JNK-1-IN-1 is a JNK-1 inhibitor. JNK-1-IN-1 also inhibits MKK7 with an IC50 of 7.8μM. JNK-1-IN-1 bind to MKK7cp and acts as an inhibitor of JNK-1[1].
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and Akt. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors[1].
6,8-Diprenylorobol, a prenylated isoflavone, is a nature product that could be isolated from the leaves of Cudrania tricuspidata. 6,8-Diprenylorobol antiproliferative effect and induces apoptosis through activation of p53 and generation of ROS[1][2].
HPK1-IN-17 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-17 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019238067A1, compound 73)[1].
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway[1][2][3][4][5][6].
SS47, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell treatment. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies[1].
SKF-86002 dihydrochloride is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 dihydrochloride inhibits lipopolysaccharide (LPS)-stimulate human monocyte IL-1 and TNF-α production (IC50 = 1 μM). SKF-86002 dihydrochloride inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3].
Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and Akt. Isoprocurcumenol promotes the proliferation of keratinocytes[1][2][3].
LJH685 is a potent , specific and selective RSK inhibitor, inhibits RSK1, 2, and 3 biochemical activities with IC50 of 4 to 13 nM.IC50 value: 4 to 13 nM [1]Target: RSKin vitro: LJH685 efficiently inhibits RSK activity in cells. LJH685 RSK inhibition correlates with antiproliferative effects in MAPK pathway-dependent cancer cell lines only in anchorage-independent growth setting. The EC 50 values of LJH685 is 0.73 and 0.79 μM in MDA-MB-231 and H358. [1]
ACA-28 (compound 2a) is a potent ERK MAPK signaling modulator. ACA-28 selectively inhibits cancer cell growth by inducing apoptosis with ERK hyperactivationACA-28 inhibits cell growth of melanoma cells (SK-MEL-28) and normal melanocytes (NHEM), with IC50 values of 5.3 and 10.1 μM, respectively[1].
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM. Shows proliferation inhibition in human breast cancer cell line MCF-7 and produces a cell cycle block in G1 phase[1].
GW284543 (UNC10225170) hydrochloride is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein[1].
TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
Losmapimod is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM[1].
Natsudaidain is a kind of polymethoxyflavone. Natsudaidain can be isolated from Citrus plants. Natsudaidain inhibits tumor necrosis factor-α and cyclooxygenase-2 production n by suppressing p38 MAPK phosphorylation on mast cells[1].
PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior[1][2].
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth[1].
Belvarafenib is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.
Vemurafenib-d5 (PLX4032-d5) is the deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
Ganoderterpene A attenuates LPS-induced inflammation and apoptosis via suppressing MAPK and TLR-4/NF-κB pathways in BV-2 cells.
SR-3306 is a selective, potent, highly brain penetrant JNK inhibitor.
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
PD 198306 is a selective MAPK/ERK-kinase (MEK) inhibitor. PD 198306 results in an observable reduction in the Streptozocin induced increase in the level of active ERK1 and 2. Antihyperalgesic effects[1].
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation[1].
B-Raf IN 14 (Comp 25) is a BRAF inhibitor with IC50 value of 11.08 μM, which can be used in cancer-related research[1].
MW150 (MW01-18-150SRM) is a selective inhibitor of p38αMAPK isoform with a ki of 101 nM[1].
SR15006 is a inhibitor of Krüppel-like factor 5 (KLF5) with an IC50 of 41.6 nM in DLD-1/pGL4.18hKLF5p cells)[1].
NMDAR/TRPM4-IN-2 (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. NMDAR/TRPM4-IN-2 shows neuroprotective activity. NMDAR/TRPM4-IN-2 prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. NMDAR/TRPM4-IN-2 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss[1].
B-Raf IN 11 (ZINC72115182) is a selective B-RafV600E inhibitor (IC50=76 nM), shows selectivity for B-RafV600E over B-RafWT with selectivity of 3.1-fold. B-Raf IN 11 can be used in colorectal cancer research[1]