2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. SOS1
  5. SOS1 Inhibitor

SOS1 Inhibitor

SOS1 Inhibitors (54):

Cat. No. Product Name Effect Purity
  • HY-125817
    BI-3406
    		Inhibitor 99.95%
    BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
  • HY-114398
    BAY-293
    		Inhibitor 98.97%
    BAY-293, a valuable chemical probe, blocks RAS activation via disruption of the KRAS-SOS1 interaction with an IC50 of 21 nM. BAY-293 is a potent inhibitor of Son of Sevenless 1 (SOS1). SOS1 is the guanine nucleotide exchange factor (GEF) and activator of RAS.
  • HY-145926
    MRTX0902
    		Inhibitor 99.75%
    MRTX0902 is an orally active and potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).
  • HY-134885
    RMC-0331
    		Inhibitor 98.96%
    RMC-0331 (RM-023) is a potent, selective and orally bioavailable SOS1 inhibitor. RMC-0331 is an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction.
  • HY-151881
    SOS1-IN-15
    		Inhibitor 99.51%
    SOS1-IN-15 (Compound 37) is an orally active SOS1 inhibitor with an IC50 of 5 nM. SOS1-IN-15 is a promising agent candidate for the research of KRAS-driven cancer.
  • HY-176170
    SOS1-IN-19
    		Inhibitor
    SOS1-IN-19 (Compound 10i) is a potent inhibitor of SOS1 (Son of Sevenless 1) with an IC50 value of 165.2 nM. SOS1-IN-19 blocks KRAS activation by preventing GDP/GTP exchange in KRAS signaling pathway. SOS1-IN-19 is promising for research of KRAS-driven cancers (e.g., NSCLC and colorectal cancer).
  • HY-172221
    SOS1-IN-18
    		Inhibitor
    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.
  • HY-P2265A
    SAH-SOS1A TFA
    		Inhibitor 99.16%
    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.
  • HY-151517
    SOS1-IN-14
    		Inhibitor 99.60%
    SOS1-IN-14 is a potent, selective and orally active SOS1 inhibitor with an IC50 value of 3.9 nM. SOS1-IN-14 can be absorbed in the intestine via a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 can be used to research KRAS-mutated cancers. SOS1-IN-14 has better potent tumor suppression than BI-3406 (HY-125817).
  • HY-148278
    BI-0474
    		Inhibitor 99.83%
    BI-0474 is a potent KRASG12C 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.
  • HY-144962
    SOS1-IN-11
    		Inhibitor 98.22%
    SOS1-IN-11 is a potent SOS1 inhibitor with an IC50 value of 30 nM.
  • HY-101796
    NSC-70220
    		Inhibitor 99.42%
    NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect.
  • HY-161235
    BTX-7312
    		Inhibitor 98.35%
    BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers pERK and pS6 and shows antiproliferative activity in various KRAS-mutated cells.
  • HY-163939
    RGT-018
    		Inhibitor 99.77%
    RGT-018 is a potent and orally active SOS1 inhibitor with anti-tumor effects. RGT-018 exerts anti-cancer cell proliferation activity by inhibiting KRAS activation.
  • HY-161233
    BTX-6654
    		Inhibitor
    BTX-6654 is a target-dependent and -specific cereblon-based bifunctional SOS1 PROTAC degrader. BTX-6654 reduces downstream signaling markers pERK and pS6, and displays antiproliferative activity in cells harboring various KRAS mutations.
  • HY-158310
    SOS1/EGFR-IN-1
    		Inhibitor 99.54%
    SOS1/EGFR-IN-1 (compound SE-9) is a dual-target inhibitor for the prostate cancer. SOS1/EGFR-IN-1 inhibits effectively SOS1(IC50=42.13±1.55 nM) and EGFR(IC50=1.01±0.04 nM) by inhibiting their downstream effector molecules. SOS1/EGFR-IN-1 induces apoptosis and G1 phase cell cycle arrest, reducing angiogenesis and migration. SOS1/EGFR-IN-1 shows significant antitumor effects in prostate cancer cells PC-3 (IC50=0.45±0.03 μM).
  • HY-114398A
    (S)-BAY-293
    		Inhibitor
    (S)-BAY-293 is a negative control of BAY 293. BAY 293 is a potent KRAS-SOS1 interaction inhibitor.
  • HY-144212
    SOS1-IN-8
    		Inhibitor
    SOS1-IN-8 is a potent SOS1 inhibitor with IC50s of 11.6 and 40.7 nM for SOS1-G12D and SOS1-G12V, respectively (WO2022017339A1, compound 2).
  • HY-153989
    SOS1-IN-16
    		Inhibitor
    SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitory activity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research.
  • HY-144211
    SOS1-IN-7
    		Inhibitor
    SOS1-IN-7 (compound 18-p1) is a potent SOS1 inhibitor with IC50s of 20 and 67 nM for SOS1-G12D and SOS1-G12V, respectively.