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mutants

" in MedChemExpress (MCE) Product Catalog:

1282

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2

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13

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18

Biochemical Assay Reagents

39

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2

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10

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46

Natural
Products

1

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37

Isotope-Labeled Compounds

26

Click Chemistry

8

Oligonucleotides

2

GMP Molecules

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-134813
    MRTX1133
    Maximum Cited Publications
    46 Publications Verification

    		 Ras Cancer
    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 .
    MRTX1133
  • HY-153724
    BI-2865
    10+ Cited Publications

    		 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-14588
    Lopinavir
    15+ Cited Publications

    ABT-378

    		 HIV HIV Protease SARS-CoV Infection Neurological Disease Cancer
    Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
    Lopinavir
  • HY-114226
    Olutasidenib
    3 Publications Verification

    FT-2102

    		 Isocitrate Dehydrogenase (IDH) Inflammation/Immunology Cancer
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
    Olutasidenib
  • HY-165559
    Trpvicin

    		TRP Channel Inflammation/Immunology
    Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC50s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology .
    Trpvicin
  • HY-136789
    Tuxobertinib
    1 Publications Verification

    BDTX-189

    		 EGFR Cancer
    Tuxobertinib (BDTX-189) is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. Tuxobertinib shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity .
    Tuxobertinib
  • HY-141640
    MS154

    		PROTACs EGFR Cancer
    MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)) .
    MS154
  • HY-123636
    UPCDC-30245

    		p97 Cancer
    UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM . UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A . UPCDC-30245 can be used in the research of cancer .
    UPCDC-30245
  • HY-129545
    DS-1001b
    2 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity .
    DS-1001b
  • HY-145594
    Safusidenib
    2 Publications Verification

    AB-291; DS-1001

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma . Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively .
    Safusidenib
  • HY-19706
    ARS-853
    5 Publications Verification

    		 Ras Apoptosis Cancer
    ARS-853 is a cell-active, selective, covalent KRAS G12C inhibitor with an IC50 of 2.5 μM. ARS-853 inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation .
    ARS-853
  • HY-16271
    Kevetrin hydrochloride
    4 Publications Verification

    4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride

    		 MDM-2/p53 Apoptosis Cancer
    Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
    Kevetrin hydrochloride
  • HY-128888
    (R,R)-GSK321

    		Isocitrate Dehydrogenase (IDH) Cancer
    (R,R)-GSK321 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. (R,R)-GSK321 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity .
    (R,R)-GSK321
  • HY-115282A
    JNJ-63576253
    1 Publications Verification

    TRC-253

    		 Androgen Receptor Cancer
    JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
    JNJ-63576253
  • HY-111836
    NRX-252114

    		Molecular Glues β-catenin Cancer
    NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation .
    NRX-252114
  • HY-122862
    RAS inhibitor Abd-7
    3 Publications Verification

    		 Ras Cancer
    RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
    RAS inhibitor Abd-7
  • HY-E70884
    Endoglycosidase S2 (D184M mutant)

    EndoS2 D184M

    		 Glycosidase Others
    Endoglycosidase S2 (D184M mutant) (EndoS2 D184M) is a mutant endoglycosidase. Endoglycosidase S2 (D184M mutant) promotes the transfer of glyco-oxazoline donors with defined glycoforms to the Fc region of IgG antibodies .
    Endoglycosidase S2 (D184M mutant)
  • HY-145759
    Mutant p53 modulator-1
    1 Publications Verification

    		 MDM-2/p53 Cancer
    Mutant p53 modulator-1 is a mutant p53 modulator. Mutant p53 modulator-1 reduces the progression of cancers that contain a p53 mutation (extracted from patent WO2021231474A1, compound 231B) .
    Mutant p53 modulator-1
  • HY-108636
    RETRA

    		MDM-2/p53 Cancer
    RETRA is a mutant p53-dependent activator of p73 that suppresses mutant p53-bearing cancer cells. RETRA increases the expression level of p73, and a release of p73 from the blocking complex with mutant p53, which produces tumor-suppressor effects .
    RETRA
  • HY-159493
    BI2536-PEG2-Halo

    		Polo-like Kinase (PLK) Cancer
    BI2536-PEG2-Halo is a bifunctional molecule containing a ligand for Halo tag and a Polo-like kinase 1 (PLK1) inhibitor BI-2536 (HY-50698). BI2536-PEG2-Halo inhibits the proliferation of 293T cells with Halo-p53R273H(FL)-mCherry tag (IC50=23 nM), exhibits selective toxicity against p53 mutant cancer cells .
    BI2536-PEG2-Halo
  • HY-171499
    Cenersen

    EL625

    		 MDM-2/p53 Cancer
    Cenersen (EL625) is an oligonucleotide targeting TP53. Cenersen can eliminate the activity of TP53 gain-of-function mutants and increase the sensitivity of lymphoma cells to cytotoxic chemotherapy in vitro. Cenersen can be used for the study of chronic lymphocytic leukemia (CLL) .
    Cenersen
  • HY-148070
    FLT3-IN-17

    		FLT3 FAK Cytochrome P450 Cancer
    FLT3-IN-17 inhibits CYPs and FLT3 mutants activity (IC50s: <0.5 nM for D835Y). FLT3-IN-17 is also a FAK inhibitor, with an IC50 value of 12 nM. FLT3 ligand-2 can be used in the research of cancers .
    FLT3-IN-17
  • 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-131312
    Crelosidenib

    LY3410738; Mutant IDH1-IN-6

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
    Crelosidenib
  • HY-153974
    BBT-176

