New Research Chemicals Archives - TheKaneShop

PF-06700841

andreas — Tue, 28 Apr 2020 08:23:35 +0000

PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

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Tofacitinib (CP-690550）

andreas — Tue, 28 Apr 2020 08:13:02 +0000

Tofacitinib (CP-690550,Tasocitinib) is a novel inhibitor of JAK3 with IC50 of 1 nM in cell-free assays, 20- to 100-fold less potent against JAK2 and JAK1.

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Ruxolitinib

andreas — Tue, 28 Apr 2020 08:05:41 +0000

Ruxolitinib (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

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PF-06651600

andreas — Tue, 28 Apr 2020 07:58:53 +0000

PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.

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Baricitinib (LY3009104)

andreas — Tue, 28 Apr 2020 07:49:18 +0000

Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

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Favipiravir

andreas — Tue, 14 Apr 2020 08:57:27 +0000

•Favipiravir is a novel antiviral drug now in clinical trials for the treatment of influenza.

•It acts as a pseudo purine nucleic acid in virus-infected cells.

•Favipiravir inhibits the RNA polymerase of many different RNA viruses.

•It blocks replication of many strains of influenza virus, including the H7N9 avian virus.

•Favipiravir is also active against many arena-, bunya-, flavi-, alpha-, picorna- and noroviruses.

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Nocodazole

andreas — Mon, 29 Apr 2019 03:16:34 +0000

Nocodazole is an anti‐mitotic drug that has long been used as an experimental tool in cell biology. Although nocodazole is known to bind with high affinity to tubulin and to inhibit microtubule assembly, very little has been done on its precise mechanism of action. In fact, its binding to the different isotypes of tubulin has never been addressed. Although the nocodazole binding site overlaps with that of colchicine, the two drugs are structurally quite different. The tubulin molecule is an α/β heterodimer; both α and β exist as various isotypes whose distribution and drug‐binding properties are significantly different. In this study, we measured the binding affinity of nocodazole for purified tubulin isotypes. Using fluorescence quenching analysis, we found that the binding kinetics of nocodazole with each type of tubulin best fits a two‐affinity Michaelis‐Menten binding model. The apparent dissociation constants for the high‐affinity binding sites are 0.52 ± 0.02 for αβ_II, 1.54 ± 0.29 for αβ_III, and 0.29 ± 0.04 for αβ_IV. Thus, nocodazole has the highest affinity for αβ_IV and the lowest affinity for αβ_III. Knowledge of the isotype specificity of nocodazole may allow for development of novel therapeutic agents based on this drug.

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UK-5099

andreas — Mon, 29 Apr 2019 02:55:52 +0000

UK-5099 is a potent inhibitor of the mitochondrial pyruvate carrier (MPC). UK-5099 ihibits pyruvate-dependent O₂ consumption with an IC₅₀ of 50 nM.IC50 & Target: IC50: 50 nM (MPC)^[1]In Vitro: The trypanosomal pyruvate carrier is found to be rather insensitive to inhibition by alpha-cyano-4-hydroxycinnamate (K_i=17 mM) but can be completely blocked by UK-5099 (K_i=49 microM)^[2]. UK-5099 also inhibits the monocarboxylate transporter (MCT) ^[3]. UK5099 significantly inhibits the glucose-stimulated rise in oxygen consumption in a dose-dependent manner and at 150 μM reduced oxygen consumption below basal levels. UK5099 reduces ATP levels and increases ADP and AMP levels in 832/13 cells^[4]. The UK5099 treated cells show significantly higher proportion of side population fraction and express higher levels of stemness markers Oct3/4 and Nanog. UK5099 application may be an ideal

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Rebastinib (DCC-2036)

andreas — Wed, 24 Oct 2018 11:15:50 +0000

Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.

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