Products Archive - 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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SM04554

andreas — Thu, 19 Mar 2020 02:21:40 +0000

SM04554 is a topical compound that modulates the WNT pathway. The WNT pathway is one of the primary signalling pathways that regulate the self-renewal and differentiation of adult stem cells. It also plays other important roles: from hair follicle cycling to hair follicle morphogenesis.

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Equol

andreas — Tue, 30 Apr 2019 01:38:22 +0000

Equol (4′,7-isoflavandiol) is an isoflavandiol metabolized from daidzein, a type of isoflavone found in soybeans and other plant sources, by bacterial flora in the intestines.While endogenous estrogenic hormones such as estradiol are steroids, equol is a nonsteroidal estrogen. However, only about 30-50% of people have intestinal bacteria that make equol. Equol can exist in two enantiomeric forms, (S)-equol and (R)-equol.(S)-Equol preferentially binds estrogen receptor beta.

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S-Equol

andreas — Tue, 30 Apr 2019 01:36:08 +0000

(S)-equol is under development for the treatment of menopausal symptoms such as hot flashes and benign prostatic hyperplasia.

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BIO

andreas — Tue, 30 Apr 2019 01:30:52 +0000

BIO is a cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC₅₀= 5 nM). Its specificity has been tested against various cyclin-dependent kinases (CDKs) (IC₅₀s = 83, 300, 320, and 10,000 nM for Cdk5/p25, Cdk2/A, Cdk1/B, and Cdk4/D₁, respectively). BIO was also tested for its specificity towards many other commonly studied kinases (IC₅₀ ≥10 µM), including MAP kinases, PKA, PKC isoforms, PKG, CK, and IRTK. Inhibition of GSK by BIO has been shown to result in the activation of the Wnt signaling pathway and sustained pluripotency in human and mouse embryonic stem cells (ESCs). BIO is reported to maintain self-renewal in human and mouse ESCs as well as induce the differentiation of neonatal cardiomyocytes.

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