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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T68730 |
AVE1231
|
Potassium Channel | Membrane transporter/Ion channel |
AVE1231 是一种 TASK-1 通道阻滞剂,抑制 TASK-1 ,可用于研究心房颤动。 | |||
T3348 |
PIK-293
PIK293 |
PI3K | PI3K/Akt/mTOR signaling |
PIK-293 是一种 IC87114 的类似物,是一种 PI3K 的抑制剂,其对 p110δ (IC50:0.24 μM)、p110β (IC50:10 μM)、p110γ (IC50:25 μM) 和 p110α (IC50:100 μM)。 | |||
T5418 |
BAY-293
|
Raf; Ras | GPCR/G Protein; MAPK |
BAY-293 是化学探针,是一种有效的细胞活性 SOS1 抑制剂,可破坏 KRAS-SOS1 相互作用,IC50为 21 nM。 | |||
T69857 |
DB293
|
||
DB293 is an inhibitor of PIT-1 and BRN-3 transcription factors. DB293 binds as head-to-tail stacked dimers in the minor groove of 5'-ATGA sequence, thereby leading to an increase in the size of minor groove. | |||
T41214 |
(S)-BAY-293
BAY 294,BAY 293 Negative Control |
Ras | GPCR/G Protein; MAPK |
(S)-BAY-293 是一种有效的 pan-KRAS 抑制剂,可用于研究原发性非小肺癌和胰腺癌。 | |||
T83393 |
293P-1
|
||
293P-1是一种特异性靶向肝细胞的组织特异性多肽,其序列为SNNNVRPIHIWP。 | |||
T19700 |
IBC 293
IBC293,1-异丙基-1H-1,2,3-苯并噻唑-5-羧酸,IBC-293 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
IBC 293 对 GPR109B 的选择性高于烟酸受体 GPR109A。 IBC 293 是 GPR109B 的高选择性激动剂,GPR109B 是一种在脂肪细胞中表达的人类孤儿 G 蛋白偶联受体。 | |||
T16569 |
Praliciguat
IW-1973 |
Others; Guanylate cyclase | GPCR/G Protein; Others |
Praliciguat (IW-1973) 是一种有效且具有口服活性的可溶性鸟苷酸环化酶 (sGC) 刺激剂,还增强 NO 信号传导,可作为血管扩张剂。在 HEK-293 细胞中,它能够刺激 sGC,EC50值为 197 nM。 | |||
T9019 |
JHU37152
JHU 37152 |
AChR | Neuroscience |
JHU37152 (JHU 37152) 是一种可透过血脑屏障的DREADD 激动剂。 在 HEK-293 细胞的荧光和基于 BRET 的测定中,对hM3Dq 和hM4Di DREADDs 的EC50值分别为 5 和 0.5 nM。 | |||
T6934 |
Pexmetinib
ARRY-614 |
Tie-2; p38 MAPK; Autophagy | Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Pexmetinib (ARRY-614) 是一种口服生物可利用的双重 p38 MAPK/Tie-2 抑制剂,可研究急性骨髓性白血病。在 HEK-293 细胞系中的 IC50 为 4 nM/18 nM。 | |||
T11076 |
Dooku1
|
Others | Others |
Dooku1 是Yoda1 的类似物,是一种内源性Piezo1通道的选择性拮抗剂,能够抑制Yoda1 诱导的主动脉舒张。它在HEK 293 细胞以及HUVEC 中测得对2 μM Yoda1 诱导的钙离子流的IC50值分别为1.3 μM 和1.5 μM。 | |||
T9018 |
JHU37160
JHU 37160 |
AChR | Neuroscience |
JHU37160 (JHU 37160) 是一种可透过血脑屏障的 DREADD 激动剂。在 HEK-293 细胞的荧光和基于 BRET 的测定中,对hM3Dq 和hM4Di DREADDs 的EC50值分别为 18.5 和 0.2 nM。 | |||
T2092 |
Amitifadine hydrochloride
DOV-21947 hydrochloride,EB-1010 hydrochloride |
Dopamine Receptor; 5-HT Receptor; Serotonin Transporter; Norepinephrine | GPCR/G Protein; Neuroscience |
Amitifadine hydrochloride (EB-1010 hydrochloride) 是一种 5-羟色胺-去甲肾上腺素-多巴胺的再摄取抑制剂(SNDRI),其在 HEK 293 细胞中测得的 IC50值分别为 12, 23, 96 nM。 | |||
T4967 |
NPS-2143 hydrochloride
2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈盐酸盐,NPS-2143 HCL |
CaSR | GPCR/G Protein |
NPS-2143 hydrochloride (NPS-2143 HCL) 是一种口服具有活性的溶钙剂,是钙敏感受体(CaSR)的选择性拮抗剂。它能够激活表达人 Ca2+受体的 HEK 293 细胞中的 Ca2+受体,从而增加胞浆 Ca2+浓度(IC50=43 nM)。 | |||
