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11

抑制剂 & 化合物

4

重组蛋白

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Cat. No.	Product Name	Target	Signaling Pathways
T39772	BRK inhibitor P21d hydrochloride BRK inhibitor P21d hydrochloride
	BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK/PTK6), displaying an IC50 of 30 nM. Additionally, it effectively suppresses p-SAM68 with an IC50 value of 52 nM. This compound, BRK inhibitor P21d hydrochloride, serves as a valuable tool for evaluating the efficacy of BRK inhibitors in xenograft breast tumor models, enabling the assessment of their in vivo activity.
T17098	Tilfrinib	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	Tilfrinib 是一种有效的选择性乳腺肿瘤激酶(Brk)抑制剂（IC50 = 3.15 nM），具有抗增殖和抗肿瘤活性。
T69980	XMU-MP-2	BTK; Protease	Angiogenesis; Proteases/Proteasome; Tyrosine Kinase/Adaptors
	XMU-MP-2 是一种有效和选择性的蛋白酶抑制剂，具有抗癌活性，在小鼠异种移植模型中抑制致癌 BRK 驱动的肿瘤的生长。
T16853	SB-633825	BTK	Angiogenesis; Tyrosine Kinase/Adaptors
	SB-633825 can inhibit cancer cell growth and angiogenesis. SB-633825 is an effective and ATP-competitive inhibitor of TIE2, LOK, and BRK (IC50s: 3.5 nM, 66 nM, 150 nM, respectively).
T41169	P21d hydrochloride
	P21d hydrochloride is a potent and selective breast tumor Ki nase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B Ki nase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also activein vivoand orally bioavailable.
T67693	PF-6689840
	PF-6689840是一种有效的选择性II 型PTK6/Brk 抑制剂,在生化检测中IC50为54 nM；在过表达PTK6 WT 的工程化HET293T 细胞中抑制Y342处的PTK6磷酸化,IC50为0.25 uM；表现出优异的激酶选择性,与I 型抑制剂相比；抑制肿瘤细胞生长,这与细胞中PTK6的表达水平无关。
T70424	EBI-907
	EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases i...
T1835	Ibrutinib 伊布替尼,依鲁替尼,PCI-32765	Tyrosine Kinases; Src; BTK; Ligands for Target Protein for PROTAC	Angiogenesis; PROTAC; Tyrosine Kinase/Adaptors
	Ibrutinib (PCI-32765) 是一种不可逆的、选择性的 Btk 抑制剂，IC50=0.5 nM，它是一种 Btk 配体，用于合成一系列 PROTAC 分子，如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞，浓度为 10 和 100 nM 时，分别降解 73% 和 89% Btk。
T13564L2	AZ7550 trimesylate salt AZ7550 Mesylate,AZ7550 trimesylate salt (1421373-99-0 free base)	MLK	MAPK
	AZ7550 trimesylate salt (AZ7550 Mesylate) 是奥希替尼的活性代谢产物，AZ7550 trimesylate salt 抑制 IGF1R 活性，可用于研究非小细胞肺癌。
T13564	AZ7550	MLK; FAK; EGFR; FLT; Tyrosine Kinases; PYK2; MNK; IGF-1R; ACK; BTK; ALK; Drug Metabolite	Angiogenesis; Cytoskeletal Signaling; JAK/STAT signaling; MAPK; Metabolism; Tyrosine Kinase/Adaptors
	AZ7550 是 AZD9291 的活性代谢物，可抑制 IGF1R 活性，IC50为 1.6 μM。
T13564L	AZ7550 hydrochloride AZ7550 hydrochloride (1421373-99-0 free base)	EGFR; IGF-1R	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	AZ7550 hydrochloride (AZ7550 hydrochloride ) 是 AZD9291 的活性代谢物，可抑制 IGF1R 活性，IC50为 1.6 μM。

化合物

BRK inhibitor P21d hydrochloride

Cat.No: T39772

Synonym: BRK inhibitor P21d hydrochloride

Cat.No: T17098

Target: BTK

Cat.No: T69980

Target: BTK, Protease

Cat.No: T16853

Target: BTK

P21d hydrochloride

Cat.No: T41169

Cat.No: T67693

Cat.No: T70424

Cat.No: T1835

Synonym: 伊布替尼,依鲁替尼,PCI-32765

Target: Tyrosine Kinases, Src, BTK, Ligands for Target Protein for PROTAC

AZ7550 trimesylate salt

Cat.No: T13564L2

Synonym: AZ7550 Mesylate,AZ7550 trimesylate salt (1421373-99-0 free base)

Target: MLK

Cat.No: T13564

Target: MLK, FAK, EGFR, FLT, Tyrosine Kinases, PYK2, MNK, IGF-1R, ACK, BTK, ALK, Drug Metabolite

AZ7550 hydrochloride

Cat.No: T13564L

Synonym: AZ7550 hydrochloride (1421373-99-0 free base)

Target: EGFR, IGF-1R

Species：

Expression System：

Tag：

Cat. No.	Product Name	Species	Expression System
TMPY-04377	Brk Protein, Human, Recombinant (GST) BRK,protein tyrosine kinase 6	Human	Baculovirus Insect Cells
	Brk Protein, Human, Recombinant (GST) is expressed in Baculovirus insect cells with GST tag. The predicted molecular weight is 78 kDa and the accession number is Q13882-1.
TMPY-04440	Brk Protein, Mouse, Recombinant (His & GST) BRK,Tksk,protein tyrosine kinase 6,tks,Sik	Mouse	Baculovirus Insect Cells
	Brk Protein, Mouse, Recombinant (His & GST) is expressed in Baculovirus insect cells with His and GST tag. The predicted molecular weight is 79.8 kDa and the accession number is Q64434.
TMPY-01059	BMPR2 Protein, Human, Recombinant (His) POVD1,PPH1,BMPR3,BRK-3,BMPR-II,bone morphogenetic p...	Human	HEK293 Cells
	BMPR2 Protein, Human, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 15.6 kDa and the accession number is Q13873.
TMPY-00683	BMPR2 Protein, Human, Recombinant (His & hFc) BMPR3,BRK-3,PPH1,BMPR-II,bone morphogenetic protein...	Human	HEK293 Cells
	BMPR2 Protein, Human, Recombinant (His & hFc) is expressed in HEK293 mammalian cells with His and hFc tag. The predicted molecular weight is 42 kDa and the accession number is Q13873.

重组蛋白

Brk Protein, Human, Recombinant (GST)

Cat.No: TMPY-04377

Species: Human

Expression System: Baculovirus Insect Cells

Brk Protein, Mouse, Recombinant (His & GST)

Cat.No: TMPY-04440

Species: Mouse

Expression System: Baculovirus Insect Cells

BMPR2 Protein, Human, Recombinant (His)

Cat.No: TMPY-01059

Species: Human

Expression System: HEK293 Cells

BMPR2 Protein, Human, Recombinant (His & hFc)

Cat.No: TMPY-00683

Species: Human

Expression System: HEK293 Cells

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