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43

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T12462	PI3Kδ-IN-1	PI3K	PI3K/Akt/mTOR signaling
	PI3Kδ-IN-1 是高效，选择性的 PI3Kδ 抑制剂，IC50 为 1.7 nM。
T12365	PARP/PI3K-IN-1	PARP; PI3K	Chromatin/Epigenetic; DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	PARP/PI3K-IN-1 是一种新型双重聚（ADP-核糖）聚合酶(PARP）和磷酸肌醇 3-激酶(PI3K)双重抑制剂，具有抗癌、抗肿瘤和抗癌细胞增殖活性，可用于研究乳腺癌、胰腺癌和肺癌。
T12589	PI3Kα/mTOR-IN-1	PI3K; mTOR	PI3K/Akt/mTOR signaling
	PI3Kα/mTOR-IN-1是一种有效的 PI3Kβ/mTOR 双重抑制剂。在细胞测定中，PI3Kα/mTOR-IN-1的 IC50为7nM，在无细胞测定中 mTOR 和PI3Kβ的Kis 分别为12.5nM 和10.6nM。
T5831	Selective PI3Kδ Inhibitor 1	PI3K	PI3K/Akt/mTOR signaling
	Selective PI3Kδ Inhibitor 1 是一种 PI3Kδ 抑制剂 (IC50 = 0.9 nM)。
T30874	Chemodosimeter 1 Pi-Probe-1,Chemodosimeter-1
	Chemodosimeter 1 is designed as a highly selective phosphate ion (PI) sensor capable of demonstrating exogenous and endogenous ATP-catalysed PI production and is the first probe capable of tracking PI production and enrichment through half-channel closure
T1826	PI3K-IN-1 Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409	DNA-PK; PI3K	DNA Damage/DNA Repair; PI3K/Akt/mTOR signaling
	PI3K-IN-1 (Voxtalisib Analogue) 是 PI3K 抑制剂，PI3K-IN-1(25 μM) 能够阻断 PI3K/Akt 信号通路。
T12463	PI3kδ inhibitor 1	PI3K	PI3K/Akt/mTOR signaling
	PI3kδ inhibitor 1 is a selective inhibitor of PI3Kδ (IC50 of 3.8 nM).
T12461	PI3Kdelta inhibitor 1	PI3K	PI3K/Akt/mTOR signaling
	PI3Kdelta inhibitor 1 is a potent, selective and orally available inhibitor of PI3Kδ with an IC50 of 1.3 nM.
T12460	PI3K/mTOR Inhibitor-1	PI3K	PI3K/Akt/mTOR signaling
	PI3K/mTOR Inhibitor-1 is a potent, orally bioavailable dual inhibitor of PI3K/mTOR (PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ/mTOR with IC50s of 20/376/204/46/186 nM)
T12455	PI3K/HDAC-IN-1	PI3K	PI3K/Akt/mTOR signaling
	PI3K/HDAC-IN-1 is a potent PI3K and HDAC dual inhibitor(IC50s of 8.1 nM and 1.4 nM, respectively).
T12464	PI3Kγ inhibitor 1	PI3K	PI3K/Akt/mTOR signaling
	PI3Kγ inhibitor 1 is a inhibitor of PI3Kδ and PI3Kγ.
TMIH-0273	Hydroxyzine dihydrochloride-d10 (R)-2-(2-(4-((4-chlorophenyl)(phenyl)methyl)pi perazin-1-yl-2,2,3,3,5,5,6,6-d8)ethoxy)ethan-1, 1-d2-1-ol dihydrochloride
	Hydroxyzine dihydrochloride-d10 是 Hydroxyzine dihydrochloride 的氘代化合物。
T63497	PI3Kδ/γ-IN-1
	PI3Kδ/γ-IN-1 是选择性的 PI3Kδ/γ 有效抑制剂，能够用于血液系统恶性肿瘤的治疗。
T62997	PI3K/AKT-IN-1
	PI3K/AKT-IN-1 是一种有效的、双重的 PI3K/AKT 抑制剂，能够作用于 PI3Kγ (IC50: 6.99 μM)、PI3Kδ (IC50: 4.01 μM) 和 AKT (IC50: 3.36 μM)。PI3K/AKT-IN-1 通过抑制 PI3K/AKT 通路，诱导 caspase 3 依赖性凋亡，表现出抗癌作用。
T74402	FAP-PI3KI1
	FAP-PI3KI1 是一种成纤维细胞活化蛋白 (FAP) 靶向 PI3K 抑制剂，可选择性靶向表达 FAP 的人特发性肺纤维化 (IPF)细胞并有效抑制胶原蛋白合成，减少胶原蛋白沉积。
T74360	MEK/PI3K-IN-1
	MEK/PI3K-IN-1（compound 6r）是一种高效的MEK/PI3K抑制剂，IC50值为124 nM（MEK1）、130 nM（PI3Kα）及236 nM（PI3Kδ）。该化合物能够降低pAKT和pERK1/2的活性，并展现对肿瘤细胞的抗增殖作用。
T62948	PI3Kβ-IN-1
	PI3Kβ-IN-1 是一种选择性的、口服具有活力的 PI3Kβ 抑制剂 (IC50: 2 nM)。
T60982	PI5P4Ks-IN-1
	PI5P4Ks-IN-1 (compound 7) 是一种与PI5P4Kγ结合的活性化合物。
T62103	COX-2/PI3K-IN-1
	COX-2/PI3K-IN-1 (compound 5d) 是一种 PI3K 的有效抑制剂 (IC50: 1.14 nM)。COX-2/PI3K-IN-1 是一种 COX-2 的选择性抑制剂 (Ki: 3.24 nM)。COX-2/PI3K-IN-1 显示出抗炎和抗癌效果。
T62289	PI3KC2α-IN-1
