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12

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T74997	ERK-IN-6
	ERK-IN-6 (compound 6g) 是有效的食管鳞状细胞癌 (ESCC) 的抗增殖剂。ERK-IN-6 通过ERK 通路诱导细胞凋亡。ERK-IN-6 可用于食管鳞状细胞癌的研究。
TP1904L	FSLLRY-NH2 TFA(245329-02-6 free base)	Protease-activated Receptor	GPCR/G Protein
	FSLLRY-NH2 TFA(245329-02-6 free base) 是一种蛋白酶激活受体 2 (PAR2) 抑制剂。在 ICR 小鼠中逆转紫杉醇诱导的机械异常性疼痛、热痛觉过敏和 PKC 激活。阻断分离的心脏成纤维细胞中的 ERK 活化和胶原蛋白生成。还可以减轻皮肤癣菌相关瘙痒小鼠模型的症状。
T36674	DMU-212	Apoptosis; ERK	Apoptosis; MAPK
	DMU-212 是具有口服活性的白藜芦醇的甲基化衍生物，表现出抗分裂、抗增殖、抗氧化和促进细胞凋亡的活性。它通过诱导凋亡和激活ERK1/2蛋白阻止有丝分裂。
T61705	MIF-IN-6
	MIF-IN-6 (compound 2d) is an effective inhibitor of macrophage migration inhibitory factor (MIF), exhibiting an IC50 of 1.4 μM and a Ki value of 0.96 μM. MIF-IN-6 effectively reduces MIF-induced ERK phosphorylation and impedes A549 cell proliferation [1].
T62751	KRAS inhibitor-12
	KRAS inhibitor-12 (compound 6-1) 是一种 KRAS G12C 的有效抑制剂 (IC50: 0.537 μM)。KRAS inhibitor-12 在 MIA PaCA-2，A549 细胞中表现出 p-ERK 抑制作用，其 IC50 值分别为 1.3，3.7 μM。 KRAS inhibitor-12 具有潜力进行胰腺癌，结直肠癌和肺癌的研究。
T79072	KRAS G12D modulator-1	Ras	GPCR/G Protein; MAPK
	KRAS G12D modulator-1（compound 6）是高效KRAS G12D调节剂，NEA-G12D、PPI-G12D 和 pERK-AGS的IC50范围为1-10 μM，适用于癌症研究。
T63164	KRAS inhibitor-13
	KRAS inhibitor-13 (compound 5-6) 是一种 KRAS G12C 的有效抑制剂 (IC50: 0.883 μM)。KRAS inhibitor-13 在 MIA PaCA-2，A549 细胞中具有 p-ERK 抑制效果，其 IC50 值分别为 5.9，>100 μM。 KRAS inhibitor-13 具有潜力进行胰腺癌、结直肠癌和肺癌的研究。
TP1948L	PBP 10 acetate(794466-43-6 Free base)
	PBP 10 acetate(794466-43-6 Free base) 是一种选择性甲酰肽受体 2 (FPR2) 拮抗剂。 PBP 10 acetate 选择性抑制 FPR2 介导的 NADPH 氧化酶活性，但对中性粒细胞中的 FPR1 信号传导没有影响。 PBP 10 acetate 在体外表现出 PIP2 结合活性并阻断细胞运动。 PBP 10 acetate 通过抑制病毒诱导的 ERK 激活而表现出针对流感病毒的抗病毒活性。
T71328	Theobromine-d6
	Theobromine-d6 is intended for use as an internal standard for the quantification of theobromine by GC- or LC-MS. Theobromine is a methylxanthine alkaloid and derivative of caffeine that has been found in cocoa beans and has diverse biological activities. It is an adenosine A1 receptor antagonist. Theobromine increases AMPK phosphorylation and inhibits adipocyte differentiation, ERK and JNK phosphorylation, and IL-6 and TNF-α production in 3T3-L1 preadipocytes cultured in differentiation medium....
T36676	Rineterkib hydrochloride
	Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C...
T35897	ASK120067
	ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT...
T36679	Rp-cAMPS sodium salt
	Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 μM and 4.5 μM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5][6]. A membrane-permeable competitive cAMP antagonist (Rp-cAMPS) that blocks PKA activation by binding to the regulatory subunits without dissociating the kinase holoenzyme also inhibits synaptic plasticity but has no effect on normal synaptic t...

化合物

Cat.No: T74997

FSLLRY-NH2 TFA(245329-02-6 free base)

Cat.No: TP1904L

Target: Protease-activated Receptor

Cat.No: T36674

Target: Apoptosis, ERK

Cat.No: T61705

KRAS inhibitor-12

Cat.No: T62751

KRAS G12D modulator-1

Cat.No: T79072

Target: Ras

KRAS inhibitor-13

Cat.No: T63164

PBP 10 acetate(794466-43-6 Free base)

Cat.No: TP1948L

Cat.No: T71328

Rineterkib hydrochloride

Cat.No: T36676

Cat.No: T35897

Rp-cAMPS sodium salt

Cat.No: T36679

Cat. No.	Product Name	Target	Signaling Pathways
T2940	6-Hydroxyflavone 6-羟基黄酮,6-HF	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	6-Hydroxyflavone (6-HF) 是天然存在的黄酮化合物，具有抗炎作用。它对牛血红蛋白糖基化具有抑制作用。它能激活 AKT、ERK 1/2、JNK 信号通路，有效促进成骨细胞分化。它能抑制 LPS 诱导的 NO 的产生。
T6S1597	Mulberroside A 桑皮苷 A,桑皮苷A	TNF; Tyrosinase; Interleukin	Apoptosis; Immunology/Inflammation; Proteases/Proteasome
	Mulberroside A 是桑中的一种主要活性成分，可降低TNF-α、IL-1β和IL-6的表达，抑制 NALP3、caspase-1 和 NF-κB 的激活以及 ERK、JNK 和 p38 的磷酸化。它抑制蘑菇酪氨酸酶，具有抗炎和抗细胞凋亡作用。
T75554	6-O-Isobutyrylbritannilactone
	6-O-Isobutyrylbritannilactone 是一种天然的黑素生成抑制剂。6-O-Isobutyrylbritannilactone 是一种倍半萜，可从英菊花中分离得到。6-O-Isobutyrylbritannilactone 抑制 IBMX 诱导 B16F10 细胞产生黑色素。6-O-Isobutyrylbritannilactone 也调控 ERK、PI3K/AKT 和 CREB，在斑马鱼胚胎模型中显示出抗黑色素原活性。

天然产物

6-Hydroxyflavone

Cat.No: T2940

Synonym: 6-羟基黄酮,6-HF

Target: GABA Receptor

Cat.No: T6S1597

Synonym: 桑皮苷 A,桑皮苷A

Target: TNF, Tyrosinase, Interleukin

6-O-Isobutyrylbritannilactone

Cat.No: T75554

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