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13

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T39275	Befotertinib D-0316,Befotertinib	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	Befotertinib (D-0316) 是一种 EGFR 酪氨酸激酶抑制剂，可用于 EGFR T790M 阳性非小细胞肺癌的研究。
T8636	Ibrutinib deacryloylpiperidine IBT4A,5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMine,伊布替尼中间体N-2	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Ibrutinib deacryloylpiperidine (IBT4A) 是 Ibrutinib 的杂质之一。它是一种不可逆的、选择性的 Btk 抑制剂 (IC50:0.5 nM)。
T10190	7-BIA	Phosphatase	Metabolism
	7-BIA 是一种受体型蛋白酪氨酸磷酸酶 D (PTPRD) 抑制剂，具有抗抗成瘾作用，可用于研究神经性疼痛。
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。
T9543	Syk Inhibitor II hydrochloride	Others	Others
	Syk Inhibitor II hydrochloride 信号传导的影响在狼疮中可能很突出。
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。
T37079	VEGFR2 Kinase Inhibitor II
	Vascular endothelial growth factor receptor 2 (VEGFR2, also known as KDR and FLK1) is a receptor tyrosine kinase that regulates angiogenesis, vascular development, and embryonic hematopoiesis in response to VEGF isoforms A, C, and D. VEGFR2 kinase inhibitor II is a reversible, cell-permeable inhibitor of VEGFR2's kinase activity (IC50 = 70 nM). It less potently inhibits the platelet-derived growth factor receptor β (PDGFRβ; IC50 = 920 nM) and related receptor and non-receptor tyrosine kinases. V...
T36367	RK-682 (calcium salt)
	Protein tyrosine phosphatases (PTPs) remove phosphate from tyrosine residues of cellular proteins. Reversible phosphorylation catalyzed by the coordinated actions of protein tyrosine kinases and phosphatases is key to the regulation of the signaling events that control cell growth and proliferation, differentiation, and survival or apoptosis, as well as adhesion and motility. RK-682, a bioactive compound originally isolated from the fermentation of Streptomyces sp. 88-682, is an inhibitor of the...
T36384	DL-Tyrosine-13C9,15N L-Tyrosine-13C9,15N
	L-Tyrosine-13C9,15N is intended for use as an internal standard for the quantification of L-tyrosine by GC- or LC-MS. L-Tyrosine is a non-essential amino acid.1It is produced by hydroxylation of phenylalanine by phenylalanine hydroxylase but can also be obtained from dietary sources or degradation of endogenous proteins, resulting in L-tyrosine release.1,2L-Tyrosine is a precursor in the biosynthesis of catecholamine neurotransmitters, melanins, and thyroid hormones.3Plasma, skeletal muscle, and...
T68389	LY2457546
	LY2457546 is a potent and orally bioavailable inhibitor of multiple receptor tyrosine kinases involved in angiogenic and tumorigenic signalling. LY2457546 demonstrates potent activity against targets that include VEGFR2 (KDR), PDGFRβ, FLT-3, Tie-2 and members of the Eph family of receptors. In vivo, LY2457546 inhibited VEGF-driven autophosphorylation of lung KDR in the mouse and rat in a dose and concentration dependent manner. LY2457546 was well tolerated and exhibited efficacy in a 13762 synge...
T35583	Hirudin (54-65; non-sulfated) (trifluoroacetate salt)
	Hirudin (54-65; non-sulfated) is a desulfated peptide fragment of hirudin, an anticoagulant produced byH. medicinalis.1It inhibits fibrin clot formation induced by isolated bovine thrombin with an IC50value of 3.7 μM.2 1.Niehrs, C., Huttner, W.B., Carvallo, D., et al.Conversion of recombinant hirudin to the natural form by in vitro tyrosine sulfation. Differential substrate specificities of leech and bovine tyrosylprotein sulfotransferasesJ. Biol. Chem.265(16)9314-9318(1990) 2.Payne, M.H., Krste...
T36648	Tucatinib hemiethanolate
	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ...
T36643	PKI-166 hydrochloride
	Potent EGFR-kinase inhibitor (IC50 = 0.7 nM). Displays >3000-fold selectivity against a panel of serine/threonine kinases. Reduces metastasis and angiogenesis in a mouse model of pancreatic cancer. Antihypertensive and orally bioavailable. Bruns et al (2000) Blockade of the epidermal growth factor receptor signaling by a novel tyrosine kinase inhibitor leads to apoptosis of endothelial cells and therapy of human pancreatic carcinoma. Cancer Res. 60 2926 PMID:10850439 \|Ulu et al (2013) Epidermal ...

