48
1
Cat. No. | Product Name | Target | Signaling Pathways |
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T79125 | Protein kinase inhibitor 5 | Trk receptor | Tyrosine Kinase/Adaptors |
Protein kinase inhibitor 5 作为一种有效的TRK-A抑制剂,其IC50值达到1.8 nM,且能抑制细胞活力。 | |||
T9034 |
MK2-IN-3
MK2 Inhibitor III |
MAPK | MAPK |
MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM),能够抑制 U937 细胞及体内 TNFα 的生成。 | |||
T5508 |
PF-AKT400
(S)-N-[[3-氨基-1-(5-乙基-7H-吡咯并[2,3-D]嘧啶-4-基)吡咯烷-3-基]甲基]-2,4-二氟苯甲酰胺,AKT protein kinase inhibitor |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
PF-AKT400 (AKT protein kinase inhibitor) 是 ATP 竞争性的、选择性的 Akt 抑制剂,对 PKBα(IC50=0.5 nM) 的选择性比 PKA(IC50=450 nM) 高 900 倍。 | |||
T79126 |
Protein kinase inhibitor 5 sulfate hydrate
|
Trk receptor | Tyrosine Kinase/Adaptors |
Protein kinase inhibitor 5 sulfate hydrate 作为TRK-A抑制剂,具有高效性,其IC50值仅为1.8 nM,能有效抑制细胞活力。 | |||
T60109 |
Protein kinase inhibitor H-7
5-(2-methylpiperazine-1-sulfonyl)isoquinoline,蛋白激酶抑制剂H-7,1-(5-Isoquinolinylsulfonyl)-2-methylpiperazine |
PKC | Chromatin/Epigenetic; Cytoskeletal Signaling |
Protein kinase inhibitor H-7 (5-(2-methylpiperazine-1-sulfonyl)isoquinoline) 是有效的蛋白激酶 C (PKC) 和环核苷酸依赖性蛋白激酶抑制剂,抑制 PKC 的 Ki 值为 6 μM。 | |||
T7196 |
HG-10-102-01
[4-[[5-氯-4-(甲基氨基)-2-嘧啶基]氨基]-3-甲氧基苯基]-4-吗啉基甲酮 |
LRRK2 | Autophagy |
HG-10-102-01 是富含亮氨酸重复激酶 2 和突变型G2019S 抑制剂,IC50分别为20.3 nM 和3.2 nM。 | |||
T4489 |
AKT-IN-1
AZD26,AZD-26,6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺,AZD 26 |
Akt | Cytoskeletal Signaling; PI3K/Akt/mTOR signaling |
AKT-IN-1 (AZD-26) 是一种变构的 AKT 抑制剂,其 IC50=1.042 μM。 | |||
T8656 |
CAY10404
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T |
Apoptosis; Akt; COX | Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; PI3K/Akt/mTOR signaling |
CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) 是一种有效且高度选择性的 COX-2 和 COX-1 抑制剂。 它还是 PKB/Akt 和 MAPK 信号通路的有效抑制剂,可诱导 NSC-LC 细胞凋亡,具有镇痛、抗炎和抗癌活性。 | |||
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。 | |||
T2287 |
PIK-75 hydrochloride
PIK-75 HCl,2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐,PIK-75 |
Apoptosis; DNA-PK; PI3K | Apoptosis; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
PIK-75 hydrochloride (PIK-75 HCl) 是一种可逆的 DNA-PK 和 p110α-选择性抑制剂,抑制 DNA-PK,p110α和 p110γ,可诱导凋亡。 | |||
T6747 |
8-Bromo-cAMP sodium salt
8-Br-Camp sodium salt,8-溴腺苷-3',5'-环单磷酸钠,8-Bromo-cAMP(sodium salt),8-Bromo-cAMP |
PKA | Tyrosine Kinase/Adaptors |
8-Bromo-cAMP sodium salt (8-Br-Camp sodium salt) 是一种环 AMP 依赖性蛋白激酶 (PKA) 激活剂,是一种环 AMP 类似物。 | |||
T62684 |
Lartesertib
ATM Inhibitor-5,M4076 |
ATM/ATR | DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling |
Lartesertib (ATM Inhibitor-5) 是一种丝氨酸/苏氨酸蛋白激酶 ATM 的抑制剂,具有潜在的抗癌活性,可用于研究肺癌。 | |||
T10727 |
Cdc7-IN-5
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CDK | Cell Cycle/Checkpoint |
Cdc7-IN-5 是一种有效的 Cdc7 激酶抑制剂。Cdc7 是一种丝氨酸苏氨酸蛋白激酶酶,在细胞周期中对 DNA 复制的启动至关重要。 | |||
T77570 |
AP-C2
|
PKA | Tyrosine Kinase/Adaptors |
AP-C2 是一种有效的小分子鸟苷 3',5'-环单磷酸 (cGMP) 依赖性蛋白激酶 II (cGKII) 抑制剂,对 cGKII 的 pIC50 为 5.2。 | |||
T6250 |
H-89 dihydrochloride