	PI3KC2α-IN-1 是一种 PI3KC2α 的有效抑制剂，其 IC50 值为 95 nM。PI3KC2α-IN-1 能够与 PI3KC2α 的 ATP 结合位点相互作用。PI3KC2α-IN-1 损伤内吞膜的动力学过程和膜重塑。PI3KC2α-IN-1 能够用于研究血栓形成、糖尿病和癌症。
T78178	PI5P4Kα-IN-1	Others	Others
	PI5P4Kα-IN-1（化合物13）是一种针对PI5P4Kα和PI5P4Kβ具有选择性抑制作用的化合物（IC50分别为2 μM和9.4 μM）。它适用于癌症、代谢和免疫紊乱相关研究。
T72713	PI3K/VEGFR2-IN-1	PI3K	PI3K/Akt/mTOR signaling
	PI3K/VEGFR2-IN-1是一种具有双重抑制效应的化合物，对PI3K和VEGFR2的IC50分别为2.21 μM和68 μM，能够诱导细胞凋亡(apoptosis)，在癌症研究中应用。
T79710	PI3Kα/HDAC6-IN-1	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	PI3Kα/HDAC6-IN-1（化合物21j）是一种针对PI3Kα/HDAC6的双重抑制剂，其IC50值分别为2.9 nM和26 nM。该化合物还能抑制AKT(Ser473)的磷酸化，诱导α-微管蛋白的积累，并促进其乙酰化，但对乙酰化组蛋白H3和H4无显著影响。在L-363细胞系中，PI3Kα/HDAC6-IN-1显示了高效的抑制活性（IC50=0.17 μM），表现出良好的抗癌潜力。
T72227	PI3K/Akt/CREB activator 1
	PI3K/Akt/CREB activator 1 是一种口服有效的PI3K/Akt/CREB 的激活剂。PI3K/Akt/CREB activator 1 通过 PI3K/Akt/CREB 通路上调脑源性神经营养因子，促进神经元增殖，诱导 Neuro-2a 细胞分化成神经元样形态，加速海马原代神经元轴突-树突极化的建立。PI3K/Akt/CREB activator 1 可用于血管性痴呆 (VaD) 的研究。
T81465	PI5P4K-β-IN-1
	PI5P4K-β-IN-1（compound vs1）是一款针对PI5P4K-β具有高效抑制活性的化合物，其IC50值为0.80 μM。
T60390	PI-55 6-(2-hydroxy-3-methylbenzylamino)purine	Others	Others
	PI-55 (6-(2-hydroxy-3-methylbenzylamino)purine) is a cytokinin receptor inhibitor that exhibits structural similarity to 6-benzylaminopurine (BAP). It competitively inhibits BAP binding on the specific Arabidopsis receptors CRE1/AHK4 and AHK3. Furthermore, PI-55 effectively suppresses cytokinins-induced haustorium formation and enhances parasite aggressiveness [1].
T4578	Tipranavir PNU-140690	SARS-CoV; HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Tipranavir 是一种蛋白酶抑制剂，对1种以上蛋白酶抑制剂耐药的HIV-1具有抑制作用。Tipranavir 可有效抑制 HIV-1 蛋白酶酶活性和二聚化，对抗多种蛋白酶抑制剂(PI)的HIV-1分离株具有有效的活性（IC50 为 66-410 nM）。Tipranavir 对SARS-CoV-2 3CLpro 活性有抑制作用。
T19323	Fluorescein diacetate 荧光素二乙酸酯,3,6-Diacetoxyfluoran,Di-O-acetylfluorescein	Others	Others
	Fluorescein diacetate (Di-O-acetylfluorescein) 是一种人谷胱甘肽硫转移酶 Pi 的荧光底物，是一种细胞渗透性的酯酶底物。
T30585	Brecanavir GW-640385,GW-640385X,UNII-E367I8C7FI,CHEMBL206031,GW-0385
	Brecanavir is a tyrosyl-based arylsulfonamide, high affinity, protease inhibitor (PI) for the treatment of human immunodeficiency virus type 1.
T80723	ZK-PI-9
	ZK-PI-9 是一种抑制海藻糖酶且能够抑制雌性蛹中几丁质酶活性的杀虫剂。
T80724	ZK-PI-5
	ZK-PI-5为一有效的海藻糖酶抑制剂，调控Spodoptera frugiperda繁殖。该化合物展现成为创新杀虫剂的可能，可用于害虫防治。
T6143L	PI-103 Hydrochloride
	PI-103 Hydrochloride 是一种有效的PI3K 和mTOR 双重抑制剂，抑制p110α，p110β，p110δ，p110γ，mTORC1和mTORC2，IC50分别为 8 nM，88 nM，48 nM，150 nM，20 nM 和 83 nM。PI-103 Hydrochloride 也可抑制DNA-PK，IC50为 2 nM。PI-103 Hydrochloride 诱导细胞自噬 (autophagy)。
T72328	Cyclopropenone probe 1
	Cyclopropenone probe 1 可以通过在催化活性位点共价结合，特异且有效地修饰三阴性乳腺癌驱动因子 GSTP1。
T60355	LY367385 hydrochloride
	LY367385 hydrochloride 是一种高效且选择性的mGluR1a 拮抗剂，抑制喹喹啉诱导的磷酸肌醇水解的IC50值为 8.8 μM，而对 mGlu5a 的IC50值大于 100 μM。LY367385 hydrochloride 具有神经保护，抗惊厥和抗癫痫作用。
T36938	PtdIns-(3)-P1 (1,2-dioctanoyl) (sodium salt) PtdIns-(3)-P1 (1,2-dioctanoyl) (sodium salt)
	The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3)-P1 (1,2-dioctanoyl) is a synthetic analog of natural PtdIns featuring C8:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and DAG stereochemistry as the natural compound. PtdIns-(3)-P1 can be phosphorylated to di- (PtdIns-P2; PIP2) and triphosphates (Ptd...
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...
