58
6
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP1271L |
Calmodulin-Dependent Protein Kinase II 290-309 acetate
Calmodulin-Dependent Protein Kinase II 290-309 acetate (115044-69-4 Free base) |
CaMK | Neuroscience |
Calmodulin-Dependent Protein Kinase II 290-309 acetate 是 Ca2+/calmodulin-dependent protein kinase II 的有效拮抗剂(IC50 = 52 nM)。 | |||
T14860 |
CaMKII-IN-1
|
CaMK; Autophagy | Autophagy; Neuroscience |
CaMKII-IN-1是高效的 CaMKII 选择性抑制剂,IC50为63nM,对 CaMKIV, MLCK, p38a, Akt1,和 PKC 这些靶点几乎无作用。 | |||
T2697 |
KN-93
|
CaMK; Autophagy | Autophagy; Neuroscience |
KN-93是 Ca2+/钙调蛋白依赖性激酶 II (CaMKII) 的选择性抑制剂,Ki 为370 nM,可竞争性阻断 CaM 与激酶的结合。 | |||
TP2310 |
Autocamtide-2-related inhibitory peptide
|
CaMK; Autophagy | Autophagy; Neuroscience |
Autocamtide-2-related inhibitory peptide 是一种高度特异性和有效的 CaMKII 抑制剂,IC50 为 40 nM。 | |||
T6605 |
NH125
|
CaMK; Virus Protease; PKA; Antibacterial; PKC; Autophagy; Antifungal | Autophagy; Chromatin/Epigenetic; Cytoskeletal Signaling; Microbiology/Virology; Neuroscience; Tyrosine Kinase/Adaptors |
NH125 是一种真核延长因子 2 激酶(eEF-2K/CaMKIII)的高效选择性抑制剂,诱导 eEF2 磷酸化,对 eEF-2K 作用的 IC50值为 60 nM。 | |||
TP1271 |
Calmodulin-Dependent Protein Kinase II (290-309)
Calmodulin-Dependent Protein Kinase II(290-309) |
||
Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II. | |||
TQ0137 |
A-484954
A 484954 |
CaMK; Parasite; Autophagy | Autophagy; Microbiology/Virology; Neuroscience |
A-484954 (A 484954) 是一种高度特异性的真核延伸因子-2 抑制剂,其 IC50值为 280 nM。 | |||
TP1716 |
Calmodulin-Dependent Protein Kinase II (281-309)
Calmodulin-Dependent Protein Kinase II 281-309 |
||
Calmodulin-Dependent Protein Kinase II (281-309) is a synthetic peptide that can be phosphorylated at Thr286 by PKC and inhibits CaM kinase II (IC50 = 80 nM). | |||
T2694 |
KN-62
|
CaMK; P2X Receptor; Autophagy | Autophagy; Membrane transporter/Ion channel; Neuroscience |
KN-62 是一种选择性的、可逆的钙调蛋白依赖性蛋白激酶 II (CaMK-II) 抑制剂,直接与 CaMK-II 酶的钙调蛋白结合位点结合,对大鼠脑 CaMK-II 的IC50值为 0.9 μM。它是非竞争性的P2X7受体拮抗剂,IC50约为 15 nM。 | |||
T3546 |
STO-609
STO 609 |
CaMK; AMPK; Autophagy | Autophagy; Chromatin/Epigenetic; Neuroscience; PI3K/Akt/mTOR signaling |
STO-609 是一种特异性和细胞渗透性的 Ca2+/钙调蛋白依赖性蛋白激酶激酶抑制剂,用于重组 CaM-KKα 和 CaM-KKβ,Ki 值分别为 80 和 15 ng/mL。它抑制 Hela 细胞溶解物中的 AMP 活化蛋白激酶激酶活性,IC50值约为 0.02 g/ml。 | |||
T14069 |
A-3 hydrochloride
|
CaMK; Casein Kinase; PKA; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism; Neuroscience; Stem Cells; Tyrosine Kinase/Adaptors |
A-3 hydrochloride 是一种细胞可渗透的、可逆的、ATP 竞争性非选择性拮抗剂。它抑制 PKA 、酪蛋白激酶 II 和肌球蛋白轻链激酶,Ki 值分别为4.3 µM、5.1 µM 和7.4 µM。它还抑制 PKC 和酪蛋白激酶 I 的活性,Ki 分别为 47 µM 和 80 µM。 | |||
