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Search Results for " ht1080 "

15

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2320	Indacaterol	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Indacaterol 是一种超长效β-肾上腺素受体激动剂。
T1239	Indacaterol maleate 马来酸茚达特罗,QAB149	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Indacaterol maleate (QAB149) 是一种超长效的 β-肾上腺素受体激动剂。
T8649	TMBIM6 antagonist-1 BAX-inhibitor-1,1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮,BIA	mTOR	PI3K/Akt/mTOR signaling
	TMBIM6 antagonist-1 (BAX-inhibitor-1) 是有潜力的TMBIM6拮抗剂，能够抑制 TMBIM6 与 mTORC2 结合，抑制 mTORC2 活性，调节TMBIM6 释放 Ca2+。
T2586	Cabozantinib 卡博替尼,XL184,BMS-907351	Apoptosis; VEGFR; FLT; c-Met/HGFR; c-RET; TAM Receptor; c-Kit	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	Cabozantinib (XL184) 是一种多靶点酪氨酸激酶受体抑制剂，可以抑制 VEGFR2、c-Met、Kit、Axl 和 Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM)。Cabozantinib 具有抗肿瘤和抗血管生成活性。
T5164	Cabozantinib hydrochloride XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼	VEGFR; FLT; c-Met/HGFR; TAM Receptor; c-Kit; ROR	Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors
	Cabozantinib hydrochloride (XL184) 是一种有效的泛酪氨酸激酶抑制剂，可抑制 VEGFR2、c-Met、Kit、Axl 和 Flt4（IC50：0.035、1.3、4.6、7 和 6 nM）。
T36675	ERK Inhibitor
	ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 μM). This prevents its interaction with protein substrates without inhibiting catalytic activity. ERK inhibitor blocks ERK-specific phosphorylation of ribosomal S6 kinase-1 and ternary complex factor Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2. Presumably through its effects on ERK, ERK inhibitor completely prevents proliferation of HeLa cells (IC50 = 15-20 μM), A549 lung carcinoma cells (I...
T64357	FA16 FA 16,FA-16	Ferroptosis	Apoptosis
	FA16 是一种选择性、代谢稳定的铁死亡 (ferroptosis) 诱导剂，IC50 值为1.26 μM。FA16 是 2-(三氟甲基) 苯并咪唑的衍生物。FA16 对胱氨酸/谷氨酸反转运蛋白 (system Xc-) 介导了细胞内谷氨酸和细胞外胱氨酸的交换有抑制作用。FA16 在 HepG2 异种移植瘤模型中显著抑制肿瘤生长。
T74796	PROTAC GPX4 degrader-1
	PROTACGPX4 degrader-1 (DC-2) 是GPX4的PROTAC 降解剂，其在HT1080 细胞中的DC50值为 0.03 μM。
T83017	Antiproliferative agent-40
	抗增殖剂-40（化合物9）对HT1080和MCF-7细胞系展示了明显的抑制效果，其IC50值分别为52 μM和8.2 μM。
T18635	PROTAC RAR Degrader-1	Others	Others
	PROTAC RAR Degrader-1 comprises a cIAP1 ligand binding group, a linker and a RAR ligand binding group. PROTAC RAR Degrader-1 is an RAR degrader. Maximal RAR degradation at 30 μM concentration in HT1080 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].
T83018	Antiproliferative agent-39
	Antiproliferative agent-39 (Compound 12)于 A549、SNU-638、Col2、HT1080、MCF-7 细胞系展现抑制增殖作用，其 IC50 值分别为 11、25、14、11, 6.3 μM。
T62698	mIDH1-IN-1
	mIDH1-IN-1 (compound 43) 是一种有效的、选择性的 mIDH1 (异柠檬酸脱氢酶 1 突变体) 抑制剂 (IC50: 961.5 nM)。mIDH1-IN-1 可以有效抑制 HT1080 细胞内 2-HG (2-hydroxyglutarate) 的产生 (EC50: 208.6±8.0 nM)。mIDH1-IN-1 对 IDH1 突变体 U-87 细胞表现出明显的抗增殖效果(IC50: 41.8 nM)。mIDH1-IN-1 是一种抗肿瘤剂，能够用于研究 IDH1 突变实体瘤。
T69618	XR3054
	XR3054 is a novel inhibitor of farnesyl protein transferase (FPTase). XR3054 inhibited the proliferation of the prostatic cancer cell lines LnCAP and PC3 and the colon carcinoma SW480 and HT1080 (IC50 values of 12.4, 12.2, 21.4 and 8.8 microM, respectively) but was relatively inactive when tested against a panel of breast carcinoma cell lines. The activity did not relate to the presence of mutant or wild-type ras in the cell lines tested. In conclusion XR3054 inhibits ras farnesylation, MAP kina...
T25006	AGI-14100 AGI 14100	Dehydrogenase	Metabolism
	AGI-14100 是一种新型且可口服的 mIDH1 抑制剂。AGI-14100 用于治疗原发性人类髓性白血病。
T78758	IHMT-IDH1-053	Isocitrate Dehydrogenase (IDH)	Metabolism
	IHMT-IDH1-053（compound 16）为高选择性不可逆IDH1R132H突变抑制剂，IC50值仅为4.7 nM。对IDH1wt和IDH2wt/突变体活性低。该化合物在IDH1R132H突变293T细胞中显著抑制2-羟基戊二酸（2-HG）生成，IC50为28 nM。IHMT-IDH1-053通过与IDH1R132H蛋白的Cys269残基形成共价键，结合至NADPH结合袋附近的变构袋。此外，它能够抑制携带IDH1R132突变的HT1080细胞系及原代AML细胞增殖。