T37030	PtdIns-(4)-P1 (1,2-dioctanoyl) (ammonium salt) PtdIns-(4)-P1 (1,2-dioctanoyl) (ammonium salt)
	The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(4)-P1 (1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) featuring C8:0 fatty acids at the sn-1 and sn-2 positions. The compound contains the same inositol and diacylglycerol (DAG) stereochemistry as the natural compound. PtdIns-(4)-P1 can be phosphorylated to di- ...
T71287	CDKI-83
	CDKI-83 is a potent CDK9 inhibitor. The compound shows effective anti-proliferative activity in human tumour cell lines with GI50 <1 μM, and is capable of inducing apoptosis in A2780 human ovarian cancer cells as determined by the activated caspase-3, Annexin V/PI double staining and accumulated cells at the sub-G1 phase of cellcycle. The research results suggest that combined inhibition of CDK9 and CDK1 may result in the effective induction of apoptosis and CDKI-83 has the potential to be devel...
T36805	TPC2-A1-N TPC2-A1-N
	TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1].
T36937	PtdIns-(1,2-dioctanoyl) (sodium salt)
	The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(1,2-dioctanoyl) is a synthetic analog of natural phosphatidylinositol (PtdIns) containing C8:0 fatty acids at the sn-1 and sn-2 positions. The compound features the same inositol and diacyl glycerol (DAG) stereochemistry as that of the natural compound. The short fatty acid chains of this anal...
T70962	MHY219
	MHY219 is a novel HDAC inhibitor. MHY219 induces apoptosis via up-regulation of androgen receptor expression in human prostate cancer cells. MHY219 was shown to enhance the cytotoxicity on DU145 cells (IC50, 0.36 μM) when compared with LNCaP (IC50, 0.97 μM) and PC3 cells (IC50, 5.12 μM). MHY219 showed a potent inhibition of total HDAC activity when compared with SAHA. MHY219 increased histone H3 hyperacetylation and reduced the expression of class I HDACs (1, 2 and 3) in prostate cancer cells. M...
T36939	PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) (ammonium salt) PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) (ammonium salt)
	The phosphatidylinositol (PtdIns) phosphates represent a small percentage of total membrane phospholipids. However, they play a critical role in the generation and transmission of cellular signals. PtdIns-(3,4,5)-P3, also known as PIP3, is resistant to cleavage by PI-specific phospholipase C (PLC). Thus, it is likely to function in signal transduction as a modulator in its own right, rather than as a source of inositol tetraphosphates. PIP3 can serve as an anchor for the binding of signal transd...
T37120	1,2,3-Triundecanoyl Glycerol
	1,2,3-Triundecanoyl glycerol is a triacylglycerol that contains undecanoic acid at thesn-1,sn-2, andsn-3 positions. Dietary administration of a 7:3 (w/w) mixture of 1,2,3-triundecanoyl glycerol and corn oil prevents fasting-induced decreases in plasma glucose, alanine, and insulin levels, as well as the ratio of insulin to glucagon, in rats compared with dietary administration of corn oil alone.1 1.Pi-Sunyer, F.X., Conway, J.M., Lavau, M., et al.Glucagon, insulin, and gluconeogenesis in fasted o...

