CaMK

特异性亚型抑制剂

• CaMKII Selective
• CaMKIII Selective

CaMK产品

目录号	产品描述	文献引用	实验数据
S1421	Staurosporine Staurosporine (CGP 41251) 是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。	EMBO J, 2020, 39(5):e102608 Genes Dev, 2020, 34(7-8):526-543 Cell Rep, 2020, 10;30(10):3411-3423 e7
S7436	NH125 NH125 是一种选择性eEF-2 kinase抑制剂，IC50为60 nM,其选择性高于PKC, PKA和CaMKII 125倍 , 同时它也是强效的 histidine kinase 抑制剂。	Acta Pharmacol Sin, 2018, 10.1038/s41401-018-0165-9 Drug Des Devel Ther, 2018, Drug Des Devel Ther BMC Cancer, 2016, 16(1):813	MDA-MB-231 or T47D cells were pretreated with 300 nM NH125 for 1 h, followed by treatment with 8 μM TBMS1 for 24 h. The protein levels were measured by Western blot.
S8274	STO-609 STO-609 是特异性的CaM-KK的抑制剂，抑制CaM-KKα和CaM-KKβ的活性，Ki值分别为80 ng/ml和15 ng/ml，并抑制其自身磷酸化活性。STO-609 可抑制 AMPKK 活性并抑制自噬。	J Neuroinflammation, 2020, 17(1):187 FASEB J, 2018, 10.1096/fj.201800463 Front Mol Neurosci, 2018, 11:98
S6787New	KN-93 KN-93 是一种具有细胞渗透性和竞争性的 Ca2+/calmodulin-dependent protein kinase II (CaMK-II) 的可逆抑制剂，对于兔心肌 CaM 激酶活性的Ki值为2.58 μM。	Clin Exp Pharmacol Physiol, 2020, 47(5):848-856
S7423	KN-93 Phosphate KN-93 Phosphate 是一种强效的特异性的Ca2+/calmodulin-dependent protein kinase II (CaMKII)抑制剂，其 Ki 为 0.37 μM,对 APK, PKC, MLCK 或 Ca2+-PDE 没有明显的抑制活性。KN-93 可减弱CaMKII诱导的自噬。	EMBO J, 2020, 39(5):e102608 Redox Biol, 2020, 28:101381 Free Radic Biol Med, 2020, 28;152:336-347	Paeoniflorin (PF) protects the heart against MI-induced injury in DM mice. Heart function was analyzed by measuring fractional shortening {FS = [LV end diastolic diameter (LVEDD)-LVend systolic diameter (LVESD)]×100/LVEDD} and LV ejection fraction [LVEF = (LVEDD2−LVESD2)/LVEDD2].
S2642New	1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1 (1-NA-PP 1)是一种高度选择性的、有效的 pan-PKD 抑制剂，对于PKD1、PKD2和PKD3的IC50值分别为154.6 nM、133.4 nM和109.4 nM。1-Naphthyl PP1是 Src family kinases (v-Src, c-Fyn) 和 the tyrosine kinase c-Abl 的选择性抑制剂， 对于v-Src、c-Fyn、c-Abl、CDK2和CAMK II的IC50值分别为1.0 μM、 0.6 μM、0.6 μM、18 μM 和 22 μM。
S7422	KN-62 KN-62是有效的、特异的CaMKⅡ抑制剂，Ki值为0.9 nM。同时也是一种非竞争性purinergic receptor P2RX7的拮抗剂（IC50=15 nM)。KN-62对CaMKⅡ是高选择性的，相对于对PKA、PKC和MLCK的选择性。同等抑制CaMKI和CaMKIV，抑制CaMK V的Ki值为0.8 μM。	Am J Transplant, 2020, 10.1111/ajt.16071 J Med Chem, 2020, 10.1021/acs.jmedchem.9b01779 Cell Metab, 2019, 29(4):979-992	(F) HEK239 cells were transfected with Flag-Cyclin D1 and Cyclin D1 siRNAs for 12 h, then cells were subjected to immunoblot detection. (G) DIV7 cortical neurons were treated with 10 μM KN62 or 15 μM Ntide and transfected with or without Cyclin D1 siRNAs for 24 h (Left panel), then apoptosis was determined. MW, molecular weight; kDa, kilodalton. All data in this figure represent the means ± SEM of three independent experiments. *P < 0.05.
S7188	CID755673 CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂，IC50值分别为180 nM, 280nM,以及227 nM，选择性比其它CAMKs高大约200倍。	Nat Cell Biol, 2019, 21(6):778-790 Cancer Res, 2018, 78(18):5274-5286 Aging (Albany NY), 2018, 10(12):3736-3744
S6221	Methyl cinnamate Methyl cinnamate 是花椒(Zanthoxylum armatum)的活性成分，是一种广泛使用的具有抗菌和 tyrosinase 抑制剂活性的天然香料化合物。Methyl cinnamate 通过激活3T3-L1前脂肪细胞中的 CaMKK2--AMPK 信号通路来抑制脂肪细胞分化。
S3766	Tanshinone IIA sulfonate (sodium) Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen; a potent negative allosteric modulator of the human purinergic receptor P2X7.