T10667 |
Calmidazolium chloride
R 24571,钙调蛋白抑制剂 |
CaMK; Autophagy | Autophagy; Neuroscience |
Calmidazolium chloride (R 24571) 是一种钙调蛋白拮抗剂,对CaM 依赖性磷酸二酯酶和钙调蛋白诱导的红细胞Ca2+转运ATP 酶活化有拮抗作用,IC50分别为0.15和0.35 μM。Calmidazolium chloride 结合CaMK 的Kd 值为3 nM。Calmidazolium chloride 在抗癌领域有研究的价值。 | |||
T4185 |
lavendustin C
HDBA,NSC 666251,N-(2,5-二羟基苄基)-5-氨基水杨酸 |
CaMK; EGFR; Tyrosinase; Src | Angiogenesis; JAK/STAT signaling; Neuroscience; Proteases/Proteasome; Tyrosine Kinase/Adaptors |
lavendustin C (NSC 666251) 是 Ca2+钙调蛋白依赖性激酶 II 抑制剂,IC50为 0.2 µM。它抑制 EGFR 相关酪氨酸激酶和 pp60c-src(+)激酶,IC50分别为 0.012 和 0.5 µM。 | |||
T8389 |
Trifluoperazine
三氟拉嗪,trifluoroperazine |
CaMK; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; P-gp; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Trifluoperazine (trifluoroperazine) 是一种多巴胺 D2 受体抑制剂,可治疗精神分裂症。它是NUPR1抑制剂,具有抗癌活性。它是α1-adrenergic 受体拮抗剂,是流感病毒形态发生的可逆抑制剂。 | |||
T1222 |
Trifluoperazine dihydrochloride
Trifluoperazine 2HCl,盐酸三氟拉嗪,SKF5019,Urinox |
CaMK; Dopamine Receptor; Influenza Virus; Adrenergic Receptor; P-gp; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience |
Trifluoperazine dihydrochloride (SKF5019) 是一种抗精神病药物,靶向中枢多巴胺受体。它是流感病毒形态发生的可逆抑制剂,是NUPR1抑制剂,具有抗癌活性。它是钙调蛋白抑制剂,还可抑制 P-糖蛋白,可研究精神分裂症。 | |||
T76488 |
Calmodulin Dependent Protein Kinase Substrate
|
||
CalmodulinDependent Protein Kinase Substrate 为Ca2+及钙调蛋白(CaM)依赖的CaMK底物肽,属合成肽底物类。 | |||
T75959 |
Calmodulin-Dependent Protein Kinase II(290-309) acetate
|
||
Calmodulin-Dependent Protein Kinase II (290-309) acetate 是有效的 CaMK 拮抗剂, 抑制抑制 Ca2+/钙调蛋白依赖性蛋白激酶II 的IC50值为52 nM。 | |||
T76487 |
Calmodulin Dependent Protein Kinase Substrate Analog
|
||
CalmodulinDependent Protein Kinase Substrate Analog 是一种 Ca2+- 和钙调蛋白 (CaM) 依赖性蛋白激酶 (CaMK) 底物肽。CalmodulinDependent Protein Kinase Substrate Analog 是一种合成蛋白激酶的肽底物。 | |||
T20792 |
W-7 hydrochloride
N-(6-氨基己基)-5-氯-1-萘磺胺盐酸盐,W 7 HCl,W7 HCl,W-7 HCl |
CaMK; Apoptosis; Myosin; PDE | Apoptosis; Cytoskeletal Signaling; Metabolism; Neuroscience |
W-7 hydrochloride (W-7 HCl) 是一种选择性的钙调蛋白拮抗剂。它抑制Ca2+-钙调蛋白依赖性磷酸二酯酶和肌球蛋白轻链激酶,IC50值分别为 28 μM 和 51 μM。它可诱导细胞凋亡,具有抗癌活性。 | |||
TP1403L |
Syntide 2 acetate(108334-68-5 free base)
|
CaMK | Neuroscience |
Syntide 2 acetate(108334-68-5 free base) 是一种合成肽,被 Ca2+/钙调蛋白依赖性蛋白激酶 II (CaMKII; Km = 12 µM) 识别为底物。 | |||
TP1217L |
Autocamtide 2 TFA(129198-88-5 free base)
|
CaMK | Neuroscience |
Autocamtide 2 TFA(129198-88-5 free base) 是钙/钙调蛋白依赖性蛋白激酶 II (CaMKII) 的高选择性肽底物。 Autocamtide 2 TFA 可用于 CaMKII 活性测定。 | |||
T68162 |
Tiflucarbine
Tiflucarbina |
5-HT Receptor; PDE | GPCR/G Protein; Metabolism; Neuroscience |
