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mutated

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107

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

    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.
    Mutated 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-100886
    BAY1082439

    		PI3K Apoptosis Cancer
    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-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-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 .
    Mutated 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 .
    Mutated EGFR-IN-3
  • HY-112477
    Chk2-IN-1

    		Checkpoint Kinase (Chk) Choline Kinase 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-168056
    KRAS ligand 5

    		Others Others
    KRAS ligand 5 is the target protein ligand for PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can specifically degrade KRAS mutated proteins .
    KRAS ligand 5
  • HY-123359
    RTC14

    		DNA/RNA Synthesis Dystrophin Others
    RTC14 is a read-through compound (RTC) that can induce ribosomes to bypass nonsense mutations in mRNA and allow the production of full-length functional proteins. RTC14 has the potential to be used in the research of various genetic disorders, such as nonsense mutations in the ataxia-telangiectasia mutated (ATM) gene and the dystrophin gene .
    RTC14
  • HY-149662
    TMDJ-035

    		Calcium Channel Cardiovascular Disease 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-162441
    pan-KRAS-IN-8

    		Ras Cancer
    pan-KRAS-IN-8 (Compound 38) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.07 and 0.18 nM, respectively .
    pan-KRAS-IN-8
  • HY-162440
    pan-KRAS-IN-7

    		Ras Cancer
    pan-KRAS-IN-7 (Compound 25) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.35 and 0.51 nM, respectively .
    pan-KRAS-IN-7
  • HY-162442
    pan-KRAS-IN-9

    		Ras Cancer
    pan-KRAS-IN-9 (Compound 52) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.24 and 0.30 nM, respectively .
    pan-KRAS-IN-9
  • HY-162443
    pan-KRAS-IN-10

    		Ras Cancer
    pan-KRAS-IN-10 (Compound 58) is an inhibitor for in human tumor mutated genes KRAS, which inhibits proliferation of KRAS mutated cells AsPC-1 (G12D mutant) and SW480 (G12V mutant) with IC50 of 0.7 and 0.24 nM, respectively .
    pan-KRAS-IN-10
  • HY-162386
    UM4118

    		Cuproptosis Cancer
    UM4118 is a copper ionophore that can initiate a mitochondrial-based noncanonical form of cell death known as cuproptosis. UM4118 exhibits high sensitivity in SF3B1-mutated and adverse risk acute myeloid leukemia (AML), and can be used for AML research .
    UM4118
  • HY-10638
    AP23464

    		c-Kit Apoptosis Cancer
    AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells .
    AP23464
  • HY-164462
    BHA536

    		PKC NF-κB Apoptosis Cancer
    BHA536 is an orally active selective inhibitor for PKCα/β and NF-kB signaling pathway. BHA536 inhibits the proliferation of CD79-mutated ABC DLBCL cell, arrests cell cycle at G1 phase, and induces apoptosis in TMD8 cell. BHA536 exhibits antitumor efficacy in mice .
    BHA536
  • 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
    5+ Cited Publications

    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-149508
    Nrf2-IN-3

    		Keap1-Nrf2 Reactive Oxygen Species (ROS) Cancer
    Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
    Nrf2-IN-3
  • 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-19323A
    (S)-Ceralasertib
    2 Publications Verification

    (S)-AZD6738

    		 ATM/ATR Cancer
    (S)-Ceralasertib ((S)-AZD6738) is the S-enantiomer of Ceralasertib (HY-19323). (S)-Ceralasertib is the inhibitor for ataxia telangiectasia mutated and rad3 related (ATR) .
    (S)-Ceralasertib
  • 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-14687
    (rac)-Talazoparib

    (rac)-BMN-673; (rac)-LT-673

    		 PARP Cancer
    (rac)-Talazoparib ((rac)-BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac)-Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac)-Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac)-Talazoparib exhibits antitumor efficacy in mouse models .
    (rac)-Talazoparib
  • 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 Dystrophin 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-104067
    Naphthol AS-MX phosphate

