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KN-62,CaM激酶II抑制剂, P2X7 的异构调节剂

CaM激酶II抑制剂。P2X 7拮抗剂。
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货号 (SKU) 包装规格 是否现货 价格 数量
K125637-5mg
 5mg 现货 Stock Image
K125637-25mg
 25mg 现货 Stock Image
K125637-100mg
 100mg 现货 Stock Image
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Calmodulin-dependent kinase II Inhibitor (2) CaMK (32) P2X Receptor (58) P2X7 Allosteric modulator (9) 神经元信号传导 (3330) 膜转运器/离子通道 (1833)
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基本描述

英文别名 KN62 | KN-62 | MFCD00083180 | NCGC00162398-03 | [4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate. | Ponceau BNA | [4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-pheny
规格或纯度 Moligand™, ≥98%
英文名称 KN-62
生化机理 KN-62 对 Ca2+/calmodulin 依赖性蛋白激酶 II（CaMKII；Ki=0.9 μM）具有强效的选择性抑制作用，可使细胞停滞在 S 期。在表达 III 型腺苷酸环化酶（III-AC）的 HEK-293 细胞中，10 μM 的 KN-62 可阻断 CaMKII 对 III-AC 的磷酸化，并抑制激素刺激的 Ca2+ 振荡。此外，KN-62 还是 P2X7 受体的强效非竞争性拮抗剂（IC50 = 15 nM）。与酶的钙调素结合位点相互作用。据报道，在较高浓度下可抑制 GSK3β、PRAK 和 MAPKAP-K2。也是强效的非竞争性拮抗剂
储存温度 -20°C储存
运输条件 超低温冰袋运输
作用类型 变构调节剂
作用机制 P2X7 的异构调节剂
备注 如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍

KN-62是可渗透入细胞的CaM激酶II抑制剂，IC50为0.9 μM，直接与该酶的钙调蛋白结合位点结合，同时还是非竞争性P2X7受体拮抗剂，IC50为15 nM。A potent and selective inhibitor of CaMKII

KN-62 is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.9 μM.
A potent and selective inhibitor of CaMKII

AI解读

关联靶点（人）

P2RX7 Tchem P2X嘌呤受体 7(P2X purinoceptor 7) (26 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KIT Tclin Stem cell growth factor receptor (10667 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DAPK3 Tchem Death-associated protein kinase 3 (2108 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAPK14 Tchem MAP kinase p38 alpha (12866 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCZ Tchem Protein kinase C zeta (2414 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MYLK Tchem Myosin light chain kinase, smooth muscle (1267 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR2 Tclin Fibroblast growth factor receptor 2 (3405 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FGFR1 Tclin Fibroblast growth factor receptor 1 (9149 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK2B Tchem CaM kinase II beta (1626 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
P2RX4 Tchem P2X purinoceptor 4 (516 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
P2RX7 Tchem P2X purinoceptor 7 (5534 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SRC Tclin Tyrosine-protein kinase SRC (10310 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT2 Tchem Serine/threonine-protein kinase AKT2 (4301 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT3 Tchem Serine/threonine-protein kinase AKT3 (3157 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IKBKB Tchem Inhibitor of nuclear factor kappa B kinase beta subunit (5554 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DAPK2 Tchem Death-associated protein kinase 2 (740 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA4 Tchem Ribosomal protein S6 kinase alpha 4 (2104 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ROCK1 Tclin Rho-associated protein kinase 1 (4723 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PKN2 Tchem Protein kinase N2 (1991 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSK Tchem Tyrosine-protein kinase CSK (2395 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA5 Tchem Ribosomal protein S6 kinase alpha 5 (3355 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCE Tchem Protein kinase C epsilon (1520 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCG Tchem Protein kinase C gamma (2471 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKCI Tchem Protein kinase C iota (2821 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKD1 Tchem Protein kinase C mu (1904 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RAF1 Tclin Serine/threonine-protein kinase RAF (4169 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SYK Tclin Tyrosine-protein kinase SYK (7372 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ITK Tclin Tyrosine-protein kinase ITK/TSK (3699 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA1 Tchem Ribosomal protein S6 kinase alpha 1 (2796 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPS6KA6 Tchem Ribosomal protein S6 kinase alpha 6 (2027 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CAMK1 Tchem CaM kinase I alpha (1664 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