Tiflucarbine 是一种潜在的非选择性5-HT激动剂,具有抗抑郁活性。Tiflucarbine 剂量依赖性的增加了大鼠脑中可溶性钙调蛋白(CaM)依赖性磷酸二酯酶的比活性。 | |||
T4530 |
KN-92 phosphate
KN-92 磷酸盐,KN92-H3PO4 |
CaMK | Neuroscience |
KN-92 phosphate (KN92-H3PO4) 是 KN-93 的非活性衍生物,不能抑制 CaM 激酶活性。它可作为阐明 KN-93 的拮抗活性的对照化合物。KN-93 能够渗透细胞,是一种可逆的 CaMKII 竞争性抑制剂。 | |||
T8543 |
KN-92 hydrochloride
|
CaMK | Neuroscience |
KN-92 hydrochloride 是 KN-93 的非活性衍生物,对 CaM 激酶无抑制作用。它可作为对照化合物用于阐明 KN-93 的拮抗活性。KN-93 是一种可渗透细胞的、可逆的、竞争性的 CaMKII 抑制剂。 | |||
T68064 |
Elziverine
|
CaMK | Neuroscience |
Elziverine是一种可口服的小分子钙调蛋白拮抗剂。Elziverine体外处理以浓度依赖性方式抑制了SHRSP,WKY和Wistar大鼠中Ca负载诱导的棘皮细胞形成。Elziverine可用于治疗神经疾病,可用于研究认知障碍。 | |||
TP1909L1 |
CALP2 acetate(261969-04-4 free base)
|
CaMK; PDE | Metabolism; Neuroscience |
CALP2 acetate 是一种钙调蛋白拮抗剂,对与 CaM EF-hand/Ca2+-结合位点具有高亲和力,Kd 为 7.9 µM。它有效抑制粘附和脱粒。它也是肺泡巨噬细胞的强激活剂。它抑制 CaM 依赖性磷酸二酯酶活性并增加细胞内 Ca2+ 浓度。 | |||
TP1910L1 |
CALP1 acetate
CALP1 acetate(145224-99-3 free base) |
CaMK | Neuroscience |
CALP1 acetate 是一种钙调蛋白 (CaM) 激动剂(Kd 为 88 µM),可与 CaM EF-hand/Ca2+ 结合位点结合。 CALP1 通过抑制钙通道的开放来阻断钙流入和细胞凋亡(IC50 为 44.78 µM)。 CALP1 阻断谷氨酸受体通道并阻断储存操作的非选择性阳离子通道。 CALP1 激活依赖于 CaM 的磷酸二酯酶活性。 | |||
T2170 |
SKF-96365 hydrochloride
1-[2-(4-甲氧基)-2-[3-(4-甲氧基苯基)丙氧基]乙基]咪唑,SKF96365 |
Apoptosis; Potassium Channel; Calcium Channel; TRP/TRPV Channel; Autophagy | Apoptosis; Autophagy; Membrane transporter/Ion channel; Metabolism |
SKF-96365 hydrochloride (SKF96365) 是store-operated Ca2+entry 抑制剂,也是TRP channel 阻滞剂。它显著抑制豚鼠离体心脏 hERG、hKCNQ1/hKCNE1、hKir2.1 和 hKv4.3 电流,延长QTc 间期。它通过诱导结直肠癌细胞的细胞周期阻滞和凋亡起抗肿瘤作用。 | |||
T16752 |
Rimacalib
SMP 114 |
CaMK | Neuroscience |
Rimacalib is an inhibitor of Ca2+/calmodulin-dependent protein kinase II (IC50s: ~1 μM for CaMKIIα and ~30 μM for CaMKIIγ). | |||
T26973 |
Cefatrizine
Cephatriazine,BL-S-640,BLS640,S 640P,BL S 640 |
||
Cefatrizine is an inhibitor of eukaryotic elongation factor-2 kinase, a unique calcium/calmodulin-dependent protein kinase, is well known to regulate apoptosis, autophagy and ER stress in many types of human cancers. | |||
T32348 |
K 259-3
K2593 |
||
K 259-3 是 K 259-2 的甲酯,是钙调素依赖性环核苷酸磷酸二酯酶的抑制剂。 | |||
TP1403 |
Syntide 2
|
||
Syntide-2 is a synthetic peptide recognized as a substrate by Ca2+/calmodulin-dependent protein kinase II (CaMKII; Km = 12 µM). | |||
T71530 |
K252d
|
||
K252d is an indolocarbazole alkaloid found in Nocardiopsis. It is a PKC inhibitor that inhibits PKC isolated from rat brain, as well as, calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart. | |||
T27032 |
CK59
CK-59,CK 59 |
||