目录号	产品描述	文献引用	实验数据
S1421	Staurosporine Staurosporine (CGP 41251) 是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM作用较弱，对PKCζ (1086 nM)的活性很低。同时 对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。	EMBO J,2020, 39(5):e102608 Genes Dev,2020, 34(7-8):526-543 Cell Rep,2020, 10;30(10):3411-3423 e7
S7436	NH125 NH125 是一种选择性eEF-2 kinase抑制剂，IC50为60 nM,其选择性高于PKC, PKA和CaMKII 125倍 , 同时它也是强效的 histidine kinase 抑制剂。	Acta Pharmacol Sin,2018, 10.1038/s41401-018-0165-9 Drug Des Devel Ther,2018, Drug Des Devel Ther BMC Cancer,2016, 16(1):813	MDA-MB-231 or T47D cells were pretreated with 300 nM NH125 for 1 h, followed by treatment with 8 μM TBMS1 for 24 h. The protein levels were measured by Western blot.
S8274	STO-609 STO-609 是特异性的CaM-KK的抑制剂，抑制CaM-KKα和CaM-KKβ的活性，Ki值分别为80 ng/ml和15 ng/ml，并抑制其自身磷酸化活性。STO-609 可抑制 AMPKK 活性并抑制自噬。	J Neuroinflammation,2020, 17(1):187 FASEB J,2018, 10.1096/fj.201800463 Front Mol Neurosci,2018, 11:98
S6787New	KN-93 KN-93 是一种具有细胞渗透性和竞争性的 Ca2+/calmodulin-dependent protein kinase II (CaMK-II) 的可逆抑制剂，对于兔心肌 CaM 激酶活性的Ki值为2.58 μM。	Clin Exp Pharmacol Physiol,2020, 47(5):848-856
S7423	KN-93 Phosphate KN-93 Phosphate 是一种强效的特异性的Ca2+/calmodulin-dependent protein kinase II (CaMKII)抑制剂，其 Ki 为 0.37 μM,对 APK, PKC, MLCK 或 Ca2+-PDE 没有明显的抑制活性。KN-93 可减弱CaMKII诱导的自噬。	EMBO J,2020, 39(5):e102608 Redox Biol,2020, 28:101381 Free Radic Biol Med,2020, 28;152:336-347	Paeoniflorin (PF) protects the heart against MI-induced injury in DM mice. Heart function was analyzed by measuring fractional shortening {FS = [LV end diastolic diameter (LVEDD)-LVend systolic diameter (LVESD)]×100/LVEDD} and LV ejection fraction [LVEF = (LVEDD2−LVESD2)/LVEDD2].
S2642New	1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1 (1-NA-PP 1)是一种高度选择性的、有效的 pan-PKD 抑制剂，对于PKD1、PKD2和PKD3的IC50值分别为154.6 nM、133.4 nM和109.4 nM。1-Naphthyl PP1是 Src family kinases (v-Src, c-Fyn) 和 the tyrosine kinase c-Abl 的选择性抑制剂， 对于v-Src、c-Fyn、c-Abl、CDK2和CAMK II的IC50值分别为1.0 μM、 0.6 μM、0.6 μM、18 μM 和 22 μM。
S7422	KN-62 KN-62是有效的、特异的CaMKⅡ抑制剂，Ki值为0.9 nM。同时也是一种非竞争性purinergic receptor P2RX7的拮抗剂（IC50=15 nM)。KN-62对CaMKⅡ是高选择性的，相对于对PKA、PKC和MLCK的选择性。同等抑制CaMKI和CaMKIV，抑制CaMK V的Ki值为0.8 μM。	Am J Transplant,2020, 10.1111/ajt.16071 J Med Chem,2020, 10.1021/acs.jmedchem.9b01779 Cell Metab,2019, 29(4):979-992	(F) HEK239 cells were transfected with Flag-Cyclin D1 and Cyclin D1 siRNAs for 12 h, then cells were subjected to immunoblot detection. (G) DIV7 cortical neurons were treated with 10 μM KN62 or 15 μM Ntide and transfected with or without Cyclin D1 siRNAs for 24 h (Left panel), then apoptosis was determined. MW, molecular weight; kDa, kilodalton. All data in this figure represent the means ± SEM of three independent experiments. *P < 0.05.
S7188	CID755673 CID755673是一种具有细胞活性的泛PKD1/2/3抑制剂，IC50值分别为180 nM, 280nM,以及227 nM，选择性比其它CAMKs高大约200倍。	Nat Cell Biol,2019, 21(6):778-790 Cancer Res,2018, 78(18):5274-5286 Aging (Albany NY),2018, 10(12):3736-3744

目录号	产品描述	文献引用	实验数据
S6221	Methyl cinnamate Methyl cinnamate 是花椒(Zanthoxylum armatum)的活性成分，是一种广泛使用的具有抗菌和 tyrosinase 抑制剂活性的天然香料化合物。Methyl cinnamate 通过激活3T3-L1前脂肪细胞中的 CaMKK2--AMPK 信号通路来抑制脂肪细胞分化。

目录号	产品描述	文献引用	实验数据
S3766	Tanshinone IIA sulfonate (sodium) Sodium tanshinone IIA sulfonate (STS) is a water-soluble derivative of tanshinone IIA isolated as the main pharmacologically active natural compound from a traditional Chinese herbal medicine, the dried root of Salvia miltiorrhiza Bunge known as Danshen; a potent negative allosteric modulator of the human purinergic receptor P2X7.