Showing 673–688 of 5741 results

JNJ-64619178

JNJ-64619178 is a PRMT5 inhibitor with high selectivity and potency (subnanomolar range, PRMT5-MEP-50 IC50=0.14 nM) under different in vitro and cellular conditions, paired with favorable pharmacokinetics and safety properties.

NCT-503

NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs.

PKM2 Inhibitor (Compound 3k)

PKM2 inhibitor(Compound 3K) displays PKM2 inhibitory activity with the IC50 value of 2.95 μM. The IC50 value for PKM1 is 4-5-fold higher than that for PKM2.

Sodium Dichloroacetate (DCA)

Dichloroacetate, a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

α-Cyano-4-Hydroxycinnamic Acid (α-CHCA)

4-Chloro-α-cyanocinnamic acid (α-CHCA) is a classic monocarboxylate transporters (MCT) inhibitor. α-cyano-4-hydroxycinnamate (CHC) has a 10-fold selectivity for MCT1 compared to other MCTs.

Vorasidenib (AG-881)

Vorasidenib (AG-881) is an orally available inhibitor of mutated forms of both isocitrate dehydrogenase 1 and 2 (IDH1 and IDH2).

Derazantinib(ARQ-087)

Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.

Adenosine DiAldehyde (ADOX)

Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.

HDM201

HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.

C188-9

C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.

NGP 555

NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically.

CP2

CP2 is a cyclic peptide that inhibits the JmjC histone demethylases KDM4 with IC50 values of 42 nM and 29 nM for KDM4A and KDM4C, respectively.

S 38093

S 38093 is a histamine H3 antagonist/inverse agonist with a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors.

LYN-1604

LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.