18
2
Cat. No. | Product Name | Target | Signaling Pathways |
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T5399 |
GeA-69
|
PARP | Chromatin/Epigenetic; DNA Damage/DNA Repair |
GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂,Kd 值为 2.1 µM。 | |||
T22990 |
ML-090
Fluoflavine |
NADPH-oxidase; Others | Immunology/Inflammation; Others |
ML-090 是 NOX1 特异性抑制剂 (IC50 = 90 nM),对 NOX1 的特异性高于 NOX2、NOX3、NOX4(所有 IC50 > 10 μM)100倍。 | |||
T8851 |
I3MT-3
HMPSNE |
Hippo pathway | Stem Cells |
I3MT-3 (HMPSNE) 是一种有效的、具有细胞膜渗透性的、选择性的 3-巯基丙酮酸硫转移酶 (3MST)的抑制剂,IC50值为2.7 μM,对其他硫化氢/磺胺制硫酶没有活性。它靶向位于 3MST 活性位点的过硫半胱氨酸残基。 | |||
T11718 |
JI051
JI-051 |
Gamma-secretase | Neuroscience; Proteases/Proteasome; Stem Cells |
JI051 具有抗肿瘤作用,能够与癌症相关蛋白伴侣 prohibitin 2 (PHB2) 相互作用,通过抑制 Notch 下游效应基因 Hes1 转录来促使细胞周期停滞,抑制HEK293 细胞和胰腺癌细胞增殖。 | |||
T6911 |
NSC-87877 disodium
NSC87877 |
Apoptosis; Phosphatase | Apoptosis; Metabolism |
NSC-87877 disodium (NSC87877) 是一种有效的Shp2和Shp1蛋白质酪氨酸磷酸酶抑制剂,IC50值分别为0.318 μM 和0.355 μM。NSC-87877还抑制双特异性磷酸酶26。 | |||
T4378 |
MS049
|
Histone Methyltransferase | Chromatin/Epigenetic |
MS049 是一种有效的、选择性的和细胞活性的 PRMT4 和 PRMT6 双重抑制剂,IC50 分别为 34 和 43 nM。它可降低 HEK293 细胞的 Med12me2a 和 H3R2me2a 水平。 | |||
T13423 |
(1R,2R)-2-PCCA hydrochloride
(1R,2R)-2-PCCA(hydrochloride) |
Others | Others |
(1R,2R)-2-PCCA hydrochloride 是一种具有有效性、选择性和可穿过血脑屏障的 GPR88 受体激动剂,在 WT 小鼠纹状体膜中 EC50 值为1140 n。(1R,2R)-2-PCCA hydrochloride 可用于研究中枢神经系统。 | |||
T16112 |
ML67-33
|
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) (EC50s: 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively). ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. | |||
T35906 |
Padanamide A
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Padanamide A is a bacterial metabolite originally isolated from a marine Streptomyces species. It is active against five strains of P. falciparum (EC50s = 160-340 nM), is not cytotoxic to HEK293 or HepG2 human cell lines, but is cytotoxic to Jurkat T lymphocytes with an IC50 value of approximately 60 μg/ml. | |||
T78600 |
VU0029251
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VU0029251为mGluR5部分拮抗剂,表现出对该受体的较高亲和力(Ki: 1.07 μM)。在表达大鼠mGluR5的HEK293细胞膜上,可抑制谷氨酸引起的钙动员(IC50: 1.7 μM)。 | |||
T37199 |
Bilaid C
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Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Siana... | |||
T37409 |
DPC-AJ1951 (trifluoroacetate salt)
DPC-AJ1951 (trifluoroacetate salt) |
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DPC-AJ1951 is a peptide agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR; EC50 = 0.15 nM in HEK293 cells expressing human PPR). It induces cAMP production in SAOS-2 and UMR106 cells that endogenously express human and rat PPR, respectively (EC50s = 2.2 and 1.1 nM, respectively). DPC-AJ1915 stimulates osteoclast-mediated bone resorption in fetal rat long-bone explant cultures and increases collagen synthesis and cell proliferation in neonatal mouse parietal bone explants... | |||
T80240 |
Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
