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KRAS+inhibitor

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76

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-173632

    Ras Cancer
    AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers .
    AMG410
  • HY-153723
    BI-2493
    4 Publications Verification

    Ras Cancer
    BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research .
    BI-2493
  • HY-126247

    Ras Cancer
    BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (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.
    BI-2852
  • HY-148098
    Pan KRas-IN-1
    1 Publications Verification

    Ras Cancer
    Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
    Pan KRas-IN-1
  • HY-137497

    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 .
    KRAS inhibitor-9
  • HY-125847
    Salvianolic acid F
    1 Publications Verification

    Ras PI3K Akt Caspase Apoptosis Bcl-2 Family NF-κB MMP Cancer
    Salvianolic acid F is a KRAS inhibitor, especially for KRAS G12D. Salvianolic acid F inhibits NF-kB, MMP-9, and NO simultaneously. Salvianolic acid F inhibits cancer cell growth, invasion, and migration and induces apoptosis via the EP300/PI3K/AKT pathway in vitro. Salvianolic acid F inhibits the growth of KRAS-dependent lung cancer cells via the PI3K/AKT signaling pathway in vivo. Salvianolic acid F can be used in the research of various cancers, including KRAS G12D-driven non-small cell lung cancer (NSCLC) and ovarian cancer .
    Salvianolic acid F
  • HY-159652
    KRAS inhibitor-31
    1 Publications Verification

    Ras Cancer
    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 KRas G12V, respectively .
    KRAS inhibitor-31
  • HY-175870

    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-159190

    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-122914
    KRAS inhibitor-3
    1 Publications Verification

    Ras Cancer
    KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
    KRAS inhibitor-3
  • HY-176785S

    Ras Apoptosis p38 MAPK Caspase TNF Receptor Cancer
    MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
    MCB-294
  • HY-138295

    Ras Cancer
    KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1 .
    KRAS inhibitor-10
  • HY-164350

    Ras ERK p38 MAPK Cancer
    KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .
    KRAS inhibitor-27
  • HY-179253

    Ras Cancer
    KRAS-IN-47 is a KRAS inhibitor with IC50 < 50 nM against KRAS G12V. KRAS-IN-47 can be used for the study of cancers .
    KRAS-IN-47
  • HY-122641

    Phosphodiesterase (PDE) Cancer
    Deltasonamide 1 is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
    Deltasonamide 1
  • HY-159474

    Ras Cancer
    KRAS inhibitor-24 (compound 115c) is a pyridopyrimidine KRAS inhibitor, with an IC50 of < 100 nM for KRas G12V, KRas WT and KRas G12R .
    KRAS inhibitor-24
  • HY-177511

    Ras p38 MAPK Raf MEK ERK Cancer
    KRAS G12D-IN-30 (Compound 4) is a KRAS inhibitor. KRAS G12D-IN-30 inhibits the activation of the downstream MAPK signaling cascade (Raf1-MEK-ERK) by blocking the activity of the KRAS G12 mutant. KRAS G12D-IN-30 can be used for the research of cancer .
    KRAS G12D-IN-30
  • HY-178042

    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-169311

    Ras Cancer
    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 KRAS G12V 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 .
    KRAS inhibitor-37
  • HY-135865

    Ras Cancer
    KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B .
    KRAS inhibitor-7
  • HY-126247B

    Drug Derivative Ras Cancer
    (R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (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.
    (R)-BI-2852
  • HY-159476

    Ras Cancer
    KRAS inhibitor-26 (compound 194a) is a potent KRAS G12V inhibitor (IC50: ≤100 nM). KRAS inhibitor-26 can be used for cancer research .
    KRAS inhibitor-26
  • HY-146544

    Ras Cancer
    KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC50 of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC50s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers .
    KRAS inhibitor-14
  • HY-122641D

    Phosphodiesterase (PDE) Cancer
    Deltasonamide 1 TFA is a PDE6δ-KRas inhibitor. Deltasonamide 1 can inhibit PDE6δ-KRas with a KD of 203 pM. Deltasonamide 1 can be used for the research of tumors .
    Deltasonamide 1 TFA
  • HY-156555

    Ras Cancer
    pan-KRAS-IN-3 (Example 84) is a pan-KRAS inhibitor. pan-KRAS-IN-3 can be used for research of cancers . pan-KRAS-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    pan-KRAS-IN-3
  • HY-176250

    Ras ERK Cancer
    KRAS-IN-43 (Compound 9) is a pan-KRAS inhibitor with IC50 values of 0.15 μM, 0.14 μM, and 0.47 μM against KRAS G12V, KRAS G12C and wild-type KRAS, respectively. KRAS-IN-43 disrupts the interaction between KRAS and cRAF, and inhibits ERK phosphorylation. KRAS-IN-43 is promising for research of KRAS mutation-related cancers (such as pancreatic cancer, colorectal cancer, and lung cancer) .
    KRAS-IN-43
  • HY-130260

    Ras Cancer
    KRAS inhibitor-4 (compound F12) is a potent KRAS inhibitor and developed as anticancer agents .
    KRAS inhibitor-4
  • HY-151288

    Ras Cancer
    KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC50 value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research .
    KRAS inhibitor-21
  • HY-146543

