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18

抑制剂 & 化合物

1

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T5399	GeA-69	PARP	Chromatin/Epigenetic; DNA Damage/DNA Repair
	GeA-69 是一种选择性变构 PARP14 大结构域 2 (MD2) 抑制剂，Kd 值为 2.1 µM。
T0373	Erlotinib OSI-744,NSC 718781,CP358774,埃罗替尼,R1415	EGFR; Autophagy	Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Erlotinib (NSC-718781) 是一种直接作用的EGFR 酪氨酸激酶抑制剂，用于治疗非小细胞肺癌，对人 EGFR 的IC50为 2 nM。它可降低完整肿瘤细胞的 EGFR 自磷酸化，IC50为 20 nM。
T7724	Tepoxalin RWJ-20485,RWJ20485,ORF20485,替泊沙林,ORF-20485,RWJ 20485,ORF 20485	Lipoxygenase; COX	Immunology/Inflammation; Metabolism; Neuroscience
	Tepoxalin (RWJ 20485) 是有效的5-脂氧合酶和环氧合酶抑制剂，表现出强大的抗炎活性和较小的胃肠道刺激性。
T16087	Quiflapon 喹夫拉朋,MK-591	Apoptosis; FLAP	Apoptosis; Immunology/Inflammation
	Quiflapon (MK-591) 是一种选择性和特异性的FLAP 抑制剂，可诱导细胞凋亡。它也是口服白三烯生物合成抑制剂，在完整的人和诱导的大鼠多形核白细胞 PMNLs 中，其IC50值分别为 3.1 nM 和 6.1 nM。
TP2008L	Lyn peptide inhibitor acetate Lyn peptide inhibitor acetate(222018-18-0 free base)	IL Receptor	Immunology/Inflammation
	Lyn peptide inhibitor acetate(222018-18-0 free base) 是一种有效的细胞渗透性 Lyn 偶联 IL-5 受体信号通路抑制剂，同时保持其他信号完整。它阻断 Lyn 活化并抑制 Lyn 酪氨酸激酶与 IL-3/GM-CSF/IL-5 受体的 βc 亚基的结合。它可用于哮喘、过敏和其他嗜酸性粒细胞疾病的研究。
TP1956L	PKC ζ pseudosubstrate acetate PKC ζ pseudosubstrate acetate (799764-07-1 free base)	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	PKC ζ pseudosubstrate acetate 是蛋白激酶 C (PKC) ζ 的抑制剂；附着于细胞通透性触角足结构域载体肽。由 PKC ζ 假底物结构域的氨基酸 113-129 组成，通过二硫键连接到触角足结构域载体肽。 Antennapedia 肽在 4 或 37°C 时被完整细胞积极吸收，确保快速有效地吸收抑制肽。一旦进入细胞，二硫键在细胞质中被还原，导致抑制肽的释放。通过 PKC ζ 非依赖性途径诱导肥大细胞脱粒。
T1467	Acemetacin 阿西美辛,K-708,TVX 1322	COX	Immunology/Inflammation; Neuroscience
	Acemetacin (TVX 1322) 是一种非甾体抗炎类的化合物。
T33955	PF-6808472 OX-44,OX44,PF 6808472,OX 44,PF6808472
	PF-6808472 is a cell permeable covalent probe suitable for click chemistry designated to measure kinase selectivity in intact cells. PF-6808472 contains sulfonyl fluoride group, which react with conserved lysine residue within kinase ATP binding site.
TP1451	TAT peptide
	TAT peptide corresponds to the polycationic aa49-57 region of TAT protein. TAT peptide is a cell-penetrating peptide (CPP) used to cargo larger molecules through the lipophilic barrier of the cellular membranes to deliver them inside the cells with intact
TP1956	PKC ζ pseudosubstrate
	Inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the inhibitor peptide. Once inside the cell, the disulphide bonds are subjected to reduction in the cytoplasm leading to release of the ...
T79819	AMB639752
	AMB639752为一种高效DGKα抑制剂，能通过抑止整合体内DGKα活性，复原因重复刺激导致的SAP缺失型淋巴细胞的细胞死亡(RICD)。此化合物适合于X连锁淋巴增生性疾病1(XLP-1)的相关研究。
T30783	CDy9 CDy 9,CDy-9
	CDy9 is a highly selective fluorescent probe for the detection and isolation of mESC using fluorescence microscopy and flow cytometry. CDy9 allows the detection and isolation of intact stem cells with marginal impact on their function and capabilities. CD
TP1955	PKC β pseudosubstrate
	Selective cell-permeable peptide inhibitor of protein kinase C (IC50 ~ 0.5 μM). Consists of amino acids 19 - 31 of PKC pseudosubstrate domain linked by a disulphide bridge to a cell permeabilisation Antennapedia domain vector peptide. The Antennapedia pep
T38107	JJH260 JJH260
	JJH260 is an N-hydroxy hydantoin carbamate that inhibits androgen-induced gene 1 (AIG1), an enzyme that hydrolyzes fatty acid esters of hydroxy fatty acids (FAHFAs). It blocks the hydrolysis of 9-PAHSA with an IC50 value of 0.57 μM. JJH260 also inhibits the novel FAHFA hydrolase androgen-dependent TFPI-regulating protein (ADTRP; IC50 = 8.5 μM), as well as the serine hydrolase ABHD6 and the lysophospholipases LYPLA1 and LYPLA2. JJH260 inhibits the FAHFA hydrolase activity of LNCaP and T cell lysa...
TP1971	Pseudo RACK1
	Activator of protein kinase C; attached to cell permeabilization Antennapedia domain vector peptide. Consists of peptide derived from the C2 domain of PKC β linked by a disulfide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide i
T35915	Erlotinib-13C6 Erlotinib-13C6
	Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR[1]. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer[1].Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process[2]...
T36806	TPC2-A1-P TPC2-A1-P
	TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na2+ mobilisation from TPC2 than TPC-A1-N . TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells[1][2][3]. Two-pore channels (TPC1-3) are ancient members of the voltage-gated ion channel superfamily. TPCs are expressed throughout the en...
T37297	Ru360
	Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects[1][2]. Ru360 permeates slowly into the cell, and specifically inhibits mitochondrial calcium uptake in intact cardiomyocytes and in isolated heart. 1 μm Ru360 is taken up by myocardial ce...