CK59 is a reversible inhibitor of calcium-calmodulin-dependent kinase II (CaMKII). CK59 inhibits multiple voltage-gated calcium channels, including the L-type channel during depolarization in a dose-dependent manner. The IC50 for CK59 was approximately 50 | |||
TP2054 |
Calcineurin Autoinhibitory Peptide
|
||
Selective inhibitor of Ca2+-calmodulin-dependent protein phosphatase (calcineurin) (IC50 ~ 10 μM). Does not inhibit PP1, PP2A or CaM kinase II (IC50 > 100 mM). | |||
TP1217 |
Autocamtide 2
Autocamtide II |
||
Autocamtide-2 is a highly selective peptide substrate for calcium/calmodulin-dependent protein kinase II (CaMKII), which belongs to the CAMK Ser/Thr protein kinase family. | |||
T76408 |
Autocamtide-3
|
||
Autocamtide-3, 含Thr287的13个氨基酸组成的多肽,为CaMKII(Ca2+/钙调蛋白依赖性激酶 II) (CaMK) 的选择性底物。 | |||
T21557 |
KN-93 hydrochloride
|
||
KN-93 hydrochloride 是一种具有细胞渗透性,可逆和竞争性的钙调蛋白依赖性激酶II 型 (CaMKII) 抑制剂,Ki 为370 nM。 | |||
TP1829 |
Autocamtide 2, amide
|
||
Autocamtide 2, amide is a substrate (100 μM final concentration) for CaMK family assays.Autocamtide-2 Peptide is a highly selective peptide substrate for calcium/calmodulin-dependent protein kinase II (CaMKII), a member of the CAMK Ser/Thr protein kinase | |||
T75315 | Phenacaine | ||
Phenacaine (Holocaine)为一种局部麻醉剂,能够在大脑及心脏红细胞中抑制特定的钙调素依赖性Ca2+-ATP酶与环核苷酸磷酸二酯酶刺激产生。 | |||
T3650 |
STO-609 acetate
|
CaMK | Neuroscience |
STO-609 acetate 是选择性的、细胞可渗透的 Ca2+-钙调蛋白依赖性蛋白激酶激酶抑制剂(Ki:80/15 ng/ml,对于 CaM-KKα/KKβ);竞争 ATP 结合位点。它比 CaMK1/2/4、PKC、MLCK、PKA 和 p42 MAPK 显示 > 80 倍的选择性。 | |||
T60515 | CaMKIIα-IN-1 | ||
CaMKIIα-IN-1 (Compound 4d) 是一种具有口服活性的 Ca 2+/钙调素依赖性蛋白激酶 II α (CaMKIIα) 抑制剂。CaMKIIα-IN-1对 CaMKIIα WT hub 的 Kd 值为 219 nM。CaMKIIα-IN-1 表现出良好的代谢稳定性。 | |||
T75754 |
Syntide 2 TFA
|
||
Syntide 2 (TFA) 是一种由Ca2+和钙调蛋白 (CaM) 依赖的蛋白激酶 II (CaMKII) 特异性识别的底物肽,它通过选择性地抑制赤霉素 (GA) 反应而不影响组成和脱落酸的调节事件。 | |||
T75864 |
Calcineurin autoinhibitory peptide TFA
|
||
Calcineurin autoinhibitory peptide TFA 为选择性Ca2+/钙调蛋白依赖性蛋白磷酸酶(钙调神经磷酸酶)抑制剂,IC50约为10 μM。该化合物能够保护神经元不受兴奋性神经元死亡影响。 | |||
TP1910 |
CALP1
|
||
Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit | |||
T83684 |
Myelin Basic Protein Peptide (mouse, bovine) TFA
Gln-Lys-Arg-Pro-Ser-Gln-Arg-Ser-Lys-Tyr-Leu,MBP Peptide |
||
Myelin基础蛋白(MBP)肽是PKC的肽底物,相比PKA、酪蛋白激酶1(CK1)、CK2、磷酸化酶激酶及钙/钙调蛋白依赖性蛋白激酶(CaMKII),它对PKC有选择性。MBP肽已用于监测原发性人类肾动脉平滑肌细胞中的PKC活性。 | |||
T83740 |
Ziptide TFA
|
||
Ziptide是多种丝氨酸/苏氨酸蛋白激酶的肽底物,包括MAPK激活蛋白激酶2(MAPKAPK2)、MAPKAPK3、MAPKAPK5、checkpoint kinase 1(Chk1)、AMP激活蛋白激酶(AMPK)和钙/钙调蛋白依赖型蛋白激酶II(CamKII)。它被用来评估CamKII活性以用于抑制剂的开发。 | |||
T37969 |
12(S)-HpETE
|
||
