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Results for "

H358

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56

Inhibitors & Agonists

1

Peptides

2

Isotope-Labeled Compounds

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-153346
    Elironrasib
    2 Publications Verification

    RMC-6291

    		 Ras ERK Apoptosis Cancer
    Elironrasib is an orally active and covalent inhibitor of KRAS G12C(ON). Elironrasib forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
    Elironrasib
  • HY-148517
    AZD0095
    4 Publications Verification

    		 Monocarboxylate Transporter Cancer
    AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205) .
    AZD0095
  • 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-162431
    Calderasib

    MK-1084

    		 Ras Cancer
    Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research .
    Calderasib
  • 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-160023
    Elisrasib

    D3S-001

    		 Ras PERK Cancer
    Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
    Elisrasib
  • HY-128522
    ARS-1323-alkyne

    		Ras Cancer
    ARS-1323-alkyne is a covalent inhibitor probe that covalently binds to the Switch-II pocket (S-IIP) of the KRAS G12C mutant protein. ARS-1323-alkyne visualizes the covalent modification of KRAS G12C and quantitatively measures the binding efficiency of the inhibitor to the target. ARS-1323-alkyne can be used to validate the target occupancy of KRAS G12C inhibitors and the synergistic mechanism of combination therapy .
    ARS-1323-alkyne
  • 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 .
    KRAS inhibitor-9
  • HY-18707
    K-Ras(G12C) inhibitor 12

    		Ras Apoptosis Cancer
    K-Ras(G12C) inhibitor 12 is an irreversible inhibitor of K-Ras(G12C). K-Ras(G12C) inhibitor 12 can alter the nucleotide-binding preference of K-Ras and block its interaction with effector proteins. K-Ras(G12C) inhibitor 12 can reduce cell viability and induce apoptosis in lung cancer cell lines with G12C mutations. K-Ras(G12C) inhibitor 12 has anti-tumor activity .
    K-Ras(G12C) inhibitor 12
  • 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-176812
    VVD-849

    		Ras PI3K Akt Cancer
    VVD-849 is a RAS ligand. VVD-849 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α and promotes RAS/PI3K interaction. VVD-849 partially inhibits pAKT (S473) in HER2-overexpressing tumors. VVD-849 can be used for the research of cancers such as breast cancer .
    VVD-849
  • HY-176811
    VVD-442

    		Ras PI3K Akt Cancer
    VVD-442 is an inhibitor targeting PI3Kα. VVD-442 covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, induces conformational changes, and disrupts the interaction between PI3K p110α and RAS proteins. VVD-442 also blocks RAS-mediated PI3K activation. VVD-442 can be used in research related to RAS-mutant cancers and HER2-overexpressing cancers .
    VVD-442
  • 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-148278
    BI-0474

    		SOS1 Ras Cancer
    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 .
    BI-0474
  • HY-U00416
    ARS-1323

    		Ras Cancer
    ARS-1323 is a KRAS G12C inhibitor. ARS-1323 specifically binds to the cysteine residue on the mutant K-Ras protein, locks it in the GDP-bound conformation, thereby blocking K-Ras activation and downstream signaling pathways. ARS-1323 can be used to investigate the signal transduction mechanisms and growth characteristics of tumor cells driven by K-Ras G12C .
    ARS-1323
  • HY-138294
    RAS/RAS-RAF-IN-1
    2 Publications Verification

    		 Ras Raf Cancer
    RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity .
    RAS/RAS-RAF-IN-1
  • HY-144269
    SHR902275

    		Raf Cancer
    SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
    SHR902275
  • HY-169311
    KRAS inhibitor-37

    		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-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-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-144271
    RAF-IN-1

