Axon Medchem BV

IM-12 is an inhibitor of <b>GSK-3β</b>, with an <b>IC₅₀</b> of 53 nM, and also enhances Wnt signalling.

(R)-(-)-Rolipram is a potent and cAMP-specific PDE4 inhibitor with IC50 of 0.22 uM; 2.5-fold more potent than (+)-rolipram (IC50= 2.58 uM) in inhibiting membrane-bound PDE 4. IC50 value: Target: PDE4 in vitro: In intact eosinophils, (-)-rolipram (EC50 = 0.19 +/- 0.02 microM) was 10-fold more potent than (+)-rolipram (EC50 = 1.87 ...

MI 2(MALT1 inhibitor) is a small molecule and irreversible inhibitor of MALT1 with IC50 of 5.84 uM(suppression of proliferation in ABCDLBCL). IC50 value: 5.84 uM Target: MALT1 MI-2 selectively killed ABC-DLBCL cell lines with CD79A/B, CARMA1, and/or MYD88 mutations but not those occurring in proteins downstream of MALT1, including t...

AK-7 is a selective and brain-permeable SIRT2 inhibitor; is neuroprotective in Huntington disease mouse models. IC50 value: Target: SIRT2 AK-7 treated R6/2 mice performed significantly better than vehicle treated littermates on the accelerating rotarod at 8 and 11 weeks of age.

FR180204 is a potent and selective ATP-competitive inhibitor of ERK1 and ERK2 with Ki value of 0.31 uM and 0.14 uM respectively; has IC50 values of 0.51 and 0.33 μM in enzymatic assays against ERK1 and ERK2, respectively. IC50 value: 0.31 uM/0.14 uM(Ki for ERK1/ERK2); 0.51uM/0.33 μM(ERK1/ERK2) [1] [2] Target: ERK1/2 inhibitor in vi...

iCRT 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT) (IC50 = 40.3 nM in assays of Wnt pathway activity). IC50 value: 40.3 nM [1] Target: Wnt inhibitor Thought to directly influence the interaction between β-catenin and TCF4.

SJ-172550 is the first MDMX inhibitor with EC50 of 0.84 uM; binds reversibly to MDMX and effectively kills retinoblastoma cells in which the expression of MDMX is amplified. IC50 value: 0.84 uM(EC50) [1] Target: MDMX inhibitor in vitro: Unlike SJ-134433 and SJ-044557, SJ-172550 was stable in solution and did not modify the MDMX prot...

Eluxadoline is a mixed <b>μ-</b> and <b>κ-opioid receptor</b> agonist and <b>δ-opioid receptor</b> antagonist.

GW311616A(GW311616 Hcl) is a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase(HNE) with IC50 of 22 nM. IC50 value: 22 nM [1] Target: neutrophil elastase The HNE inhibitor GW311616A is selective over other human serine proteases (IC50 values >100 uM for trypsin, cathepsin G, and plasmin...

Palbociclib isethionate(PD-0332991 isethionate) is a highly specific inhibitor of Cdk4 (IC50=11 nM) and Cdk6 (IC50=16 nM), having no activity against a panel of 36 additional protein kinases. IC50 value: 11 nM/16 nM (Cdk4/Cdk6) [1] Target: Cdk4/Cdk6 in vitro: ATP competitive inhibitor of Cdk4.

CID755673 is a potent and selective cell-active small molecule inhibitor for PKD with an IC50 of 182 nM; exhibits selective PKD1 inhibition when compared with AKT, PLK1, CAK, CAMKIIα, and PKC isoforms. IC50 value: 182 nM [1] Target: PKD in vitro: In cell-based assays, CID755673 blocked phorbol ester-induced endogenous PKD1 activatio...

Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain. IC50 value: Target: Difluprednate ophthalmic emulsion 0.05% is also being studied in other ocular inflammatory diseases, including a U.S.

PS48 is an activator of <b>PDK1</b> with an <b>AC₅₀</b> of 8 μM.

SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. IC50 value: 7.2 (pKb) [1] Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses (pK(B)=7.27+/-0.04 and 7.23+/-0.03 respectively, n=8), but had no effect on...

DBeQ(JRF-12) is a selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5 μM. IC50 value: 1.5 uM Target: p97 in vitro: DBeQ blocks UbG76V-GFP, ODD-Luc and Luc-ODC degradation with IC50 of 2.6 μM, 56 μM and 45 μM in HeLa cells.

Dimethyloxallyl Glycine(DMOG) is a cell permeable, competitive inhibitor of HIF-PH(HIF-1α prolyl hydroxylase). IC50 value: Target: HIF-1α prolyl hydroxylase The pro-angiogenic factor HIF-1α is targeted for destruction in normoxic environments by the hydroxylation of a specific proline residue, P564, by the oxygen-sensing enzyme HIF-...