MAPK Signaling

TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM.

RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.

HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM.

(Rac)-Hesperetin is the racemate of Hesperetin.

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

Gypenoside L is a saponin that can be found in Gynostemma pentaphyllum.

HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.

MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay.

PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.

Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 ?M and 4.5 ?M, respectively) antagonist.

Zapnometinib (PD0184264), an active metabolite of CI-1040, is a MEK inhibitor, with an IC50 of 5.7 nM.

HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.

Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2 (MK2) pathway inhibitor.

CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM).

ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.

PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader.

HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunotherapy tool compound.

MLKL-IN-2 is a MLKL inhibitor extracted from patent WO2021224505A1, compound (i).

5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect.

(E)-Osmundacetone is the isomer of Osmundacetone.

Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects.

SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells).

MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively.

8-Chloro-cAMP is a cAMP analogue that induces growth arrest, and modulates cAMP-dependent PKA activity. 8-Chloro-cAMP has anticancer activity.