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Search Results for " a375 "

Targets Recommended: Dehydrogenase

32

抑制剂 & 化合物

11

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9974	Antiproliferative agent-13	Dehydrogenase	Metabolism
	Antiproliferative agent-13是一种具有抗增殖活性的化合物。
T24269	KPT-251 KPT251	Others	Others
	KPT-251 是一种选择性核输出抑制剂。
T11898	LXH254	Raf	MAPK
	LXH254 是B/C RAF 抑制剂。
T8745	PROTAC BRAF-V600E degrader-1 Compound 23	Raf; PROTACs	MAPK; PROTAC
	PROTAC BRAF-V600E degrader-1 (Compound 23) 选择性地诱导 BRAF-V600E 的降解，而不是野生型 BRAF。
T23861	CAY10526 CAY-10526,BTH,CAY 10526	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	CAY10526 (BTH) 是 mPGES-1 的选择性抑制剂，可抑制 NF-κB 信号通路。
T4314	EPZ020411 EPZ020411 2HCl	Histone Methyltransferase	Chromatin/Epigenetic
	EPZ020411是一种特异性有效的 PRMT6 抑制剂， IC50 为 10 nM，比作用于 PRMT1 和 PRMT8 的选择性高10倍多。
T36902	RA375 RA375	Proteasome	Proteases/Proteasome; Ubiquitination
	RA375 是一种 RPN13（26S 蛋白酶体调节亚基）抑制剂。 RA375 激活 UPR 信号、ROS 产生和细胞凋亡。 RA375 对癌症细胞的活性比 RA190 高 10 倍，这反映了它的硝基环取代基和氯乙酰胺弹头的添加。
T15486	HLM006474	Others	Others
	HLM006474 是光谱的E2F 抑制剂，在 A375 细胞中，可抑制 E2F4 DAN 结合(IC50:29.8 µM)。
T4356	POL1-IN-1 Compound 3A	DNA/RNA Synthesis	Cell Cycle/Checkpoint; DNA Damage/DNA Repair
	POL1-IN-1 (Compound 3A) 是一种RNA 聚合酶 1 POL1抑制剂，IC50值低于 0.5 uM。它能有效抑制A375恶性黑色素瘤细胞系中RNA 聚合酶I 的转录。
T6882	LY3009120 DP-4978	Raf; Autophagy	Autophagy; MAPK
	LY3009120 (DP-4978) 是一种泛RAF 抑制剂，其抑制BRAFV600E、BRAFWT 和CRAFWT 的IC50分别为 5.8、9.1和15 nM。
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。
T2668	JNK-IN-8 JNK Inhibitor XVI	JNK; c-Kit	MAPK; Tyrosine Kinase/Adaptors
	JNK-IN-8 (JNK Inhibitor XVI) 是一种有效的JNK 抑制剂，抑制JNK1、JNK2和JNK3，IC50分别为 4.7、18.7 和 1 nM。
T6843	GDC-0623 G-868,GDC0623,RG 7421,MEK inhibitor 1	Apoptosis; MEK	Apoptosis; MAPK
	GDC-0623 (RG 7421) 是一种 ATP 竞争性的MEK1抑制剂，Ki 值为 0.13 nM。它对 A375 细胞中 BRAFV600E 的 EC50值为 7 nM，而对 HCT116 细胞中 KRAS (G13D)的 EC50值为 42 nM。
T84790	Benzyl DC-81	Others; ADC Cytotoxin	Antibody-drug Conjugate/ADC Related; Others
	Benzyl DC-81 (Compound 6a) 是一种抗癌化合物，展现对A375和MCF-7细胞线具有显著的抗增殖作用。
T36460	CAY10736 CAY10736	Others	Others
	CAY10736 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.827-9.89 μM). CAY10736 inhibits migration and epithelial-to-mesenchymal transition (EMT) of A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 2.4 and 1.59 μM, respectively) and increases the production of reactive oxygen species (ROS) in these cells in a ...
T61226	hDHODH-IN-9	Others	Others
	hDHODH-IN-9 (Compound 3k) is a highly potent inhibitor of hDHODH, exhibiting an IC50 of 0.34 μM. It displays significant cytotoxic activity against MCF-7 and A375 cells, while maintaining good selectivity. With its characteristics, hDHODH-IN-9 holds promise for cancer disease research [1].
T63365	RAF-IN-1	Others	Others
	RAF-IN-1 是 b/cRAF 的有效抑制剂，能够作用于 cRAF (IC50: 3.8 nM)、bRAFwt (IC50: 36 nM)，bRAFV600E (IC50: 29.4 nM)，能够抑制携带 bRAFV600E 突变的 A375 和 H358 细胞系，其 GI50分别为 3.4 和 2.9 nM。
T36468	ARN14988	Others	Others
	ARN14988 is a potent inhibitor of acid ceramidase (IC50 = 12.8 nM for the human enzyme). It inhibits acid ceramidase activity and increases levels of C16 dihydro ceramide and C16 ceramide in A375, G361, M14, MeWo, MNT-1, and SK-MEL-28 melanoma cells. ARN14988 also reduces growth of A375 and G361 melanoma cells (EC50s = 41.8 and 67.7 μM, respectively).
T36497	CAY10735 CAY10735	Others	Others
