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Targets Recommended: Serine/threonin kinase

27

抑制剂 & 化合物

1

天然产物

5

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
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。
T4223	Mitapivat PKR-IN-1	PKM	Metabolism
	Mitapivat (PKR-IN-1) 是口服具有活性的变构丙酮酸激酶 (pyruvate kinase) 激活剂，其AC50=20 nM。它在广泛的 PKLR 基因型中增加酶活性、蛋白质稳定性和 ATP 水平。它有潜在的恢复 PK 缺乏的糖酵解途径活性的作用。
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。
T25172	BPKDi	Others	Others
	BPKDi is a potent and selective inhibitor of PKD (protein kinase D).
T8957L	CRT0066101 dihydrochloride(956121-30-5 free base)	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	CRT0066101 dihydrochloride(956121-30-5 free base) 是 PKD 的抑制剂。
T22033	ARC 239 dihydrochloride	Norepinephrine	Neuroscience
	ARC 239 dihydrochloride 是一种选择性 α2B 肾上腺素受体拮抗剂。
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。
T1858	CID-797718 CID 797718	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	CID-797718 是一种潜在的 PKD 结合剂。
T3311	GSK6853	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK6853 是一种强选择性RPF1乙酰赖氨酸抑制剂，pKd 为9.5，其选择性是其它的乙酰赖氨酸的 1600 倍。
T1808	kb-NB77-78	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	kb-NB77-78 是一种 CID797718 的类似物，但不影响 PKD。它是母体化合物 CID755673（PKD1 抑制剂）的合成副产物。
T26646	AQW051 AQ W051,VQW-765,AQW-051	AChR	Neuroscience
	AQW051 (VQW-765)是一种口服活性alpha -7烟碱乙酰胆碱受体(α7-nAChR)特异性激活剂，与重组人alpha7-nAChR 表达相互作用(pKD 值7.56)。alpha7-nAChR 被认为是治疗与神经障碍相关的认知障碍的一个有吸引力的靶点，因此VQW-051经常用于焦虑障碍和急性焦虑的研究
T2153	1-NM-PP1 PP1 Analog II,1 nM-PP1	Serine/threonin kinase; CDK; Src	Angiogenesis; Cell Cycle/Checkpoint; Metabolism; Tyrosine Kinase/Adaptors
	1-NM-PP1 (PP1 Analog II) 是一种有效的Src 家族激酶抑制剂，是一种细胞渗透性 PP1 类似物，对 v-Src-as1 与 c-Fyn-as1 的IC50值分别为 4.3 nM、3.2 nM。
T1232	Mepyramine maleate 马来酸吡纳明,Pyrilamine maleate,吡拉明马来酸盐	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Mepyramine maleate (Pyrilamine maleate) 是一种组胺 H1 拮抗剂，对 H1、H2 和 H3 受体的 Kd 值分别为 0.8、5200 和大于 3000 nM，对 H1 受体的 pKd 值为 9.4。它是感冒药的常见成分，具有温和的催眠特性和局部麻醉作用，可用于胃肠外和局部过敏。
T8957	CRT0066101	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	CRT0066101 是 PKD 的抑制剂。
T12554	PROTAC EED degrader-2	Others; PROTACs	Others; PROTAC
	PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27),is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.11.
T12553	PROTAC EED degrader-1	Others; PROTACs	Others; PROTAC
	PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.
T61163	Protein kinase D inhibitor 1	Others	Others
	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].
T75861	ANQ-11125 TFA
	ANQ-11125 TFA 是一种有效的、选择性胃动素拮抗剂，pKd 值为 8.24。ANQ-11125 TFA 在体外阻断 motilide 引起的收缩。
T60718	3-IN-PP1	Others	Others
	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。
T84405	CRT0066101 hydrochloride	Others	Others
	Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This s...
T28631	RX821002 RX-821002,RX 821002	Others	Others
	RX821002 is a potent and selective antagonist of α2-adrenoceptor with low affinity for imidazoline sites. RX821002 displays selectivity for the α2D over the α2A subtypes (pKd values are 9.7 and 8.2 respectively).
T15443	GSK8814	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK8814 is a selective and ATAD2/2B bromodomain chemical probe and inhibitor (binding constant pKd=8.1 and a pKi=8.9 in BROMOscan). GSK8814 displays 500-fold selectivity for ATAD2 over BRD4 BD1. GSK8814 binds to ATAD2 and BRD4 BD1 (pIC50s: 7.3 and 4.6).
T21795	CRT5	Others	Others
	CRT5 是一种吡嗪苯甲酰胺，对经 VEGF 处理的内皮细胞中的所有三种 PKD 亚型 (对 PKD1、PKD2 和 PKD3 的 IC50s 分别为 1、2 和 1.5 nM) 都是一种有效的选择性抑制剂，并且 CRT5 减少 VEGF 诱导的内皮细胞迁移、增殖和微管生成。
T18673	(S,R,S)-AHPC-O-Ph-PEG1-NH2 VH032-O-Ph-PEG1-NH2	Others	Others
	(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) serves as an E3 ligase ligand-linker conjugate, integrating a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. This compound is utilized in PROTAC EED degrader-1, a PROTAC that targets EED with a potency (pKD) of 9.02[1].
T60953	BSc5367	Others	Others
	BSc5367 是Nek1激酶结构域的有效抑制剂，IC50值为 11.5 nM。Nek1 是一种NIMA 相关的蛋白激酶，在细胞周期调节、DNA 修复和微管调节中起着关键作用。Nek1 功能障碍在肌萎缩侧索硬化症 (ALS)、多囊肾病 (PKD) 和几种类型的放疗耐药性癌症中发挥关键作用。BSc5367 为更好的理解上述疾病提供了有用工具。

