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Results for "

mutated

" in MedChemExpress (MCE) Product Catalog:

66

Inhibitors & Agonists

2

Screening Libraries

5

Peptides

3

Inhibitory Antibodies

2

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3

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1

Antibodies

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-78869
    Mutated EGFR-IN-1

    Osimertinib analog

    		 EGFR Cancer
    Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.
    <em>Mutated</em> EGFR-IN-1
  • HY-12029
    WZ8040

    		EGFR Cancer
    WZ8040 is an irreversible mutated EGFR T790M inhibitor and inhibits EGFR phosphorylation. WZ8040 displays 100-fold greater activity against the mutated EGFR than the normal .
    WZ8040
  • HY-128860
    Mutated EGFR-IN-2

    		EGFR Cancer
    Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=＜1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity .
    <em>Mutated</em> EGFR-IN-2
  • HY-130608
    Mutated EGFR-IN-3

    		EGFR Cancer
    Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively .
    <em>Mutated</em> EGFR-IN-3
  • HY-112477
    Chk2-IN-1

    		Checkpoint Kinase (Chk) Cancer
    Chk2-IN-1 (compound 1) is a potent and selective inhibitor of checkpoint kinase 2 (Chk2), with IC50s of 13.5 nM and 220.4 nM for Chk2 and Chk1, respectively. Chk2-IN-1 can elicit a strong ataxia telangiectasia mutated (ATM)-dependent Chk2-mediated radioprotection effect .
    Chk2-IN-1
  • HY-149480
    ERD-3111

    		PROTACs Estrogen Receptor/ERR Cancer
    ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
    ERD-3111
  • HY-134481
    FLT3-IN-10

    		FLT3 Cancer
    FLT3-IN-10 (compound 7c) is a potent inhibitor of FMS-like tyrosine kinase 3 (FLT3). FLT3-IN-10 has the potential for the research of FLT3-mutated acute myeloid leukemia (AML) .
    FLT3-IN-10
  • HY-149662
    TMDJ-035

    		Calcium Channel Inflammation/Immunology
    TMDJ-035 is a selective RyR2 inhibitor. TMDJ-035 suppresses abnormal Ca 2+ waves and transients in isolated cardiomyocytes from RyR2-mutated mice. TMDJ-035is a tool for studying the mechanism and dynamics of RyR2 channel gating .
    TMDJ-035
  • HY-136360
    MI-3454
    2 Publications Verification

    		 Epigenetic Reader Domain Cancer
    MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis .
    MI-3454
  • HY-112210
    Shield-1
    2 Publications Verification

    Shld1

    		 FKBP Others
    Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD) .
    Shield-1
  • HY-107720
    ARL 17477

    		NO Synthase Cancer
    ARL-17477 is a dual inhibitor of NOS1and the autophagy-lysosomal system with anticancer activity and can inhibit tumor growth in KRAS-mutated cancers .
    ARL 17477
  • HY-144214
    ATR-IN-10

    		ATM/ATR Cancer
    ATR-IN-10 is a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase with an IC50 value of 2.978 μM.
    ATR-IN-10
  • HY-157941
    ART0380

    		ATM/ATR Cancer
    ART0380 is a potent and selective ATR kinase inhibitor. ART0380 has selective antitumor activity that can be used for the research of Ataxia-Telangiectasia Mutated (ATM) aberrant cancers .
    ART0380
  • HY-141478
    Antitumor agent-28

    		ATM/ATR Cancer
    Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity .
    Antitumor agent-28
  • HY-147580
    BTK-IN-10

    		Btk Cancer
    BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111) .
    BTK-IN-10
  • HY-122631
    TG693

    		CDK Others
    TG693 is an orally active inhibitor of CLK1. TG693 regulates the mutated exon 31 of the dystrophin gene in vivo. TG693 is used in Duchenne muscular dystrophy (DMD) research .
    TG693
  • HY-149508
    Nrf2-IN-3

    		Keap1-Nrf2 Cancer
    Nrf2-IN-3 (Compound R16) is a Nrf2 inhibitor. Nrf2-IN-3 binds KEAP1 mutants (G333C mKEAP1) and repairs the disrupted KEAP1/NRF2 interactions. Nrf2-IN-3 sensitizes KEAP1-mutated cancer cells to Cisplatin (HY-17394) and Gefitinib (HY-50895) by repairing the mKEAP1/NRF2 complex .
    Nrf2-IN-3
  • HY-118806
    AC-42

    		mAChR Neurological Disease
    AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively .
    AC-42
  • HY-147582
    BTK-IN-12

