Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12927 | SK1-IN-1 | S1P Receptor | GPCR/G Protein |
SK1-IN-1 is a potent inhibitor of sphingosine kinase 1 (SPHK1)(IC50 of 58 nM). | |||
T30485 |
SK1-I
BML 258,BML-258,BML258,BML-258 HCl |
||
BML-258 HCl was removed and discontinued. | |||
T60798 |
SK1- I hydrochloride
|
||
SK1-I hydrochloride (BML-258 hydrochloride) 是鞘氨醇类似物,能够增强细胞自噬并显示抗癌活性。SK1-I hydrochloride 是同工酶特异性SPHK1竞争抑制剂 (Ki = 10 μM)。 | |||
T12256 |
NS8593 hydrochloride
NS8593 HCl |
Potassium Channel | Membrane transporter/Ion channel |
NS8593 hydrochloride (NS8593 HCl) 是选择性的 SK 通道抑制剂。它可逆抑制 SK3介导的电流,Kd 值为 77 nM。它抑制所有 SK1-3亚型的 Ca2+依赖性 (在 0.5 μM Ca2+时,Kd 分别为 0.42、0.60 和 0.73 μM),并且不影响中间电导和大电导的钙激活钾通道。 | |||
T8840 |
PF-543 hydrochloride
PF-543 |
Apoptosis; S1P Receptor; Autophagy; LPL Receptor | Apoptosis; Autophagy; GPCR/G Protein |
PF-543 hydrochloride (PF-543) 是一种选择性可逆和鞘氨醇竞争性SPHK1抑制剂,对SPHK1的选择性是 SPHK2 的 100 倍以上。它还是全血中 1-磷酸鞘氨醇形成的有效抑制剂,诱导细胞凋亡、坏死和自噬。 | |||
T6085 |
PF-543
Sphingosine Kinase 1 Inhibitor II,PF 543 |
Apoptosis; S1P Receptor; Autophagy; LPL Receptor | Apoptosis; Autophagy; GPCR/G Protein |
PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种选择性可逆和鞘氨醇竞争性 SPHK1抑制剂,可诱导细胞凋亡、坏死和自噬。它对 SPHK1的选择性是 SPHK2 的 100 倍以上。它还抑制全血中 1-磷酸鞘氨醇形成,IC50为 26.7 nM。 | |||
T9697 |
ASK1-IN-1
|
ASK | Apoptosis |
ASK1-IN-1 是一种凋亡信号调节激酶 1(SK1) 抑制剂,具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。 | |||
T2701 |
GSK1292263
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
GSK1292263 是口服具有活性的 GPR119 激动剂,对人和大鼠 GPR119的pEC50分别为 6.9 和 6.7,它可用于研究 2 型糖尿病 (T2DM) 。 | |||
T5427 |
GSK1940029
SCD inhibitor 1 |
Dehydrogenase; Stearoyl-CoA Desaturase (SCD) | Metabolism |
GSK1940029 (SCD inhibitor 1) 是酰基-辅酶A 去饱和酶 (SCD) 抑制剂。 | |||
TQ0311 |
GSK163090
|
Dopamine Receptor; 5-HT Receptor | GPCR/G Protein; Neuroscience |
GSK163090 是选择性和具有口服活性的5-HT1A/1B/1D 受体拮抗剂,pKi 值分别为 9.4、8.5 和 9.7。它抑制血清素再摄取转运蛋白的功能活性,pKi 值为 6.1,具有抗抑郁和抗焦虑活性。 | |||
T8861 |
GSK199
|
PAD | Chromatin/Epigenetic |
GSK199 是可逆的 PAD4选择性抑制剂,当缺少钙离子时,其 IC50值为 200 nM。 | |||
T15424 |
GSK1379725A
|
Epigenetic Reader Domain | Chromatin/Epigenetic |
GSK1379725A 是一种选择性 BPTF 配体,Kd 为 2.8 μM。 | |||
T27453 |
GSK1733953A
DG70 |
Antibacterial | Microbiology/Virology |
GSK1733953A 可作为一种小分子结核分枝杆菌呼吸抑制剂,对 MenG 活性有抑制作用,IC50 值为 2.6 ± 0.6 μM。GSK1733953A 是一种具有选择性的联苯苯甲酰胺,对结核分枝杆菌去甲基萘醌甲基转移酶的催化甲基化有抑制作用,对结核分枝杆菌H4Rv的MIC为8.37 μg/ml,对耐药菌株的MIC为1.2至9.6 μg/ml。GSK1733953A 是治疗结核病的候选化合物。 | |||
T2079 |
GSK126
GSK2816126A,EZH2 inhibitor |
Histone Methyltransferase | Chromatin/Epigenetic |
GSK126 (GSK2816126A) 是一种选择性的EZH2甲基转移酶抑制剂,IC50为 9.9 nM。 | |||
T6021 |
GSK1324726A
I-BET726 |
Apoptosis; Epigenetic Reader Domain | Apoptosis; Chromatin/Epigenetic |
GSK1324726A (I-BET726) 是一种选择性有效的BET 蛋白抑制剂,高亲和力结合到BRD2、BRD3和BRD4,IC50值分别为 41 nM、31 nM 和 22 nM。 | |||
T9377 |
ASK1-IN-2
|
Apoptosis; ASK; MAPK | Apoptosis; MAPK |
ASK1-IN-2 是一种口服有活性的凋亡信号调节激酶 1 抑制剂(IC50:32.8 nM)。它可用于研究溃疡性结肠炎。 | |||
T24105 |
GSK121
GSK-121,GSK 121 |
PAD | Chromatin/Epigenetic |
GSK121 Trifluoroacetate 是PAD4的选择性抑制剂。 | |||
T3171 |
GSK137647A
GSK 137647 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
