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mutant

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1278

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18

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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-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-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-12475
    Mutant IDH1-IN-1
    2 Publications Verification

    Agios 135

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
    Mutant IDH1-IN-1
  • 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-13984
    NT-1
    1 Publications Verification

    EGFR mutant-IN-3

    		 EGFR ERK Apoptosis Drug Derivative Cancer
    NT-1 (EGFR mutant-IN-3) is a potent mutant EGFR inhibitor and an analog of Osimertinib (HY-15772). This mutant EGFR inhibitor suppresses FGFR WT with an IC50 of 0.4 nM. NT-1 also inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M. NT-1 exerts deeper inhibition on p-EGFR and p-ERK, and induces tumor cell apoptosis. NT-1 can be used in colorectal cancer research .
    NT-1
  • HY-D1056C5
    Lipopolysaccharides, from S. enterica serotype minnesota Re 595 (Re mutant)

    LPS, from Salmonella enterica (Serotype minnesota Re 595 (Re mutant))

    		 Toll-like Receptor (TLR) Bacterial Inflammation/Immunology
    Lipopolysaccharides (LPS), from S. enterica (Salmonella enterica) serotype minnesota Re 595 (Re mutant) is prepared from Salmonella enterica strain Re 595 (Re mutant). The structure in the LPS of strain Re 595 was shown to induce secretion and aggregation in human platelets .
    It is recommended to prepare a solution with concentration ≥2 mg/mL. Vortex thoroughly for more than 10 minutes. Due to the adsorption characteristics of LPS, silanized container or low adsorption centrifuge tubes should be used for aliquoting and storage, and mix thoroughly before use.
    Lipopolysaccharides, from S. enterica serotype minnesota Re 595 (Re mutant)
  • 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-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-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-13972
    Mutant IDH1 inhibitor
    2 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1 inhibitor is a potent mutant IDH1 R132H inhibitor with IC50 of < 72 nM.
    Mutant IDH1 inhibitor
  • 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-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-18717
    Mutant IDH1-IN-2
    2 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-2 is a inhibitor of mutant Isocitrate dehydrogenase (IDH) proteins, with IC50 of in LS-MS biochemical assay, IC50 of 16.6 nM in Fluorescence biochemical assay.
    Mutant IDH1-IN-2
  • HY-E70883
    Endoglycosidase S (D233Q mutant)

    EndoS D233Q

    		 Glycosidase Others
    Endoglycosidase S (D233Q mutant) (EndoS D233Q) is a mutant endoglycosidase, which catalyzes the glycosylation of Trastuzumab (HY-P9907)-GlcNAc with the functionalized, non-natural glycans to give glycosylated monoclonal Abs (mAbs) carrying two glycans each functionalized with two reaction handles .
    Endoglycosidase S (D233Q mutant)
  • HY-E70879
    Endoglycosidase M (N175Q mutant)

    EndoM N175Q

    		 Glycosidase Others
    Endoglycosidase M (N175Q mutant) (EndoM N175Q) can transfer natural N-glycans or oxazoline N-glycans to any peptide or protein with a GlcNAc residue to form a β1-4-glycosidic linkage. Endoglycosidase M (N175Q mutant) is a useful tool in the synthesis of homogeneous glycopeptides and glycoproteins .
    Endoglycosidase M (N175Q mutant)
  • 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-126298
    RAF mutant-IN-1

    		Raf Cancer
    RAF mutant-IN-1 is a RAF kinase inhibitor, extracted from patent WO2019107987A1, with IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAF V600E and B-RAF WT, respectively .
    RAF mutant-IN-1
  • 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-114459
    Mutant IDH1-IN-4

    		Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-4 (compound 434) is an inhibitor of mutant Isocitrate dehydrogenase 1 (IDH 1), with IC50 values of ≤ 0.5 μM for mutant IDH1 in R132H, HT1080 and U87R132H cells .
    Mutant IDH1-IN-4
  • HY-132920
    KRAS mutant protein inhibitor 1

    		Ras Cancer
    KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential research in cancer.
    KRAS mutant protein inhibitor 1
  • HY-175213
    Mutant IDH1-IN-7

    		Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
    Mutant IDH1-IN-7
  • HY-E70880
    Endoglycosidase CC (N180H mutant)

    EndoCC N180H

    		 Glycosidase Others
    Endoglycosidase CC (N180H mutant) (EndoCC N180H) is a mutant endoglycosidase, which efficiently and specifically recognizes core fucose and O-GlcNAc .
    Endoglycosidase CC (N180H mutant)
  • HY-E70881
    Endoglycosidase F3 (D165A mutant)

    EndoF3 D165A

    		 Glycosidase Others
    Endoglycosidase F3 (D165A mutant) (EndoF3 D165A) is a mutant endoglycosidase, which efficiently and specifically recognizes core fucose and O-GlcNAc .
    Endoglycosidase F3 (D165A mutant)
  • HY-131312A
    Crelosidenib gentisate

    LY3410738 gentisate; mutant IDH1-IN-6 gentisate

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 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. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes .
    Crelosidenib gentisate
  • 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

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