Presentation is loading. Please wait.

Presentation is loading. Please wait.

Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. Paralog-selective inhibitors of GSK3α and GSK3β were designed and.

Published byEarl McKenzie Modified over 5 years ago

Similar presentations

Presentation on theme: "Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. Paralog-selective inhibitors of GSK3α and GSK3β were designed and."— Presentation transcript:

1 Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized.
Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. (A) General synthetic scheme for synthesis of the pyrazolo-tetrahydroquinolinone scaffold. TFA, trifluoroacetic acid; TFE, 2,2,2-trifluoroethanol. (B) IC50 values for the inhibition of GSK3α and GSK3β were determined at Km of ATP in a motility shift microfluidic assay (Caliper) measuring phosphorylation of a synthetic substrate. Values are average of three or more experiments. Data are shown as IC50 values in μM ± SD. Compounds were tested in duplicate in a 12-point dose curve with threefold dilution starting at 33.3 μM. (C) Kinome-wide selectivity for BRD0705 and BRD3731 represented on a kinome phylogenetic tree. Each inhibitor was screened against 311 kinases at a 10 μM concentration. Kinases with >50% inhibition are depicted (percentage inhibition proportional to size of red dot). Florence F. Wagner et al., Sci Transl Med 2018;10:eaam8460 Published by AAAS

Download ppt "Fig. 2 Paralog-selective inhibitors of GSK3α and GSK3β were designed and characterized. Paralog-selective inhibitors of GSK3α and GSK3β were designed and."

Similar presentations

Fig. 1. (A) Development of the free calcium ions measured by the calcium ion selective electrode (black line) at pH = 9.25 in comparison with the dosed.

Fig. 1. (A) Development of the free calcium ions measured by the calcium ion selective electrode (black line) at pH = 9.25 in comparison with the dosed.
Structures of CK1 inhibitors and their effects on CK1 activity in vitro. Structures of CK1 inhibitors and their effects on CK1 activity in vitro. (A) Structures.

Structures of CK1 inhibitors and their effects on CK1 activity in vitro. Structures of CK1 inhibitors and their effects on CK1 activity in vitro. (A) Structures.
Fig. 2. Effects of AZD4785 on proliferation and MAPK pathway signaling in KRAS mutant and wild-type cancer cells in vitro. Effects of AZD4785 on proliferation.

Fig. 2. Effects of AZD4785 on proliferation and MAPK pathway signaling in KRAS mutant and wild-type cancer cells in vitro. Effects of AZD4785 on proliferation.
Fig. 5. Protective efficacy of the combination of PGT121 + PGDM1400 against a mixed SHIV challenge in rhesus monkeys. Protective efficacy of the combination.

Fig. 5. Protective efficacy of the combination of PGT121 + PGDM1400 against a mixed SHIV challenge in rhesus monkeys. Protective efficacy of the combination.
Fig. 6. dAST directly from clinical samples using dPCR and dLAMP for quantification. dAST directly from clinical samples using dPCR and dLAMP for quantification.

Fig. 6. dAST directly from clinical samples using dPCR and dLAMP for quantification. dAST directly from clinical samples using dPCR and dLAMP for quantification.
BET inhibition and depletion repress the expression of BRCA1 and RAD51

BET inhibition and depletion repress the expression of BRCA1 and RAD51
Fig. 4 Bacterial taxonomic groups that discriminate among RYGB-, SHAM-, and WMS-derived samples. Bacterial taxonomic groups that discriminate among RYGB-,

Fig. 4 Bacterial taxonomic groups that discriminate among RYGB-, SHAM-, and WMS-derived samples. Bacterial taxonomic groups that discriminate among RYGB-,
Fig. 5. Correlation of tail and long bone growth velocities with Cxm serum concentrations in mice. Correlation of tail and long bone growth velocities.

Fig. 5. Correlation of tail and long bone growth velocities with Cxm serum concentrations in mice. Correlation of tail and long bone growth velocities.
β-ARs signal cooperatively with mutant EGFR and inactivate LKB1

β-ARs signal cooperatively with mutant EGFR and inactivate LKB1
In vivo prophylactic and therapeutic efficacy of C12G6 in mice

In vivo prophylactic and therapeutic efficacy of C12G6 in mice
JQ1 directly represses the promoter activities of BRCA1 and RAD51

JQ1 directly represses the promoter activities of BRCA1 and RAD51
Fig. 2. Mutant KRAS mediates resistance to PARPi and sensitivity to PARPi and MEKi Mutant KRAS mediates resistance to PARPi and sensitivity to PARPi and.

Fig. 2. Mutant KRAS mediates resistance to PARPi and sensitivity to PARPi and MEKi Mutant KRAS mediates resistance to PARPi and sensitivity to PARPi and.
Synergistic effect of S63845 with lapatinib, trastuzumab, or docetaxel

Synergistic effect of S63845 with lapatinib, trastuzumab, or docetaxel
Fig. 3. Frequencies of amino acids at critical PGT121 and 10-1074 contact sites in the SHIV-SF162P3 challenge stock. Frequencies of amino acids at critical.

Fig. 3. Frequencies of amino acids at critical PGT121 and contact sites in the SHIV-SF162P3 challenge stock. Frequencies of amino acids at critical.
Fig. 3. BET inhibition reduces homologous recombination.

Fig. 3. BET inhibition reduces homologous recombination.
Fig. 8. mRIPO elicits neutrophil influx followed by DC and T cell infiltration into tumors. mRIPO elicits neutrophil influx followed by DC and T cell infiltration.

Fig. 8. mRIPO elicits neutrophil influx followed by DC and T cell infiltration into tumors. mRIPO elicits neutrophil influx followed by DC and T cell infiltration.
Fig. 2. In vitro sealing properties of the MeTro sealant.

Fig. 2. In vitro sealing properties of the MeTro sealant.
Fig. 4 Bone tissue formation within the Ti-mesh channels.

Fig. 4 Bone tissue formation within the Ti-mesh channels.
Fig. 2. GPC3 expression in normal and tumor tissues.

Fig. 2. GPC3 expression in normal and tumor tissues.
Increased ADMA in pregnancy is associated with SGA birth outcomes

Increased ADMA in pregnancy is associated with SGA birth outcomes

Similar presentations

Ads by Google