    		Raf Cancer
    RAF-IN-1 is a potent b/cRAF inhibitor with an IC50s of 3.8 nM, 36 nM, 29.4 nM for cRAF, bRAF wt, and bRAF V600E. RAF-IN-1 shows cell growth inhibition with GI50s of 3.4 and 2.9 nM for H358 and A375 cell line bearing bRAF V600E mutation, respectively .
    RAF-IN-1
  • 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-142946
    KRAS G12C inhibitor 44

    		Ras Cancer
    KRAS G12C inhibitor 44 (compound 54) is a potent and orally active KRAS G12C inhibitor. KRAS G12C inhibitor 44 shows anti-proliferation activities with IC50s of 0.016, 0.028 µM in MIA PaCA-2, H358 cells, respectively. KRAS G12C inhibitor 44 shows antitumor effects in vivo .
    KRAS G12C inhibitor 44
  • HY-172221
    SOS1-IN-18

    		SOS1 Ras ERK Cancer
    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 .
    SOS1-IN-18
  • HY-115663
    C620-0696

    		Epigenetic Reader Domain c-Myc Cancer
    C620-0696 is an inhibitor targeting the brom domain of BPTF, with a KD value of 35.5 μM. C620-0696 can exert cytotoxic effects on A549 and H358 cells, inhibiting the expression of c-Myc. C620-0696 inhibits cell migration and colony formation, and induces apoptosis and cell cycle arrest. C620-0696 can be used in the research of non-small cell lung cancer .
    C620-0696
  • HY-144323
    YF135

    		PROTACs PERK Cancer
    YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
    YF135
  • HY-173250
    YN14-H

    		PROTACs Ras Apoptosis Cancer
    YN14-H is a PROTAC degrader targeting KRAS G12C. YN14-H inhibits cell growth in NCI-H358 and MIA PaCa-2 cells (IC50 values of 0.042, 0.021 μM, DC50 values of 28.9, 18.1 nM, respectively). YN14-H significantly induces apoptosis and inhibits migration. YN14-H demonstrates favorable pharmacokinetic properties and excellent antitumor activity in vivo. (Structure Note: Pink: target protein ligand (HY-173252); Blue: E3 ligase ligand (HY-125905); Black: linker (HY-Y0840); E3 ligase ligand + linker (HY-173253) .
    YN14-H
  • HY-164389
    SML-10-70-1

    		Ras Cancer
    SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC50 of 26.6-47.6 μM .
    SML-10-70-1
  • HY-174088
    CDK4/6/BRD4-IN-2

    		CDK Discoidin Domain Receptor Apoptosis Reactive Oxygen Species (ROS) DNA/RNA Synthesis Cancer
    CDK4/6/BRD4-IN-2 (Compound PJ2) is a dual inhibitor of CDK4/6 and BRD4 with IC50 values for CDK4, CDK6, BRD4 (BD1), and BRD4 (BD2) of 168.75, 292.45, 23.17, and 3.12 nM respectively. CDK4/6/BRD4-IN-2 has a strong inhibitory effect on non-small cell lung cancer (NSCLC) cell lines. CDK4/6/BRD4-IN-2 induces cell cycle arrest, senescence and apoptosis through ROS-mediated DNA damage. CDK4/6/BRD4-IN-2 can also effectively inhibit the migration and invasion of NCI-H358 cells. CDK4/6-IN-2 can be used for the study of KRAS-mutated NSCLC .
    CDK4/6/BRD4-IN-2
  • HY-115907
    K20

    		Ras ERK Apoptosis Cancer
    K20 is a potent and selective KRas G12C inhibitor with an IC50 of 1.16 µM. K20 shows anticancer activity in H358 cells (IC50= 0.78 µM). K20 decreases the levels of phosphorylated Erk and leads to cancer cell apoptosis. K20 suppresses NCI-H358 tumor growth with a TGI of 41% without causing obvious toxicity .
    K20
  • HY-142945
    KRAS G12C inhibitor 43

    		Ras Cancer
    KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively .
    KRAS G12C inhibitor 43
  • HY-146061
    KRAS G12C inhibitor 48