    		Btk Cancer
    BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8) .
    BTK-IN-12
  • HY-161236
    KRAS ligand 4

    		Ras Cancer
    KRAS ligand 4 (Compound 2) is a bifunctional depressant based on SOS1. KRAS ligand 4 reduces the downstream signaling markers pERK and pS6 and shows anti-proliferative activity in multiple KRAS mutated cells .
    KRAS ligand 4
  • HY-19897
    4SC-203

    4SC-203 is a potent multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively FLT3/STK1, FLT3 mutated forms, and VEGFRs .
    4SC-203
  • HY-P99489
    Budigalimab

    ABBV 181; PR 1648817

    		 PD-1/PD-L1 Cancer
    Budigalimab (ABBV 181; PR 1648817) is a humanized IgG1 monoclonal antibody targeting programmed cell death 1 (PD-1) receptor. Budigalimab is Fc mutated thus to reduce Fc receptor interactions and limit effector function .
    Budigalimab
  • HY-P2096
    Hexapeptide-11

    		Reactive Oxygen Species ATM/ATR MDM-2/p53 Infection
    Hexapeptide-11 is a bioactive peptide with anti-aging effect. Hexapeptide-11 protects fibroblasts against oxidative stress-mediated premature cellular senescence by mediating a downregulation of cellular proteins, such as ataxia telangiectasia mutated (ATM) and p53 .
    Hexapeptide-11
  • HY-123307
    Quizalofop

    Xylafop

    		 Acetyl-CoA Carboxylase Others
    Quizalofop (Xylafop) is a herbicide that inhibits acetyl-CoA carboxylase (ACCase) to reduce the synthesis of fatty acids. Quizalofop can be used to screen EMS (HY-W015854) mutated microalgae for research on improving the performance of microalgae biofuel production .
    Quizalofop
  • HY-160765
    WNTinib

    APS-8-100-2

    		 Wnt Apoptosis Cancer
    WNTinib (APS-8-100-2) is a multi-kinase inhibitor that selectively antagonizes β-catenin (CTNNB1) mutated hepatocellular carcinoma (HCC). WNTinib downregulates oncogenicWntsignaling by inhibiting KIT/MAPK and downstream EZH2 activation .
    WNTinib
  • HY-N0735
    Phellodendrine chloride

    		Autophagy Cancer
    Phellodendrine chloride is a plant alkaloid found in Phellodendron amurense. Phellodendrine chloride suppresses the proliferation of KRAS mutated pancreatic cancer cells through inhibition of nutrients uptake via macropinocytosis . Phellodendrine chloride promotes autophagy by regulating the AMPK/mTOR pathway and reduce the intestinal damage of ulcerative colitis .
    Phellodendrine chloride
  • HY-132593
    Rovanersen

    WVE-120101

    		 Huntingtin Neurological Disease
    Rovanersen (WVE-120101) is an antisense oligonucleotide that specifically targets mutated mRNA copies of the huntington (HTT) gene without affecting healthy mRNA of HTT gene, thereby preventing the production of faulty Huntingtin protein. Rovanersen can be used for huntington’s disease research .
    Rovanersen
  • HY-150617
    Lartesertib

    M4076; ATM Inhibitor-5

    		 ATM/ATR Cancer
    Lartesertib (M4076) is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1) .
    Lartesertib
  • HY-150617A
    (Rac)-Lartesertib

    (Rac)-M4076; (Rac)-ATM Inhibitor-5

    		 ATM/ATR Cancer
    (Rac)-Lartesertib ((Rac)-M4076; (Rac)-ATM Inhibitor-5) is an isoform of Lartesertib (HY-150617), which is a potent inhibitor of serine/threonine protein kinase ATM (extracted from patent WO2022058351A1) .
    (Rac)-Lartesertib
  • HY-100886
    BAY1082439

    BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .
    BAY1082439
  • HY-P99728
    Melredableukin alfa

    RG7835; RO7049665

    		 Interleukin Related Inflammation/Immunology
    Melredableukin alfa (RO-7049665) is a fusion protein that consists of a human IgG1-κ fused to a mutated human interleukin 2 (IL2 mutein) via a peptide linker. Melredableukin alfa can be used for the research of autoimmune hepatitis and ulcerative colitis .
    Melredableukin alfa
  • HY-131864
    SJF-1528

    		EGFR PROTACs Cancer
    SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 also degrades HER2 .
    SJF-1528
  • HY-145566
    Envonalkib

