Search Result
Results for "
mutant
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
17
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-145759
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MDM-2/p53
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Cancer
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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) .
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- HY-13972
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- HY-13984
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EGFR
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Cancer
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Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
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- HY-114459
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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 .
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- HY-18717
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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.
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- HY-12475
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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.
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- HY-131312
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mutant IDH1-IN-6
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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 .
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- HY-158319
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Apoptosis
Isocitrate Dehydrogenase (IDH)
NAMPT
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Cancer
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Mutant IDH1/NAMPT-IN-1 (Compound 23h) is a dual inhibitor of mutant isocitrate dehydrogenase 1 (mutant IDH1) (IC50=14.93 nM) and nicotinamide phosphoribosyltransferase (NAMPT) (IC50=12.56 nM). Mutant IDH1/NAMPT-IN-1 can induce apoptosis. Mutant IDH1/NAMPT-IN-1 crosses the blood-brain barrier effectively .
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- HY-155005
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EGFR
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Cancer
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EGFR mutant-IN-2 (Compound D51) is an EGFR mutant inhibitor. EGFR mutant-IN-2 inhibits the EGFR L858R/T790M/C797S mutant with an IC50 value of 14 nM. EGFR mutant-IN-2 inhibits the EGFR del19/T790M/C797S mutant with an IC50 value of 62 nM. EGFR mutant-IN-2 has favorable PK parameters, safety properties, in vivo stability, and antitumor activity .
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- HY-132920
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Ras
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Cancer
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KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential research in cancer.
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- HY-125841
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EGFR
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Cancer
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EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFR L858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFR WT (IC50 >1.0 μM) .
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- HY-126298
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Raf
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Cancer
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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 .
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- HY-118731
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Reverse Transcriptase
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Infection
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TNK-6123 is a potent Emivirine (HY-15353) analogue with improved activity against drug-resistant HIV mutants. TNK-6123 improves activity against Lys103Asn mutant RT .
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- HY-123636
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p97
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Cancer
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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 .
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- HY-108636
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MDM-2/p53
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Cancer
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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 .
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- HY-141566
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Histone Methyltransferase
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Cancer
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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 .
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- HY-153767
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MDM-2/p53
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Cancer
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PK095 is a p53 mutant stabilizer. PK095 can be used for research of cancer .
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- HY-131067
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EGFR
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Cancer
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EMI56, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI56 inhibits EGFR triple mutants .
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- HY-150927
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Ras
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Cancer
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G12Si-2, an analog of G12Si-1 (HY-150926), is a negative control tool. G12Si-2 is not a covalent inhibitor of the G12S mutant of K-Ras .
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- HY-N10502
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MDM-2/p53
HSP
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Cancer
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Colletofragarone A2 can be be isolated from the fungus Colletotrichum sp. (13S020). Colletofragarone A2 inhibits mutant p53 and HSP90 with anti-cancer activity. Colletofragarone A2 promotes degradation and aggregation of mutant p53 and suppressing tumor growth in vivo .
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- HY-114226
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FT-2102
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Isocitrate Dehydrogenase (IDH)
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Inflammation/Immunology
Cancer
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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) .
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- HY-110144
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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 .
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- HY-160449
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MDM-2/p53
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Cancer
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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 .
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- HY-15352
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DPC 083
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Reverse Transcriptase
HIV
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Infection
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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 .
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- HY-18948
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GSK321
1 Publications Verification
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Isocitrate Dehydrogenase (IDH)
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Cancer
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GSK321 is a potent inhibitor of mutant isocitrate dehydrogenase 1 (IDH1) enzymes. GSK321 has high inhibitory and selectivity for mutant IDH1 enzymes. GSK321 can be used for the research of acute myeloid leukemia .
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- HY-149464
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Ras
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Cancer
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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 .
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- HY-164542
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Isocitrate Dehydrogenase (IDH)
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Cancer
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TQ05310 is an orally available inhibitor of IDH2 mutants, targeting both IDH2-R140Q (IC50=136.9 nM) and IDH2-R172K (IC50=37.9 nM) mutants. TQ05310 inhibits the production of 2-hydroxyglutarate (2-HG) and induces differentiation of cells expressing IDH2-R140Q and IDH2-R172K by inhibiting the enzymatic activity of mutant IDH2. TQ05310 can be used for the study of acute myeloid leukemia .
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- HY-118169
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Others
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Infection
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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 .
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- HY-153724
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BI-2865
1 Publications Verification
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Ras
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Cancer
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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) .
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- HY-126047
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Others
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Others
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(S)-(-)-Anatabine is a Ti plasmid mutant.
(S)-(-)-Anatabine has the activity of inducing tobacco blastoma to transform
into nicotinic alkaloids. (S)-(-)-Anatabine can be used in the study of
biotransformation of cotyl teratoma .
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- HY-145594
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AB-291; DS-1001
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Isocitrate Dehydrogenase (IDH)
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Cancer
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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 .
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- HY-129545
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Isocitrate Dehydrogenase (IDH)
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Cancer
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DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity .
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- HY-106918
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R86183; TIBO R 86183
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Reverse Transcriptase
HIV
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Infection
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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 .
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- HY-124761
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Polo-like Kinase (PLK)
Autophagy
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Cancer
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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 .
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- HY-19634
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Sirtuin
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Cancer
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YK-3-237, a SIRT1 activator, targets mutant p53. YK-3-237 inhibits the proliferation of triple-negative breast cancer cells .
