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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
SOS1 protein
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "SOS1 protein" in MCE Product Catalog:
58
58 Publications Verification
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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2 Cited Publications
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MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a Ki of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma .
Cat. No.: HY-P2265A
CAS No.: 2896737-31-6
BI-0474 is a potent KRAS G12C 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 .
Cat. No.: HY-163582
CAS No.: 3036155-26-4
PROTAC SOS1 degrader-7 (Example 15) is a PROTAC degrader that targets SOS1 protein degradation by recruiting cereblon. PROTAC SOS1 degrader-7 is applicable to research on the SOS1-RAS signaling pathway and tumors associated with KRAS mutations .
Cat. No.: HY-P2265
CAS No.: 1652561-87-9
Cat. No.: HY-153674
PROTAC SOS1 degrader-4 (Compound 10) is a PROTAC degrader that targets the SOS1 protein for degradation by recruiting cereblon. It degrades SOS1 in NCI-H358, A-427, SW-620, and DLD-1 cells and inhibits the proliferation of various KRAS-mutant tumor cells, making it a useful tool for cancer research .
Cat. No.: HY-134813A
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
Cat. No.: HY-172221
SOS1-IN-18 (Compound 8) is the inhibitor for Son of Sevenless 1 protein (SOS1) with a KD of 2.6 nM, and inhibits SOS1-KRAS G12C interaction with an IC50 of 3.4 nM. SOS1-IN-18 inhibits the phosphorylation of ERK in H358 with an IC50 of 31 nM, inhibits the proliferation of H358 with an IC50 of 5 nM .
Cat. No.: HY-161173
CAS No.: 2836273-61-9
PROTAC SOS1 degrader-5 is a potent SOS1 PROTAC degrader with a DC50 value of 13 nM. PROTAC SOS1 degrader-5 induces CRBN-dependent ubiquitination and degradation of SOS1 protein, inhibits the proliferation of KRAS G12C-mutated cancer cells, and suppresses tumor growth in xenograft models. PROTAC SOS1 degrader-5 can be used in studies related to KRAS G12C-mutated non-small cell lung cancer .
Cat. No.: HY-168638
CAS No.: 3027977-34-7
Research Areas:
PROTAC SOS1 ligand 1, a BI-3406 (HY-125817) analog, is a ligand for target SOS1 protein for PROTACT SIAIS562055 (HY-168637) .
Cat. No.: HY-181807
SOS1/KRAS-IN-2 (Compound 20) is a SOS1::KRAS G12C protein-protein interaction inhibitor with a IC50 of 4.11 nM. SOS1/KRAS-IN-2 blocks the interaction between SOS1 and KRAS G12C. SOS1/KRAS-IN-2 induces cell Apoptosis. SOS1/KRAS-IN-2 exhibits anticancer activity against colorectal cancer and tongue squamous cell carcinoma .
Cat. No.: HY-175575
CAS No.: 3027979-08-1
Research Areas:
SOS1 ligand-2 is a SOS1 ligand that can be used for PROTAC synthesis. SOS1 ligand-2 serves as the target protein ligand for PROTAC SOS1 degrader-4 (HY-153674). SOS1 ligand-2 is applicable to the research of KRAS-mutant cancers .
Cat. No.: HY-184586
SOS1-IN-28 is an orally active, blood-brain barrier permeable SOS1 inhibitor with an IC50 value of 0.11 μM. SOS1-IN-28 disrupts the SOS1: KRAS protein-protein interaction, with an IC50 of 0.29 μM for the KRAS-RAF interaction. SOS1-IN-28 blocks GTP loading of KRAS, inhibits RAS-MAPK pathway activity, and reduces cancer cell proliferation. SOS1-IN-28 can be used for the research of KRAS G12C-mutant lung cancer .
Cat. No.: HY-P704193
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: SOS1; Son Of Sevenless Homolog 1 (Drosophila), Isoform CRA_d; Prev. GINGF; Guanine Nucleotide Exchange Factor; HGF; Uncharacterized protein SOS1; GF1; Alternate SOS1; Gingival Fibromatosis, Hereditary, 1; GGF1; Son Of Sevenless Homolog 1; NS4; SOS-1; SOS
Species:
Source:
Cat. No.: HY-W115490
CAS No.: 2377645-90-2
Target:
Research Areas:
4-Chloro-3-(2,4-dioxo-1,3-diazinan-1-yl)benzoic acid is an E3 ligase ligand that can be used in the recruitment of CRBN protein. 4-Chloro-3-(2,4-dioxo-1,3-diazinan-1-yl)benzoic acid can used to synthesis of PROTAC SOS1 degrader-4 (HY-153674) .
Cat. No.: HY-L260
79 compounds
KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2.
MCE KRAS Targeted Compound Library contains 79 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