化合物

Cat.No: T2320

Target: Adrenergic Receptor

Indacaterol maleate

Cat.No: T1239

Synonym: 马来酸茚达特罗,QAB149

Target: Adrenergic Receptor

TMBIM6 antagonist-1

Cat.No: T8649

Synonym: BAX-inhibitor-1,1-（2-氨基苯基）-3-（3-硝基苯基）-2-丙烯-1-酮,BIA

Target: mTOR

Cat.No: T2586

Synonym: 卡博替尼,XL184,BMS-907351

Target: Apoptosis, VEGFR, FLT, c-Met/HGFR, c-RET, TAM Receptor, c-Kit

Cabozantinib hydrochloride

Cat.No: T5164

Synonym: XL184,Cabozantinib hydrochloride (849217-68-1(free base)),BMS-907351,盐酸卡博替尼

Target: VEGFR, FLT, c-Met/HGFR, TAM Receptor, c-Kit, ROR

Cat.No: T36675

Cat.No: T64357

Synonym: FA 16,FA-16

Target: Ferroptosis

PROTAC GPX4 degrader-1

Cat.No: T74796

Antiproliferative agent-40

Cat.No: T83017

PROTAC RAR Degrader-1

Cat.No: T18635

Target: Others

Antiproliferative agent-39

Cat.No: T83018

Cat.No: T62698

Cat.No: T69618

Cat.No: T25006

Synonym: AGI 14100

Target: Dehydrogenase

Cat.No: T78758

Target: Isocitrate Dehydrogenase (IDH)

Cat. No.	Product Name	Target	Signaling Pathways
T3860	Isoliquiritin apioside	MMP; p38 MAPK; NF-κB	MAPK; NF-κB; Proteases/Proteasome
	Isoliquiritin apioside 可抑制癌细胞和内皮细胞的侵袭和血管生成，显著降低 PMA 诱导的MMP9活性增加，并抑制 PMA 诱导的MAPK 和NF-κB 活化。
T20819	Ammonium iron(III) citrate 柠檬酸铁铵,柠檬酸铁 (III) 铵,Ferric ammonium citrate	Others; Ferroptosis	Apoptosis; Others
	Ammonium iron(III) citrate (Ferric ammonium citrate) 是一种非运铁蛋白结合的铁的生理形式，会引起的细胞内铁超负荷从而导致细胞铁死亡，能增强蛋白质产生。
T4S21320	ISOGINKGETIN 异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮	MMP; Others	Others; Proteases/Proteasome
	ISOGINKGETIN (4',4'''-Dimethylamentoflavone) 是一种MMP9抑制剂，也是一种Pre-mRNA Splicing 抑制剂。
TN2029	p-Hydroxy-5,6-dehydrokawain 4'-Hydroxydehydrokawain,4'-羟基-5,6-脱氢醉椒素	Others	Others
	p-Hydroxy-5,6-dehydrokawain (4'-Hydroxydehydrokawain) 是一种分离自 Kawain 的天然产物。

天然产物

Isoliquiritin apioside

Cat.No: T3860

Target: MMP, p38 MAPK, NF-κB

Ammonium iron(III) citrate

Cat.No: T20819

Synonym: 柠檬酸铁铵,柠檬酸铁 (III) 铵,Ferric ammonium citrate

Target: Others, Ferroptosis

Cat.No: T4S21320

Synonym: 异银杏素,4',4'''-Dimethylamentoflavone,异银杏双黄酮

Target: MMP, Others

p-Hydroxy-5,6-dehydrokawain

Cat.No: TN2029

Synonym: 4'-Hydroxydehydrokawain,4'-羟基-5,6-脱氢醉椒素

Target: Others

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