Protein kinase inhibitor H-89 dihydrochloride,H 89 2HCl,5-Isoquinolinesulfonamide |
PKA; S6 Kinase; Autophagy | Autophagy; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
H-89 dihydrochloride (5-Isoquinolinesulfonamide) 是一种选择性 cAMP 依赖性蛋白激酶A(PKA) 抑制剂,IC50值为 48 nM。也可轻微抑制 PKG、PKC 和酪蛋白激酶活性。 | |||
T9609 |
GRK5-IN-2
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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。 | |||
TP1897L1 |
JIP-1 (153-163) acetate(438567-88-5 free base)
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JNK | MAPK |
JIP-1 (153-163) acetate(438567-88-5 free base) 是c-Jun N-末端激酶 (JNK) 的肽抑制剂,基于 JNK-interacting protein-1 (JIP-1) 的残基 153-163。以微摩尔范围内的亲和力与 JNK 结合,并抑制 p38 和 ERK。 | |||
T72322 |
R 59-022 hydrochloride
DKGI-I hydrochloride,Diacylglycerol kinase inhibitor I hydrochloride,DKGI-I hydrochloride ; Diacylglycerol kinase inhibitor I hydrochloride |
5-HT Receptor; PKC | Chromatin/Epigenetic; Cytoskeletal Signaling; GPCR/G Protein; Neuroscience |
R 59-022 hydrochloride (DKGI-I hydrochloride) 是一种 5-HT Receptor 拮抗剂,可激活蛋白激酶 C (PKC)。R 59-022 hydrochloride 是一种 DGK 抑制剂 (IC50:2.8 µM),可抑制 OAG 磷酸化为 OAPA。R 59-022 增强血小板中凝血酶诱导的甘油二酯的产生,并抑制嗜中性粒细胞中磷脂酸的产生。 | |||
T27416 |
GLPG0259
GLPG-0259,GLPG 0259 |
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GLPG-0259 is an inhibitor of mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5). | |||
T71274 |
GLPG0259 A
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GLPG0259 A is a small-molecule inhibitor of mitogen-activated protein kinase-activated protein kinase 5 (MAPKAPK5), a kinase enzyme that plays a role in important inflammatory pathways. | |||
T75739 |
PKI(5-24) TFA
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PKI(5-24) TFA 是一种强效、竞争性、合成的PKA(cAMP 依赖性蛋白激酶) 抑制剂,Ki 为 2.3 nM。PKI(5-24) TFA 对应于天然存在的热稳定蛋白激酶抑制剂中的 5-24 残基。 | |||
T16709 |
R 59-022
Diacylglycerol kinase inhibitor I,DKGI-I |
Others | Others |
R 59-022 is a 5-HTR antagonist and activates protein kinase C (PKC). R 59-022 is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neu | |||
T82258 |
GRL018-21
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GRL018-21为一种高效、高选择性G蛋白偶联受体激酶5 (GRK5) 抑制剂,其IC50值仅为10 nM。 | |||
T36019 |
PKA Inhibitor (5-24) (trifluoroacetate salt)
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PKI PKA Inhibitor (5-24) is a synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase) (Ki= 2.3 nM) derived from the active site of the skeletal muscle inhibitor protein.1It mimics the protein substrate by binding to the catalytic site through the arginine-cluster basic subsite.1The prominent enzyme-substrate interaction site occurs where PKA catalytic subunit residues Tyr235and Phe239form a sandwich-like structure with residue Phe10of PKI (5-24).2 | |||
T40395 |
ζ-Stat trisodium
NSC37044 trisodium,ζ-Stat trisodium |
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ζ-Stat trisodium (NSC37044 trisodium) is a potent and selective inhibitor of protein kinase C-ζ (PKC-ζ), exhibiting an IC50 of 5 μM. It effectively suppresses the proliferation of melanoma cell lines and promotes apoptosis. Moreover, ζ-Stat trisodium demonstrates notable antitumor activity in vitro. | |||
