LGX818 is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.

K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).

JNK-IN-8 is a potent and irreversible JNK inhibitor that inhibits the phosphorylation of c-Jun.

GW806742X is a novel VEGFR inhibitor.

GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM); displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fms.

DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.

Dabrafenib is an orally bioavailable inhibitor of B-raf (BRAF) protein with potential antineoplastic activity.

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively. Phase 3.

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

B-Raf IN 1 is a highlt potent and selective B-Raf inhibitor with IC50 of 24 nM; equipotent against c-Raf (IC50= 25 nM).

BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.

BIRB 796 (Doramapimod) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.

BI-D1870 is a small molecule, specific inhibitor of p90 RSK (ribosomal S6 kinase) isoforms RSK1, RSK2, RSK3 and RSK4, both in vitro and in vivo, with IC50s are 31 nM, 24 nM, 18 nM, 15 nM, respectively.

BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

BI-3406 (compound I-6) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhib

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.

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

APS-2-79 is a novel modulator of KSR-dependent MAPK signalling,KSR2,IC50=120 nM

6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).

PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors.

NecroIr1 is an iridium(III) complex, serves as necroptosis inducers in Cisplatin-resistant lung cancer cells (A549R). NecroIr1 selectively accumulates in mitochondria, leading to oxidative stress and loss of mitochondrial membrane potential (MMP). NecroIr1 activates receptor-interacting serine-threonine kinase 3 (RIPK3) and Mixed Lineage Kinase (MLKL), and regulates CDK4 expression.

ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC).

ASN007(ERAS 007, ERK-IN-3) is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with 2 nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.

Tinlorafenib (PF-07284890) (compound 10) is an orally active BRAF kinase inhibitor, with IC50s of 4.25 and 2.7 nM for BRAFV600E/V600K respectively. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies[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

PLX8394 (PLX-8394) is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF (V600E), WT BRAF and CRAF, respectively.PLX8394 suppresses mutant BRAF cells without activating the MAPK pathway in cells bearing upstream activation, overcame several known mechanisms of resistance to first-generation RAF inhibitors.PLX8394 inhibits ERK signaling by specifically disrupting BRAF-containing dimers, including BRAF homodimers and BRAF-CRAF heterodimers, but not CRAF homodimers or ARAF-containing dimers.As a BRAF-specific dimer breaker, PLX8394 selectively inhibits ERK signaling in tumors driven by dimeric BRAF mutants, including BRAF fusions and splice variants as well as BRAF V600 monomers, but spares RAF function in normal cells in which CRAF homodimers can drive signaling.

MRTX849 acid, a derivative of MRTX849, can be used in the synthesis of PROTAC LC-2. LC-2 is a potent and first-in-class PROTAC capable of degrading endogenous KRAS G12C (DC50s between 0.25 and 0.76 μM).

DS89002333 is an orally active and potent PRKACA inhibitor, with an IC50 of 0.3 nM. DS89002333 shows good anti-tumor activity in an FL-HCC patient-derived xenograft model (expressing the DNAJB1-PRKACA fusion gene). DS89002333 can be used in study of fibrolamellar hepatocellular carcinoma (FL-HCC).