Cat. No. | Product Name | Target | Signaling Pathways |
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T35723 |
GRK-IN-1
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4-Amino-5-(bromomethyl)-2-methylpyrimidine is a heterocyclic building block.1,2 It has been used in the synthesis of vitamin B1 analogs and thiaminephosphoric acid esters. |1. Abblard, J., Cronenberger, L., and Pacheco, H. Synthesis of the analogs of vitamin B1. Chim. Ther. 8(1), 98-110 (1973).|2. Leichssenring, G., and Joachim, S. The synthesis of thiaminephosphoric acid esters. Chem. Ber. 95, 767-772 (1962). | |||
T9609 |
GRK5-IN-2
|
GRK | GPCR/G Protein |
GRK5-IN-2 是基于吡啶的双环化合物,抑制 G 蛋白偶联受体激酶 5 。它调节胰岛素的表达和/或释放,在代谢疾病中有研究价值。 | |||
T61556 |
GRK6-IN-2
|
GRK | GPCR/G Protein |
GRK6-IN-2 是一种高效的 G 蛋白偶联受体激酶 6 (GRK6)抑制剂,具有潜在的抗肿瘤活性。GRK6-IN-2具有研究多发性骨髓瘤。 | |||
TP2025 |
GRK2i
|
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GRK2 inhibitory polypeptide that specifically inhibits Gβγ activation of GRK2. Corresponds to the Gβγ-binding domain and acts as a cellular Gβγ antagonist. | |||
T25464 |
GRK2 Inhibitor
βARK1 Inhibitor |
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GRK2 Inhibitor is an inhibitor of β-Adrenergic Receptor Kinase 1 (β ARK1). | |||
T63203 | GRK5-IN-4 | ||
GRK5-IN-4 是选择性的、有效的、共价 GRK5(G 蛋白偶联受体激酶 5) 抑制剂(IC50: 1.1 μM)。GRK5-IN-4 对 GRK5 的选择性是 GRK2 的90倍。GRK5-IN-4 能够用于研究心力衰竭。 | |||
T62599 |
GRK5-IN-3
|
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GRK5-IN-3 是一种 G 蛋白偶联受体激酶 5 (GRK5) 的共价抑制剂。GRK5-IN-3 对 GRK5 (IC50: 0.22 μM) 和 GRK6 (IC50: 0.41 μM)有显著的抑制作用。 | |||
T62518 | GRK6-IN-1 | ||
GRK6-IN-1 (compound 18) 是一种有效的 G 蛋白偶联受体激酶 6 (GRK6) 抑制剂 (IC50: 120 nM)。其中 GRK6 是多发性骨髓瘤 (MM) 细胞存活所需的关键激酶。GRK6-IN-1 具有潜力进行多发性骨髓瘤的研究。 | |||
T75935 |
GRK2i TFA
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GRK2i TFA 是一个 GRK2抑制多肽,特异性抑制 Gβγ 活化 GRK2。 GRK2i TFA 对应于 Gβγ结合域,并作为细胞 Gβγ 拮抗剂。 | |||
T79913 |
GRK2 Inhibitor 2
|
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GRK2 Inhibitor 2 (Compound 8h) 作为一种高效的抑制剂,对GRK2有显著的抑制活性(IC50: 19 nM),同样对Aurora-A也表现出抑制作用(IC50: 137 nM)。该化合物能增强GRK2过表达的HEK293细胞中β-AR介导的cAMP积累。此外,GRK2 Inhibitor 2适用于充血性心力衰竭(HF)的相关研究。 | |||
T13714L |
GRK2-IN-1 hydrochloride (2055990-90-2 free base)
GRK2-IN-1 hydrochloride |
GRK | GPCR/G Protein |
GRKs-IN-1 hydrochloride has remarkable potency against and selectivity for G protein-coupled receptor kinase 2 GRK2 (IC50: 130 nM) and GRK5 (IC50: 7.1 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。 | |||
T24106 |
GSK2163632A
GSK-2163632-A,GSK 2163632 A |
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GSK2163632A is an insulin-like growth factor 1 receptor inhibitor that acts by binding to a novel region of the GRK active site cleft. |