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Cat. No. Product Name Field of Application Chemical Structure
DC21177 JNJ 39758979 Featured JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity.
DC24048 NVP-BKM120 hydrochloride Featured A potent, selective, orally bioavailable inhibitor of class I PI3K isoforms with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/β/δ/γ, respectively.
DC23552 AS-2444697 HCl Featured A potent, selective, orally bioavailable IRAK-4 inhibitor that potently inhibits human and rat IRAK-4 activity with subnanomolar order, >30-fold selectivity over IRAK-1.
DC21607 SB-649868 Featured SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).
DC11748 LY2033298 Featured LY2033298 is a robust allosteric potentiator that is highly selective for the human M4 muscarinic acetylcholine receptor subtype. LY2033298 enhances inhibition by oxotremorine of light-induced phase shifts in hamster circadian activity rhythms.
DC11691 NSC95397 Featured A potent, selective, reversible Cdc25 dual specificity phosphatase inhibitor with Ki of 32/96/40 nM for Cdc25A/B/C, respectively.
DC11978 SB 265610 Featured SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist.
DC21321 ML349 Featured A potent, specific acyl protein thioesterase 2 (APT-2, LYPLA2) inhibitor with IC50 of 144 nM and Ki of 120 nM, >20-fold selectivity over APT-1 and serine hydrolase enzyme family.
DC23074 Sivelestat Featured A potent, specific and competitive inhibitor of human neutrophil elastase with IC50 of 44 nM.
DC23494 GRI 977143 Featured A potent, specific and nonlipid agonist of LPA2 receptor with EC50 of 3.3 uM, does not activate any of the other LPA GPCRs (>10 uM).
DC24105 MK-0591(Quiflapon ) Featured A potent, specific and orally active 5-Lipoxygenase-activating protein (FLAP) inhibitor with IC50 of 1.6 nM in FLAP binding assay.
DC21807 VU 0465350 Featured VU 0465350 is a potent, specific BMP receptor activin receptor-like kinase 3 (ALK3) antaognist with Ki of 92.3 nM; shows no activity for ALK2/4/5, also shows affinity for TGFBR2, VEGFR2 and AMPK; blocks SMAD phosphorylation in vitro and in vivo, and enhances liver regeneration after partial hepatectomy.
DC21794 VH 298 Featured A potent, specific cell-active VHL E3 ubiquitin ligase inhibitor that inhibits VHL/HIF-α interaction with Kd of 90 nM in ITC assays.
DC23985 Laduviglusib trihydrochloride Featured Laduviglusib (CHIR-99021) trihydrochloride is a well-characterized small molecule inhibitor that specifically targets glycogen synthase kinase-3 alpha and beta (GSK-3α/β). It exhibits potent inhibitory activity with IC50 values of 10 nM for GSK-3α and 6.7 nM for GSK-3β. Importantly, it demonstrates high selectivity, being over 500-fold more selective for GSK-3 compared to other kinases such as CDC2 and ERK2, as well as a broad range of other protein kinases.
DC24007 R-1479 Featured A potent, specific inhibitor of HCV NS5B polymerase and HCV replication (IC50=1.28 uM, replicon assay).
DC11871 MMV019313 Featured MMV019313 (MMV 019313, MMV-019313) is a potent, specific malaria bifunctional farnesyl/geranylgeranyl diphosphate synthase (FPPS/GGPPS) inhibitor with IC50 of 330 nM; shows no activity against human FPPS or GGPPS (>200 uM); exhibits distinct modes of inhibition compared with bisphosphonates, inhibits P. falciparum growth with EC50 of 268 nM, overexpression and an S228T variant of PfFPPS/GGPPS confer resistance to MMV 019313.
DC24060 YM-155 hydrochloride Featured A potent, specific survivin inhibitor that inhibits survivin promoter activity with IC50 of 0.54 nM.
DC22865 CK-0106023 Featured A potent, specific, allosteric inhibitor of KSP motor domain ATPase with Ki of 12 nM.
DC20890 ChoK-α inhibitor CK37 Featured A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM
DC26079 GW 803430 Featured A potent, specific, orally active melanin concentrating hormone receptor 1 (MCHR1) inhibitor with kI of 3.8 nM, >100-fold selectivity over a battery of GPCRs, ion channels and enzymes.
DC20928 CRT0066101 Featured A potent, specific, orally active pan-PKD (protein kinase D) inhibitor with biochemical IC50 of 1, 2.5 and 2 nM for PKD1, 2, and 3 respectively.
DC22540 Pasireotide Featured Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity. At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Pasireotide acetate) usually boasts enhanced water solubility and stability.
DC22939 NS3861 fumarate Featured NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively.
DC23938 Esomeprazole sodium Featured A proton pump inhibitor that reduces stomach acid secretion by inhibition of the H+/K+-ATPase in the parietal cells.
DC11545 IPAG Featured IPAG is a prototypic selective inhibitor of sigma1 receptor that engages the unfolded protein response and induces autophagy in cancer cells.
DC23004 PSMA-ligand-1 Featured PSMA ligand-tubulysin compounds represent a cutting-edge approach to targeted cancer therapy, combining the precision of PSMA targeting with the potent cytotoxicity of tubulysin. This strategy holds significant promise for improving outcomes in prostate cancer and other PSMA-expressing malignancies, offering a highly specific and effective treatment option with reduced systemic toxicity. As research progresses, these compounds could play a transformative role in the field of oncology.
DC22348 Zalcitabine Featured A pyrimidine analog reverse transcriptase inhibitor (NRTI) for the treatment of HIV/AIDS.
DC7054 AM580 Featured A retinoic acid analog and selective RARα agonist
DC23944 K-7174 Featured A selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).
DC23943 K-7174 dihydrochloride Featured K-7174 dihydrochloride is a selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

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