    		Ras Cancer
    KRAS G12C inhibitor 48 (compound 6e) is a potent KRAS G12C inhibitor with an IC50 of 639.91 nM. KRAS G12C inhibitor 48 (0-50 µM) shows anti-proliferative activity with IC50s of 0.796, 6.33, 16.14 µM for H358, H23, A549 cells, respectively .
    KRAS G12C inhibitor 48
  • HY-170550
    KRAS G12C inhibitor 69

    		Ras ERK Cancer
    KRAS G12C inhibitor 69 (Compound K09) is the inhibitor for mutant RAS protein KRASG12C with an IC50 of 4.36 nM. KRAS G12C inhibitor 69 inhibits the ERK phosphorylation in NCI-H358 and MIA-PACA-2 with an IC50 of 12 nM and 7 nM. KRAS G12C inhibitor 69 inhibits the proliferation of cancer cell NCI-H358 and MIA-PACA-2 with IC50 of 3.15 nM and 2.33 nM .
    KRAS G12C inhibitor 69
  • HY-145020
    KRAS G12C inhibitor 23

    		Ras Cancer
    KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1) .
    KRAS G12C inhibitor 23
  • HY-161173
    PROTAC SOS1 degrader-5

    		PROTACs Ras SOS1 Cancer
    PROTAC SOS1 degrader-5 (compound 4) is a potent PROTAC SOS1 degrader, with the DC50 of 13 nM. PROTAC SOS1 degrader-5 strongly inhibits NCI-H358 cells proliferation with an IC50 of 5 nM .
    PROTAC SOS1 degrader-5
  • HY-157888
    SHP2-IN-26

    		SHP2 Phosphatase Cancer
    SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC50 value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity .
    SHP2-IN-26
  • HY-153699
    SHP2-IN-14

    		SHP2 Cancer
    SHP2-IN-14 (compound 27) is an orally active and potent SHP2 allosteric inhibitor (IC50=7 nM) with anti-tumor activity. SHP2-IN-14 inhibits tumor progression in NCI-H358 tumor bearing mice, exhibits good pharmacokinetic characteristics and safty .
    SHP2-IN-14
  • HY-168013
    KRASG12C IN-14

    		Ras Cancer
    KRASG12C IN-14 (compound 15) is an inhibitor targeting the KRAS G12C mutation. KRASG12C IN-14 inhibits CYPA-dependent KRAS-BRAF with an IC50 of 0.002 μM. KRASG12C IN-14 inhibits ERK phosphorylation in NCI-H358 cells with an IC50 of 0.002 μM .
    KRASG12C IN-14
  • HY-168577
    KRAS G12D inhibitor 25

    		Ras EGFR Cancer
    KRAS G12D inhibitor 25 (Compound 148) is an inhibitor for KRAS G12C and HSP90α with IC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 inhibits the proliferation of MIA PaCa-2 and NCI-H358 with EC50 of < 0.1 μM and 0.1-1 μM, respectively. KRAS G12D inhibitor 25 degrades ERBB2 with a DC50 of 0.1-1 μM .
    KRAS G12D inhibitor 25
  • HY-180183
    DLG-41

    		Epigenetic Reader Domain Cancer
    DLG-41 is a GAS41 YEATS domain inhibitor (IC50: 600 nM in AlphaLISA). DLG-41 potently disrupts the association of GAS41 YEATS with chromatin in cells. DLG-41 strongly enhances levels of CDKN1A. DLG-41 has anticancer activity against NSCLC .
    DLG-41
  • HY-175244
    SOS1-IN-20

