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KRAS mutant cancer cells

" in MedChemExpress (MCE) Product Catalog:

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-156819
    Zoldonrasib
    5 Publications Verification

    RMC-9805; KRAS G12D inhibitor 18

    		 Ras Apoptosis Cancer
    Zoldonrasib (RMC-9805) is a potent and orally active KRAS G12D inhibitor.Zoldonrasib induces apoptosis in KRAS G12D mutant cancer cells. Zoldonrasib has the potential for the research of KRAS G12D mutant cancer .
    Zoldonrasib
  • HY-153724
    BI-2865
    Maximum Cited Publications
    11 Publications Verification

    		 Ras Cancer
    BI-2865 is a none-covalent pan-KRAS Inhibitor. BI-2865 binds to WT, G12C, G12D, G12V and G13D mutant KRAS with KDs of 6.9, 4.5, 32, 26, 4.3 nM respectively. BI-2865 inhibits the proliferation of G12C, G12D or G12V mutant KRAS expressing BaF3 cells (mean IC50: roughly 140 nM) .
    BI-2865
  • HY-173629
    RMC-5127

    		Ras Apoptosis Cancer
    RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
    RMC-5127
  • HY-132844
    Tunlametinib

    HL-085

    		 MEK Cancer
    Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer) .
    Tunlametinib
  • HY-176523
    KRAS G12D-IN-29

    		Ras Cancer
    KRAS G12D inhibitor 29 (Compound Formula (I)) is an orally active and selective KRAS G12D mutant inhibitor. KRAS G12D inhibitor 29 blocks downstream signaling pathways mediated by KRAS G12D, suppressing tumor cell proliferation. KRAS G12D inhibitor 29 is promising for research of KRAS G12D mutation-related cancers (such as pancreatic cancer, lung cancer, colorectal cancer) .
    KRAS G12D-IN-29
  • HY-162960
    pan-KRAS-IN-18

    		Ras Cancer
    pan-KRAS-IN-18 is a panKRAS inhibitor that inhibits KRAS WT and KRAS G12V with IC50s of 29 and 9 nM, respectively. pan-KRAS-IN-18 exhibits antiproliferative activity in KRAS-mutant cell lines. pan-KRAS-IN-18 can be used for lung cancer research .
    pan-KRAS-IN-18
  • HY-173405
    VVD-699

    		Ras PI3K Akt Cancer
    VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .
    VVD-699
  • HY-114436
    MRTX-1257
    5 Publications Verification

    		 Ras Cancer
    MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257
  • HY-164315
    KRAS G12C inhibitor 67

    		Ras PERK Cancer
    KRAS G12C inhibitor 67 (Example 35) is an orally active KRAS G12C inhibitor. KRAS G12C inhibitor 67 inhibits pERK and active KRas. KRAS G12C inhibitor 67 selectively inhibits the growth of various KRAS G12C mutant tumor cell lines. KRAS G12C inhibitor 67 exhibits anticancer activity against esophageal cancer, bladder cancer, colorectal cancer, lung cancer, and pancreatic cancer .
    KRAS G12C inhibitor 67
  • HY-176954
    RSC-1255

    		Proton Pump Ras Autophagy Apoptosis Cancer
    RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a Kd = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRAS G13D and KRAS G12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers .
    RSC-1255
  • HY-156671
    RMC-4998

    		Ras PI3K ERK mTOR Apoptosis Cancer
    RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .
    RMC-4998
  • HY-161176
    PROTAC KRAS G12D degrader 1

    		PROTACs Ras ERK Cancer
    PROTAC KRAS G12D degrader 1 is a selective PROTAC KRAS G12D degrader. PROTAC KRAS G12D degrader 1 inhibits proliferation of KRAS G12D-mutant cells and suppresses ERK phosphorylation. PROTAC KRAS G12D degrader 1 inhibits tumor growth in mice bearing AsPC-1 xenografts. PROTAC KRAS G12D degrader 1 can be used for the study of KRAS G12D-driven cancers.(Pink: KRAS ligand (HY-175892), Blue: VHL Ligand (HY-112078), Black: Linker, E3 ligase ligand-linker conjugate (HY-175893)) .
    PROTAC KRAS G12D degrader 1
  • HY-B0984
    Fendiline hydrochloride
    3 Publications Verification

    		 Calcium Channel Ras STING Autophagy Infection Cardiovascular Disease Cancer
    Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
    Fendiline hydrochloride
  • HY-176792
    ACBI-4

    		PROTACs Ras Cancer
    ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRAS G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .
    ACBI-4
  • HY-162809
    XMU-MP-9

    		Ras Cancer
    XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used for the study of colon, lung and pancreatic cancer .
    XMU-MP-9
  • HY-175870
    Eras-4001

