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14

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T9755	MRTX0902 UNII-CRG69FR93G	Raf	MAPK
	MRTX0902 是一种有效且高选择性的 SOS1 抑制剂，IC50 为 46 nM，Ki 为 2 nM。
T16143	MRTX-1257	Ras	GPCR/G Protein; MAPK
	MRTX-1257 是选择性的、可口服的不可逆共价KRAS G12C 抑制剂，其在 H358 细胞中测得 KRAS 依赖 ERK 磷酸化的IC50值为 900 pM。
T9575	MRTX9768	Histone Methyltransferase	Chromatin/Epigenetic
	MRTX-9768 是一种有效的、选择性的、具有口服活性的 PRMT5-MTA 复合体抑制剂，可选择性靶向 MTAP/CDKN2A 缺失的肿瘤。
T9303	MRTX1133	Ras	GPCR/G Protein; MAPK
	MRTX1133 是一种 KRAS G12D 抑制剂 (KD=0.2 pM)，具有强效性、选择性和非共价性。MRTX1133 对 KRAS G12D 突变的肿瘤具有抑制活性，而对 KRAS 野生型肿瘤无抑制活性。
T40254	MRTX-1719	Histone Methyltransferase	Chromatin/Epigenetic
	MRTX-1719 是有效的PRMT5/MTA 复合体选择性抑制剂，其对PRMT5/MTAMTAPDELSDMA 细胞系的IC50值为 <10 nM。
T64000	MRTX-EX185
	MRTX-EX185 是一种有效的负载 GDP 的 KRAS 和 KRAS (G12D) 抑制剂，对 KRAS (G12D) 的 IC50=90 nM。MRTX-EX185 也能够结合 GDP 负载的 HRAS。
T37130	MRTX1133 formic
	MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells[1][2]. MRTX1133 demonstrates dose-dependent inhibition of the KRAS pathway tumor regression in G12D mutant tumor models[2]. [1]. Xiaolun Wang, et al.Kras g12d inhibitors.WO2021041671A1.[2]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available onli...
T40189	MRTX849 acid MRTX849 acid
	MRTX849 acid, a derivative of MRTX849, is employed in the synthesis of PROTAC LC-2. LC-2, a potent and pioneering PROTAC, exhibits the ability to efficiently degrade endogenous KRAS G12C with DC50 values ranging between 0.25 and 0.76 μM.
T80429	π-TRTX-Hm3a	Sodium Channel	Membrane transporter/Ion channel
	π-TRTX-Hm3a 是一种含有37个氨基酸的肽，源自多哥星暴狼蛛 (Heteroscodra maculata) 的毒液。该化合物 pH 依赖性抑制酸敏感离子通道 1a (ASIC1a)，其 IC50 值为 1-2 nM，并且能够增强 ASIC1b 的活性，EC50 值为 46.5 nM。
T36630	MRTX9768 hydrochloride
	MRTX9768 hydrochloride is a potent, orally active PRMT5 inhibitor. MRTX9768 hydrochloride is a synthetic lethal-based inhibitor binding the PRMT5-MTA complex[1]. MRTX9768 inhibits SDMA and cell proliferation in HCT116 MTAP-del cells (SDMA IC50 3 nM; prolif. IC50 11 nM) with marked selectivity over HCT116 MTAP-WT cells (SDMA IC50 544 nM; prolif. IC50 861 nM)[1].MRTX9768 selectively targets MTAP/CDKN2A-deleted tumors[2][1]. In xenograft studies, oral administration of MRTX9768 demonstrates dose-de...
T80179	GrTx1	Sodium Channel	Membrane transporter/Ion channel
	GrTx1是一种从Grammostola rosea蜘蛛的毒液中分离的肽毒素。该分子能够阻断sodium channel，对Nav1.1，Nav1.2，Nav1.3，Nav1.4，Nav1.6和Nav1.7具有不同的抑制作用，IC50值分别为0.63 µM, 0.23 µM, 0.77 µM, 1.29 µM, 0.63 µM和0.37 µM，适用于神经疾病的研究领域。
T80437	μ-TRTX-Hd1a	Sodium Channel	Membrane transporter/Ion channel
	μ-TRTX-Hd1a为特异性NaV 1.7抑制剂，源自蜘蛛毒液。该化合物作为门控修饰剂，通过与人NaV 1.7通道域II中S3b-S4桨基序互作，实现抑制功能。
T40156	MRTX849 analog 24 MRTX849 analog 24
	MRTX849 analog 24 is an alkyne-containing click probe analogue of the MRTX849 inhibitor for KRAS G12C. It is specifically designed for studying the functionality of MRTX849.
T40190	MRTX849 ethoxypropanoic acid
	MRTX849 ethoxypropanoic acid is a compound that contains a ligand for KRAS G12C and a PROTAC linker. It is commonly employed in the synthesis of PROTAC LC-2, which is a highly effective and innovative PROTAC. LC-2 has been proven to degrade endogenous KRAS G12C with remarkable potency, exhibiting DC50 values ranging from 0.25 to 0.76 μM.

化合物

Cat.No: T9755

Synonym: UNII-CRG69FR93G

Target: Raf

Cat.No: T16143

Target: Ras

Cat.No: T9575

Target: Histone Methyltransferase

Cat.No: T9303

Target: Ras

Cat.No: T40254

Target: Histone Methyltransferase

Cat.No: T64000

MRTX1133 formic

Cat.No: T37130

Cat.No: T40189

Synonym: MRTX849 acid

Cat.No: T80429

Target: Sodium Channel

MRTX9768 hydrochloride

Cat.No: T36630

Cat.No: T80179

Target: Sodium Channel

Cat.No: T80437

Target: Sodium Channel

MRTX849 analog 24

Cat.No: T40156

Synonym: MRTX849 analog 24

MRTX849 ethoxypropanoic acid

Cat.No: T40190

Cat. No.	Product Name	Target	Signaling Pathways
T34295	Resiniferatoxin RTX,[3H]resiniferatoxin,树脂毒素	IL Receptor	Immunology/Inflammation
	Resiniferatoxin ([3H]resiniferatoxin) 抑制 Th1 细胞因子的产生，有助于防御 T.spiralis 感染，并可用于免疫反应调节剂的研究。

天然产物

Resiniferatoxin

Cat.No: T34295

Synonym: RTX,[3H]resiniferatoxin,树脂毒素

Target: IL Receptor

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