    NASTRp

    		 Epigenetic Reader Domain Cancer
    Naphthol AS-MX phosphate (NASTRp) is a small molecule inhibitor of the CREB (cyclic adenosine phosphate reaction element binding protein)-CBP (CREB binding protein) transcription factor complex. Naphthol AS-MX phosphate shows antitumor activity against lung cancer cells, inhibiting tumor cell proliferation (IC50=3.701 μmol/L), colony formation, and anchored independent growth in soft AGAR. Naphthol AS-MX phosphate can be used in the study of KRAS mutated lung cancer, especially for KRAS mutated lung cancer with poor chemotherapy resistance and prognosis .
    Naphthol AS-MX phosphate
  • HY-164466
    CAD204520

    		Calcium Channel Notch Cancer
    CAD204520, a SERCA inhibitor (IC50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL) .
    CAD204520
  • 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-161235
    BTX-7312

    		SOS1 Molecular Glues Ras Cancer
    BTX-7312 is a cereblon-based SOS1 bifunctional degrader and a molecular glue. BTX-7312 reduces downstream signaling markers pERK and pS6 and shows antiproliferative activity in various KRAS-mutated cells .
    BTX-7312
  • HY-159607
    PRT3789

    		PROTACs Epigenetic Reader Domain Cancer
    PRT3789 is a SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 shows synergistic anti-proliferation effects with Adagrasib (HY-130149) in cancer cells. PRT3789 inhibits SMARCA4-mutated lung cancer proliferation. PRT3789 inhibits tumor growth in SMARCA4-deleted NSCLC models. Pink: SMARCA4 ligand (HY-44824) ; Blue: VHL ligand (HY-159465) ; Black: linker; VHL ligand+linker (HY-172738) .
    PRT3789
  • HY-177081
    Envometinib

    		MEK Cancer
    Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma .
    Envometinib
  • HY-19897
    4SC-203

    		FLT3 VEGFR Cancer
    4SC-203 is a potent multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively FLT3/STK1, FLT3 mutated forms, and VEGFRs .
    4SC-203
  • 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-132593A
    Rovanersen sodium

    WVE-120101 sodium

    		 Huntingtin Neurological Disease
    Rovanersen sodium 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 sodium can be used for huntington’s disease research .
    Rovanersen sodium
  • 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-164923
    SPA107

    Hemiasterlin methyl ester

    		 Microtubule/Tubulin Cancer
    SPA107 (Hemiasterlin methyl ester) is a Hemiasterlin (HY-117371) analog. SPA107 inhibits the polymerization of tubulin, exhibits antimitotic activity (IC50 of 0.5 nM) and cytotoxicity in p53 mutated MCF-7 cell with IC50 of 0.5 nM .
    SPA107
  • HY-150617A
    (Rac)-Lartesertib

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

    		 ATM/ATR STING PD-1/PD-L1 Cardiovascular Disease Inflammation/Immunology Cancer
    (Rac)-Lartesertib ((Rac)-M4076) is an isoform of Lartesertib (HY-150617). Lartesertib (M4076) is an inhibitor of the serine/threonine protein kinase ATM with high potency. Lartesertib can inhibit the growth of multiple hematopoietic cell lines. Additionally, when combined with the ATR inhibitor Tuvusertib (HY-111451), Lartesertib can promote the death of tumor cells, activate the immune signaling pathway, and exhibit anti-tumor activity .
    (Rac)-Lartesertib
  • 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-N0735
    Phellodendrine chloride
    1 Publications Verification

    		 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-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-168860
    Antituberculosis agent-13

    		Bacterial Infection Cancer
    Antituberculosis agent-13 (Compound 11) inhibits Mycobacterium tuberculosis, that inhibits Mtb wildtype and mutated strains with IC50 of 4-62.5 nM. Antituberculosis agent-13 exhibits anti-leukemia activity that inhibits MOLM-13 with IC50 of 3.8 μM .
    Antituberculosis agent-13
  • HY-123891
    NS-062

    		EGFR Cancer
    NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC50 of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .
    NS-062
  • 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 stimulates the IP-accumulation and calcium mobilization in CHO cells .
    AC-42
  • 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

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