| DC70702 |
PLX8394
Featured
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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. |
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| DC70703 |
PMD-026 |
PMD-026 (PMD026) is an oral, reversible small molecule inhibitor of ribosomal S6 kinase (RSK1-4) with IC50 of 2 nM (RSK1), 0.7 nM (RSK2), 0.9 nM (RSK3) and 2 nM (RSK4).PMD-026 decreased YB-1 phosphorylation as well as AR V7 mRNA and AR variants expressions in 22Rv1 cells.PMD-026 suppressed cell proliferation alone and in combination with the second-generation antiandrogens enzalutamide and darolutamide by inducing cellular apoptosis and G2/M arrest.PMD-026 suppressed tumor growth, and the combination of PMD-026 and enzalutamide inhibited tumor growth more prominently than single treatment in mouse xenograft models. |
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| DC70729 |
Ral inhibitor 1 |
Ral inhibitor 1 is a covalent inhibitor of RalB (Ras-like GTPase) activation, inhibits guanine exchange factor Rgl2-mediated nucleotide exchange of Ral GTPase, selectively inhibits Ral over Ras; Ral inhibitor 1 inhibits RalB/Rgl2 interaction through covalent reaction at Tyr-82 with IC50 of 49.5 uM; Ral (Ras-like) GTPases are directly activated by oncogenic Ras GTPases. |
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| DC70730 |
Ras binder 2C07
Featured
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Ras binder 2C07 is a switch-II binding ligand which binds Ras GDP and GTP states. |
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| DC70768 |
SF-3-030 |
SF-3-030 is a novel ATP-dependent/catalytic site inhibitor of ERK1/2, inhibits A375 cell viability with IC50 of 4.9 uM.SF-3-030 showed selective inhibition of cancer cell lines with activating mutations in the ERK1/2 pathway.SF-3-030 inhibited viability of four melanoma cell lines containing either BRAF or NRas mutations with IC50 of 5-10 uM.SF-3-030 selectively regulates ERK-dependent immediate early gene expression, causes differential changes in AP-1 protein levels characterized by inhibition of Fra-1, FosB, and the alternative splice variant FosB2 but no effect on c-Fos levels, and induces ROS mediates inhibition of A375 cell proliferation. |
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| DC70826 |
TAT-K-tetracosapeptide |
TAT-K-tetracosapeptide is K-tetracosapeptide fused to a cell-permeable TAT peptide, K-tetracosapeptide (K-TC) is a peptide of 24 amino acids corresponding to the helix a5 in KRAS4B, potent inhibitor of KARATE.TAT-K-tetracosapeptide blocks insulin-induced phosphorylation of AKT and its downstream effector TBC1D4, a Rab GTPase-activating protein.TAT-K-tetracosapeptide strongly inhibits insulin-induced transport of GLUT4-GFP to the plasma membrane and glucose uptake in adipocytes. |
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| DC70846 |
TH-Z835 |
TH-Z835 is a potent, mutant selective KRAS (G12D) inhibitor with IC50 of 1.6 uM.TH-Z835 binds to both GDP-bound and GMPPNP-bound KRAS G12D with similar affinities, efficiently disrupt KRAS–CRAF interaction, but do not bind to wide type and G12C mutant KRAS.TH-Z835 reduced the pERK level in PANC-1 cells with an IC50 <2.5 uM, exhibited anti-proliferative effects for KRAS(G12D)-bearing pancreatic cancer cell lines PANC-1 and KPC with IC50 of <0.5 uM, induced arrest at the G1 phase of the cell cycle.TH-Z835 displayed anti-tumor effects alone and in combination with anti-PD-L1 antibody in xenograft pancreatic tumor models. |
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| DC70855 |
Tunlametinib |
Tunlametinib is a benzoheterocyclic compound as MEK modulator with potential for treatment of cancer and inflammation. |
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| DC70870 |
URML-3881 |
URML-3881 (URML3881) is a potent, specific MEK1/2 inhibitor IC50 of 30 nM in a cell-free kinase inhibition assay.URML-3881 shows no inhibition among a panel of other kinases including MEK 3 and MEK5, which are activated in alternative MAPK signaling pathways.URML-3881 reduces MAPK pathway activity in clear cell ovarian cancer (CCOC).URML-3881 causes reduced CCOC viability due to induction of tumor cell apoptosis and inhibition of proliferation.URML-3881 abrogates cisplatin-induced prosurvival MAPK signaling in CCOC, resulting in durable and dramatic tumor regression in vivo. |
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| DC70899 |
VUBI1 |
VUBI1 is a potent activator of SOS1 which modulates the KRAS pathway, binds directly to SOS1 (Kd=44 nM);
VUBI1 increase nucleotide exchange on RAS in vitro at sub-micromolar concentration, rapidly enhances cellular RAS-GTP levels, and invoke biphasic signaling changes in phosphorylation of ERK 1/2 (Hela pERK ICW EC50=5.9 uM). |
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| DC71036 |
EO 1428 |
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. |
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| DC71131 |
U0124 |
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. |
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| DC71618 |
18:0-22:6 DG |
18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol that can bind to RasGRP and modulate MAP kinases activation. |
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| DC71619 |
GDC-6036-NH |
GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research. |
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| DC71620 |
MRTX-EX185 formic |
MRTX-EX185 formic is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC50 of 90 nM for KRAS(G12D). MRTX-EX185 formic also binds GDP-loaded HRAS. |
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| DC71621 |
(Rac)-Antineoplaston A10 |
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10, which is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. |
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| DC71688 |
HA-100 |
HA-100 is an inhibitor of cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase. |
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| DC71908 |
Everafenib |
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib and Vemurafenib. Everafenib has efficacy in an intracranial mouse model of metastatic melanoma. |
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| DC71909 |
Exarafenib
Featured
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Exarafenib (RAF/KIN_2787) is a potent, orally active pan-RAF inhibitor. Exarafenib has anticancer activity by suppression of downstream MAPK pathway signaling. Exarafenib can be used for cancer research. |
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| DC71910 |
Tinlorafenib
Featured
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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]. |
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| DC71911 |
G12Si-1 |
G12Si-1 is a selective K-Ras(G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras(G12S). G12Si-1 shows good ability to covalently engage recombinant K-Ras(G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange. |
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| DC71912 |
G12Si-2 |
G12Si-2, an analog of G12Si-1, is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12C mutant of K-Ras. |
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| DC71996 |
8-pCPT-2'-O-Me-cAMP-AM |
8-pCPT-2'-O-Me-cAMP-AM is a cyclic AMP analogue, selectively activates Epac-Rap signaling pathway. 8-pCPT-2'-O-Me-cAMP-AM protects renal function by activating Epac from ischemia injury. 8-pCPT-2'-O-Me-cAMP-AM also stimulates insulin secretion by interaction with PKA pathway. |
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| DC72097 |
SHR2415 |
SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer. |
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| DC72131 |
DS89002333 |
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). |
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| DC72236 |
B-Raf IN 11 |
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 |
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| DC72237 |
BI-0474
Featured
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BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models. |
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| DC72490 |
ASN007 |
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. |
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| DC72491 |
ZG1077 |
ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC). |
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| DC72550 |
NecroIr1 |
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. |
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