    		Ras Cancer
    Eras-4001 (Compound 14-1) is a pan-KRAS inhibitor. Eras-4001 has potent antitumor activities and significantly inhibits the proliferation of wild-type and mutant (such as KRAS G12D, KRAS G12V and KRAS G12C) cancer cells. Eras-4001 effectively inhibits tumor growth in GP2D and Panc0403 xenograft mouse models .
    Eras-4001
  • HY-B0984A
    Fendiline
    3 Publications Verification

    		 Calcium Channel Ras STING Autophagy Infection Cardiovascular Disease Cancer
    Fendiline, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
    Fendiline
  • HY-159190
    HRX-0233

    		MAPKAPK2 (MK2) Cancer
    HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
    HRX-0233
  • HY-P2265A
    SAH-SOS1A TFA

    		SOS1 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). 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 TFA
  • HY-178042
    SS-3091

    		Ras Akt ERK Cancer
    SS-3091 is a pan-KRas inhibitor active across KRas G12D, KRas G12C, KRas G12V, KRas G12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRas G12 mutations. SS-3091 can be used for the research of KRas-driven cancers .
    SS-3091
  • HY-124761
    Poloppin

    		Polo-like Kinase (PLK) Autophagy Mitosis Cancer
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors .
    Poloppin
  • HY-B0984R
    Fendiline hydrochloride (Standard)

    		Calcium Channel Ras STING Autophagy Reference Standards Infection Cardiovascular Disease Cancer
    Fendiline (hydrochloride) (Standard) is the analytical standard of Fendiline (hydrochloride). This product is intended for research and analytical applications. Fendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10) .
    Fendiline hydrochloride (Standard)
  • HY-156671A
    RMC-4998 formic

    		Ras PI3K ERK mTOR Apoptosis Cancer
    RMC-4998 formic is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 formic can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 formic can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 formic can be used for non-small cell lung cancer (NSCLC) research .
    RMC-4998 formic
  • HY-163299
    pan-KRAS-IN-5
    1 Publications Verification

    		 Ras Apoptosis PI3K Akt p38 MAPK Cancer
    pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research .
    pan-KRAS-IN-5
  • HY-P991571
    GC1118

    GC-1118A

    		 EGFR PERK Akt Cancer
    GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
    GC1118
  • HY-157458
    PDEδ autophagic degrader 1

    		ATTECs Phosphodiesterase (PDE) Autophagy Cancer
    PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .
    PDEδ autophagic degrader 1
  • HY-175025
    CH091138

    		PROTACs Ras Apoptosis Cancer
    CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .
    CH091138
  • HY-162445
    KRASG12D-IN-3

    		Ras PERK Cancer
    KRASG12D-IN-3 is an orally active KRAS G12D inhibitor. KRASG12D-IN-3 inhibits the growth of gastric cancer and pancreatic cancer cells. KRASG12D-IN-3 inhibits the activity of p-ERK in gastric cancer cells. KRASG12D-IN-3 can be used for the research of gastric cancer and pancreatic cancer .
    KRASG12D-IN-3
  • HY-P10436
    Braftide

    		Raf Cancer
    Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research .
    Braftide
  • HY-159591
    YK-8S

    		Ras Akt ERK Cancer
    YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .
    YK-8S
  • HY-174261
    KRAS-IN-5

    		Ras Cancer
    KRAS-IN-5 (Compound Ex 6) is an orally active and selective inhibitor targeting KRAS mutants (including KRAS G12D, KRAS G12V, KRAS WT) with a GNE IC50 value of 1.3 nM against KRAS G12D. KRAS-IN-5 blocks tumor cell proliferation by inhibiting KRAS-mediated signaling pathways (e.g., reducing ERK phosphorylation). KRAS-IN-5 is promising for research of KRAS mutation-related cancers, such as pancreatic cancer, colorectal cancer, lung cancer .
    KRAS-IN-5
  • HY-179403
    KRASG12C IN-17

    		Ras Cancer
    KRASG12C IN-17 is an orally active covalent KRAS G12C inhibitor, showing strong inhibitory activity in KRAS G12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRAS G12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer .
    KRASG12C IN-17
  • HY-P2265
    SAH-SOS1A

    		SOS1 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 .
    SAH-SOS1A
  • HY-172237
    Sosimerasib

    		Ras Cancer
    Sosimerasib is an orally active KRAS G12C inhibitor. Sosimerasib can be used in research related to non-small cell lung cancer .
    Sosimerasib
  • HY-178497
    ZJK-807

    		PROTACs Ras p38 MAPK TNF Receptor Inflammation/Immunology Cancer
    ZJK-807 is a highly effective and selective PROTAC degrader targeting KRASG12D (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRASG12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506) .
    ZJK-807
  • HY-114436S
    MRTX-1257-d6

    		Isotope-Labeled Compounds Cancer
    MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
    MRTX-1257-d6
  • HY-176870
    KRAS-IN-42