T83640 |
RIPK2-IN-5
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RIP kinase | Apoptosis; NF-κB |
RIPK2-IN-5 是一种受体相互作用蛋白激酶 2 (RIPK2) 抑制剂,具有潜在的抗炎活性,可用于研究免疫功能异常引起的疾病。 | |||
T64116 | B-Raf IN 5 | ||
B-Raf IN 5 是蛋白激酶 B-Raf 的有效抑制剂 (IC50: 2.0 nM)。B-Raf IN 5 可抵抗快速代谢,切不结合二级靶点 PXR。B-Raf IN 5 对癌症疾病表现出研究潜力。 | |||
T76399 |
PKI(5-22)amide
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PKI(5-22)amide 是环 AMP 依赖性蛋白激酶 (PKA) 抑制剂的活性片段。PKI(5-22)amide 抑制PKA 激活,但不能减弱 CRF1 受体的同源脱敏作用。 | |||
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。 | |||
T63008 | PERK-IN-5 | ||
PERK-IN-5 是一种高度选择性的、高效的、口服具有活力的蛋白激酶 R 样内质网 (ER) 激酶 (PERK) 抑制剂,能够作用于 PERK (IC50: 2 nM) 与 p-eIF2α (IC50: 9 nM)。在 786-O 肾细胞癌异种移植瘤模型中,PERK-IN-5 可以明显抑制肿瘤生长。 | |||
T74374 |
ERK1/2 inhibitor 4
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ERK1/2 inhibitor 5 是一种有效的ERK1/2抑制剂。丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中起着极其重要的作用,而细胞外信号调节激酶 (ERK) 是MAPK 家族的成员。ERK1/2 inhibitor 5 具有研究或预防癌症、炎症或其他增殖性疾病的潜力。 | |||
T63340 |
CCG-273220
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CCG-273220 是 G 蛋白偶联受体 (GPCR) 激酶 5 (GRK5) 共价抑制剂 (IC50: 220 nM)。CCG-273220 可以共价结合GRK5亚家族特异性残基 Cys474 ,而对GRK5的选择性比 GRK2 高。 | |||
T76482 |
PKI (5-24),amide
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PKI (5-24),amide (IP20-amide)为对应于cAMP依赖性蛋白激酶热稳定抑制蛋白活性部分的20残基肽。该化合物是一种高效的cAMP依赖性蛋白激酶(PKA)抑制剂,具有2.3 nM的Ki值。 | |||
T82990 |
AP-C4
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AP-C4是cGMP依赖性蛋白激酶II(cGKII)的抑制剂,具有pIC50值为5.2,但不影响cGKII依赖性阴离子分泌。 | |||
T35541 |
Lipoxygenin
|
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Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin... | |||
T35827 |
Epsilon-V1-2
PKCε Inhibitor Peptide,Protein Kinase Cɛ Inhibitor Peptide,ɛV1-2 |
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Protein kinase C (PKC ) is a calcium-independent, phospholipid- and diacylglycerol-dependent serine/threonine kinase involved in diverse signaling pathways, including those involved in neuronal signaling, cytoskeletal function, and inflammation.[1] PKC inhibitor peptide is a synthetic peptide corresponding to an amino acid sequence found in the amino terminal C2 domain of most mammalian forms of PKC .[2] It selectively and reversibly inhibits the translocation of PKC to intracellular membrane... | |||
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。 | |||
T82991 |
AP-C3
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AP-C3为cGMP依赖性蛋白激酶II (cGKII) 的有效抑制剂,其pIC50值为6.3。该化合物仅对cGKII依赖性阴离子分泌表现出微弱的抑制作用。 | |||
T61693 |
AAK1-IN-5
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AAK1-IN-5 is a potent and specific inhibitor of adaptor protein-2-associated kinase 1 (AAK1), characterized by its ability to penetrate the central nervous system and its oral bioavailability. It displays high selectivity, with an AAK1 inhibitory potency (IC 50) of 1.2 nM, a binding affinity (K i) of 0.05 nM, and an inhibitory potency against cellular AAK1 activity (cell IC 50) of 0.5 nM. AAK1-IN-5 holds promise for investigating neuropathic pain in scientific research [1]. | |||
