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Search Results for " sk1 "

Targets Recommended: S1P Receptor

64

抑制剂 & 化合物

1

重组蛋白

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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	Others	Others
	BML-258 HCl was removed and discontinued.
T60798	SK1- I hydrochloride	Others	Others
	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) 。
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。
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。
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。
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。
T15424	GSK1379725A	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK1379725A 是一种选择性 BPTF 配体，Kd 为 2.8 μM。
T2079	GSK126 GSK2816126A,EZH2 inhibitor	Histone Methyltransferase	Chromatin/Epigenetic
	GSK126 (GSK2816126A) 是一种 EZH2 甲基转移酶抑制剂 (IC50=9.9 nM)，具有有效性和选择性。GSK126 具有抗肿瘤活性，可以抑制肿瘤细胞增殖、抑制血管生成。
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。
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。
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。
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。
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。
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)。
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。
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+。
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。
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.
T27452	GSK1723980	Others	Others
	GSK1723980 is a novel noncompetitive rTbIPMK inhibitor.
T73141	GSK1790627	Others	Others
	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	Others	Others
	GSK1482160 is a potent and selective P2X7 receptor allosteric modulator.
T60252	HSK16149	Others	Others
	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。
T11477	GSK1059865	Others	Others
	GSK1059865 is a potent antagonist of the orexin 1 receptor.
T39874	GSK143 dihydrochloride	Others	Others
	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.
T35897	ASK120067	Others	Others
	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...
T38626	GSK143	Others	Others
	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.
T27448	GSK1331258 GSK 1331258,GSK-1331258	Others	Others
	GSK1331258 is a selective, orally bioavailable positive modulators of mGluR2.
T25467	GSK1360707 GSK-1360707,GSK 1360707	Others	Others
	GSK1360707 is a selective triple reuptake inhibitor (TRI).
T71069	GSK1842799 HCl	Others	Others
	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.
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.
T70171	GSK1379767A	Others	Others
	GSK1379767A is a dual inhibitor of BPTF and Brd4.
T71343	GSK1997132B	Others	Others
	GSK1997132B is a potent, metabolically stable and centrally penetrant PPARγ partial agonist.
T32001	GSK124576A GSK-124576A,GSK 124576A	Others	Others
	GSK124576A is a bioactive chemical.
T38619	GSK1795091 CRX-601	Others	Others
	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.
T27447	GSK1104252A GSK 1104252A,GSK-1104252A	Others	Others
	GSK1104252A is a potent and selective agonist of GPR119.
T11478L	GSK1521498 free base	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	GSK1521498 free base is a potent and selective antagonist of the μ-opioid receptor. GSK1521498 free base also has the potential for disorders of compulsive consumption of food, alcohol, and drugs.
T64011	GSK1820795A	Others	Others
	GSK1820795A 作为替米沙坦类似物是hGPR132a 的选择性拮抗剂。GSK1820795A 阻断了 N-acylamides 对表达hGPR132a 的酵母细胞的活化。GSK1820795A 也是血管紧张素 II 拮抗剂和部分PPARγ激动剂 (compound 38) 。
T34653	SK1071	Others	Others
	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	Others	Others
	GSK106 is a negative control used in binding and functional assays for PAD4 inhibitors.
T68912	GSK1030058A	Others	Others
	GSK1030058A is a novel inhibitor of polo-like kinase

化合物

Cat.No: T12927

Target: S1P Receptor

Cat.No: T30485

Synonym: BML 258,BML-258,BML258,BML-258 HCl

Target: Others

SK1- I hydrochloride

Cat.No: T60798

Target: Others

NS8593 hydrochloride

Cat.No: T12256

Synonym: NS8593 HCl

Target: Potassium Channel

PF-543 hydrochloride

Cat.No: T8840

Synonym: PF-543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

Cat.No: T6085

Synonym: Sphingosine Kinase 1 Inhibitor II,PF 543

Target: Apoptosis, S1P Receptor, Autophagy, LPL Receptor

Cat.No: T9697

Target: ASK

Cat.No: T2701

Target: GPR

Cat.No: TQ0311

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T8861

Target: PAD

Cat.No: T5427

Synonym: SCD inhibitor 1

Target: Dehydrogenase, Stearoyl-CoA Desaturase (SCD)

