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27

抑制剂 & 化合物

6

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9779 Protein kinase inhibitor 6

Protein kinase inhibitor 6 是一种蛋白激酶抑制剂。
T2458 CID755673

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
CID755673是一种高效选择性 PKD1抑制剂,IC50为182 nM。
T1863 CID 2011756

CID2011756,CID-2011756

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
CID 2011756 是一种具有抗肿瘤活性的ATP 竞争性广谱PKD 抑制剂,对 PKD1 的IC50值为 3.2 µM,在细胞中对 PKD2 和 PKD3 的IC50值分别为 0.6 和 0.7 µM。
T2062 kb NB 142-70

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
kb NB 142-70 是一种PKD 有效抑制剂,具有抗肿瘤活性,对 PKD1、PKD2 和 PKD3 的IC50值分别为 28.3 nM、58.7 nM 和 53.2 nM。
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。
T6440 CGP 57380

N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺,MNK1 Inhibitor

Apoptosis; MNK Apoptosis; MAPK
CGP 57380 (MNK1 Inhibitor) 是细胞渗透的吡唑-嘧啶类化合物,是一种具有选择性的Mnk1抑制剂,IC50值为 2.2 μM。
T61163 Protein kinase D inhibitor 1

Protein kinase D inhibitor 1 (compound 17m) is a potent pan-PKD inhibitor. It exhibits inhibitory activity in the low nanomolar range, with IC50 values ranging between 17 and 35 nM. By inhibiting protein kinase D, this compound effectively suppresses cortactin phosphorylation, which is known to be PKD-dependent [1].
T2492 Perifosine

NSC 639966,D21266,KRX-0401,哌立福新

Apoptosis; Akt; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
Perifosine (KRX-0401) 是一种具有口服活性的烷基磷酸胆碱 Akt 抑制剂,具有抗肿瘤活性。
TQ0104 CRT0066101 dihydrochloride

CRT0066101二盐酸盐

Serine/threonin kinase Cell Cycle/Checkpoint; Metabolism
CRT0066101 dihydrochloride 是一种选择性PKD 有效抑制剂,对PKD1、2和3的IC50值分别为1、2.5和2 nM。
T13017 STL127705

Compound L,7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione

DNA-PK; Others DNA Damage/DNA Repair; Others; PI3K/Akt/mTOR signaling
STL127705 (Compound L) 是一种有效的 Ku 70/80 异二聚体蛋白抑制剂,抑制 Ku70/80-DNA 相互作用,IC50 为 3.5 μM。 它抑制 Ku 依赖性 DNA-PKCS 激酶的激活,IC50 为 2.5 μM。
T9256 N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine

Serine/threonin kinase; PKC Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism
N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine 是一种新型 2,6-naphthyridine,通过高通量筛选 (HTS) 鉴定为双蛋白激酶C/D (PKC/PKD) 抑制剂。
T4511 ST271

ST 271

Phospholipase; Tyrosine Kinases Metabolism; Tyrosine Kinase/Adaptors
ST271 是蛋白质酪氨酸激酶 (PTK) 抑制剂,抑制 fMet-Leu-Phe 和 PAF 引起的 phospholipase D 活化的IC50值分别为 6.7 和 9 μM。
T6904 Necrosulfonamide

(E)-Necrosulfonamide

MLK MAPK
Necrosulfonamide ((E)-Necrosulfonamide) 是一种坏死性凋亡抑制剂,通过选择性靶向(MLKL),可阻止 MLKL-RIP1-RIP3 坏死小体复合体与其下游效应子相互作用。MLKL 是诱导坏死过程中 RIP3 的重要底物。
T77504 JAK1/2/3 Inhibitor 1

PKA Tyrosine Kinase/Adaptors
JAK1/2/3 Inhibitor 1 是一种有效的蛋白激酶抑制剂。2,4-dichlorothieno[3,2-d]pyrimidine 具有抗肿瘤活性可抑制多种癌细胞株的生长。它通过与癌细胞的骨架结合,抑制新蛋白质的生成,从而抑制癌细胞的生长。
T25172 BPKDi