化合物

Cat.No: T12462

Target: PI3K

Cat.No: T12365

Target: PARP, PI3K

PI3Kα/mTOR-IN-1

Cat.No: T12589

Target: PI3K, mTOR

Selective PI3Kδ Inhibitor 1

Cat.No: T5831

Target: PI3K

Chemodosimeter 1

Cat.No: T30874

Synonym: Pi-Probe-1,Chemodosimeter-1

Cat.No: T1826

Synonym: Voxtalisib Analogue,Voxtalisib (SAR245409, XL765) Analogue,XL765,SAR245409

Target: DNA-PK, PI3K

PI3kδ inhibitor 1

Cat.No: T12463

Target: PI3K

PI3Kdelta inhibitor 1

Cat.No: T12461

Target: PI3K

PI3K/mTOR Inhibitor-1

Cat.No: T12460

Target: PI3K

Cat.No: T12455

Target: PI3K

PI3Kγ inhibitor 1

Cat.No: T12464

Target: PI3K

Hydroxyzine dihydrochloride-d10

Cat.No: TMIH-0273

Synonym: (R)-2-(2-(4-((4-chlorophenyl)(phenyl)methyl)pi perazin-1-yl-2,2,3,3,5,5,6,6-d8)ethoxy)ethan-1, 1-d2-1-ol dihydrochloride

