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KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRasG12V, respectively .
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRASG12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
pan-KRAS degrader 1 (Compound 1) is a panKRAS degrader with a surface plasmon resonance (SPR) dissociation constant Ki value of 25 nM for KRASG12V .pan-KRAS degrader 1 has antitumor activity .
pan-KRAS-IN-7 (Compound 25) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.35 and 0.51 nM, respectively .
pan-KRAS-IN-8 (Compound 38) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.07 and 0.18 nM, respectively .
pan-KRAS-IN-9 (Compound 52) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.24 and 0.30 nM, respectively .
pan-KRAS-IN-10 (Compound 58) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.7 and 0.24 nM, respectively .
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .
K-Ras-IN-1 is a small molecule K-Ras inhibitor. K-Ras-IN-1 binds to K-Ras (WT), K-Ras (G12D), K-Ras (G12V), and H-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. K-Ras-IN-1 is promising for research of pancreatic, colon and lung cancer .
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRASG12C cancer models, and demonstrates good tolerability across various RAS cancer models .
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
The Kras4B protein interacts specifically with GPR31, dependent on farnesylation. This binding suggests a regulatory role for Kras4B in association with GPR31, emphasizing the importance of the farnesylation process. Comprehensive exploration into the molecular details of this interaction is crucial to understand the precise mechanisms and functional implications in cellular processes or signaling pathways. Kras4B Protein, Human (G12V, His) is the recombinant human-derived Kras4B protein, expressed by E. coli , with N-6*His labeled tag.
KRAS Protein, a pivotal Ras family member, binds GDP/GTP and possesses intrinsic GTPase activity. Its crucial role in regulating cell proliferation emphasizes its significance in cellular processes. Notably, KRAS plays a prominent role in promoting oncogenic events, particularly in colorectal cancer (CRC), inducing transcriptional silencing of tumor suppressor genes (TSGs) in a ZNF304-dependent manner. This multifaceted functionality underscores KRAS as a key player in cellular dynamics, relevant in both normal and pathological processes. KRAS Protein, Human (G12V, His) is the recombinant human-derived KRAS protein, expressed by E. coli , with N-6*His labeled tag and G12V mutation. The total length of KRAS Protein, Human (G12V, His) is 184 a.a., with molecular weight of 25-30 kDa, observed by reducing SDS-PAGE.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*1101 KRAS G12V Complex Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*1101 KRAS G12V Complex Protein, Human (HEK293, His-Avi), has molecular weight of 42-46 kDa.
HLA-A*0301 collaborates with B2M to present viral and tumor peptides that direct CD8-positive T cells to respond against infected or transformed cells. It can also present self-peptides to avoid self-reaction. HLA-A*0301 KRAS G12V Complex Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*0301 KRAS G12V Complex Protein, Human (HEK293, His-Avi), has molecular weight of 55-60 kDa.
HLA-A*0301 collaborates with B2M to present viral and tumor peptides that direct CD8-positive T cells to respond against infected or transformed cells. It can also present self-peptides to avoid self-reaction. HLA-A*0301 KRAS G12V Complex Tetramer Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*0301 KRAS G12V Complex Tetramer Protein, Human (HEK293, His-Avi), has molecular weight of 260-265 kDa.
HLA-A*1101as, a pivotal MHCI molecule, presents viral and tumor-derived peptides, guiding T cell immune responses against infected or transformed cells. Collaborating with B2M, it displays a diverse peptide repertoire. Both the presented peptide and MHCI contribute to antigen recognition specificity. HLA-A*1101 typically presents 8 to 13 amino acid intracellular peptides, binding different peptides with allele-specific motifs. It plays a crucial role in controlling infections, presenting immunodominant epitopes from HIV-1, EBV, HBV, and contributing to the immune response against SARS-CoV-2. HLA-A*1101 KRAS G12V Complex Protein, Human (Biotinylated, VVGAVGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*1101 KRAS G12V Complex Protein, Human (Biotinylated, VVGAVGVGK, HEK293, His-Avi), has molecular weight of 51-60 kDa.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*1101 KRAS G12V Complex Tetramer Protein, Human (HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*1101 KRAS G12V Complex Tetramer Protein, Human (HEK293, His-Avi), has molecular weight of 260-265 kDa.
HLA-A*0301 collaborates with B2M to present viral and tumor peptides, guiding CD8-positive T cell responses against infected or transformed cells. It can also present self-peptides, avoiding autoreactivity. The antigen recognition specificity involves the peptide and MHC residues, with HLA-A*0301 presenting 8 to 13 amino acid peptides, characterized by allele-specific binding motifs. Specific alleles, like A*01:01 and A*03:01, present a distinct repertoire of peptides, including viral and tumor epitopes. HLA-A*0301 KRAS G12V Complex Protein, Human (Biotinylated, VVGAVGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*0301 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*0301 KRAS G12V Complex Protein, Human (Biotinylated, VVGAVGVGK, HEK293, His-Avi), has molecular weight of 52-60 kDa.
HLA-A*1101as is a key MHCI molecule that presents viral and tumor-derived peptides that direct T cell immune responses against infected or transformed cells. It collaborates with B2M to showcase a diverse peptide library. HLA-A*0301 KRAS G12V Complex Protein, Human (VVGAVGVGK, HEK293, His-Avi) is a recombinant protein dimer complex containing HLA-A*1101 and B2M/Beta-2-microglobulin Protein, expressed by HEK293 , with C-Avi, C-His labeled tag and VVGAVGVGK peptide. HLA-A*0301 KRAS G12V Complex Protein, Human (VVGAVGVGK, HEK293, His-Avi), has molecular weight of 56-65 kDa.
KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRasG12V, respectively .
