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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10358
    MK-2206 dihydrochloride
    Maximum Cited Publications
    462 Publications Verification

    MK-2206 (2HCl)

    		 Bcl-2 Family Apoptosis mTOR Akt GSK-3 Cardiovascular Disease Inflammation/Immunology Cancer
    MK-2206 dihydrochloride (MK-2206 2HCl) is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia .
    MK-2206 dihydrochloride
  • HY-16985
    Darolutamide
    5+ Cited Publications

    ODM-201; BAY-1841788

    		 Androgen Receptor Cancer
    Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
    Darolutamide
  • HY-18690
    Enasidenib
    15+ Cited Publications

    AG-221

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively.
    Enasidenib
  • HY-100002
    ML162
    10+ Cited Publications

    		 Glutathione Peroxidase Ferroptosis Cancer
    ML162 is a covalent glutathione peroxidase 4 (GPX4) inhibitor. ML162 has a selective lethal effect on mutant RAS oncogene-expressing cell lines
    ML162
  • HY-13223
    Crenolanib
    15+ Cited Publications

    CP-868596

    		 FLT3 PDGFR Autophagy Cancer
    Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
    Crenolanib
  • HY-156681
    Tersolisib
    1 Publications Verification

    STX-478; STX-478-101; LY4064809

    		 PI3K Cancer
    STX-478 (compound 80) is an oral CNS-penetrant allosteric mutant-selective PI3Kα inhibitor. STX-478 shows robust and durable tumor regression and can be used in cancer research .
    Tersolisib
  • HY-10624
    THIQ
    1 Publications Verification

    		 Melanocortin Receptor Metabolic Disease
    THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
    THIQ
  • HY-153306
    Zovegalisib
    1 Publications Verification

    RLY-2608

    		 PI3K Cancer
    Zovegalisib (RLY-2608) is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. Zovegalisib inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
    Zovegalisib
  • HY-114778
    Fluzoparib
    4 Publications Verification

    SHR3162; Fuzuloparib

    		 PARP Cancer
    Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
    Fluzoparib
  • HY-15734
    AGI-6780
    5+ Cited Publications

    		 Isocitrate Dehydrogenase (IDH) Cancer
    AGI-6780 that potently and selectively inhibits the tumor-associated mutant IDH2 R140Q with IC50 of 23±1.7 nM. AGI-6780 is less potent against IDH2 WT with IC50 of 190±8.1 nM.
    AGI-6780
  • HY-129550
    BI-4020

    		EGFR Cancer
    BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
    BI-4020
  • HY-79077
    Osimertinib dimesylate
    180+ Cited Publications

    AZD-9291 dimesylate; Mereletinib dimesylate

    		 EGFR Cancer
    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFR L858R and EGFR L858R/T790M, respectively.
    Osimertinib dimesylate
  • HY-18690A
    Enasidenib mesylate
    15+ Cited Publications

    AG-221 mesylate

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
    Enasidenib mesylate
  • HY-104036
    IDH-305
    4 Publications Verification

    		 Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)) .
    IDH-305
  • HY-18082
    AGI-5198
    15+ Cited Publications

    IDH-C35

    		 Isocitrate Dehydrogenase (IDH) Cancer
    AGI-5198 (IDH-C35) is a potent and selective mutant IDH1 R132H inhibitor with an IC50 of 0.07 μM.
    AGI-5198
  • HY-13237
    GSK2578215A
    4 Publications Verification

    		 LRRK2 Autophagy Mitophagy Neurological Disease Cancer
    GSK2578215A is a potent and highly selective LRRK2 inhibitor, which exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.
    GSK2578215A
  • HY-19729
    Naquotinib
    5 Publications Verification

    ASP8273

    		 EGFR Cancer
    Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
    Naquotinib
  • HY-12872
    Nazartinib
    5+ Cited Publications

    EGF816

    		 EGFR Cancer
    Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
    Nazartinib
  • HY-112256
    ACP-105
    5+ Cited Publications

    		 Androgen Receptor Inflammation/Immunology
    ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
    ACP-105
  • 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-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-19985
    PF-06459988

    		EGFR Cancer
    PF-06459988 is an orally activity, irreversible and mutant-selective inhibitor of EGFR mutant forms. PF-06459988 demonstrates high potency and specificity to the T790M-containing double mutant EGFRs. PF-06459988 can be used for the research of cancer .
    PF-06459988
  • HY-12475
    Mutant IDH1-IN-1
    2 Publications Verification

    Agios 135

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1 R132H and IDH1 R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research .
    Mutant IDH1-IN-1
  • HY-18997
    PLX7904
    3 Publications Verification

    PB04

    		 Raf Cancer
    PLX7904 is a potent and selective BRAF inhibitor, with IC50 of appr 5 nM against BRAF V600E in mutant RAS expressing cells.
    PLX7904
  • HY-154959
    AZD4747

    		Ras Cancer
    AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
    AZD4747
  • HY-136379
    CID44216842
    2 Publications Verification

    Cdc42-IN-1

    		 Ras Cancer
    CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe .
    CID44216842
  • HY-153361
    YD23

    		PROTACs Epigenetic Reader Domain Inflammation/Immunology Cancer
    YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 cells and H1975 cells. YD23 induces degradation of SMARCA2, which is synthetic lethal to SMARCA4. YD23 reduces chromatin accessibility only in SMARCA4 deficient cells, including cell cycle and cell growth regulatory genes. YD23 selectively inhibits growth of SMARCA4 mutant lung cancer cells. YD23 has potent tumor growth inhibitory activity in SMARCA4-mutant xenografts. YD23 can be used for the study of non-small cell lung cancer (NSCLC) .
    YD23
  • 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-142161
    ABD957
    3 Publications Verification