化合物

Cat.No: T5399

Target: PARP

Cat.No: T0373

Synonym: OSI-744,NSC 718781,CP358774,埃罗替尼,R1415

Target: EGFR, Autophagy

Cat.No: T7724

Synonym: RWJ-20485,RWJ20485,ORF20485,替泊沙林,ORF-20485,RWJ 20485,ORF 20485

Target: Lipoxygenase, COX

Cat.No: T16087

Synonym: 喹夫拉朋,MK-591

Target: Apoptosis, FLAP

Lyn peptide inhibitor acetate

Cat.No: TP2008L

Synonym: Lyn peptide inhibitor acetate(222018-18-0 free base)

Target: IL Receptor

PKC ζ pseudosubstrate acetate

Cat.No: TP1956L

Synonym: PKC ζ pseudosubstrate acetate (799764-07-1 free base)

Target: PKC

Cat.No: T1467

Synonym: 阿西美辛,K-708,TVX 1322

Target: COX

Cat.No: T33955

Synonym: OX-44,OX44,PF 6808472,OX 44,PF6808472

Cat.No: TP1451

PKC ζ pseudosubstrate

Cat.No: TP1956

Cat.No: T79819

Cat.No: T30783

Synonym: CDy 9,CDy-9

PKC β pseudosubstrate

Cat.No: TP1955

Cat.No: T38107

Synonym: JJH260

Cat.No: TP1971

Cat.No: T35915

Synonym: Erlotinib-13C6

Cat.No: T36806

Synonym: TPC2-A1-P

Cat.No: T37297

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。

天然产物

Cat.No: T3889

Target: Prostaglandin Receptor, AMPK

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