T1730 |
NPS-2143
SB262470,NPS 2143,SB 262470A,2-氯-6-[(2R)-3-[[1,1-二甲基-2-(2-萘基)乙基]氨基]-2-羟基丙氧基]苯腈 |
Calcium Channel; CaSR | GPCR/G Protein; Membrane transporter/Ion channel; Metabolism |
NPS-2143 (SB 262470A) 是口服活性溶钙剂, 是选择性钙敏感受体拮抗剂。它通过激活表达人 Ca2+受体的 HEK 293 细胞中的 Ca2+受体而引起的胞浆 Ca2+浓度增加,IC50值为43 nM。 | |||
T5345 |
V-9302
|
Others | Others |
V-9302 是一种跨膜谷氨酰胺通量的竞争性拮抗剂。它选择性的靶向氨基酸转运体 ASCT2 (SLC1A5),不影响 ASCT1。它能够阻碍 HEK-293 细胞中由 ASCT2 介导的谷氨酰胺摄取 (IC50=9.6 μM)。 | |||
T74577 |
Milpocitide
|
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Milpocitide为针对低密度脂蛋白受体(human LDL receptor, LDLR)(293-333)的肽片段(EGF-like domain 1)的化合物。 | |||
T15404 | GNE-6468 | Others | Others |
GNE-6468 is a potent and selective agonist of RORγ(RORc) (EC50: 13 nM for HEK-293 cell). | |||
T15398 |
GNE-0946
|
Others | Others |
GNE-0946 is a potent and selective agonist of RORγ (EC50: 4 nM for HEK-293 cell). | |||
T27422 |
GNE-293
GNE293 |
||
GNE-293 is a potent and selective PI3Kδ inhibitor. | |||
T10271 |
AHR antagonist 4
|
Others | Others |
AHR antagonist 4 is a potent aryl hydrocarbon receptor (AHR) antagonist(example 293; IC50: 82.2 nM).It has anti-cancer effects. | |||
T81137 |
SNX7886
|
PROTACs | PROTAC |
SNX7886为高效CDK8/19蛋白降解剂,在293细胞中可分别降解CDK8与CDK19至90%及80%。 | |||
T26621 |
AMP-579
RPR100579,RPR 100579,AMP 579,RPR-100579 |
||
AMP-579 is an adenosine A1 receptor agonist. AMP-579 also acts as a A2b-adenosine receptor agonist in human 293 cells and rabbit hearts. | |||
T14190 |
Alniditan
Alnitidan |
5-HT Receptor | GPCR/G Protein; Neuroscience |
Alniditan is a receptors agonist of 5-HT1B/1D in HEK 293 cells (IC50: 1.7 and 1.3 nM). For 5-HT1B/1D receptors, the pKi values are 8.96 and 9.40, respectively. | |||
T25109 |
ARN-6039
ARN 6039,ARN6039 |
||
ARN-6039 is an orally available inverse agonist of RORγ for Autoimmune Neuroinflammatory Demyelinating Disease. The activity of ARN-6039 against RORγ was demonstrated in a RORγ-activated IL-17A Prom/LUCPorter assay in HEK 293 cells (360 nM) and in IL-17 r | |||
T63608 |
P-gp inhibitor 5
|
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P-gp inhibitor 5 是 P 糖蛋白 (P-gp) 的有效抑制剂,在 1.25 μM 和 2.5 μM 时 P-gp 抑制倍数分别为 2.5 和 3.0。P-gp inhibitor 5 对某些癌细胞表现出抗增殖效果。P-gp inhibitor 5 能够恢复细胞对 Vincristine 和 Paclitaxel 的敏感性,进而逆转 ABCB1/Flp-InTM-293 和 KBvin 的多药耐药 (MDR) 表型。 | |||
T38984 |
Z-Ala-Ala-Asn-AMC
Cbz-Ala-Ala-Asn-AMC,Z-Ala-Ala-Asn-AMC |
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Z-Ala-Ala-Asn-AMC, also known as Cbz-Ala-Ala-Asn-AMC, serves as a substrate for legumain. The overexpression of legumain in 293 HEK-Leg cells results in efficient cleavage of Cbz-Ala-Ala-Asn-AMC. | |||
T63456 |
Antimalarial agent 12
|