	CAY10735 is an anticancer compound.1 It inhibits proliferation in a panel of melanoma and breast, pancreatic, and lung cancer cell lines (IC50s = 0.674-11.56 μM). CAY10735 inhibits migration of and the epithelial-to-mesenchymal transition (EMT) in A375 and B16/F10 melanoma cells in vitro in a concentration-dependent manner. It reduces the viability of spheroid A375 and B16/F10 cells (IC50s = 3.04 and 1.24 μM, respectively) and increases production of reactive oxygen species (ROS) in these cells ...
T79048	MEK-IN-6 hydrate	MEK	MAPK
	MEK-IN-6 hydrate（compound 69）为MEK抑制剂，其对A375细胞展现出强效性，IC50仅为2 nM。
T79047	MEK-IN-6	ERK	MAPK
	MEK-IN-6（Example 69）是一种针对MEK的抑制剂，在A375细胞中有效抑制ERK1/2（THR202/Tyr204）的磷酸化，其IC50值为2 nM。此化合物主要应用于癌症研究领域。
T78190	ERK1/2 inhibitor 9	ERK	MAPK
	ERK1/2 inhibitor 9 (Probe 1)为共价ERK1/2抑制剂，具备亚微摩尔级别的细胞活性(A375 GI50=0.47 μM)，能够下调磷酸化ERK1/2。通过与反式环辛烯(TCO)标记的Tz-Thalidomide相结合，ERK1/2 inhibitor 9可形成ERK-CLIPTAC，进而触发ERK1/2的降解。
T36035	CAY10784	Others	Others
	CAY10784 is a STAT3 inhibitor (IC50= 0.74 μM in a reporter assay) and a derivative of WP1066 .1It inhibits proliferation of HeLa, Caco-2, A549, A375, U87MG, and HL-60 cancer cells (IC50s = 1.8, 1.8, 3, 2.8, 2.3, and 1.2 μM, respectively) but not PC3 or HT-29 cancer cells (IC50s = >10 μM for both). CAY10784 is also active againstH. pyloriandC. jejuni(MICs = 1.6 and 4.7 μM, respectively).2 1.Lü, Z., Li, X., Li, K., et al.Structure-activity study of nitazoxanide derivatives as novel STAT3 pathway i...
T79144	PROTAC MEK1 Degrader-1	PROTACs	PROTAC
	PROTACMEK1Degrader-1是一种针对MEK1的PROTAC，显示出pIC50值为7.0。该化合物由MEK1抑制剂与von Hippel-Lindau配体构成，能够抑制ERK1/2的磷酸化，并对A375细胞展现出抗增殖活性。
T76003	MSG606 TFA
	MSG606 TFA, a potent antagonist of the human MC1 receptor (IC50 = 17 nM), functions as a partial agonist at the human MC3 and MC5 receptors (EC50 values of 59 and 1300 nM, respectively). It demonstrates binding affinity for A375 melanoma cells in vitro and selectively reverses induced hyperalgesia in female mice without affecting male mice.
T64150	CX-5461 dihydrochloride	Others	Others
	CX-5461 dihydrochloride 是一种有效的、口服具有活力的 Pol I 介导的 rRNA synthesis 抑制剂，能够作用于 HCT-116 细胞 (IC50: 142 nM)，A375 细胞 (IC50: 113 nM) 和 MIA PaCa-2 细胞 (IC50: 54 nM)，对 Pol II 作用较小 (IC50≥25 μM)。
T28862	ST-168 ST168,ST 168	Others	Others
	ST-168 is a potent inhibitor of PI3K and MEK. ST-168 displays improved PI3K and MEK1 isoform inhibition. ST-168 demonstrated a 2.8-, 2.7-, 23-, and 2.5-fold improved inhibition toward the PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ isoforms and a 2.2-fold improvement
T36968	ARN-21934	Topoisomerase	DNA Damage/DNA Repair
	ARN-21934 是高选择性的人拓扑异构酶 II α 抑制剂，具有血脑屏障通透性。依托泊苷抑制 DNA 松弛的IC50为120 μM，ARN-21934 抑制 DNA 松弛的IC50为 2 μM。ARN-21934具有良好的体内药代动力学特性。
T63542	SHR902275	Others	Others
	SHR902275 是选择性的、有效的、口服具有活力的 RAF 抑制剂，能够靶向 RAS 突变癌症。 SHR902275 能够作用于 cRAF (IC50: 1.6 nM)、bRAFwt (IC50: 10 nM)、bRAFV600E (IC50: 5.7 nM)。SHR902275 具有细胞生长抑制效果，能够作用于 H358 细胞 (GI50: 1.5 nM)、A375 细胞 (GI50: 0.17 nM)、Calu6 细胞 (GI50: 0.4 nM) 和 SK-MEL2 细胞 (GI50: 0.32 nM)。
T70424	EBI-907	Others	Others
	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...
T35525	PI3-Kinase α Inhibitor 2 PI3-Kinase α Inhibitor 2	Others	Others
	Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3' hydroxyl position of PIs to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3. PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits, whereas PI3Kγ is a class 1B PI3K composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit. PI3Kα inhibitor 2 is a selective inhibitor of PI3Kα with IC50 values of 2, 16, 660, and 220 nM for the α, β, γ, and 2Cβ isoforms, respectively. It...
T36848	Combretastatin A-1 Combretastatin A1	Akt; Microtubule Associated	Cytoskeletal Signaling; PI3K/Akt/mTOR signaling
	Combretastatin A-1 是一种有效的微管抑制剂，具有抗肿瘤和抗血管活性，通过微管蛋白解聚介导的 AKT 失活抑制 Wnt/β-catenin 通路发挥作用，可用于研究肝癌。