Cat.No: T6021

Synonym: I-BET726

Target: Apoptosis, Epigenetic Reader Domain

Cat.No: T27453

Synonym: DG70

Target: Antibacterial

Cat.No: T15424

Target: Epigenetic Reader Domain

Cat.No: T2079

Synonym: GSK2816126A,EZH2 inhibitor

Target: Histone Methyltransferase

Cat.No: T24105

Synonym: GSK-121,GSK 121

Target: PAD

Cat.No: T3171

Synonym: GSK 137647

Target: GPR

Cat.No: T9377

Target: Apoptosis, ASK, MAPK

Cat.No: T67857

Target: ASK

Cat.No: T3513

Synonym: GSK180736

Target: ROCK, GRK, PKA

Cat.No: T37450

Target: p38 MAPK

Cat.No: T2357

Synonym: GSK 1059615,GSK-1059615

Target: Apoptosis, PI3K, mTOR

Cat.No: T3079

Target: IGF-1R, JNK, S6 Kinase, ALK

Cat.No: TQ0066

Synonym: GSK189254

Target: Histamine Receptor

Cat.No: T6848

Synonym: GSK101

Target: Calcium Channel, TRP/TRPV Channel

Cat.No: T6003

Synonym: GSK 4529

Target: Apoptosis, Raf, VEGFR, IGF-1R, Syk

GSK1521498 free base (hydrochloride)

Cat.No: T11478

Target: Opioid Receptor

Cat.No: T27452

Target: Others

Cat.No: T73141

Target: Others

Cat.No: T27450

Synonym: GSK 1482160,GSK-1482160

Target: Others

Cat.No: T60252

Target: Others

Cat.No: T11477

Target: Others

GSK143 dihydrochloride

Cat.No: T39874

Target: Others

Cat.No: T35897

Target: Others

Cat.No: T38626

Target: Others

Cat.No: T27448

Synonym: GSK 1331258,GSK-1331258

Target: Others

Cat.No: T25467

Synonym: GSK-1360707,GSK 1360707

Target: Others

Cat.No: T71069

Target: Others

Cat.No: T15425

Target: Others

Cat.No: T11479

Target: Opioid Receptor

Cat.No: T70171

Target: Others

Cat.No: T71343

Target: Others

Cat.No: T32001

Synonym: GSK-124576A,GSK 124576A

Target: Others

Cat.No: T38619

Synonym: CRX-601

Target: Others

Cat.No: T27447

Synonym: GSK 1104252A,GSK-1104252A

Target: Others

GSK1521498 free base

Cat.No: T11478L

Target: Opioid Receptor

Cat.No: T64011

Target: Others

Cat.No: T34653

Target: Others

Cat.No: T24104

Synonym: GSK-106,GSK 106

Target: Others

Cat.No: T68912

Target: Others

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-01635	PCSK1 Protein, Human, Recombinant (His) proprotein convertase subtilisin/kexin type 1,SPC3,...	Human	HEK293 Cells
	Neuroendocrine convertase 1, also known as Prohormone convertase 1, Proprotein convertase 1, PCSK1 and NEC1, is an enzyme which belongs to the peptidase S8 family and Furin subfamily. PCSK1 is an enzyme that performs the proteolytic cleavage of prohormones to their intermediate (or sometimes completely cleaved) forms. It is present only in neuroendocrine cells such as brain, pituitary and adrenal, and most often cleaves after a pair of basic residues within prohormones but can occasionally cleav...

重组蛋白

PCSK1 Protein, Human, Recombinant (His)

Cat.No: TMPY-01635

Species: Human

Expression System: HEK293 Cells

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