GSK137647A (GSK 137647) 是一种选择性FFA4激动剂,作用于人类和大小鼠FFA4的pEC50分别为6.3、6.1和6.2。 | |||
T37450 |
SSK1
|
p38 MAPK | MAPK |
SSK1 是一种选择性杀死衰老细胞的化合物,是一种针对 β-galactosidase 的前体,可减轻机体炎症反应。SSK1 可激活衰老细胞中 p38 MAPK 和 MKK3/MKK6 的磷酸化水平,促使衰老细胞线粒体 DNA 损伤。 | |||
T67857 |
ASK1-IN-4
|
ASK | Apoptosis |
ASK1-IN-4 是一种ASK1抑制剂,IC50 = 0.2 μM。 | |||
T3513 |
GSK180736A
GSK180736 |
ROCK; GRK; PKA | Cell Cycle/Checkpoint; Cytoskeletal Signaling; GPCR/G Protein; Stem Cells; Tyrosine Kinase/Adaptors |
GSK180736A 是 Rho 相关卷曲螺旋激酶 1 (ROCK1) 抑制剂,IC50值为 100 nM。它也是选择性的ATP-竞争性 G 蛋白偶联受体激酶 2 抑制剂,IC50值为 0.77 μM,其选择性比其他 GRK 高 100 倍以上。 | |||
T6003 |
GSK1904529A
GSK 4529 |
Apoptosis; Raf; VEGFR; IGF-1R; Syk | Angiogenesis; Apoptosis; MAPK; Tyrosine Kinase/Adaptors |
GSK1904529A (GSK 4529) 是一种选择性,具有口服活性和 ATP 竞争性的胰岛素样生长因子 1 受体和胰岛素受体抑制剂,IC50值分别为 27 和 25 nM。它具有抗肿瘤活性。 | |||
T6848 |
GSK1016790A
GSK101 |
Calcium Channel; TRP/TRPV Channel | Membrane transporter/Ion channel; Metabolism |
GSK1016790A (GSK101) 是选择性瞬时受体电位香草酸 4 通道激活剂,可引起 HEK 细胞中 Ca2+流入并升高细胞内 Ca2+。 | |||
T3079 |
GSK1838705A
|
IGF-1R; JNK; S6 Kinase; ALK | Angiogenesis; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
GSK1838705A 是一种高效的、可逆的IGF-IR (IC50:2.0 nM) 和胰岛素受体 (IC50:1.6 nM)抑制剂,也可抑制ALK (IC50:0.5 nM)。 | |||
T2357 |
GSK1059615
GSK 1059615,GSK-1059615 |
Apoptosis; PI3K; mTOR | Apoptosis; PI3K/Akt/mTOR signaling |
GSK1059615 是一种 PI3Kα/β/δ/γ可逆的抑制剂,同时也抑制 mTOR,IC50值分别为 0.4 nM/0.6 nM/2 nM/5 nM 和 12 nM,已用于研究淋巴瘤、实体瘤、子宫内膜癌、实体瘤癌和转移性乳腺癌治疗的试验。 | |||
TQ0066 |
GSK189254A
GSK189254 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
GSK189254A (GSK189254) 是一种有效的特异性组胺 H3 受体拮抗剂,对人类和大鼠H3的pKi 值分别为9.59到9.90和8.51到9.17之间。 | |||
T73141 |
GSK1790627
|
||
GSK1790627 是 Trametinib 的 N-脱乙酰代谢物。Trametinib 是一种具有口服活性的MEK 抑制剂,可激活自噬并诱导细胞凋亡。 | |||
T27450 |
GSK1482160
GSK 1482160,GSK-1482160 |
||
GSK1482160 is a potent and selective P2X7 receptor allosteric modulator. | |||
T27452 |
GSK1723980
|
||
GSK1723980 is a novel noncompetitive rTbIPMK inhibitor. | |||
T11478 |
GSK1521498 free base (hydrochloride)
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
GSK1521498 free base (hydrochloride) is a selective antagonist of the μ-opioid receptor (MOR). It is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. | |||
T60252 |
HSK16149
|
||
HSK16149 是一种新型的电压门控钙离子通道(VGCC)α2δ亚基选择性配体,具有镇痛活性。 | |||
T25467 |
GSK1360707
GSK-1360707,GSK 1360707 |
||
GSK1360707 is a selective triple reuptake inhibitor (TRI). | |||
T11477 | GSK1059865 | Others | Others |
GSK1059865 is a potent antagonist of the orexin 1 receptor. | |||
T38626 |
GSK143
|
||
GSK143 is a potent orally active and highly selective inhibitor of spleen tyrosine kinase (SYK) with a pIC 50 of 7.5. Furthermore, GSK143 effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. In addition, GSK143 exhibits promising anti-inflammatory properties by reducing inflammation and impeding the recruitment of immune cells in the intestinal muscularis of mice. | |||
T35897 |
ASK120067
|
||
ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... | |||
T27448 |
GSK1331258
GSK 1331258,GSK-1331258 |
||
GSK1331258 is a selective, orally bioavailable positive modulators of mGluR2. | |||
