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Results for "

G12D

" in MCE Product Catalog:

10

Inhibitors & Agonists

1

Dye Reagents

2

Peptides

Cat. No. Product Name Target Research Areas
  • HY-134811
    KRAS G12D inhibitor 1

    Ras Cancer
    KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation.
  • HY-134813
    MRTX1133

    Ras Cancer
    MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells.
  • HY-P2265
    SAH-SOS1A

    Ras 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.
  • HY-P2265A
    SAH-SOS1A TFA

    Ras Cancer
    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) and 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.
  • HY-18674
    K-Ras-IN-1

    Ras Cancer
    K-Ras-IN-1 is a K-Ras inhibitor. K-Ras-IN-1 binds to K-Ras (WT), K-Ras (G12D), K-Ras (G12V), and H-Ras. K-Ras-IN-1 has potential for the research of pancreatic, colon and lung carcinomas.
  • HY-137497
    KRAS inhibitor-9

    Ras Apoptosis Cancer
    KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
  • HY-126247
    BI-2852

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRAS G12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRAS G12D versus KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
  • HY-114491A
    Rineterkib hydrochloride

    Raf ERK Cancer
    Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 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.
  • HY-114491
    Rineterkib

    Raf ERK Cancer
    Rineterkib (compound B) is an orally active RAF and ERK1/2 inhibitor in the study 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.
  • HY-136265
    BC-LI-0186

    Aminoacyl-tRNA Synthetase Cancer
    BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research.