    		 MAGL Cancer
    ABD957 is a potent and selective covalent inhibitor of the ABHD17 family of depalmitoylases, with an IC50 of 0.21 μM for ABHD17B. ABD957 can block N-Ras signaling and the growth of NRAS-mutant AML cells .
    ABD957
  • HY-19803
    Naquotinib mesylate
    5 Publications Verification

    ASP8273 mesylate

    		 EGFR Cancer
    Naquotinib mesylate (ASP8273 mesylate) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.
    Naquotinib mesylate
  • HY-13897
    CNX-2006

    		EGFR Cancer
    CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFR T790M.
    CNX-2006
  • HY-146243
    TH-Z835

    		Ras Apoptosis Cancer
    TH-Z835 is a mutant selective KRAS (G12D) inhibitor with an IC50 of 1.6 μM. TH-Z835 inhibits both mantGMPPNP/GPPNP exchange and GPPNP/mantGMPPNP exchange .
    TH-Z835
  • HY-176792
    ACBI-4

    		PROTACs Ras Cancer
    ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRAS G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .
    ACBI-4
  • HY-134877
    BAY 2476568

    		EGFR ERK Akt Cancer
    BAY 2476568 is a potent and mutant-selective inhibitor targeting EGFR exon20 insertion variants. BAY 2476568 potently inhibits the kinase activity of EGFR exon20 insertion mutants (insASV, insSVD, insNPG) with IC50 values of 0.09 nM, 0.21 nM, and 0.11 nM, respectively. BAY 2476568 inhibits EGFR (Y1068) phosphorylation and reduces the phosphorylation of ERK1/2 and Akt (S473) in Ba/F3 cells expressing EGFR exon20 insertion mutants (insASV, insSVD). BAY 2476568 can be used for the study of non-small cell lung cancer (NSCLC) driven by EGFR exon20 insertion mutations .
    BAY 2476568
  • HY-15003
    ATH686

    		FLT3 Apoptosis Cancer
    ATH686 is a potent, selective and ATP-competitive FLT3 inhibitor. ATH686 target mutant FLT3 protein kinase activity and inhibit the proliferation of cells harboring FLT3 mutants via induction of apoptosis and cell cycle inhibition. ATH686 has antileukemic effects .
    ATH686
  • HY-151523
    KRas G12R inhibitor 1

    		Ras Cancer
    KRas G12R inhibitor 1 is a covalent inhibitor targeting the common oncogenic mutant KRas G12R with selectivity for the mutant arginine. KRas G12R inhibitor 1 possesses an α,β-diketoamide and exploits strong nucleophilicity of the mutant cysteine and irreversibly binds in the Switch II region of KRas. KRas G12R inhibitor 1 can be researched for K-Ras (G12R)-driven cancer such as pancreatic ductal adenocarcinoma (PDAC) .
    KRas G12R inhibitor 1
  • 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-160287
    NVS MLLT-1

    		Epigenetic Reader Domain Cancer
    NVS MLLT-1 (compound 3), a chemical probe, is a potent and selective MLLT1 inhibitor with Kd values of 0.18 μM, 0.24 μM, and 0.22 μM for wild-type, T1 mutants, and T3 mutants, respectively .
    NVS MLLT-1
  • HY-156681A
    (S)-Tersolisib

    (S)-STX-478; (S)-STX-478-101; (S)-LY4064809

    		 PI3K Cancer
    (S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
    (S)-Tersolisib
  • 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-13223A
    Crenolanib benzenesulfonate
    15+ Cited Publications

    CP 868596-26

    		 Autophagy PDGFR FLT3 Cancer
    Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
    Crenolanib benzenesulfonate
  • HY-173155
    AKT1-IN-9

    		Akt Cancer
    AKT1-IN-9 (4) is a selective mutant AKT1(E17K) inhibitor, with EC50 values of 9 nM and 995 nM in LAPC4-CR and SkBr3 cells, respectively .
    AKT1-IN-9
  • HY-100214
    EAI001

    		EGFR Cancer
    EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFR L858R/T790M. EAI001 can be used for research of cancer .
    EAI001
  • HY-175025
    CH091138

    		PROTACs Ras Apoptosis Cancer
    CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .
    CH091138
  • HY-P3277
    KRpep-2d

    		Ras Cancer
    KRpep-2d is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
    KRpep-2d
  • HY-W423595
    BEBT-109

    		EGFR Cancer
    BEBT-109 is a potent pan-mutant-selective EGFR inhibitor. BEBT-109 has improved pharmacokinetic properties. BEBT-109 can be used for multiple mutant-EGFR-driven non-small cell lung cancer (NSCLC) research .
    BEBT-109
  • HY-135805A
    (Rac)-JBJ-04-125-02

    		EGFR Cancer
    (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor .
    (Rac)-JBJ-04-125-02
  • HY-130253
    IRAK4-IN-6

    		IRAK Cancer
    IRAK4-IN-6 is an orally efficacious and selective IRAK4 inhibitor with an IC50 of 4 nM, and targetes MyD88 L265P mutant diffuse large B cell lymphoma .
    IRAK4-IN-6
  • HY-135914
    JBJ-02-112-05

    		EGFR Cancer
    JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFR L858R/T790M .
    JBJ-02-112-05
  • HY-139047
    SW157765

    		GLUT Cancer
    SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs .
    SW157765

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