    		EGFR Cancer
    BBT-176 is an orally effective EGFR inhibitor. BBT-176 has inhibitory activity against multiple EGFR C797S mutant cell lines. BBT-176 is commonly used in cancer research .
    BBT-176
  • 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-77113
    B-Raf IN 11

    		Raf Cancer
    B-Raf IN 11 is a B-Raf V600E mutant kinase inhibitor with an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. B-Raf IN 11 inhibits the kinase activities of B-Raf V600E mutant and wild-type B-Raf kinase. B-Raf IN 11 is applicable to relevant research on colorectal cancer .
    B-Raf IN 11
  • HY-143319
    SPH5030

    		EGFR Cancer
    SPH5030 is a selective and irreversible HER2 inhibitor. SPH5030 inhibits HER2 WT and EGFR WT with IC50s of 3.51 and 8.13 nM, respectively. SPH5030 shows excellent activities against HER2 mutants. SPH5030 can be used for the research of cancer .
    SPH5030
  • HY-142160
    GNE-9815

    		Raf Cancer
    GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
    GNE-9815
  • HY-P5082
    α-Synuclein 4554W

    		α-synuclein Neurological Disease
    α-Synuclein 4554W is an inhibitor of α-Synuclein (aSyn) aggregation with associated toxicity. α-Synuclein 4554W consists of GIVNGVKA sequences, previously identified through intracellular library screening. α-Synuclein 4554W reduces fibril formation of aSyn mutants assocaited with Parkinson’s disease .
    α-Synuclein 4554W
  • HY-177511
    KRAS G12D-IN-30

    		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-101489A
    GZD856 formic

    		PDGFR Bcr-Abl Apoptosis Cancer
    GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity . GZD856 (formic) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GZD856 formic
  • HY-W004705
    (2-Aminophenyl)methanol

    2-Hydroxymethylaniline

    		 Chloride Channel Neurological Disease
    (2-Aminophenyl)methanol (2-Hydroxymethylaniline) is a molecular chaperone to rescue P123S mutant pendrin. (2-Aminophenyl)methanol has the advantages of low dose, long-term effect and low toxicity. (2-Aminophenyl)methanol can be used for the study of Pendred syndrome (a syndromic deafness) .
    (2-Aminophenyl)methanol
  • HY-153767
    PK095

    		MDM-2/p53 Cancer
    PK095 is a p53 mutant stabilizer. PK095 can be used for research of cancer .
    PK095
  • HY-149464
    ARN22089

    		Ras Cancer
    ARN22089 is a oral active novel class of trisubstituted pyrimidine, blocks the interaction of CDC42 GTPases with specific downstream effectors. ARN22089 blocks tumor growth in BRAF mutant mouse melanoma model .
    ARN22089
  • HY-19634
    YK-3-237
    1 Publications Verification

    		 Sirtuin Cancer
    YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells .
    YK-3-237
  • HY-126905
    ZMC3

    NSC328784

    		 Reactive Oxygen Species (ROS) Cancer
    ZMC3 (NSC328784) is a zinc chelator. ZMC3 shows Zinc metallochaperone properties. ZMC3 shows enhanced sensitivity in p53-R175H mutant cells. ZMC3 increases the cell ROS level .
    ZMC3
  • 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-15519
    LBW242

    		IAP FLT3 Cancer
    LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells .
    LBW242
  • HY-131067
    EMI56

    		EGFR Cancer
    EMI56, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI56 inhibits EGFR triple mutants .
    EMI56
  • HY-141566
    EZH2-IN-5

    		Histone Methyltransferase Cancer
    EZH2-IN-5 is a potent EZH2 inhibitor with IC50 values of 1.52 nM and 4.07 nM for wild-type and mutant Tyr641 EZH2, respectively .
    EZH2-IN-5
  • HY-110144
    TC-E 5008

    		Isocitrate Dehydrogenase (IDH) Cancer
    TC-E 5008 is a potent mutant IDH1 inhibitor with Ki values of 190 nM and 120 nM for R132H and R132C IDH1 mutants, respectively. TC-E 5008 exhibits very weak activity against WT-IDH1 with a Ki value of 12.3 μM. TC-E 5008 has anti-proliferative activity on multiple ER positive breast cancer cell lines .
    TC-E 5008
  • HY-138072
    EMI1

    		EGFR Cancer
    EMI1 is an EGFR ex19del/T790M/C797S and EGFR L858R/T790M/C797S inhibitor. EMI1 can be used for the research of mutant EGFR-associated, drug-resistant non-small-cell lung cancer (NSCLC) .
    EMI1
  • HY-P2360
    G12

    Ras 5-17

    		 Ras Others
    G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
    G12
  • HY-160449
    p53 Activator 10

    		MDM-2/p53 Cancer
    p53 Activator 10 (Example C-2) is a compound that targets the y220c mutant of p53. p53 Activator 10 activation is involved in the downstream effects of tumor suppression .
    p53 Activator 10
  • HY-15352
    BMS 561390

    DPC 083

    		 Reverse Transcriptase HIV Infection
    BMS 561390 (DPC 083) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains .
    BMS 561390
  • 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-118169
    A-Factor

    		Bacterial Infection
    A-Factor is an inducer of streptomycin biosynthesis in an inactive mutant of Streptomyces griseus. In addition, A-Factor can also induce spore formation during conidial development of Magnaporthe oryzae .
    A-Factor
  • HY-106918
    Tivirapine

    R86183; TIBO R 86183

    		 Reverse Transcriptase HIV Infection
    Tivirapine (R86183) is a nonnucleoside HIV-1 RT inhibitor against HIV-1-induced cytopathic effects with an EC50 value of 4 nM. Tivirapine inhibits the Yl8lC mutant of HIV-1 RT .
    Tivirapine

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