12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LO, resulting in the synthesis of 5(S)-HETE, leukotriene B4 (LTB4), and 5(S),12(S)-DiHETE. Rat lung metabolizes 12(S)-HpETE to 8,11,12- and 10,11,12-trihydroxyeicostrienoic acids. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and e... | |||
T80269 |
AC3-I, myristoylated
Autocamtide-3 Derived Inhibitory Peptide |
CaMK | Neuroscience |
AC3-I, myristoylated 为一种具有高度特异性的 CaMKII 抑制剂,为 Autocamtide-3 衍生的生物活性肽。通过将 Autocamtide-3 中的 Thr-9 磷酸化位点替换为 Ala,赋予该肽抗蛋白水解能力,从而制备出该肉豆蔻酰化形式。 | |||
T78154 |
CS640
|
||
CS640是一种钙调蛋白依赖性激酶选择性抑制剂,对CaMK1D、CaMK1B、CaMK1A、CaMK1G、PIP5K1C、MEK5、RIPK4和MLK3的抑制作用的IC50值分别为0.08、0.03、0.001、0.001、11.2、0.025、5.69和2.75μM。此外,CS640对CYP450 2C9和CYP450 2C19的IC50值分别为6和10μM。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2144 |
Tacrolimus
他克莫司,Fujimycin,FK506,FR900506 |
Phosphatase; Others; Antibacterial; Antibiotic; mTOR; Autophagy | Autophagy; Metabolism; Microbiology/Virology; Others; PI3K/Akt/mTOR signaling |
Tacrolimus (Fujimycin) 可与 FKBP12 结合形成高亲和力复合物 (Ki: 0.2 nM),抑制钙/钙调蛋白依赖性蛋白磷酸酶的活性。 | |||
T3904 |
Gomisin J
|
Calcium Channel; AMPK | Chromatin/Epigenetic; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling |
Gomisin J 是在五味子中发现的小分子量木脂素,具有血管舒张活性,在非酒精性脂肪性肝病方面有研究潜力。 它通过激活 AMPK、LKB1 和 Ca2+/钙调蛋白依赖性蛋白激酶 II 以及抑制 HepG2 细胞中的胎球蛋白 A 来调节脂肪生成酶和脂肪分解酶以及炎症分子的表达,从而抑制脂质积累。 | |||
T3826 |
Polygalasaponin F
异牡荆苷,瓜子金皂苷己 |
NF-κB; TLR; Akt; PI3K | Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; PI3K/Akt/mTOR signaling |
Polygalasaponin F 是从瓜子金中提取的齐墩果烷型三萜皂苷,可通过调节TLR4-PI3K/AKT-NF-kB 信号通路减少神经炎症细胞因子的分泌,能降低炎性细胞因子肿瘤坏死因子 α 的释放。 | |||
T70221 |
Dibefurin
|
||
Dibefurin is a metabolite that inhibits the activity of calcineurin, a calcium/calmodulin-dependent protein phosphatase involved in the activation of T lymphocytes. | |||
T15636 |
K-252a
Antibiotic K 252a,Antibiotic SF 2370,SF2370 |
Others | Others |
K-252a is a staurosporine analog isolated from Nocardiopsis sp. soil fungi. K-252a inhibits protein kinase (IC50: 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively). | |||
TN4551 | Methyl orsellinate | Phosphatase; cAMP; Antifection | GPCR/G Protein; Metabolism; Microbiology/Virology |
Methyl orsellinate is a phytotoxic compound, it exhibits antifungal activity, it can cause significant inhibition of radicle growth of Amaranthus hypochondriacus and Echinochloa crus-galli, interact with bovine-brain calmodulin and inhibit the activation of the calmodulin-dependent enzyme cAMP phosphodiesterase. Methyl orsellinate can inhibit PTP1B activity with 50% inhibitory concentration values of 277 +/- 8.6 microM, the selective inhibition of PTP1B has been widely recognized as a potential ... |