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Ras-Raf-MAPK-ERK

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Cat. No. Product Name Field of Application Chemical Structure
DC79786 KRAS inhibitor-42
KRAS inhibitor-42 (compound 8) is a potent USP7 inhibitor. KRAS inhibitor-42 has high affinity against GDP-bound KRASG12D with a Ki of 2.7 μM.
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DC79776 WEIZ-WX-04-008
WEIZ-WX-04-008 (Compound 1) is a covalent Lysine-targeting MKK7 inhibitor with IC50 of 738 nM.
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DC79767 R-03201195
R-03201195 is an efficient and selective p38 MAP kinase inhibitor with an IC50 for p38α of 0.7 nM. R-03201195 has inhibitory activity against TNF-α in THP-1 cells and against IL-1β in human whole blood, with IC50 values of 0.25 and 0.57 nM respectively. R-03201195 BIRB-1017 can be used for inflammatory diseases such as rheumatoid arthritis.
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DC79523 Sonvuterkib
Sonvuterkib (WX001) is a potent and orally active extracellular signal-regulated kinases (ERK) inhibitor with IC50 values of 1.4, 0.54 nM for ERK1, ERK2, respectively. Sonvuterkib inhibits cell proliferation. Sonvuterkib shows anticancer activity.
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DC79399 WMJ-J-09
WMJ-J-09 is an HDAC inhibitor with IC50 values of 7.5 nM (HDAC1), 21.3 nM (HDAC2), 18.4 nM (HDAC3), 90.9 nM (HDAC8), 3.9 nM (HDAC6) and 8715.7 nM (HDAC4). WMJ-J-09 blocks the cell cycle and induces apoptosis in cancer cells. WMJ-J-09 induces cancer cell death through the LKB1-AMPK-p38MAPK-p63-survivin signaling cascade.WMJ-J-09 inhibits HDAC enzyme activity, leading to acetylation of key proteins and thereby regulating cancer cell death. WMJ-J-09 can be used in HCT116 cells and FaDu cells research[1][2].
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DC79364 ADT-1004
ADT-1004 is an inhibitor of RAS. ADT-1004 can be studied in research for Ras-mediated diseases.
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DC79186 A2073
A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.
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DC79093 PHI-501
PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.
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DC79014 BMS-626531
BMS-626531 is a potent and selective p38α MAP kinase inhibitor. BMS-626531 can be used for the research of cancer.
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DC78940 (R)-MK-8353
(R)-MK-8353 ((R)-SCH900353) is the R-enantiomer of MK-8353). MK-8353 (SCH900353) is a potent, selective and orally active ERK1 and ERK2 inhibitor with IC50s of 23.0 nM and 8.8 nM, respectively.
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DC78875 MCB-294
MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer.
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DC78722 Z56
Z56 is a Ras protein inhibitor. Z56 can be used for the research of cancer, such as pancreatic cancer.
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DC78697 Z52
Z52 is a Ras protein inhibitor. Z52 can be used for the research of cancer, such as pancreatic cancer.
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DC78696 Z52-L16
Z52-L16 is Drug-Linker Conjugates for ADC, which is composed of a linker and a Ras inhibitor Z52. Z52-L16 can be used for the research of cancer, such as pancreatic cancer.
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DC78669 JNK-9L
JNK-9L (Compound 9l) is a BBB-penetrable and ATP-competitive JNK inhibitor with IC50s of 0.099 and 0.148  μM for JNK1 and JNK3, respectively. JNK-9L significantly inhibits c-jun phosphorylation and Streptozotocin-induced ROS generation with an IC50 of 0.8  nM. JNK-9L can be used for neurodegenerative disorders like Parkinson’s disease research.
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DC78652 (S)-AZD0022
(S)-AZD0022 is an isomer of AZD0022, AZD0022 is a selective and orally active KRASG12D inhibitor. AZD0022 inhibits KRAS pathway suppression in the GP2D xenograft model.