    		Ras Cancer
    KRAS-IN-42 (Compound Z1063) is a covalent KRAS G12D mutants inhibitor. KRAS-IN-42 is promising for research of KRAS G12D-mutant cancers (e.g., non-small cell lung cancer, colorectal cancer) .
    KRAS-IN-42
  • HY-W1126467
    RAS-IN-5

    		Ras Cancer
    RAS-IN-5 (Example 2) is a RAS inhibitor. RAS-IN-5 significantly inhibits the interaction between RAF1 and active KRAS mutant protein or HRAS WT protein. RAS-IN-5 significantly inhibits the cell viability of KRAS, NRAS, and EGFR mutant cells. RAS-IN-5 can be used in the research of colorectal cancer, liver cancer, and non-small cell lung cancer .
    RAS-IN-5
  • HY-156671B
    RMC-4998 TFA

    		Ras PI3K ERK mTOR Apoptosis Cancer
    RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 TFA can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 TFA can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 TFA can be used for for non-small cell lung cancer (NSCLC) research .
    RMC-4998 TFA
  • HY-173329
    KRAS-IN-41

    		Ras Cancer
    KRAS-IN-41 is an inhibitor of KRAS with IC50 values of <0.01 μM for KRAS G12D and KRAS G12V. KRAS-IN-41 inhibits RAS mutant cell lines, GP2D (KRAS-G12D) and SW620 (KRAS-G12V). KRAS-IN-41 can be used in cancer research .
    KRAS-IN-41
  • HY-172919
    PDEδ/NAMPT IN-1

    		Phosphodiesterase (PDE) NAMPT Apoptosis Cancer
    PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) (KD=0.410 nM) and nicotinamide phosphoribosyl transferase (NAMPT) (IC50=2.21 nM). PDEδ/NAMPT IN-1 blocks KRAS-related signal transduction and interferes with the synthesis of nicotinamide adenine dinucleotide (NAD +), inducing apoptosis in KRAS mutant pancreatic cancer cells. PDEδ/NAMPT IN-1 is promising for research of KRAS mutant pancreatic cancer .
    PDEδ/NAMPT IN-1
  • HY-163636
    Deltaflexin3

    A-442b

    		 Phosphodiesterase (PDE) Ras Cancer
    Deltaflexin3 is a potent PDE6D inhibitor. Deltaflexin3 reduces the signaling of Ras and selectively decreases the KRAS mutant and PDE6D-dependent cancer cells growth .
    Deltaflexin3
  • HY-164492
    LSN3074753

    		Raf Cancer
    LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation .
    LSN3074753
  • HY-174254
    AKT-IN-28

    		Akt Apoptosis Caspase PARP β-catenin Cancer
    AKT-IN-28 is an Akt allosteric inhibitor, a derivative of Shikonin (HY-N0822). AKT-IN-28 effectively binds to the allosteric site of Akt through hydrophobic and hydrogen interactions with Kd of 2.07 μM. AKT-IN-28 significantly inhibits Akt activity, induces cell apoptosis, arrests cell cycle in G2/M phase, and suppresses proliferation, migration and metabolism of KRAS mutant colorectal cancer cells .
    AKT-IN-28
  • HY-161654
    PROTAC SOS1 degrader-10

    		SOS1 PROTACs Ras Cancer
    PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
    PROTAC SOS1 degrader-10
  • HY-164513
    NHTD

    		Ras Phosphodiesterase (PDE) Cancer
    NHTD is a KRAS-PDEδ inhibitor. NHTD targets the prenyl-binding pocket of PDEδ, altering the cellular localization of KRAS, thereby inhibiting the proliferation of KRAS-mutant cancer cells and inducing apoptosis. NHTD can be used for research on KRAS-driven non-small cell lung cancer (NSCLC) .
    NHTD
  • HY-151999
    KRAS G12C inhibitor 65

    		Ras Cancer
    KRAS G12C inhibitor 65 is a potent and covalent KRAS G12C inhibitor that traps KRAS G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer .
    KRAS G12C inhibitor 65
  • HY-174851
    KRAS G12C-IN-70

    		Ras Cancer
    KRAS G12C-IN-70 is a selective KRAS G12C mutant inhibitor. KRAS G12C-IN-70 blocks KRAS G12C-mediated downstream signaling pathways (e.g., RAF-MEK-ERK) and inhibits tumor cell proliferation. KRAS G12C-IN-70 is promising for research of KRAS G12C mutation-related tumors (such as non-small cell lung cancer, colorectal cancer) .
    KRAS G12C-IN-70
  • HY-137971
    (±)-Spiro-oxanthromicin A

    		Ras Cancer
    (±)-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 .
    (±)-Spiro-oxanthromicin A
  • HY-168512
    BRAFV600E-IN-1

    		Raf Cancer
    BRAFV600E-IN-1 (compound 9S) is a BRAF inhibitor. BRAFV600E-IN-1 has a significant apoptosis-inducing effect in cell lines expressing mutant KRAS and cancer cells expressing BRAFV600E .
    BRAFV600E-IN-1

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