protein kinase d

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。

CID755673是一种高效选择性 PKD1抑制剂，IC50为182 nM。

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。

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。

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].

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。

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。

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。

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。

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。

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。

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)。

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。

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

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。

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

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 as in some cancers. Sphinganine can block protein kinase C activation in some cases but not others.

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 release, with a 50% release dose (RD50) value of ~5 μg ml.

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 receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998)

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, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019)

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].

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。

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。

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。