    		SOS1 Ras Potassium Channel Cancer
    SOS1-IN-20 (Compound 12f) is an orally active SOS1 inhibitor with an IC50 of 5.11 nM against KRAS G12C::SOS1. By disrupting the interaction between KRAS and SOS1, SOS1-IN-20 inhibits KRAS activation and downstream signal transduction. SOS1-IN-20 has an IC50 of 253 nM for p-ERK in PC-9 cells and 16.71 μM for hERG channel . SOS1-IN-20 can inhibit the proliferation of tumor cells and has antitumor activity .
    SOS1-IN-20
  • HY-163595
    KRAS G12D-IN-31

    		Ras Cancer
    KRAS G12D-IN-31 is a potent KRAS G12D inhibitor with an IC50 of < 100 nM. KRAS G12D-IN-31 inhibits the proliferation of RAS-dependent cells (KRAS G12C, KRAS G12D, KRAS G12V and KRAS WT). KRAS G12D-IN-31 can be used to study non-small cell lung cancer, gastric cancer, colon cancer, and malignant melanoma .
    KRAS G12D-IN-31
  • HY-175326
    SOS1-IN-21

    		SOS1 Cancer
    SOS1-IN-21 is an orally active inhibitor of son of Sevenless 1 (SOS1) with an IC50 of 15 nM. SOS1 is a guanine nucleotide exchange factor (GEF) that activates KRAS by facilitating the exchange of GDP for GTP. SOS1-IN-21 exhibits potent antiproliferative activity, with IC50 values of 16 nM in NCI-H358 and 17 nM in Mia Paca-2 cell proliferation assays. SOS1-IN-21 exhibits significant antitumor activity in the Mia Paca-2 xenograft model. SOS1-IN-21 can be used for the study of KRAS mutant tumors, such as pancreatic cancer .
    SOS1-IN-21
  • HY-163594
    KRAS-IN-59

    		Ras Cancer
    K-Ras-IN-58 is a K-RAS inhibitor and shows inhibitory activity against KRASG12D, KRASG12C and KRAS WT. K-Ras-IN-58 inhibits proliferation of cancer cells .
    KRAS-IN-59
  • HY-147635
    KRAS G12C inhibitor 54

    		Ras Cancer
    KRAS G12C inhibitor 54 (Compound 1) is a KRAS G12C inhibitor .
    KRAS G12C inhibitor 54
  • HY-160220S
    KRAS inhibitor-23

    		Ras Cancer
    KRAS inhibitor-23 (Isomer 2 of compound i) is a potent inhibitor of KRAS that plays an important role in cancer research .
    KRAS inhibitor-23
  • HY-132979
    KRAS G12C inhibitor 18

    		Ras Cancer
    KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities .
    KRAS G12C inhibitor 18
  • HY-151968
    KRAS G12C inhibitor 57

    		Ras Cancer
    KRAS G12C inhibitor 57 (Compound 50) is a potent, selective, covalent and orally active KRAS G12C inhibitor with an IC50 of 0.21 μM in KRAS G12C/SOS1 binding assay. KRAS G12C inhibitor 57 induces cancer cell apoptosis .
    KRAS G12C inhibitor 57
  • HY-P10226
    PGD97

    		Chloride Channel CFTR Endocrinology
    PGD97 is a selective cyclic peptide inhibitor against CAL/CFTR interactions, with a KD value of 6 nM towards the CAL PDZ domain for its desulfide cyclized form. PGD97 (desulfide cyclized form) has selectivity ≥ 130-fold compared to NHERF1/2 PDZ domains. PGD97 is capable of stabilizing F508del-CFTR at the cell membrane and improving CFTR function required for proper fluid homeostasis in tne lung. PGD97 can be used for the research of cystic fibrosis .
    PGD97
  • HY-151286
    Antitumor agent-73

    		STAT Cancer
    Antitumor agent-73 is a Diosgenin (HY-N0177) derivative, which inhibits STAT3 signaling and activates Pdia3/ERp57 exogenously. Antitumor agent-73 shows potent anti-tumor activity against various cancer cell lines, 7.9-341.7-fold stronger than Diosgenin .
    Antitumor agent-73

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