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Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2是一类具有生物活性的肽,作为蛋白酶激活受体1 (PAR-1) 的选择性激动剂,其特异性优于PAR-2。该肽通过HEK293细胞进行的基于细胞的钙信号传导测定确认了其对PAR-1的高特异性,并可用于研究PAR-1在体内的激活。PAR-1除了介导凝血酶的多种细胞作用外,还与PAR-4协作,参与调控凝血酶诱导的被分类为“凝血型”的肝细胞癌。 | |||
T83867 |
UNC8153 TFA
|
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UNC8153 是一种 NSD2(组蛋白-赖氨酸 N-甲基转移酶)的降解剂,其通过诱导NSD2的降解,具有350 nM的50%降解常数(DC50)值,并且在20 µM浓度下对NSD2具有选择性,而不选择NSD1和NSD3。在MM.1S多发性骨髓瘤细胞中,UNC8153 (10 µM) 能够诱导NSD2降解并减少组蛋白H3赖氨酸36位二甲基化(H3K36me2),这一效应可以被泛素激活酶抑制剂MLN4924所抑制。它减少了表达带有在1099位上谷氨酸到赖氨酸激活突变的NSD2(NSD2E1099K)的MM.1S细胞的增殖,但在20 µM浓度下,对表达野生型NSD2的MDA-MB-231、U2OS或HEK293细胞无效。UNC8153 (20 µM) 降低了在迁移实验中MM.1S细胞的附着能力。 | |||
T83779 |
EP4 Antagonist 14
Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14 |
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EP4 antagonist 14是一种前列腺素E2(PGE2)受体亚型EP4的拮抗剂,其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募(IC50 = 0.9 nM)。EP4 antagonist 14(10 µM)能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达,这些mRNA编码Il-4、巨噬细胞甘露糖受体1(Mrc1)、几丁质酶样蛋白3(Chil3)、趋化因子(C-X-C)基序配体1(Cxcl1)、表达在髓样细胞上的触发受体2(Trem2)和精氨酸酶-1(Arg1)。在体内,EP4 antagonist 14(每天30 mg/kg),结合抗PD-1抗体,能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。 | |||
T83763 |
EPI-X4 TFA
Endogenous Peptide Inhibitor of CXCR4 |
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EPI-X4是一种源于人血清白蛋白408-423氨基酸的内源性肽段,是趋化因子(C-X-C基序)受体4 (CXCR4)的拮抗剂。在0.8至1,000µM的浓度范围内,EPI-X4能抑制表达CXCR4的HEK293细胞中由趋化因子(C-X-C基序)配体12 (CXCL12)诱发的钙离子动员和受体内化。EPI-X4还能抑制CXCL12诱导的Jurkat T细胞和人类CD34+造血干细胞的迁移。体内实验中,EPI-X4(16µmol/kg)在急性过敏性气道高嗜酸性粒细胞疾病的小鼠模型中减少了Cxcr4依赖的炎症细胞气道浸润。慢性肾脏病患者尿液中EPI-X4的水平增高,并与肾小球滤过率(GFR)成反比。 | |||
T83735 |
Pap12-6 TFA
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Pap12-6是一种从蝶类P. xuthus幼虫中发现的papiliocin十二个N-端氨基酸衍生的抗菌肽。它对包括E. coli、P. aeruginosa和S. syphimurium在内的八种革兰氏阴性细菌(MIC50s = 4-8 µM)以及革兰氏阳性细菌S. aureus、耐甲氧西林的S. aureus 3126(MRSA-3126)、B. subtilis和S. epidermidis(MIC50s = 4-8 µM)具有活性,但在25 µM浓度下不影响人类红细胞、小鼠RAW 264.7巨噬细胞、人类HaCaT角质形成细胞或人类HEK293肾细胞的活性。Pap12-6在4和8 µM浓度下可引起E. coli的膜去极化。Pap12-6(10 µM)预处理可降低LPS刺激的RAW 264.7巨噬细胞中一氧化氮(NO2-)、Tnf-α和Il-6的分泌水平。在体内,Pap12-6(10 mg/kg)可以提高感染E. coli的小鼠的存活率,并且在剂量为1 mg/kg时减少感染E. coli小鼠的肺、肝和肾中菌落形成单位(CFUs)的数量。Pap12-6(1 mg/kg)在E. co... | |||
T36805 |
TPC2-A1-N
TPC2-A1-N |
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TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1]. |
Cat. No. | Product Name | Target | Signaling Pathways |
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TN1018 |
Angeloylgomisin H
当归酰戈米辛 H,当归酰戈米辛H |
PPAR | DNA Damage/DNA Repair; Metabolism |
Angeloylgomisin H 是从五味子中提取的一种木脂素类天然产物。它通过激活PPAR-γ来改善胰岛素刺激的葡萄糖摄取潜力。 | |||
T35532 |
Galegine hydrochloride
|
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Galegine hydrochloride, a guanidine derivative derived from G. officinalis, plays a role in inducing weight loss in mice and has contributed to the development of biguanides, including metformin and phenformin. This compound stimulates AMPK activation in 3T3-L1 adipocytes, L6 myotubes, H4IIE rat hepatoma, and HEK293 human kidney cell lines. Additionally, galegine hydrochloride exhibits antibacterial properties, particularly demonstrating a minimum inhibitory concentration of 4 mg/L against Staph... |