検索結果

Search Results for " A375 "

ターゲット

阻害剤

天然化合物

カタログ番号	製品名	別名	ターゲット
T9974	Antiproliferative agent-13		Dehydrogenase
	Antiproliferative agent-13 is a compound with antiproliferative activity.		Dehydrogenase
T24269	KPT-251	KPT251	Others
	KPT-251 is a selective nuclear export inhibitor.		Others
T11898	LXH254		Raf
	LXH254 is a potent C-Raf and B-Raf inhibitor.		Raf
T8745	PROTAC BRAF-V600E degrader-1	Compound 23	Raf
	PROTAC BRAF-V600E degrader-1 (Compound 23) selectively induces degradation of BRAF-V600E but not wildtype BRAF.		Raf
T23861	CAY10526	CAY-10526,BTH,CAY 10526	Prostaglandin Receptor
	CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.		Prostaglandin Receptor
T4314	EPZ020411	EPZ020411 2HCl	Histone Methyltransferase
	EPZ020411 is a specific and effective inhibitor of PRMT6 (IC50=10 nM).		Histone Methyltransferase
T36902	RA375	RA375	Proteasome
	RA375, an inhibitor of RPN13 (26S proteasome regulatory subunit), enhances UPR signaling, ROS production, and apoptosis. Demonstrating ten times the efficacy against cancer lines compared to RA190, RA375 owes its increas...		Proteasome
T15486	HLM006474		Others
	HLM006474 is a pan inhibitor of E2F. This inhibits E2F4 DNA-binding (IC50: 29.8 µM in A375 cells).		Others
T4356	POL1-IN-1	Compound 3A	DNA/RNA Synthesis
	POL1-IN-1 (Compound 3A) can effectively inhibit the transcription of RNA polymerase I in the A375 malignant melanoma cell line but has no effect on polymerase II.		DNA/RNA Synthesis
T6882	LY3009120	DP-4978	Raf , Autophagy
	LY3009120 (DP-4978) is a potent pan-Raf inhibitor with IC50 of 44 nM, 31-47 nM, and 42 nM for A-raf, B-Raf, and C-Raf in A375 cells, respectively. Phase 1.		Raf , Autophagy
T2668	JNK-IN-8	JNK Inhibitor XVI	JNK , c-Kit
	JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ in A375 cell line.		JNK , c-Kit
T36674	DMU-212		Apoptosis , ERK
	DMU-212 is a methylated derivative of Resveratrol , with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities. DMU-212 induces mitotic arrest via induction of apoptosis and activation of ERK1/2...		Apoptosis , ERK
T6843	GDC-0623	G-868,GDC0623,RG 7421,MEK inhibitor 1	Apoptosis , MEK
	GDC-0623 (RG 7421) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.		Apoptosis , MEK
T36468	ARN14988
	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,...
T36497	CAY10735	CAY10735
	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-mese...
T79048	MEK-IN-6 hydrate		MEK
	MEK-IN-6 hydrate (compound 69), a MEK inhibitor, exhibits an IC50 value of 2 nM in A375 cells [1].		MEK
T36460	CAY10736	CAY10736
	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 ...
T61226	HDHODH-IN-9
	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 chara...
T63365	RAF-IN-1
	RAF-IN-1 is a potent inhibitor of b/cRAF, acting on cRAF (IC50: 3.8 nM), bRAFwt (IC50: 36 nM), bRAFV600E (IC50: 29.4 nM) and inhibiting A375 and H358 cell lines carrying the bRAFV600E mutation with a GI50 of 3.4 and 2.9 ...
T79047	MEK-IN-6		ERK
	MEK-IN-6 (Example 69), a potent MEK inhibitor, effectively inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells, with an IC50 of 2 nM, making it valuable for cancer research [1].		ERK
T64150	CX-5461 dihydrochloride
	CX-5461 dihydrochloride is a potent, orally active inhibitor of Pol I-mediated rRNA synthesis that acts on HCT-116 cells (IC50: 142 nM), A375 cells (IC50: 113 nM) and MIA PaCa-2 cells (IC50: 54 nM), and to a lesser exten...
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 ...
T79144	PROTAC MEK1 Degrader-1		PROTACs
	PROTAC MEK1 Degrader-1, a targeted protein degradation agent, combines a MEK1 inhibitor with a von Hippel-Lindau ligand to effectively inhibit ERK1/2 phosphorylation. With a pIC50 value of 7.0, it exhibits antiproliferat...		PROTACs
T78190	ERK1/2 inhibitor 9		ERK
	ERK1/2 Inhibitor 9 (Probe 1), a covalent antagonist of ERK1/2, exhibits sub-micromolar efficacy in cellular assays (A375 GI50=0.47 μM) and facilitates the reduction of phospho-ERK1/2 levels. When conjugated with trans-cy...		ERK
T36968	ARN-21934		Topoisomerase
	ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etopo...		Topoisomerase
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...
T63542	SHR902275
	SHR902275 is a selective, potent, orally active RAF inhibitor capable of targeting RAS mutant cancers. SHR902275 acts on cRAF (IC50: 1.6 nM), bRAFwt (IC50: 10 nM), bRAFV600E (IC50: 5.7 nM). SHR902275 has cell growth inhi...
T36035	CAY10784
	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 ...
T28862	ST-168	ST168,ST 168
	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 i...
T35525	PI3-Kinase α Inhibitor 2	PI3-Kinase α Inhibitor 2
	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 ...
T36848	Combretastatin A-1	Combretastatin A1	Akt , Microtubule Associated
	Combretastatin A-1 is a potent microtubule inhibitor with anti-tumour and anti-vascular activity, acting through microtubule protein depolymerisation-mediated inactivation of AKT to inhibit the Wnt/β-catenin pathway, and...		Akt , Microtubule Associated