化合物

Cat.No: T2458

Target: Serine/threonin kinase

Cat.No: T1863

Synonym: CID2011756,CID-2011756

Target: Serine/threonin kinase

Cat.No: T2062

Target: Serine/threonin kinase

Cat.No: T4223

Synonym: PKR-IN-1

Target: PKM

CRT0066101 dihydrochloride

Cat.No: TQ0104

Synonym: CRT0066101二盐酸盐

Target: Serine/threonin kinase

Cat.No: T25172

Target: Others

CRT0066101 dihydrochloride(956121-30-5 free base)

Cat.No: T8957L

Target: Serine/threonin kinase

ARC 239 dihydrochloride

Cat.No: T22033

Target: Norepinephrine

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine

Cat.No: T9256

Target: Serine/threonin kinase, PKC

Cat.No: T1858

Synonym: CID 797718

Target: Serine/threonin kinase

Cat.No: T3311

Target: Epigenetic Reader Domain

Cat.No: T1808

Target: Serine/threonin kinase

Cat.No: T26646

Synonym: AQ W051,VQW-765,AQW-051

Target: AChR

Cat.No: T2153

Synonym: PP1 Analog II,1 nM-PP1

Target: Serine/threonin kinase, CDK, Src

Mepyramine maleate

Cat.No: T1232

Synonym: 马来酸吡纳明,Pyrilamine maleate,吡拉明马来酸盐

Target: Histamine Receptor

Cat.No: T8957

Target: Serine/threonin kinase

PROTAC EED degrader-2

Cat.No: T12554

Target: Others, PROTACs

PROTAC EED degrader-1

Cat.No: T12553

Target: Others, PROTACs

Protein kinase D inhibitor 1

Cat.No: T61163

Target: Others

Cat.No: T75861

Cat.No: T60718

Target: Others

CRT0066101 hydrochloride

Cat.No: T84405

Target: Others

Cat.No: T28631

Synonym: RX-821002,RX 821002

Target: Others

Cat.No: T15443

Target: Epigenetic Reader Domain

Cat.No: T21795

Target: Others

(S,R,S)-AHPC-O-Ph-PEG1-NH2

Cat.No: T18673

Synonym: VH032-O-Ph-PEG1-NH2

Target: Others

Cat.No: T60953

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T2S1837	Steviol 甜菊醇,NSC 226902,Hydroxydehydrostevic acid	Others	Others
	Steviol (NSC-226902) 是一种甜菊糖甙的主要代谢物。它能降低 AQP2 的表达，并促进 AQP2 的降解，从而减缓肾囊肿的生长。

