavage by the microprocessor complex to yield a hairpin precursor miRNA (pre-miRNA) in the nucleus. The pre-miRNA is then exported into the cytoplasm, where cleavage by the enzyme Dicer creates a double-stranded RNA duplex. Only a single strand from the double-stranded RNA duplex forms the mature miRNA and is incorporated into the RNA-induced silencing complex (RISC), which guides the binding of Argonaute (AGO) proteins in the RISC to the 3’untranslated region (UTR) to either repress protein translation or promote mRNA degradation. In addition to canonical miRNA biogenesis pathways, non-canonical microprocessor-independent or Dicer-independent miRNA biogenesis pathways also exist. Despite miRNAs being mostly involved in the down-regulation of gene expression, there are reports of miRNAs promoting gene expression. In addition, relationships between miRNAs and their targets are not always one-to-one in a specific cell type. In fact, a single miRNA may regulate many mRNA targets, and conversely, a single mRNA target also can be regulated by many miRNAs.
| Cat. No. | Product Name | CAS No. | Purity | Chemical Structure |
|---|---|---|---|---|
| KM2877 |
Aurintricarboxylic acid
Aurintricarboxylic acid 是高效的，αβ-亚甲基-ATP 敏感选择性 P2X1Rs 和 P2X3Rs 变构拮抗剂，对 rP2X1R 和 rP2X3R 作用的 IC50 值分别为 8.6 nM 和 72.9 nM。Aurintricarboxylic acid 是一种有效的抗流感剂，通过直接抑制神经氨酸酶 (neuraminidase) 作用。Aurintricarboxylic acid 也是拓扑异构酶 II 和凋亡抑制剂。Aurintricarboxylic acid 是选择性的 TWEAK-Fn14 信号通路抑制剂。Aurintricarboxylic acid 也是一种胱硫醚-γ-裂解酶 (CSE) 抑制剂，其 IC50 值为 0.6 μM。Aurintricarboxylic acid 是能够调节 miRNA 功能的 miRNA 调节剂。 |
4431-00-9 |
|
|
| KM10664 |
Camptothecin
Camptothecin (CPT)，一种生物碱，是一种 DNA topoisomerase I (Topo I) 抑制剂，其 IC50 值为 679 nM。Camptothecin (CPT) 对结直肠癌、乳腺癌、肺癌和卵巢癌具有强大的抗肿瘤活性，通过改变人类癌细胞中的 miRNA 表达模式来调节 hypoxia-inducible factor-1α (HIF-1α) 活性。 |
7689-03-4 | 98% |
|
| KM4334 |
Cl-amidine hydrochloride
Cl-amidine hydrochloride 是口服有效的 PAD 抑制剂，其对 PAD1、PAD3 和 PAD4 的 IC50 值分别为0.8 μM、 6.2 μM 和 5.9 μM。Cl-amidine hydrochloride 可诱导癌细胞的凋亡。Cl-amidine hydrochloride 可诱导 miR-16 (miRNA-16, microRNA-16)，引起细胞周期阻滞。Cl-Amidine hydrochloride 可阻断组蛋白 3 瓜氨酸化和中性粒细胞胞外陷阱的形成，并提高败血症小鼠的存活率。 |
1373232-26-8 | 98% |
|
| KM12539 |
Enoxacin hydrate
Enoxacin hydrate (Enoxacin sesquihydrate) 是一种氟喹诺酮，可以干扰 DNA 复制，抑制细菌 DNA 促旋酶 (IC50=126 µg/ml) 和拓扑异构酶 IV (IC50=26.5 µg/ml)。Enoxacin hydrate 是一种 miRNA 加工激活剂，可增强 siRNA 介导的 mRNA 降解并促进内源性 miRNA 的生物发生，也可增强 TAR RNA 结合蛋白 2 (TRBP) 介导的 microRNA 加工。Enoxacin hydrate 有效抑制革兰氏阳性和阴性细菌， 是一种特异性的癌症生长抑制剂。 |
84294-96-2 | 98% |
|
| KM12540 |
Enoxacin-d8
Enoxacin-d8 是 Enoxacin 的氘代物。Enoxacin (AT 2266) 是一种氟喹诺酮，可以干扰 DNA 复制，抑制细菌 DNA 促旋酶 (IC50=126 µg/ml) 和拓扑异构酶 IV (IC50=26.5 µg/ml)。Enoxacin 是一种 miRNA 加工激活剂，可增强 siRNA 介导的 mRNA 降解并促进内源性 miRNA 的生物发生，也可增强 TAR RNA 结合蛋白 2 (TRBP) 介导的 microRNA 加工。Enoxacin 有效抑制革兰氏阳性和阴性细菌， 是一种特异性的癌症生长抑制剂。 |
1329642-60-5 |
|
|
| KM10330 |
LIN28 inhibitor LI71
LIN28 inhibitor LI71 是一种高效、细胞渗透性的 LIN28 抑制剂，能消除 LIN28 介导的寡核苷酸化，其 IC50 值为 7 uM。LIN28 inhibitor LI71 能直接绑定 CSD，抑制 LIN28 对 let-7 的作用活性。 |
1357248-83-9 | 98% |
|
| KM6671 |
Lin28-let-7a antagonist 1
Lin28-let-7a antagonist 1 对 Lin28-let-7a 的结合有明显的拮抗作用，其对 Lin28A-let-7a-1 结合的 IC50 值为 4.03 μM。 |
2024548-03-4 | 98% |
|
| KM9620 |
MIR96-IN-1
MIR96-IN-1 靶向 miR-96 (miRNA-96, microRNA-96) 发夹前体结构中的 Drosha 位点，抑制其生物生成，及抑制下游靶标，并触发乳腺癌细胞的凋亡 (apoptosis)。MIR96-IN-1 结合到 RNA1，RNA2，RNA3，RNA4 和 RNA5 的 Kd 分别为 1.3，9.4，3.4，1.3 和 7.4 μM。 |
1311982-88-3 | ≥98% |
|
| KM5613 |
PIN1 inhibitor API-1
PIN1 inhibitor API-1 是一种特殊的 Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) 抑制剂 (API-1)，IC50 为 72.3 nM。PIN1 inhibitor API-1 直接特异性地与 Pin1 肽基脯氨酰异构酶 (PPIase) 结构域结合，并抑制 Pin1 顺反异构活性。PIN1 inhibitor API-1 保留 pXPO5 的活性构象，恢复 pXPO5 将前 miRNA 从细胞核转运到细胞质的能力，从而上调抗癌 miRNA 的生物发生，抑制体外和体内肝癌的发生。 |
680622-70-2 | 97% |
|
| KM18867 |
Pseudoprotodioscin
Pseudoprotodioscin，一种呋喃葡糖苷，抑制 SREBP1/2 和 microRNA 33a/b 水平，降低胆固醇和甘油三酯合成相关的基因表达。 |
102115-79-7 | 98% |
|
| KM11723 |
SID 3712249
SID3712249 (MIR-544 Inhibitor 1) 是微小 RNA-544 (miR-544) 的生物合成抑制剂。 |
522606-67-3 | 98% |
|
| KM9330 |
Targapremir-210
Targapremir-210 (TGP-210) 是一种有效的、选择性的 miR-210 (miRNA-210, microRNA-210) 抑制剂。 Targapremir-210 以高亲和力抑制 pre-miR-210 的加工 (Kd~200 nM)。 |
1049722-30-6 | 98% |
|
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