化合物

Antiproliferative agent-13

Cat.No: T9974

Target: Dehydrogenase

Cat.No: T24269

Synonym: KPT251

Target: Others

Cat.No: T11898

Target: Raf

PROTAC BRAF-V600E degrader-1

Cat.No: T8745

Synonym: Compound 23

Target: Raf, PROTACs

Cat.No: T23861

Synonym: CAY-10526,BTH,CAY 10526

Target: Prostaglandin Receptor

Cat.No: T4314

Synonym: EPZ020411 2HCl

Target: Histone Methyltransferase

Cat.No: T36902

Synonym: RA375

Target: Proteasome

Cat.No: T15486

Target: Others

Cat.No: T4356

Synonym: Compound 3A

Target: DNA/RNA Synthesis

Cat.No: T6882

Synonym: DP-4978

Target: Raf, Autophagy

Cat.No: T36674

Target: Apoptosis, ERK

Cat.No: T2668

Synonym: JNK Inhibitor XVI

Target: JNK, c-Kit

Cat.No: T6843

Synonym: G-868,GDC0623,RG 7421,MEK inhibitor 1

Target: Apoptosis, MEK

Cat.No: T84790

Target: Others, ADC Cytotoxin

Cat.No: T36460

Synonym: CAY10736

Target: Others

Cat.No: T61226

Target: Others

Cat.No: T63365

Target: Others

Cat.No: T36468

Target: Others

Cat.No: T36497

Synonym: CAY10735

Target: Others

MEK-IN-6 hydrate

Cat.No: T79048

Target: MEK

Cat.No: T79047

Target: ERK

ERK1/2 inhibitor 9

Cat.No: T78190

Target: ERK

Cat.No: T36035

Target: Others

PROTAC MEK1 Degrader-1

Cat.No: T79144

Target: PROTACs

Cat.No: T76003

CX-5461 dihydrochloride

Cat.No: T64150

Target: Others

Cat.No: T28862

Synonym: ST168,ST 168

Target: Others

Cat.No: T36968

Target: Topoisomerase

Cat.No: T63542

Target: Others

Cat.No: T70424

Target: Others

PI3-Kinase α Inhibitor 2

Cat.No: T35525

Synonym: PI3-Kinase α Inhibitor 2

Target: Others

Combretastatin A-1

Cat.No: T36848

Synonym: Combretastatin A1

Target: Akt, Microtubule Associated

Cat. No.	Product Name	Target	Signaling Pathways
T0934	Nicotinamide Nicotinic acid amide,Vitamin B3,Niacinamide,烟酰胺,Vitamin PP	Sirtuin; Endogenous Metabolite	Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism
	Nicotinamide 是维生素 B3 的吡啶核苷形式，可作为烟酰胺腺嘌呤二核苷酸或 NAD+ 的前体，可通过膳食摄入来补充，能预防或治疗黑舌病和糙皮病。
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。
TQ0170	Desacetylcinobufagin Deacetylcinobufagin,去乙酰华蟾蜍精	Others	Others
	Desacetylcinobufagin (Deacetylcinobufagin) 是一种天然化合物，可用于微生物转化。
T5S0506	Rotundic acid Rutundic acid,铁冬青酸	Apoptosis; Others; p38 MAPK; Akt; mTOR	Apoptosis; Cytoskeletal Signaling; MAPK; Others; PI3K/Akt/mTOR signaling
	Rotundic acid (Rutundic acid) 是一种从圆形肠球菌中获得的三萜类天然产物，具有抗炎和保护心脏的能力。它可通过 AKT/mTOR 和 MAPK 途径在肝细胞癌中诱导 DNA 损伤和细胞凋亡。
T5S0167	Atractylenolide I 白术内酯 I,白术内酯I；苍术内酯I	IL Receptor; TNF; TLR; JAK; STAT	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells
	Atractylenolide I 是从白术根中得到的一种倍半萜烯，具有神经保护、抗过敏、抗炎和抗癌等多种生物活性。它是一种TLR4拮抗剂，在 A375 细胞中，能够降低JAK2和STAT3的磷酸化水平。
TN3619	Cedrusin	PARP; Caspase	Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Proteases/Proteasome
	Cedrusin shows a cytotoxic effect on A375 and HeLa cells.