BPKDi is a potent and selective inhibitor of PKD (protein kinase D).
T68654 Sapintoxin D

Sapintoxin D is a fluorescent phorbol ester and selective activator of protein kinase C.
T71132 Calphostin D

Calphostin D is isolated from the fungus Cladosporium cladosporioides and is an inhibitor of protein kinase C (PKC).
T36322 C8 D-threo Ceramide (d18:1/8:0)

C8 D-threo Ceramide (d18:1/8:0)

C8 D-threo Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It is cytotoxic to U937 cells (IC50 = 17 μM) and induces nuclear DNA fragmentation 5- to 6-fold more potently than C8 ceramide . C8 D-threo Ceramide is a substrate for E. coli diacylglycerol kinase. It activates ceramide-activated protein kinase (CAPK) in U937 cells. C8 D-threo Ceramide also enhances V. cholerae cytolysin pore formation in liposome lipid membranes, as measured by calcein r...
T75501 Morin 3-O-β-D-glucopyranoside

Morin 3-O-β-D-glucopyranoside 是一种天然类黄酮,具有抗真菌、抗癌和抗氧化活性。Morin 3-O-β-D-glucopyranoside 抑制逆转录酶、蛋白酪氨酸激酶和黄嘌呤氧化酶,还具有抗 HIV、抗动脉硬化和超氧化物清除活性。
T38946 C8 Dihydroceramide

C8 Dihydroceramide

C8 Dihydroceramide acts as a negative control for C8 Ceramide, a cell-permeable analog of natural ceramides. C8 Ceramide, also known as N-Octanoyl-D-erythro-sphingosine, exhibits potent chemotherapeutic properties and anti-proliferation effects. Additionally, it stimulates dendritic cells to enhance T cell responses during viral infections. In vitro studies have also shown that C8 Ceramide induces a slight activation of protein kinase (PKC) [4].
T60718 3-IN-PP1

3-IN-PP1是一种针对蛋白激酶D(PKD)家族成员PKD1、PKD2和PKD3具有高效抑制作用的抑制剂,IC50值分别为108、94和108 nM。此外,3-IN-PP1作为一种广谱抗癌剂,能抑制多种肿瘤细胞的生长,适用于癌症研究领域。
T35781 Sphinganine (d20:0)

Sphinganine (d20:0)

Sphinganine (d20:0) is a natural isomer of dihydro-D-erythro-sphinganine (sphinganine (d18:0); that is a precursor of ceramide and sphingosine as well as a substrate for sphingosine kinases, which generate sphingosine-1-phosphate (d18:1) . In S. cerevisiae, the amount of sphinganine (d20:0) increases 10.8-fold in response to heat stress, indicating it is involved in heat stress adaptation. Sphinganine levels increase significantly in response to certain mycotoxins, including fumonisins as well ...
T81451 PKCd (8-17)

PKCd (8-17) 是源自蛋白激酶 C (PKC)d V1 结构域的生物活性肽。它能抑制由佛波醇 12-肉豆蔻酸酯 13-乙酸酯 (PMA) 诱导的 PKCd 易位和激活。此外,PKCd (8-17) 在降低心脏和脑细胞缺血损伤、促进成纤维细胞增殖、以及抑制小鼠移植冠状动脉疾病方面具有潜在应用。
T73359 NYX-2925

NYX-2925 是一种口服有效的NMDAR 调节剂。NYX-2925 恢复 mPFC 中 GluN2A 和 GluN2B 上活化的Src 和Src 磷酸化位点的水平。NYX-2925 对 CAMKII 没有影响,也没有任何成瘾或镇静/共济失调的副作用。NYX-2925 可用于多种 NMDA 受体介导的中枢神经系统疾病的研究。
T36907 1-Oleoyl Lysophosphatidic Acid