    Ras Cancer
    KRAS inhibitor-13 (compound 5-6) is a potent KRAS G12C inhibitor with an IC50 of 0.883 µM. KRAS inhibitor-13 shows p-ERK inhibition activities with IC50s of 5.9, >100 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-13 has the potential for the research of pancreatic, colorectal, and lung cancers .
    KRAS inhibitor-13
  • HY-146533

    Ras Cancer
    KRAS inhibitor-12 (compound 6-1) is a potent KRAS G12C inhibitor with an IC50 of 0.537 µM. KRAS inhibitor-12 shows p-ERK inhibition activities with IC50s of 1.3, 3.7 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-12 has the potential for the research of pancreatic, colorectal, and lung cancers .
    KRAS inhibitor-12
  • HY-146476

    Ras Cancer
    KRAS inhibitor-18 (compound 3-10) is a potent KRAS G12C inhibitor with an IC50 of 4.74 µM. KRAS inhibitor-18 shows p-ERK inhibition activities with IC50s of 66.4, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-18 has the potential for the research of pancreatic, colorectal, and lung cancers .
    KRAS inhibitor-18
  • HY-153412

    Ras Cancer
    KRAS inhibitor-22 (compound FB9/6B9) is a potent inhibitor of K-Ras. KRAS inhibitor-22 targets to Kras 4B(G12D) and (G12C), which can be used for cancer research .
    KRAS inhibitor-22
  • HY-159474A

    Ras Cancer
    (1R)-KRAS inhibitor-24 (compound 115c) is a pyridopyrimidine KRAS inhibitor, with an IC50 of < 100 nM for KRas G12V, KRas WT and KRas G12R .
    (1R)-KRAS inhibitor-24
  • HY-135864

    Ras Cancer
    KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A .
    KRAS inhibitor-6
  • HY-178501

    Ras Cancer
    KRAS-IN-45 (Compound 1.019) is a KRAS inhibitor. KRAS-IN-45 can be used for the study of cancers .
    KRAS-IN-45
  • HY-178502

    Ras Cancer
    KRAS-IN-46 (Compound 1.013) is a KRAS inhibitor. KRAS-IN-46 can be used for the study of cancers .
    KRAS-IN-46
  • HY-163489

    Ras Cancer
    pan-KRAS-IN-15 (compound 58) is a pan-KRAS inhibitor. pan-KRAS-IN-15 can be used in pancreatic cancer research .
    pan-KRAS-IN-15
  • HY-162366

    Ras Cancer
    KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor. KRAS G12D inhibitor 20 has antitumor activity .
    KRAS G12D inhibitor 20
  • HY-162439

    Ras Cancer
    pan-KRAS-IN-6 (compound 12) is a potent pan KRAS inhibitor with IC50 values of 9.79 nM (Kras G12D) and 6.03 nM (Kras G12V) .
    pan-KRAS-IN-6
  • HY-153940

    SOS1 Ras Cancer
    SOS1/KRAS-IN-1(Compound 2) is a SOS1/KRAS inhibitor, which can be used in the research of SOS1/KRAS-mediated diseases .
    SOS1/KRAS-IN-1
  • HY-137516A

    PROTACs Ras Cancer
    LC-2 epimer is a differential isomer of LC-2. LC-2 is a mutation-selective PROTAC depressant for KRAS and contains a ligand for the von Hippel Lindau E3 ligase linked to the KRAS inhibitor MRTX849 .
    LC-2 epimer
  • HY-164632

    Ras Cancer
    KRAS inhibitor-32 (compound 139A) is a KRAS inhibitor. KRAS inhibitor-32 can be used in anti-cancer research .
    KRAS inhibitor-32
  • HY-162976

    Ras Cancer
    KRAS inhibitor-35 (compound 72) is a KRAS inhibitor, with IC50 of 2 nM. KRAS inhibitor-35 can be used in tumor research .
    KRAS inhibitor-35
  • HY-162974

    Ras Cancer
    KRAS inhibitor-34 (compound 27) is a KRAS inhibitor, with IC50 of 6.4 nM. KRAS inhibitor-34 can be used in tumor research .
    KRAS inhibitor-34
  • HY-145436

    Ras Cancer
    KRAS inhibitor-11 (compound 12) is a KRAS inhibitor .
    KRAS inhibitor-11
  • HY-168442

    Ras PERK Cancer
    KRAS inhibitor-40 (Compound 41) is a KRAS inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of KRAS downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different KRAS mutation types and has antitumor activity .
    KRAS inhibitor-40
  • HY-159475

    Ras Cancer
    KRAS inhibitor-25 (compound 151a) is a pyridopyrimidine KRAS inhibitor, with an IC50 of < 100 nM against KRas G12V, KRas WT and KRas G12R .
    KRAS inhibitor-25
  • HY-169312

    Ras Cancer
    KRAS inhibitor-38 (Example 18) is a KRAS inhibitor that effectively suppresses the activity of KRAS G12C, KRAS G12D, and KRAS G12V in vivo .
    KRAS inhibitor-38
  • HY-151287

    Ras Cancer
    KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM .
    KRAS inhibitor-20

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