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Antimalarial agent 12 是有效的抗疟 (antimalarial) 药,能够抑制恶性疟原虫 Dd2 菌株、3D7 菌株生长,其 EC50值分别为155 nM、136 nM。Antimalarial agent 12 对大肠杆菌的 MIC>250,000 nM,也能够作用于 HEK-293 和 hPHep 细胞系,其 CC50值为 10,000-50,000 nM。 | |||
T40064 |
V-9302 hydrochloride
|
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V-9302 hydrochloride is a potent and selective competitive antagonist that inhibits transmembrane glutamine flux by specifically targeting the amino acid transporter ASCT2 (SLC1A5), and not ASCT1. In HEK-293 cells, V-9302 hydrochloride effectively inhibits ASCT2-mediated glutamine uptake with an IC50 value of 9.6 μM. | |||
T74917 | KPC-2-IN-1 | ||
KPC-2-IN-1,硼酸衍生物,是一种有效的 KPC-2抑制剂,其 Ki 值为 0.032 μM。KPC-2-IN-1 能增强 cefotaxime 在表达 KPC-2的大肠杆菌中的活性。KPC-2-IN-1 对人类 HEK-293 细胞显示良好的耐受性,可用于大肠杆菌耐β-lactam 类抗生素的研究。 | |||
T37800 |
PF-04449613
|
||
PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-0444... | |||
T77154 | Etrolizumab | ||
Etrolizumab (rhuMAb Beta7) 是一种肠道选择性抗-β7整合素单克隆抗体。Etrolizuma b 是针对α4β7和 αEβ7 整合素的 β7 亚基的特异性靶向活性分子。Etrolizumab 可用于炎症性肠病 (IBD) 的研究。 | |||
T61688 | Nrf2 activator-2 | ||
Nrf2 activator-2 (referred to as compound O15), an Osthole derivative, is a highly potent Nrf2 agonist exhibiting an EC 50 of 2.9 μM in 293 T cells. By effectively disrupting the binding between Keap1 and Nrf2, Nrf2 activator-2 activates the Nrf2 pathway. Furthermore, this compound significantly reduces the ubiquitination of Nrf2 in cells, indicating its potential in regulating Nrf2 activity [1]. | |||
T75785 |
Apelin-17(human, bovine) TFA
|
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Apelin-17(human, bovine) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂。Apelin-17(human, bovine) TFA 与在 HEK 293 细胞中表达的人 APJ 受体结合 (pIC50)。Apelin-17(human, bovine) TFA 阻断 HIV-1和 HIV-2毒株进入表达 APJ 的 NP-2/CD4 细胞。 | |||
T75783 |
Apelin-36(human) TFA
|
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Apelin-36(human) TFA 是一种内源性孤儿 G 蛋白偶联受体 APJ 激动剂,EC50为 20 nM。Apelin-36(human) TFA 对 HEK 293 细胞表达的人 APJ 受体有很高的亲和力 (pIC50=8.61)。Apelin-36(human) TFA 与两种主要的生物活性有关:心血管和代谢。Apelin-36(human) TFA 抑制 HIV-1和 HIV-2进入表达 APJ 的 NP2/CD4细胞。 | |||
T35836 |
PMX-205 (trifluoroacetate salt)
|
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PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Rela... | |||
T38174 | Mpro inhibitor N3 hemihydrate | ||
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively[1][2]. Mpro inhibitor N3 hemihydrate (0-0.64 μM) is able to penetrate cells to inhibit the replication of IBV viruses... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T72508 | Palmatine hydroxide | ||
Palmatine hydroxide 是不可逆的口服活性IDO-1抑制剂,其对HEK 293-hIDO-1 和 rhIDO-1的IC50值分别为3 μM和157 μM。该化合物还能非竞争性抑制(WNV)NS2B-NS3蛋白酶,IC50值为96 μM。Palmatine hydroxide展现了抗癌、抗炎、神经保护、抗细菌和抗病毒的活性。 |