Oleoyl-sn-3-Glycerophosphate,1-Oleoyl LPA,1-Oleoyl Lysophosphatidic Acid

1-Oleoyl lysophosphatidic acid is a species of lysophosphatidic acid (LPA) containing oleic acid at the sn-1 position. Phosphatidic acid is produced either directly through the action of phospholipase D (PLD) or through a two step process involving liberation of diacylglycerol (DAG) by phospholipase C (PLC) followed by phosphorylation of DAG by diglycerol kinase.[1] Hydrolysis of the fatty acid at the sn-2 position by phospholipase A2 (PLA2) yields bioactive LPA. LPA binds to one of five differe...
T36779 NG 25 (hydrochloride hydrate)

NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv...
T36722 Deltorphin II (trifluoroacetate salt)

Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid...

化合物

Protein kinase inhibitor 6
Cat.No: T9779
Synonym:
Target:
CID755673
Cat.No: T2458
Synonym:
Target: Serine/threonin kinase
CID 2011756
Cat.No: T1863
Synonym: CID2011756,CID-2011756
Target: Serine/threonin kinase
kb NB 142-70
Cat.No: T2062
Synonym:
Target: Serine/threonin kinase
PF-AKT400
Cat.No: T5508
Synonym: (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
Target: Akt
CGP 57380
Cat.No: T6440
Synonym: N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺,MNK1 Inhibitor
Target: Apoptosis, MNK
Protein kinase D inhibitor 1
Cat.No: T61163
Synonym:
Target:
Perifosine
Cat.No: T2492
Synonym: NSC 639966,D21266,KRX-0401,哌立福新
Target: Apoptosis, Akt, Autophagy
CRT0066101 dihydrochloride
Cat.No: TQ0104
Synonym: CRT0066101二盐酸盐
Target: Serine/threonin kinase
STL127705
Cat.No: T13017
Synonym: Compound L,7-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]-3-(3-fluorophenyl)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione
Target: DNA-PK, Others
N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine
Cat.No: T9256
Synonym:
Target: Serine/threonin kinase, PKC
ST271
Cat.No: T4511
Synonym: ST 271
Target: Phospholipase, Tyrosine Kinases
Necrosulfonamide
Cat.No: T6904
Synonym: (E)-Necrosulfonamide
Target: MLK
JAK1/2/3 Inhibitor 1
Cat.No: T77504
Synonym:
Target: PKA
BPKDi
Cat.No: T25172
Synonym:
Target:
Sapintoxin D
Cat.No: T68654
Synonym:
Target:
Calphostin D
Cat.No: T71132
Synonym:
Target:
C8 D-threo Ceramide (d18:1/8:0)
Cat.No: T36322
Synonym: C8 D-threo Ceramide (d18:1/8:0)
Target:
Morin 3-O-β-D-glucopyranoside
Cat.No: T75501
Synonym:
Target:
C8 Dihydroceramide
Cat.No: T38946
Synonym: C8 Dihydroceramide
Target:
3-IN-PP1
Cat.No: T60718
Synonym:
Target:
Sphinganine (d20:0)
Cat.No: T35781
Synonym: Sphinganine (d20:0)
Target:
PKCd (8-17)
Cat.No: T81451
Synonym:
Target:
NYX-2925
Cat.No: T73359
Synonym:
Target:
1-Oleoyl Lysophosphatidic Acid
Cat.No: T36907
Synonym: Oleoyl-sn-3-Glycerophosphate,1-Oleoyl LPA,1-Oleoyl Lysophosphatidic Acid
Target:
NG 25 (hydrochloride hydrate)
Cat.No: T36779
Synonym:
Target:
Deltorphin II (trifluoroacetate salt)
Cat.No: T36722
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3889 Platycodin D

