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Ras-Raf-MAPK-ERK

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Cat. No. Product Name Field of Application Chemical Structure
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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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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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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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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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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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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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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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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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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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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DC8787 NQDI-1 Featured
NQDI-1 is a specific inhibitor of ASK1 (IC50 = 3 μM; Ki = 500 nM) that demonstrates potent selectivity against various serine/threonine and tyrosine protein kinases.
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DC8725 NSC 23766 Featured
NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase.
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DC9681 Pamapimod(R-1503) Featured
Pamapimod(R-1503)is a novel p38 MAP kinase inhibitor.
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DC5100 PD 98059 Featured
PD 98059 is a selective inhibitor of MEK and blocker of MAPK
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DC5095 PD169316 Featured
PD169316 is a potent and selective p38 MAP kinase inhibitor
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DC9814 PLX7904(PB04) Featured
PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.
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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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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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DC7808 Refametinib (BAY86-9766) Featured
Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.
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DC7599 SC1(Pluripotin) Featured
SC1(Pluripotin) is a sustainer of mES self-renewal and ERK 1 inhibitor
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DC8384 Sodium Tauroursodeoxycholate (TUDC) Featured
Sodium Tauroursodeoxycholate (TUDC) is a water soluble bile salt, used for the treatment of gallstones and liver cirrhosis.
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DC7243 U0126 Featured
U0126-EtOH(U-0126) is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD098059.
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DC7242 VX-11e(TCS ERK 11e) Featured
VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK (Extracellular Signal-Regulated Kinase); antitumor agent.
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DC10979 BAY-885 Featured
BAY-885 is a highly potent, selective ERK5 (MAPK7) inhibitor with IC50 of 40 nM.
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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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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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DC70855 Tunlametinib
Tunlametinib is a benzoheterocyclic compound as MEK modulator with potential for treatment of cancer and inflammation.
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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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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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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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