T63057 |
LRRK2-IN-5
|
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LRRK2-IN-5 (compound 25) 是一种口服具有活力的、能透过血脑屏障的、选择性富含亮氨酸重复蛋白激酶 2 基因 (LRRK2) 抑制剂,对 GS LRRK2 (IC50: 1.2 μM) 和 WT LRRK2 (IC50: 16 μM) 具有抑制作用。LRRK2-IN-5 能够抑制 LRRK2 Ser1292 和 Ser925 的自磷酸化。 | |||
T63923 |
ATR-IN-5
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ATR-IN-5 是 ATR 的有效抑制剂。其中 ATR 是 PIKK 家族的成员,是一类参与基因组稳定性和 DNA 损伤修复的蛋白激酶。ATR-IN-5 对 ATR 激酶介导的疾病如增殖性疾病和癌症表现出研究潜力。 | |||
T82989 |
AP-C6
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AP-C6 是一种有效的 cGMP 依赖性蛋白激酶 II (cGKII) 抑制剂,其 pIC50 值为 6.5。该化合物能够在体外浓度依赖性地抑制人 cGKII 的活性,并能够通过抑制 PDE 来增强 cAMP 信号传导。 | |||
T83670 |
F1 TFA
Tat-IKIP (46-60),Tat-Inhibitor of NF-κB Kinase-interacting Peptide |
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F1是一种抗炎肽,由HIV-1 Tat蛋白质转导域与对应于抑制因子NF-κB激酶-相互作用肽(IKIP)46-60残基的15氨基酸肽链接而成。在5 µM浓度下,F1抑制了小鼠腹腔巨噬细胞中LPS诱导的IκB激酶α(IKKα)和IKKβ的磷酸化以及NF-κB(p65)的核内转移。在体内,F1(5 mg/kg)降低了LPS诱导的脓毒症小鼠模型中IL-6、TNF-α和IL-1β的血清水平,并增加了生存率。 | |||
T64266 | KR-39038 | ||
KR-39038 是一种口服具有活力的 GRK5 (G 蛋白偶联受体激酶 5) 抑制剂 (IC50: 0.02 μM)。KR-39038 能够抑制新生儿心肌细胞的 HDAC5 通路,明显抑制血管紧张素 II 诱导的细胞肥大,具有显著的抗心肌肥厚和改善心功能作用。KR-39038 能够用于进行心力衰竭的研究。 | |||
T82243 |
hAChE-IN-5
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GSK-3 | PI3K/Akt/mTOR signaling; Stem Cells |
hAChE-IN-5(化合物49)是一种同时针对hAChE和hBuChE的有效抑制剂,其IC50值均为0.17 μM。此外,hAChE-IN-5对GSK3β同样展现出良好的抑制活性,IC50值为0.21 μM。作为tau蛋白聚集和Aβ1-42自聚集的抑制剂,hAChE-IN-5能够结合PAS,进而阻止Aβ依赖的神经毒性。其能穿透血脑屏障(BBB),显示出成为多靶点抗阿尔茨海默病药物研究的潜力。 | |||
T36650 |
Ansatrienin B
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Ansatrienin B is an ansamycin antibiotic and antifungal agent first isolated from S. collinus and S. rishiriensis., In fetal rat long bones, it is an inhibitor of parathyroid hormone-induced calcium release (IC50 = 21 nM), which is a measure of bone resorption, and pp60c-src kinase (IC50 = 50 nM). It is an inhibitor of translation at the protein synthesis stage by specific inhibition of L-leucine incorporation (IC50 = 58 nM in A549 cells). It also inhibits TNF-α-induced expression of intercellul... | |||
T38269 | Purfalcamine | ||
Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, paras... | |||
T37590 |
ML 3403
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p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively). Laufer et al (2003) Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J.Med.Chem. 46 3230 PMID:12852754 |Kammerer et al (2007) Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T5736 |
1,3-Dicaffeoylquinic acid
CYNARIN,1,3-二咖啡酰奎宁酸,Cyclohexanecarboxylic acid, 1,3-bis[[3-(3,4-dihydroxyphenyl)-1-oxo-2-propen-1-yl]oxy]-4,5-dihydroxy-, (1S,3R,4R,5R)-,1,3-O-Dicaffeoylquinic acid,1,5-Dicaffeoylquinic acid |
Reactive Oxygen Species; Akt; PI3K | Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; NF-κB; PI3K/Akt/mTOR signaling |
1,3-Dicaffeoylquinic acid (CYNARIN) 是一种咖啡酰奎宁酸衍生物,具有抗氧化、自由基清除作用。 |