Prostaglandin Receptor; AMPK Chromatin/Epigenetic; GPCR/G Protein; Immunology/Inflammation; PI3K/Akt/mTOR signaling
Platycodin D 是从桔梗中分离得到的一种皂苷类天然产物,是AMPKα的激活剂,具有抗肥胖活性。它可刺激 TNF-α 合成或抑制 TNF-α mRNA 的降解。
TN1405 Arnicolide D

山金车内酯 D,山金车内酯D

Akt; Caspase; PI3K; STAT; mTOR Apoptosis; Cytoskeletal Signaling; JAK/STAT signaling; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells
Arnicolide D 是从石胡荽中分离出的一种倍半萜内酯,以浓度和时间依赖性方式抑制鼻咽癌细胞活力。它调节细胞周期,激活 caspase 信号通路并抑制 PI3K/AKT/mTOR 和 STAT3 信号通路。
T2974 Cyclovirobuxine D

黄杨碱,CVB-D,Bebuxine,Cyclovirobuxin D,环维黄杨星D

Apoptosis; Others; Akt; mTOR; Autophagy Apoptosis; Autophagy; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
Cyclovirobuxine D (Bebuxine) 是中药黄杨的主要活性成分,可诱导自噬并减弱Akt 和mTOR 的磷酸化。它通过抑制细胞周期进程和诱导线粒体介导的细胞凋亡抑制癌细胞的增殖,有用于心肌梗死引起的心力衰竭的研究潜力。
T5891 D-ERYTHRO-SPHINGOSINE

trans-4-Sphingenine,erythro-C18-Sphingosine,Erythrosphingosine,鞘氨醇,D-鞘氨醇

Phosphatase; Endogenous Metabolite; PKC Chromatin/Epigenetic; Cytoskeletal Signaling; Metabolism
D-erythro-Sphingosine (trans-4-Sphingenine) 是一种非常有效的p32激酶活化剂,EC50为 8 μM。它也是一种PP2A 激活剂,抑制蛋白激酶 C (PKC)。
TN1499 Cimiracemoside C

千层纸素A-7-0-Β-D-葡萄糖醛酸苷,Cimicifugoside M

AMPK Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
Cimiracemoside C (Cimicifugoside M) 是在升麻中发现的一种天然产物,可激活 AMPK 并具有抗糖尿病的潜在活性。
T19500 Palmitelaidic Acid

trans-Palmitoleic acid,9-trans-Hexadecenoic acid,软脂酸

Glucokinase; AMPK; PPAR Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; PI3K/Akt/mTOR signaling
trans-Palmitelaidic Acid (trans-Palmitoleic acid) 是palmitoleic acid 的反式异构体。Palmitoleic acid 是血清和组织中最丰富的脂肪酸之一。

天然产物

Platycodin D
Cat.No: T3889
Synonym:
Target: Prostaglandin Receptor, AMPK
Arnicolide D
Cat.No: TN1405
Synonym: 山金车内酯 D,山金车内酯D
Target: Akt, Caspase, PI3K, STAT, mTOR
Cyclovirobuxine D
Cat.No: T2974
Synonym: 黄杨碱,CVB-D,Bebuxine,Cyclovirobuxin D,环维黄杨星D
Target: Apoptosis, Others, Akt, mTOR, Autophagy
D-ERYTHRO-SPHINGOSINE
Cat.No: T5891
Synonym: trans-4-Sphingenine,erythro-C18-Sphingosine,Erythrosphingosine,鞘氨醇,D-鞘氨醇
Target: Phosphatase, Endogenous Metabolite, PKC
Cimiracemoside C
Cat.No: TN1499
Synonym: 千层纸素A-7-0-Β-D-葡萄糖醛酸苷,Cimicifugoside M
Target: AMPK
Palmitelaidic Acid
Cat.No: T19500
Synonym: trans-Palmitoleic acid,9-trans-Hexadecenoic acid,软脂酸
Target: Glucokinase, AMPK, PPAR
TargetMol Loading
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