ampC Beta-lactamase AmpC (62480 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cruzipain (33337 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcd Protein kinase C delta (192 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Prkcb Protein kinase C beta (2 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr4 Fibroblast growth factor receptor 4 (138 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Camk2g CaM kinase II gamma (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Tec Tyrosine-protein kinase TEC (25 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasmodium falciparum (966862 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
dengue virus type 2 (2400 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapt Microtubule-associated protein tau (6 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Nfe2l2 Nuclear factor erythroid 2-related factor 2 (214 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FTL Ferritin light chain (43324 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NS1 Nonstructural protein 1 (33327 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
P2X7 P2X purinoceptor (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
P2X7 P2X7 purinoceptor (1 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504763558
分子类型 小分子
IUPAC Name [4-[(2S)-2-[isoquinolin-5-ylsulfonyl(methyl)amino]-3-oxo-3-(4-phenylpiperazin-1-yl)propyl]phenyl] isoquinoline-5-sulfonate
INCHI InChI=1S/C38H35N5O6S2/c1-41(50(45,46)36-11-5-7-29-26-39-19-17-33(29)36)35(38(44)43-23-21-42(22-24-43)31-9-3-2-4-10-31)25-28-13-15-32(16-14-28)49-51(47,48)37-12-6-8-30-27-40-20-18-34(30)37/h2-20,26-27,35H,21-25H2,1H3/t35-/m0/s1
InChi Key RJVLFQBBRSMWHX-DHUJRADRSA-N
Canonical SMILES CN(C(CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7
Isomeric SMILES CN([C@@H](CC1=CC=C(C=C1)OS(=O)(=O)C2=CC=CC3=C2C=CN=C3)C(=O)N4CCN(CC4)C5=CC=CC=C5)S(=O)(=O)C6=CC=CC7=C6C=CN=C7
WGK Germany 3
PubChem CID 5312126
分子量 721.84

化学和物理性质

溶解性 DMSO
分子量 721.800 g/mol
XLogP3 5.600
氢键供体数Hydrogen Bond Donor Count 0
氢键受体数Hydrogen Bond Acceptor Count 10
可旋转键计数Rotatable Bond Count 10
精确质量Exact Mass 721.203 Da
单同位素质量Monoisotopic Mass 721.203 Da
拓扑极表面积Topological Polar Surface Area 147.000 Ų
重原子数Heavy Atom Count 51
形式电荷Formal Charge 0
复杂度Complexity 1370.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 1
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 1

安全和危险性（GHS）

WGK Germany 3
个人防护装备 Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter

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批号(Lot Number) 证书类型 日期 货号
D2102118 分析证书 23-01-13 K125637
D2102120 分析证书 23-01-13 K125637
D2102121 分析证书 23-01-13 K125637

参考文献

1. Tokumitsu H, Chijiwa T, Hagiwara M, Mizutani A, Terasawa M, Hidaka H.  (1990)  KN-62, 1-[N,O-bis(5-isoquinolinesulfonyl)-N-methyl-L-tyrosyl]-4-phenylpiperazi ne, a specific inhibitor of Ca2+/calmodulin-dependent protein kinase II..  J Biol Chem,  265  (8): (4315-20).  [PMID:2155222] [10.1021/op500134e]
2. Chessell IP, Michel AD, Humphrey PP.  (1998)  Effects of antagonists at the human recombinant P2X7 receptor..  Br J Pharmacol,  124  (6): (1314-20).  [PMID:9720806] [10.1021/op500134e]
3. Wu K et al..  (2021)  Activity- and sleep-dependent regulation of tonic inhibition by Shisa7..  Cell Rep,  34  (12): (108899).  [PMID:33761345]
4. Glasgow SD et al..  (2018)  Activity-Dependent Netrin-1 Secretion Drives Synaptic Insertion of GluA1-Containing AMPA Receptors in the Hippocampus..  Cell Rep,  25  (168-182.e6).  [PMID:30282026]
5. Jing L et al..  (2015)  Despair-associated memory requires a slow-onset CA1 long-term potentiation with unique underlying mechanisms..  Sci Rep,  5  (15000).  [PMID:26449319]
6. Luchkina NV et al..  (2014)  Developmental switch in the kinase dependency of long-term potentiation depends on expression of GluA4 subunit-containing AMPA receptors..  Proc Natl Acad Sci U S A,  111  (11): (4321-6).  [PMID:24599589]

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