Cat.No: T63497

Cat.No: T62997

Cat.No: T74402

Cat.No: T74360

Cat.No: T62948

Cat.No: T60982

COX-2/PI3K-IN-1

Cat.No: T62103

Cat.No: T62289

Cat.No: T78178

Target: Others

PI3K/VEGFR2-IN-1

Cat.No: T72713

Target: PI3K

PI3Kα/HDAC6-IN-1

Cat.No: T79710

Target: HDAC

PI3K/Akt/CREB activator 1

Cat.No: T72227

Cat.No: T81465

Cat.No: T60390

Synonym: 6-(2-hydroxy-3-methylbenzylamino)purine

Target: Others

Cat.No: T4578

Synonym: PNU-140690

Target: SARS-CoV, HIV Protease

Fluorescein diacetate

Cat.No: T19323

Synonym: 荧光素二乙酸酯,3,6-Diacetoxyfluoran,Di-O-acetylfluorescein

Target: Others

Cat.No: T30585

Synonym: GW-640385,GW-640385X,UNII-E367I8C7FI,CHEMBL206031,GW-0385

Cat.No: T80723

Cat.No: T80724

PI-103 Hydrochloride

Cat.No: T6143L

Cyclopropenone probe 1

Cat.No: T72328

LY367385 hydrochloride

Cat.No: T60355

PtdIns-(3)-P1 (1,2-dioctanoyl) (sodium salt)

Cat.No: T36938

Synonym: PtdIns-(3)-P1 (1,2-dioctanoyl) (sodium salt)

Cat.No: T36806

Synonym: TPC2-A1-P

PtdIns-(4)-P1 (1,2-dioctanoyl) (ammonium salt)

Cat.No: T37030

Synonym: PtdIns-(4)-P1 (1,2-dioctanoyl) (ammonium salt)

Cat.No: T71287

Cat.No: T36805

Synonym: TPC2-A1-N

PtdIns-(1,2-dioctanoyl) (sodium salt)

Cat.No: T36937

Cat.No: T70962

PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) (ammonium salt)

Cat.No: T36939

Synonym: PtdIns-(3,4,5)-P3 (1,2-dihexanoyl) (ammonium salt)

1,2,3-Triundecanoyl Glycerol

Cat.No: T37120

Cat. No.	Product Name	Target	Signaling Pathways
T1205	Chloramphenicol Chlornitromycin,Levomycetin,Chloromycetin,氯霉素	ribosome; HIF/HIF Prolyl-Hydroxylase; Antibacterial; Antibiotic	Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Chloramphenicol (Chloromycetin) 是一种广谱抗生素，有效抑制细菌蛋白质生物合成。它主要作用于细菌 70S 核糖体的 50S 亚基，对肽基转移酶有活性，抑制肽键的形成。
T81952	Lanosta-7,9(11),23,25(27)-tetraen-26-oic acid, 23,27-epoxy-3-oxo-
	Lanosta-7,9(11),23,25(27)-tetraen-26-oic acid, 23,27-epoxy-3-oxo- 是一种从土津皮 (山楝的根皮) 提取的羊毛甾烷型化合物。
T75278	Pristinamycin
	Pristinamycin, 一种 Streptomyces pristinaespiralis 产生的口服活性链霉素样抗生素，由化学上不相关的两部分组成：Pristinamycin I (PI) 与 Pristinamycin II (PII)。该药物对包括耐甲氧西林金黄色葡萄球菌 (MRSA)、万古霉素耐药金黄色葡萄球菌 (VRSA) 和粪肠球菌 (VREF) 在内的多种抗生素耐药革兰氏阳性菌表现出强大活性。

天然产物

Chloramphenicol

Cat.No: T1205

Synonym: Chlornitromycin,Levomycetin,Chloromycetin,氯霉素

Target: ribosome, HIF/HIF Prolyl-Hydroxylase, Antibacterial, Antibiotic

Lanosta-7,9(11),23,25(27)-tetraen-26-oic acid, 23,27-epoxy-3-oxo-

Cat.No: T81952

Cat.No: T75278

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