    TQ-B3139; CT-71

    		 Anaplastic lymphoma kinase (ALK) Cancer
    Envonalkib is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib can be used for the research of non-small cell lung cancer .
    Envonalkib
  • HY-145566A
    Envonalkib citrate

    TQ-B3139 citrate; CT-71 citrate

    		 Anaplastic lymphoma kinase (ALK) Cancer
    Envonalkib citrate is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib citrate can be used for the research of non-small cell lung cancer .
    Envonalkib citrate
  • HY-125835
    CP-10
    1 Publications Verification

    		 PROTACs CDK Cancer
    CP-10 is a PROTAC connected by ligands for Cereblon and CDK, with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6 .
    CP-10
  • HY-157887
    ADT-007

    		Ras Cancer
    ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes .
    ADT-007
  • HY-156135
    NSC194598

    		RET Others
    NSC194598 is a p53 DNA-binding inhibitor with IC50 value of 180 nM and 2-40 μM for in vitro and in vivo, respectively. NSC194598 interferes with transcriptional activation of mutated RET gene in human medullary thyroid carcinoma TT cells. NSC194598 can be used for acute toxicity to normal tissues by radiation and chemotherapy research .
    NSC194598
  • HY-149291
    A011

    		ATM/ATR Apoptosis Cancer
    A011 is a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor with an IC50 value of 1.0 nM. A011 induces Apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11 (HY-16562). A011 combines with CPT-11 shows antitumor activity .
    A011
  • HY-103713
    Seclidemstat
    4 Publications Verification

    SP-2577

    		 Histone Demethylase Cancer
    Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma .
    Seclidemstat
  • HY-118341
    Clitocine

    		Apoptosis Bcl-2 Family Cancer
    Clitocine, an adenosine nucleoside analog isolated from mushroom, is a potent and efficacious readthrough agent. Clitocine acts as a suppressor of nonsense mutations and can induce the production of p53 protein in cells harboring p53 nonsense-mutated alleles. Clitocine can induce apoptosis in multidrug-resistant human cancer cells by targeting Mcl-1. Anticancer activity .
    Clitocine
  • HY-163417
    HER2-IN-15

    		EGFR Cancer
    HER2-IN-15 (Compound 1) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-15 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
    HER2-IN-15
  • HY-163418
    HER2-IN-17

    		EGFR Cancer
    HER2-IN-17 (Compound 2) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-17 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
    HER2-IN-17
  • HY-163420
    HER2-IN-16

    		EGFR Cancer
    HER2-IN-16 (Compound 14) is an inhibitor for HER2, which inhibits the Her YVMA exon 20 insertion mutation (HER2 YVMA) with an IC50 <200 nM. HER2-IN-16 inhibits proliferation of HER2 YVMA mutated BaF3 cells with an IC50 <200 nM and amliorates non-small-cell lung cancer (NSCLC) .
    HER2-IN-16
  • HY-145312
    ATR-IN-4

    		ATM/ATR Cancer
    ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. ATR-IN-4 inhibits growth of human prostate cancer cells DU145 and human lung cancer cells NCI-H460 with IC50s of 130.9 nM and 41 .33 nM, respectively. (Patent CN112142744A, compound 13) .
    ATR-IN-4
  • HY-114358
    Tamnorzatinib

    ONO-7475

    		 TAM Receptor Trk Receptor Cancer
    Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
    Tamnorzatinib
  • HY-123319A
    Antofloxacin

    		Bacterial Antibiotic Infection
    Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
    Antofloxacin
  • HY-123319
    Antofloxacin hydrochloride

    		Bacterial Antibiotic Infection
    Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
    Antofloxacin hydrochloride
  • HY-103713A
    Seclidemstat mesylate
    4 Publications Verification

    SP-2577 mesylate

    		 Histone Demethylase Cancer
    Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma .
    Seclidemstat mesylate
  • HY-P10058
    cpm-1285m

    		Biochemical Assay Reagents Cancer
    cpm-1285m is a cell-permeable mutated peptide analogue of cpm-1285 (Bcl-2 inhibitory peptide). cpm-1285m contains a single substitution of alanine for Leu-151, and exhibits a decrease in Bcl-2 binding affinity with a reduction in IC50 of ∼15-fold. cpm-1285m can be used as a control of cpm-1285 .
    cpm-1285m
  • HY-158008
    (R)-G12Di-7

    		Ras Cancer
    (R)-G12Di-7 is a covalent ligand for KRAS-G12D, which selectively labels K-Ras-G12D·GDP and K-Ras-G12D·GppNHp. (R)-G12Di-7 exhibits inhibitory activity against G12D mutated cancer cells .
    (R)-G12Di-7

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