TN7544	(−)-Voacangarine (−)-Voacristine,NSC 306219	Others	Others
	(–)-Voacangarine, an indole alkaloid isolated from V. africana, exhibits cytotoxicity towards various cell lines including HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 values of 20 µg/ml. Additionally, it demonstrates cytostatic effects on wild-type S. cerevisiae and is cytotoxic to Δrad3-e5 and Δrad6-1 mutant strains of S. cerevisiae, which have defects in DNA strand break repair and the mutagenic repair pathway, respectively.
TN5930	Ocotillone
	Ocotillone has potent antibacterial activity against Gram-negative bacteria, P. aeruginosa and S. typhimurium, that are without hemolytic activity, whereas it has weak antimicrobial activity against Gram-positive bacteria and fungi. Ocotillone shows only
T81201	Sartorypyrone B
	Sartorypyrone B为Chevalone C的2β-乙酰氧基衍生物，由海绵源真菌Neosartorya tsunodae(KUFC 9213)的培养物中乙酸乙酯提取得到。该化合物对MCF-7、NCI-H460和A375-C5细胞系展示出较强的生长抑制活性，GI50s值分别为17.8、20.5和25.0 μM，显示其在乳腺癌、非小细胞肺癌和黑色素瘤研究中的应用潜力。
T35754	Aszonapyrone A	Others	Others
	Aszonapyrone A is a meroditerpene fungal metabolite that has been found in Neosartorya and has diverse biological activities.1,2,3 It inhibits the growth of MCF-7, NCI H460, and A375-C5 cancer cells (GI50s = 13.6, 11.6, and 10.2 μM, respectively).1 Aszonapyrone A is active against multidrug-resistant isolates of S. aureus, E. faecalis, and E. faecium (MICs = 8, 16, and 16 μg/ml, respectively) and inhibits S. aureus biofilm formation.2 It is also active against P. falciparum in vitro (IC50 = 1.34...
TN4774	Physalin A	ERK; BCL; p38 MAPK; NF-κB; Androgen Receptor; ROS; JAK; JNK; STAT; p53; Autophagy	Angiogenesis; Apoptosis; Autophagy; Chromatin/Epigenetic; Endocrinology/Hormones; Immunology/Inflammation; JAK/STAT signaling; MAPK; NF-κB; Stem Cells
	Physalin A exerts anti-tumor activity in non-small cell lung cancer cell lines by suppressing JAK/STAT3 signaling, it inhibits androgen-independent prostate cancer cell growth through activation of cell apoptosis and downregulation of androgen receptor ex

天然产物

Cat.No: T0934

Synonym: Nicotinic acid amide,Vitamin B3,Niacinamide,烟酰胺,Vitamin PP

Target: Sirtuin, Endogenous Metabolite

Cat.No: T4518

Target: ERK, NF-κB

Desacetylcinobufagin

Cat.No: TQ0170

Synonym: Deacetylcinobufagin,去乙酰华蟾蜍精

Target: Others

Cat.No: T5S0506

Synonym: Rutundic acid,铁冬青酸

Target: Apoptosis, Others, p38 MAPK, Akt, mTOR

Atractylenolide I

Cat.No: T5S0167

Synonym: 白术内酯 I,白术内酯I；苍术内酯I

Target: IL Receptor, TNF, TLR, JAK, STAT

Cat.No: TN3619

Target: PARP, Caspase

(−)-Voacangarine

Cat.No: TN7544

Synonym: (−)-Voacristine,NSC 306219

Target: Others

Cat.No: TN5930

Sartorypyrone B

Cat.No: T81201

Cat.No: T35754

Target: Others

Cat.No: TN4774

Target: ERK, BCL, p38 MAPK, NF-κB, Androgen Receptor, ROS, JAK, JNK, STAT, p53, Autophagy

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