Compounds

Antiproliferative agent-13

T9974

Synonym:

Target: Dehydrogenase

PROTAC BRAF-V600E degrader-1

Synonym: CAY-10526,BTH,CAY 10526

Target: Prostaglandin Receptor

EPZ020411

T4314

Synonym: EPZ020411 2HCl

Target: Histone Methyltransferase

Target: DNA/RNA Synthesis

LY3009120

T6882

Synonym: DP-4978

Target: Raf, Autophagy

JNK-IN-8

T2668

Synonym: JNK Inhibitor XVI

Target: Apoptosis, ERK

GDC-0623

T6843

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

Target: Apoptosis, MEK

CX-5461 dihydrochloride

PROTAC MEK1 Degrader-1

Target: Topoisomerase

Synonym: ST168,ST 168

Target:

PI3-Kinase α Inhibitor 2

T35525

Synonym: PI3-Kinase α Inhibitor 2

Target:

Combretastatin A-1

T36848

Synonym: Combretastatin A1

Target: Akt, Microtubule Associated

カタログ番号	製品名	別名	ターゲット
T4518	Licochalcone D		ERK , NF-κB
	Licochalcone D may be a potential drug for human melanoma treatment by inhibiting proliferation, inducing apoptosis via the mitochondrial pathway and blocking cell migration and invasion. Licochalcone D has cardioprotect...		ERK , NF-κB
TQ0170	Desacetylcinobufagin	Deacetylcinobufagin	Others
	Desacetylcinobufagin (Deacetylcinobufagin) , a natural product, shows potent activities against Hela and A375 cells in vitro.		Others
T5S0506	Rotundic acid	Rutundic acid	Apoptosis , Others , p38 MAPK , Akt , mTOR
	Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) c...		Apoptosis , Others , p38 MAPK , Akt , mTOR
T5S0167	Atractylenolide I		IL Receptor , TNF , TLR , JAK , STAT
	1. Atractylenolide-I has an anti-inflammatory effect by inhibiting TNF-α and IL-6 production; ameliorates sepsis syndrome, liver and kidney functions by reduction of pro-inflammatory cytokines and LPS. 2. Atractylenolide...		IL Receptor , TNF , TLR , JAK , STAT
TN3619	Cedrusin		PARP , Caspase
	Cedrusin shows a cytotoxic effect on A375 and HeLa cells.		PARP , Caspase
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 bacteri...
T35754	Aszonapyrone A
	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, ...
T81201	Sartorypyrone B
	Sartorypyrone B, a 2β-acetoxyl analogue of chevalone C, is derived from the ethyl acetate extract of the culture of Neosartorya tsunodae (KUFC 9213), a fungus associated with marine sponges. This compound demonstrates po...
TN4774	Physalin A		ERK , BCL , p38 MAPK , NF-κB , Androgen Receptor , ROS , JAK , JNK , STAT , p53 , Autophagy
	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 dow...