T39874 |
GSK143 dihydrochloride
|
||
GSK143 dihydrochloride is a highly selective, orally active inhibitor of spleen tyrosine kinase (SYK), exhibiting a pIC 50 value of 7.5. It effectively inhibits phosphorylated Erk (pErk) with a pIC 50 value of 7.1. The compound demonstrates anti-inflammatory properties and hinders the recruitment of immune cells in the intestinal muscularis of mice. | |||
T71069 |
GSK1842799 HCl
|
||
GSK1842799 is a selective S1P1 receptor agonist for multiple sclerosis. Upon phosphorylation, GSK1842799 showed subnanomole S1P1 agonist activity with >1000× selectivity over S1P3. GSK1842799 demonstrated good oral bioavailability. On the basis of the favorable in vitro ADME and in vivo PK/PD properties as well as broad toxicology evaluations, GSK1842799 was selected as a candidate for further clinical. | |||
T15425 |
GSK1702934A
|
Others | Others |
GSK1702934A is a selective TRPC3 agonist. It modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3. | |||
T70171 | GSK1379767A | ||
GSK1379767A is a dual inhibitor of BPTF and Brd4. | |||
T27447 |
GSK1104252A
GSK 1104252A,GSK-1104252A |
||
GSK1104252A is a potent and selective agonist of GPR119. | |||
T32001 |
GSK124576A
GSK-124576A,GSK 124576A |
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GSK124576A is a bioactive chemical. | |||
T38619 |
GSK1795091
CRX-601 |
||
GSK1795091 (CRX-601) is a synthetic TLR4 agonist and immunologic stimulator with demonstrated antitumor activity. It serves as a vaccine adjuvant, enhancing both mucosal and systemic immunity to influenza virus vaccines. | |||
T71343 |
GSK1997132B
|
||
GSK1997132B is a potent, metabolically stable and centrally penetrant PPARγ partial agonist. | |||
T11479 |
GSK1521498
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
GSK1521498 is a selective antagonist of the μ-opioid receptor (MOR). It is being used for the treatment of disorders of compulsive consumption of food, alcohol, and drugs. | |||
T68912 | GSK1030058A | ||
GSK1030058A is a novel inhibitor of polo-like kinase | |||
T34653 | SK1071 | ||
SK1071 is a novel migrastatin analogs, which demonstrated improved performance over migrastatin, with nanomolar IC50 values in chamber cell migration assays with tumor cells and human umbilical vein endothelial cells (HUVECs), and in wound healing assays. | |||
T24104 |
GSK106
GSK-106,GSK 106 |
||
GSK106 is a negative control used in binding and functional assays for PAD4 inhibitors. | |||
T27451 |
GSK1614343
GSK-1614343,GSK 1614343 |
||
GSK1614343 is an antagonist of ghrelin receptor. | |||
T71651 |
GSK1370319A
|
||
GSK1370319A is a potent P2X7 antagonist (IC50 = 3.2 nM). GSK1370319A inhibits ATP-induced increase in IL-1β release and caspase 1 activation in lipopolysaccharide (LPS)-primed mixed glia by blocking assembly of the inflammasome in a pannexin 1-dependent manner. GSK1370319A also inhibits ATP-induced subregion-specific neuronal loss in hippocampal organotypic slice cultures, which is dependent on its ability to prevent inflammasome assembly in glia. Significantly, GSK1370319A attenuates age-relate... |