天然产物

Cat.No: T2S1837

Synonym: 甜菊醇,NSC 226902,Hydroxydehydrostevic acid

Target: Others

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-04406	Protein Kinase D2/PRKD2 Protein, Human, Recombinant (His & GST) protein kinase D2,nPKC-D2,PKD2,HSPC187	Human	Baculovirus Insect Cells
	Serine/threonine-protein kinase D2, also known as PRKD2 and PKD2, is a cytoplasm and membrane protein that belongs to the protein kinase superfamily, CAMK Ser/Thr protein kinase family and PKD subfamily. PRKD2 / PKD2 is widely expressed. It contains one PH domain, two phorbol-ester/DAG-type zinc fingers and one protein kinase domain. PRKD2 / PKD2 is activated by DAG and phorbol esters. Phorbol-ester/DAG-type domains bind DAG, mediating translocation to membranes. Autophosphorylation of Ser-71 an...
TMPY-04456	PKC nu Protein, Human, Recombinant (GST) PRKCN,nPKC-NU,PKC-NU,PKD3,EPK2,protein kinase D3	Human	Baculovirus Insect Cells
	Serine/threonine-protein kinase D3, also known as Protein kinase C nu type, Protein kinase EPK2, PRKD3, EPK2 and PRKCN, is a cytoplasm and membrane protein that belongs to the protein kinase superfamily, CAMK Ser/Thr protein kinase family and PKD subfamily. PRKD3 / PRKCN contains one PH domain, two phorbol-ester/DAG-type zinc fingers and one protein kinase domain. Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by calcium and the second ...
TMPH-02648	PKDCC Protein, Mouse, Recombinant (His & Myc) Extracellular tyrosine-protein kinase PKDCC,Vertebr...	Mouse	Baculovirus Insect Cells
	Secreted tyrosine-protein kinase that mediates phosphorylation of extracellular proteins and endogenous proteins in the secretory pathway, which is essential for patterning at organogenesis stages. Mediates phosphorylation of MMP1, MMP13, MMP14, MMP19 and ERP29. May also have serine/threonine protein kinase activity. Required for longitudinal bone growth through regulation of chondrocyte differentiation. May be indirectly involved in protein transport from the Golgi apparatus to the plasma membr...
TMPY-04765	PKLR Protein, Human, Recombinant (His) PKRL,PKR,RPK,PKL,PK1,pyruvate kinase, liver and RBC	Human	E. coli
	Pyruvate kinase (PKLR) is a critical erythrocyte enzyme that is required for glycolysis and production of ATP. Pyruvate kinase deficiency (PKD) is the most frequent red blood cell enzyme abnormality of the glycolytic pathway and the most common cause of hereditary nonspherocytic hemolytic anemia. Over 250 PKLR-gene mutations have been described, including missense/nonsense, splicing and regulatory mutations, small insertions, small and gross deletions, causing PKD and hemolytic anemia of variabl...
TMPY-01996	SorCS1 Protein, Human, Recombinant (His) hSorCS,RP11-446H13.1,sortilin-related VPS10 domain containin...	Human	HEK293 Cells
	VPS1 domain-containing receptor SorCS1, also known as SORCS1 and SORCS, is a single-pass type I membrane protein that belongs to the SORCS family and SORCS1 subfamily. SORCS1 contains five BNR repeats and one PKD domain. SorCS1 is a member of the Vps1p-domain receptor family comprised of Sortilin, SorCS1, SorCS2, SorCS3, and SorLA. The common characteristic of these receptors is an N-terminal Vps1p domain, which either represents the only module of the luminal/extracellular moiety or is combined...

重组蛋白

Protein Kinase D2/PRKD2 Protein, Human, Recombinant (His & GST)

Cat.No: TMPY-04406

Species: Human

Expression System: Baculovirus Insect Cells

PKC nu Protein, Human, Recombinant (GST)

Cat.No: TMPY-04456

Species: Human

Expression System: Baculovirus Insect Cells

PKDCC Protein, Mouse, Recombinant (His & Myc)

Cat.No: TMPH-02648

Species: Mouse

Expression System: Baculovirus Insect Cells

PKLR Protein, Human, Recombinant (His)

Cat.No: TMPY-04765

Species: Human

Expression System: E. coli

SorCS1 Protein, Human, Recombinant (His)

Cat.No: TMPY-01996

Species: Human

Expression System: HEK293 Cells

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