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DC78607 SHY-855
SHY-855 is a pan RAS inhibitor. SHY-855 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with IC50 values of 0.3-5 μM. SHY-855 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-855 inhibits the formation of the Ras-GTP activity complex. SHY-855 can be used to the studies of pancreatic cancer and non-small cell lung cancer.
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DC78522 SHY-867
SHY-867 is a pan RAS inhibitor. SHY-867 effectively prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases with EC50 values of 0.5-3 μM. SHY-867 effectively inhibits the phosphorylation of MEK, ERK1/2, and AKT downstream of K-Ras. SHY-867 inhibits the formation of the Ras-GTP activity complex. SHY-867 can be used to the studies of pancreatic cancer and non-small cell lung cancer.
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DC78455 (R)-KRAS G12D inhibitor 28 hydrochloride dihydrate
(R)-KRAS G12D inhibitor 28 hydrochloride dehydrate is the hydrochloride dehydrate of (R)-KRAS G12D inhibitor 28. KRAS G12D inhibitor 28 (Compound 1) is a KRAS G12D inhibitor. KRAS G12D inhibitor 28 (Compound 1) can be used in the cancer research.
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DC78443 VVD-849
VVD-849 is a RAS ligand. VVD-849 binds covalently to cysteine 242 in the RAS binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT(S473) in HER2 over-expressing tumors. VVD-849 can be used cancers like breast cancer research.
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DC78414 APS03118
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research.
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DC78375 AB19
AB19 is a potent Vav1 inhibitor. AB19 inhibits Vav1 and reduces its downstream ERK phosphorylation. AB19 shows anti-proliferative activity in pancreatic cancer models. AB19 can be used for pancreatic cancer research.
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DC78346 AH001
AH001 is a orally active RhoA inhibitor, which binds a cryptic pocket proximate to GDP within RhoA with a KD of 73.16 nM. AH001 interacts with GDP, stabilizing RhoA’s interaction with its endogenous inhibitor, RhoGDIα. AH001 reduces the downstream MRTFA nuclear translocation and downregulates fibrosis/hypertrophy proteins. AH001 mitigates myocardial remodeling in multiple HF animal models, and in the 3D myocardial tissue model. AH001 exerts its cardioprotective effects through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signaling.
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DC78301 BIRB-1017
BIRB-1017 is a potent inhibitor of p38 MAP kinase. BIRB-1017 can be used in inflammation research.
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DC78191 (±)-Spiro-oxanthromicin A
(±)-Spiro-oxanthromicin A (Compound 4), a polyketide, is a K-Ras inhibitor with an IC50 of 26.7  μM. (±)-Spiro-oxanthromicin A can be isolated from soil-derived Streptomyces sp. (±)-Spiro-oxanthromicin A can mislocalize oncogenic mutant K-Ras from the plasma membrane of intact MDCK cells. (±)-Spiro-oxanthromicin A can be used for cancers research.
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DC78099 Z52/Z56 intermediate
Z52/Z56 intermediate is a key intermediate in the synthesis of RAS inhibitors.
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DC78010 VVD-442
VVD-442 is a covalent RAS-PI3K inhibitor. VVD-442 binds covalently to cysteine 242 in the RAS binding domain of PI3K p110α and blocks RAS/PI3K interaction. VVD-442 can be used cancers like breast cancer research.
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DC77981 Scrambled Tadnersen
Scrambled Tadnersen is the Negative Control of Tadnersen sodium. Tadnersen sodium, an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.
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DC77980 Scrambled Tadnersen sodium
Scrambled Tadnersen sodium is the Negative Control of Tadnersen sodium. Tadnersen sodium, an antisense oligonucleotide (ASO), selectively targets C9ORF72 transcript variants 1 and 3 that carry the expansion.
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DC77869 C3 sodium
C3 sodium is an aptamer that binds to Erk2. C3 binds to the MAP kinase insert domain, a unique site on Erk1/2. Due to this recognition profile C3 inhibits Erk2 activation by its upstream kinase MKK1.
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