化合物

Cat.No: T39275

Synonym: D-0316,Befotertinib

Target: EGFR

Ibrutinib deacryloylpiperidine

Cat.No: T8636

Synonym: IBT4A,5-(4-phenoxyphenyl)-7H-pyrrolo[2,3-d]pyriMidin-4-ylaMine,伊布替尼中间体N-2

Target: BTK

Cat.No: T10190

Target: Phosphatase

Cat.No: T4511

Synonym: ST 271

Target: Phospholipase, Tyrosine Kinases

Syk Inhibitor II hydrochloride

Cat.No: T9543

Target: Others

Morin 3-O-β-D-glucopyranoside

Cat.No: T75501

VEGFR2 Kinase Inhibitor II

Cat.No: T37079

RK-682 (calcium salt)

Cat.No: T36367

DL-Tyrosine-13C9,15N

Cat.No: T36384

Synonym: L-Tyrosine-13C9,15N

Cat.No: T68389

Hirudin (54-65; non-sulfated) (trifluoroacetate salt)

Cat.No: T35583

Tucatinib hemiethanolate

Cat.No: T36648

PKI-166 hydrochloride

Cat.No: T36643

Cat. No.	Product Name	Target	Signaling Pathways
TN1545	D-Tyrosine	Tyrosinase	Proteases/Proteasome
	D-Tyrosine，是酪氨酸的D异构体，通过抑制酪氨酸酶活性，作为黑色素合成的负向调节剂。此外，D-Tyrosine还能抑制生物膜的形成，并诱导生物膜的自我分散，同时不影响细菌的生长。
TN1053	Aloe-emodin-8-O-β-D-glucopyranoside Aloe-emodin-8-O-beta-D-glucopyranoside,芦荟大黄素-8-O-β-D-葡萄糖苷	Phosphatase	Metabolism
	Aloe-emodin-8-O-β-D-glucopyranoside (Aloe-emodin-8-O-beta-D-glucopyranoside) 是一种分离自Saussrurea lappa 中的化合物，是一种温和的人类蛋白酪氨酸磷酸酶 1B 抑制剂，其IC50=26.6 μM。
T4518	Licochalcone D	ERK; NF-κB	MAPK; NF-κB
	Licochalcone D 是一种 NF-κB p65的有效抑制剂，是一种存在于 Glycyrrhiza inflate 中的黄酮类化合物，具有抗氧化、抗炎、抗癌等作用。
T5290	(S)-2-Hydroxy-3-phenylpropanoic acid L-(−)-3-Phenyllactic acid,L-3-苯乳酸	Others; Endogenous Metabolite	Metabolism; Others
	(S)-2-Hydroxy-3-phenylpropanoic acid (L-(−)-3-Phenyllactic acid) 是苯丙氨酸的代谢产物。苯丙酮尿症患者体液中苯丙氨酸的水平升高。
T75495	Rubrofusarin 6-O-β-D-glucopyranoside
	Rubrofusarin 6-O-β-D-glucopyranoside为Rubrofusarin的糖苷形式，具有抑制蛋白酪氨酸磷酸酶 1B (PTP1B) 的活性，IC50值为87.36 μM，适用于糖尿病和抑郁症研究。
T3827	Rhein-8-glucoside calcium 大黄酸-8-O-β-D-葡萄糖苷,Rhein-8-O-β-D-glucopyranoside,Rhein-8-glucoside calcium salt	Phosphatase; Antibacterial	Metabolism; Microbiology/Virology
	Rhein-8-glucoside calcium (Rhein-8-glucoside calcium salt) salt 是一种从 Saussurea lappa 根的 EtOH 提取物中，分离得到的蒽醌类 hPTP1B 抑制剂，IC50值为11.5 μM，具有抗菌作用。

天然产物

Cat.No: TN1545

Target: Tyrosinase

Aloe-emodin-8-O-β-D-glucopyranoside

Cat.No: TN1053

Synonym: Aloe-emodin-8-O-beta-D-glucopyranoside,芦荟大黄素-8-O-β-D-葡萄糖苷

Target: Phosphatase

Cat.No: T4518

Target: ERK, NF-κB

(S)-2-Hydroxy-3-phenylpropanoic acid

Cat.No: T5290

Synonym: L-(−)-3-Phenyllactic acid,L-3-苯乳酸

Target: Others, Endogenous Metabolite

Rubrofusarin 6-O-β-D-glucopyranoside

Cat.No: T75495

Rhein-8-glucoside calcium

Cat.No: T3827

Synonym: 大黄酸-8-O-β-D-葡萄糖苷,Rhein-8-O-β-D-glucopyranoside,Rhein-8-glucoside calcium salt

Target: Phosphatase, Antibacterial

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