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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC4169 ASC-J9
ASC-J9, is antitumor agent. ASC-J9 suppresses castration-resistant prostate cancer growth via degradation of full-length and splice variant androgen receptors.
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DC7068 AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) (IC50 = 8 nM). AS-605240 displays 30-fold selectivity over PI3Kδ and PI3Kβ and 7.5-fold selectivity over PI3Kα.
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DC20684 AS2677131
AS2677131(AS 2677131, AS-2677131) is a novel potent, oral PIKfyve inhibitor that selectively decreases c-Rel binding to gene promoters of IL-12p40 and IL-1β, regulates cytokine production through PIKfyve-c-Rel pathway ( IL-12p40 IC50=4 nM).
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DC20683 AS2541019
AS2541019 is a novel potent, selective, orally active PI3Kδ inhibitor with IC50 of 20.1 nM, >100-fold selectivity over other PI3K isoforms.
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DC20682 AS2521780
AS2521780 is a potent, selective, orally bioavailable PKCθ inhibitor that inhibits combinant human PKCθ enzyme with IC50 of 0.48 nM, >30-fold higher than other PKC isoforms.
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DC22766 AS-1949490
AS-1949490 (AS1949490) is a potent, selective SHIP2 inhibitor with IC50 of 0.34/0.62 uM for mouse/human SHIP2.
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DC22002 AS1928370
AS1928370 (ASP8370) is a potent, selective, orally available TRPV1 antagonist with IC50 of 0.51 uM, shows no inhibitory effects on TRPV4, TRPA11, and TRPM8 at 10 uM.
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DC20687 AS 2553627
AS 2553627 (AS2553627) is a novel potent, selective pan-JAK inhibitor with IC50 of 0.46, 0.30, 0.14 and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively.
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DC12614 Arylsulfonamide 64B
Arylsulfonamide 64B (HIF inhibitor 64B) is a small molecule HIF pathway inhibitor, blocks hypoxia-induced expression of c-Met and CXCR4 and uveal melanoma (UM) cell migration.
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DC21451 Arterolane
Arterolane (OZ277.
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DC21452 Artefenomel
Artefenomel (OZ439) is a novel, next-generation antimalarial ozonide that demonstrates high potentcy against P. falciparum in vitro and P. berghei in vivo (K1/NF54, IC50=2.0/3.2 nM)..
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DC9495 ARRY-520 (R enantiomer)
ARRY-520 R enantiomer is the R form of ARRY-520, which is a synthetic, small molecule kinesin spindle protein (KSP) inhibitor with IC50 of 6 nM.
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DC20679 ARRY-502
ARRY-502 is an orally bioavailable, potent and selective antagonist of the prostaglandin D2 receptor (CRTh2) for treatment of mild to moderate Th2-driven asthma..
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DC8486 Varlitinib(ARRY-334543)
ARRY-334543 is a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases.
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DC12460 ARP101
ARP101 (ARP-101) is a selective MMP-2 inhibitor, induces autophagy-associated cell death in cancer cells.
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DC20678 ARN 726
ARN726 is a potent, selective, orally bioavailable N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 63 nM (r-NAAA) and 27 nM (h-NAAA).
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DC20676 ARN-3261
ARN-3261 is a potent, selective, orally available salt inducible kinase SIK2 and SIK3 inhibitor with IC50 of 11 nM and 19 nM, respectively.
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DC22000 ARN19874
ARN19874 (ARN-19874) is the first selective, cell-active inhibitor of N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) with IC50 of 33.7 uM.
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DC12569 ARN14494
ARN14494 (ARN-14494) is a potent, small molecule serine palmitoyltransferase (SPT) inhibitor with IC50 of 27.3 nM.
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DC20677 ARN 077
ARN077 is the first potent, selective N-acylethanolamine acid amidase (NAAA) inhibitor with IC50 of 7 nM on both rat NAAA and human NAAA.
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DC23605 AR-HO47108
AR-HO47108 is a potent, selective acid pump antagonist (potassium-competitive acid blocker or P-CAB) that reversiblely inhibits gastric H+/K+-ATPase with pIC50 of 7.0.
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DC12359 Arg-AMS
Arg-AMS is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.
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DC22544 AR-C155858
AR-C155858 is a potent monocarboxylate transporter MCT1 and MCT2 with Ki of 2.3 nM and <10 nM, displays no activity at MCT4.
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DC20675 AR-C102222
AR-C102222 is a potent, selective iNOS inhibitor with IC50 of 35 nM, dislapys 3,000-fold and 20-fold selectivity over eNOS and nNOS respectively.
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DC20674 AR03
AR03 (AR-03, AR 03, Ape1 repair inhibitor 03) is a novel small molecule inhibitor of DNA repair protein apurinic/apyrimidinic endonuclease 1 (APE1) endonuclease activity with IC50 of 5 uM.
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DC20673 AQW-051
AQW-051 is a novel, potent and selective, orally bioavailable, brain-penetrant α7 nAChR partial agonist with pKd of 7.56.
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DC12155 AQ-13 dihydrochloride
AQ-13 dihydrochloride is an aminoquinoline antimalarial drug that is effective against chloroquine-resistant strains of Plasmodium falciparum.
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DC23311 AQ-101
AQ-101 is a novel small-molecule anthraquinone analog that induces MDM2 protein degradation (Kd=0.37 uM) through a self-ubiquitination and proteasome-mediated mechanism, leading to activation of p53.
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DC11195 APX2014
APX2014 (APX-2014) is a novel potent inhibitor of reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) with IC50 of 0.2 uM for redox EMSA inhibition.
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DC11194 APX2009
APX2009 (APX-2009) is a novel potent inhibitor of reduction-oxidation factor 1-apurinic/apyrimidinic endonuclease 1 (Ref-1/APE1) with IC50 of 0.45 uM for redox EMSA inhibition.
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