T80153
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Calcium Channel
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Maurocalcine是一种能穿透细胞膜的激动剂,对ryanodine receptor (RyR)通道1、2、3型具有活性。在与RyR1的结合实验中,Maurocalcine诱导[3H]ryanodine的结合,表现出EC50值为2558 nM。此外,Maurocalcine对RyR2也展示出较高的表观亲和力,达14 nM。该化合物可用于体内细胞追踪及其他细胞成像技术。 |
T76213
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HXR9 hydrochloride 是一种针对 HOX/PBX 相互作用的细胞渗透性肽类竞争性拮抗剂。它通过阻碍 HOX 蛋白与 PBX,一个与旁系同源基因组 1 至 8 结合的第二转录因子,之间的相互作用来发挥作用。特别地,HXR9 hydrochloride 能够选择性抑制细胞增殖,并在表达 HOXA/PBX3 基因高水平的细胞中,如 MLL 重排的白血病细胞,促进细胞凋亡。 |
T60407
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L-Buthionine-(S,R)-sulfoximine hydrochloride 是一种有效的、可细胞渗透的,作用快的 G-谷氨酸半胱氨酸合成酶 (γ-glutamylcysteine synthetase, γ-GCS)的不可逆抑制剂并可耗尽细胞内的谷胱甘肽水平,在黑色素瘤、乳腺癌和卵巢癌标本上的 IC50值分别为1.9 μM、8.6 μM 和 29 μM。 |
T37079
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Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. VEGFR2 kinase inhibitor II blocks the growth of human umbilical vein endothelial cells stimulated with either VEGF or PDGF (IC50s = 110 nM and 2 μM, respectively). |
T78041
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Tat-peptide 168-189 是一款标记有 Tat 的细胞渗透融合肽,对应回大鼠 G3BP1 的168-189残基。此配合物末端整合了HIV Tat 序列的一个高度非保守部分,以促进其穿透细胞膜。作为Tat-peptide 168-189 TFA的阴性对照,Tat-peptide 168-189 TFA 已被证实可促进轴突生长和增加神经元的突触数目。 |
T35558
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Cyclopamine-KAAD is a potent inhibitor of hedgehog signaling with an IC50 value of 20 nM in a Shh-LIGHT2 assay. It blocks binding of BODIPY-cyclopamine to cells expressing Smoothened (Smo) in a dose-dependent manner. Cyclopamine-KAAD is cell-permeable and binds to SmoA1 to promote its exit from the endoplasmic reticulum. It inhibits the invasion and migration (45.9 and 43.3% inhibition, respectively) of Bel-7402 hepatocarcinoma cells and decreases the expression of nuclear glioma-associated oncogene 1 (Gli1) and cytosolic MMP-9, pERK1, and pERK2 proteins in a dose-dependent manner. Cyclopamine-KAAD also increases TRAIL-mediated cell death in NCH82 and NCH89 human glioblastoma cultures and upregulates expression of the death receptors DR4 and DR5 in LN229 and U251 glioma cells. |
T70377
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BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used in a pre-clinical model to explore the feasibility of targeting Syk in the treatment of retinoblastoma. |
T75811
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PBP10是一种细胞通透性和选择性的gelsolin衍生的肽抑制剂,针对甲酰基肽受体2(FPR2)具有较高选择性,相较于FPR1更为优选。该化合物为N端偶联罗丹明的10个氨基酸肽,对革兰氏阳性及革兰氏阴性菌均展现出杀菌活性,同时能够抑制微生物诱导的炎症反应。 |
T37564
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C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7/Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation, enhances cAMP-activated chloride secretion, and suppresses secretion of IL-8 in primary epithelial cells isolated from patients with cystic fibrosis.[3] |
T83713
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DC432是一种细胞内可渗透的肽类抑制剂,针对N-末端Xaa-Pro-Lys N-甲基转移酶1 (NTMT1; IC50 = 0.054 µM)。该化合物与NTMT1和NTMT2有结合作用(Kds分别为0.3和1 µM),并在10和50 µM的浓度下,通过细胞外实验抑制NTMT1对调节染色体凝缩1 (RCC1) N-末端二甲基化。DC432(100 µM)在HCT116细胞中减少了RCC1 SPKRIA基序的三甲基化。 |