ABT-869 | Dual VEGFR and PDGFR kinase inhibitor
ABT-869 (796967-16-3) ia a structurally novel, potent inhibitor of receptor tyrosine kinases inhibiting VEGFR and PDGFR and related kinases with IC50s= 3, 4, 4, 66, 3
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ABT-869 (796967-16-3) ia a structurally novel, potent inhibitor of receptor tyrosine kinases inhibiting VEGFR and PDGFR and related kinases with IC50s= 3, 4, 4, 66, 3
PF-543 (1706522-79-3) is a potent (IC50 = 2.0 nM) and selective (>100-fold over SphK2) reversible inhibitor of sphingosine kinase-1 (SphK1).1 It induced autophagy in head and neck squamous
Vacuolin-1 (351986-85-1) inhibits autophagy via inhibition of Ca2+-dependent fusion of lysosomes with the plasma membrane and the release of lysosomal content and has no effect on
(4R,4aS)-18-Ethenyl-4,4a-dihydro-3,4-bis(methoxycarbonyl)-4a,8,14,19-tetramethyl-24H,26H-benzo[b]porphine-9,13-dipropanoic acid monomethyl ester
iPHF8 is a specific inhibitor (IC50 = 2.01 µM; EC50 = 2 µM in HeLa cells) of the human non-heme 2-oxoglutarate JmjC domain oxygenase/lysine demethylase PHF8.
Lomitapide (182431-12-5) is a potent (IC50 = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia.1,2
HC-258 is a covalent inhibitor of TEAD (transcriptional enhanced associate domain), an important component of the Hippo pathway. It was able to reduce gene expression levels
STF-118804 (894187-61-2) is a potent and selective next generation inhibitor of nicotinamide phosphoribosyl transferase (NAMPT), inhibiting NAD+ biosynthesis from nicotinamide.1 It reduced the viability of most B-ALL cells
CBL0137 (1197996-80-7) is an anticancer agent that activates p53 and suppresses NF-kB via trapping of the FACT (facilitates chromatin transcription) complex, an important histone chaperone that mediates nucleosome
WM-1119 (2055397-28-7) is a potent and selective inhibitor of the MYST family histone acetyltransferase (HAT) KAT6A (MOZ) – IC50 = 6.3 nM.1,2 Induces cell cycle exit and cellular
Honokiol-DCA (HDCA; 1620160-42-0), a synthetic bis-dichloroacetate ester of the natural product honokiol, is an allosteric inhibitor of the mitochondrial chaperone TRAP1.1 It binds to an allosteric site
Selpercatinib (2152628-33-4) is a potent (IC50 = 0.45 nM)1 and selective inhibitor of RET kinase.2 Clinically relevant for the treatment of RET-altered non-small cell lung cancer3
Raltitrexed (112887-68-0) is an inhibitor of thymidylate synthase with significantly increased potency in many cancer cell lines when compared with 5-fluorouracil.1,2 It is also an inhibitor
MRTX849 (2326521-71-3) is a potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced
Dynarrestin (2222768-84-3) is a reversible inhibitor of cytoplasmic dyneins 1 and 2.1 It inhibits dynein 1-dependent microtubule binding and motility without affecting ATP hydrolysis as well
AOH1996 (2089314-64-5) inhibits proliferating cell nuclear antigen (PCNA), an enzyme critical to DNA replication and repair processes.1 It enhances the interaction between PCNA and RPB1 subunit
TH10785 (1002801-51-5) is an 8-oxo guanine DNA glycosylase 1 (OGG1) activator. Oxidative DNA damage is recognized by OGG1 which then excises 8-oxoguanine, leaving a substrate for
Ochratoxin A (303-47-9) is a mycotoxin that causes widespread contamination in foodstuffs and environments thus causing health risks to humans and animals.1 It has been shown to
JNK-IN-8 (1410880-22-6) is a potent and selective irreversible JNK inhibitor (IC50s=4.67, 18.7 and 0.98 nM for JNK1, 2 and 3 respectively).1 JNK blockade with JNK-IN-8 overcomes
S07-2010 (1223194-71-5) is a pan-aldo-keto reductase 1C (AKR1C) inhibitor (IC50’s for AKR1C isoforms: 1C1 = 470 nM, 1C2 = 730 nM, 1C3 = 190 nM, 1C4
IACS-010759 (1570496-34-2) is a potent (IC50 = 1.1 nM isolated mouse complex I) and selective inhibitor of complex I of the mitochondrial electron transport chain (OXPHOS). IACS-010759
iPHF8 is a specific inhibitor (IC50 = 2.01 µM; EC50 = 2 µM in HeLa cells) of the human non-heme 2-oxoglutarate JmjC domain oxygenase/lysine demethylase PHF8.
SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homologue (BRM), together with its close homologue Brahma-related gene 1 (BRG1),
WM-1119 (2055397-28-7) is a potent and selective inhibitor of the MYST family histone acetyltransferase (HAT) KAT6A (MOZ) – IC50 = 6.3 nM.1,2 Induces cell cycle exit and cellular
HC-258 is a covalent inhibitor of TEAD (transcriptional enhanced associate domain), an important component of the Hippo pathway. It was able to reduce gene expression levels
SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homologue (BRM), together with its close homologue Brahma-related gene 1 (BRG1),
AOH1996 (2089314-64-5) inhibits proliferating cell nuclear antigen (PCNA), an enzyme critical to DNA replication and repair processes.1 It enhances the interaction between PCNA and RPB1 subunit
Nintedanib (656247-17-5) is a potent inhibitor of VEGFR, PDGFR, FGFR (IC50 = 13-34 nM for VEGFR, 59-65 nM for PDGFR and 37-108 nM for FGFR subtypes).1 Also
Pazopanib (444731-52-6) inhibits multiple receptor tyrosine kinases including VEGFR1,2 and 3 (IC50s=10, 30, 47 nM respectively) and PDGFRα, β and c-Kit (IC50s=71, 84, 74 nM respectively)
MRTX849 (2326521-71-3) is a potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced
LDC1267 (1361030-48-9) is a potent and selective inhibitor of the TAM kinases Tyro3, Axl, and Mer (IC50s respectively: 8 nM, <5 nM, 29 nM).1 It was
JH-X-119-01 (2227368-54-7) is a highly selective (only significantly inhibited YSK4 and MEK3 in a panel of over 300 kinases) and potent (IC50 = 9 nM) covalent
Dubermatinib (1341200-45-0) is a potent (IC50 = 27 nM) inhibitor of the TAM family kinase AXL.1 It displayed potent activity against the pancreatic tumor cell line PSN-1 (IC50 =
JNK-IN-8 (1410880-22-6) is a potent and selective irreversible JNK inhibitor (IC50s=4.67, 18.7 and 0.98 nM for JNK1, 2 and 3 respectively).1 JNK blockade with JNK-IN-8 overcomes
GSK2636771 (1372540-25-4) is a potent, selective (>1000-fold over α, 10-fold over δ, and >2000-fold over γ), and orally bioavailable inhibitor of PI3Kß (IC50 = 5.2 nM).1
LDC1267 (1361030-48-9) is a potent and selective inhibitor of the TAM kinases Tyro3, Axl, and Mer (IC50s respectively: 8 nM, <5 nM, 29 nM).1 It was
Decoyinine (2004-04-8) is a non-competitive and reversible inhibitor of GMP synthase (GMPS, IC50=17.3 µM).1 GMPS was shown to be a positive regulator of invasiveness in melanoma
P053 (1022417-69-1) is a selective inhibitor of protein phosphatase 5 (PP5) – IC50 = 706 nM.1 PP5 regulates signaling cascades that are responsible for tumor initiation,
SR1078 (1246525-60-9) is an agonist of the orphan nuclear receptors RORα and RORγ.1 It attenuated intrapancreatic pathological changes in mouse models of chronic pancreatitis via restoration of the circadian
Isothiocyanate constituents of cruciferous vegetables are potent chemopreventive agents for carcinogen-induced cancers in rodents.1 Phenylhexyl isothiocyanate (PHITC; CAS 133920-06-6) was the most potent in a series
CBL0137 (1197996-80-7) is an anticancer agent that activates p53 and suppresses NF-kB via trapping of the FACT (facilitates chromatin transcription) complex, an important histone chaperone that mediates nucleosome
7-Dehydrocholesterol (434-16-2) is an endogenous cholesterol precursor and is photochemically converted to vitamin D3 in the skin.1 It has recently been found to be an endogenous
P053 (1022417-69-1) is a selective inhibitor of protein phosphatase 5 (PP5) – IC50 = 706 nM.1 PP5 regulates signaling cascades that are responsible for tumor initiation,
Isothiocyanate constituents of cruciferous vegetables are potent chemopreventive agents for carcinogen-induced cancers in rodents.1 Phenylhexyl isothiocyanate (PHITC; CAS 133920-06-6) was the most potent in a series
Indisulam (165668-41-7) was originally described as a potent antitumor agent that targeted the G1 phase of cell cycle via suppression of activation of CDK2 and cyclin
Iberdomide (1323403-33-3) is a modulator of the cullin ring ligase 4-cereblon E3 ubiquitin ligase complex with higher affinity (IC50 = 60 nM) than lenalidomide and pomalidomide
CC-90009 (1860875-51-9) is a modulator of the cullin ring ligase 4-cereblon E3 ubiquitin ligase complex that specifically targets GSPT1 (G1 to S phase transition 1; EC50
Lomitapide (182431-12-5) is a potent (IC50 = 8 nM) inhibitor of microsomal triglyceride transfer protein (MTP or MTTP) and is clinically useful in treating familial hypercholesterolemia.1,2
Decoyinine (2004-04-8) is a non-competitive and reversible inhibitor of GMP synthase (GMPS, IC50=17.3 µM).1 GMPS was shown to be a positive regulator of invasiveness in melanoma
PITSTOP2 (1332879-52-3) inhibits clathrin-mediated endocytosis via blockade of endocytic ligand association with the clathrin terminal domain leading to clathrin coat assembly inhibition.1 It was able to
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