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- HY-145022
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Ras
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Cancer
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KRAS G12C inhibitor 25 is a KRAS G12C inhibitor. KRAS G12C inhibitor 25 inhibits SOSl-assisted GDP/GTP exchanging activity of KRAS-G12C mutant (IC50=0.48 nM). From WO2021216770A1 compound 3 .
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- HY-150905
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EGFR
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Cancer
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EGFR ligand-2 (compound C4), a covalent EGFR ligand, is a EGFR mutant inhibitor with IC50s of 21 nM and 48 nM for EGFR L858R and EGFR L858R/T790M, respectively. EGFR ligand-2 can be used to synthesize PROTAC .
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- HY-131909
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Anaplastic lymphoma kinase (ALK)
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Cancer
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CJ-2360 is a potent and orally active ALK inhibitor with IC50s of 2.2, 4.0, 8.8, 6.3, and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M, and S1206Y ALK mutants, respectively. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated .
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- HY-108887
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Raf
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Cancer
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Anticancer agent 124 is an orally active, highly selective and potent pan RAF inhibitor. Anticancer agent 124 inhibits MAPK signalling in BRAF V600E, NRAS and KRAS mutant tumor cells .
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- HY-157458
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ATTECs
Phosphodiesterase (PDE)
Autophagy
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Cancer
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PDEδ autophagic degrader 1 (compound 12c) 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 .
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- HY-14588
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ABT-378
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HIV
HIV Protease
SARS-CoV
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Infection
Cancer
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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 .
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- HY-123390
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Bcr-Abl
Akt
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Cancer
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DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM .
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- HY-19617A
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EGFR
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Cancer
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EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
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- HY-19706
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ARS-853
4 Publications Verification
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Ras
Apoptosis
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Cancer
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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 .
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- HY-128888
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Isocitrate Dehydrogenase (IDH)
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Cancer
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(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 .
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- HY-164524
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Eukaryotic Initiation Factor (eIF)
Akt
NF-κB
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Cancer
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SBI-0640726 is an eIF4G1 inhibitor with antiproliferative activity in melanoma. SBI-0640726 disrupts the eIF4F translation initiation complex by inhibiting AKT and NF-kB signaling pathways. SBI-0640726 inhibits the growth of NRAS and BRAF mutant melanoma in vitro .
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- HY-159493
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Polo-like Kinase (PLK)
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Cancer
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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 .
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- HY-141640
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PROTACs
EGFR
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Cancer
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MS154 is a first-in-class E3 ligase cereblon-recruiting EGFR degrader with Kds of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutants. MS154 potently inhibits cell proliferation in lung cancer cells .
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- HY-19617
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EGFR
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Cancer
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EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
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- HY-19617B
-
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EGFR
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Cancer
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EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
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- HY-156712
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR .
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- HY-143319
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Others
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Cancer
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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 .
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- HY-161923
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EGFR
Apoptosis
Akt
ERK
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Cancer
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EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
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- HY-14588S2
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ABT-378-d7
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HIV
SARS-CoV
HIV Protease
Isotope-Labeled Compounds
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Infection
Cancer
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Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). 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 .
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- HY-142160
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Raf
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Cancer
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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 .
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- HY-155114
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HIV
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Infection
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HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1 inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC50: 0.094-12.0 μM) .
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- HY-101489
-
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PDGFR
Bcr-Abl
Apoptosis
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Cancer
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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 .
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- HY-138072
-
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EGFR
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Cancer
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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) .
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- HY-151287
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Ras
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Cancer
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KRAS inhibitor-20 is a small molecular inhibitor of KRas G12C, the oncogenic mutant. KRAS inhibitor-20 inhibits KRas G12C with the IC50 value <10 nM .
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- HY-136420
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PROTACs
Raf
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Cancer
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SJF-0628 (compound 512) is a PROTAC RAF degrader. SJF-0628 induces targeted degradation of BRAF mutants (DC50: 5.4 nM, 4.64 nM, 15.5 nM, 2.11 nM, 63.9 nM for BRAF V600E, V600K, G464V, G469A, K601E respectively). SJF-0628 has anti-tumor activity. SJF-0628 can be used for research of disorders that result from aggregation or accumulation of RAF, or the constitutive activation of RAF .
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- HY-143234
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Isocitrate Dehydrogenase (IDH)
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Cancer
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mIDH1-IN-1 (compound 43) is a potent and selective mIDH1 (mutant isocitrate dehydrogenases 1) inhibitor, with an IC50 of 961.5 nM. mIDH1-IN-1 potently inhibits intracellular 2-HG (2-hydroxyglutarate) production in HT1080 cells, with an EC50 of 208.6 ± 8.0 nM. mIDH1-IN-1 shows a significant anti-proliferation activity on IDH1 mutant-U-87 cells, with an IC50 of 41.8 nM. mIDH1-IN-1 is an antitumor agent, and can be used for IDH1 mutated solid tumors research .
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- HY-P5082
-
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α-synuclein
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Neurological Disease
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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 .
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- HY-108232
-
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Organoid
Akt
Autophagy
Apoptosis
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Cancer
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MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities .
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- HY-148070
-
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FLT3
FAK
Cytochrome P450
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Cancer
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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 .
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- HY-122914
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Ras
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Cancer
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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 .
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- HY-149508
-
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Keap1-Nrf2
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Cancer
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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 .
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- HY-10357
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Organoid
Akt
Autophagy
Apoptosis
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Cancer
|
|
MK-2206 free base is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206 free base. MK-2206 free base has anticancer activities .
|
-
- HY-136789
-
|
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 .
|
-
- HY-115282A
-
|
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) .
|
-
- HY-168514
-
|
|
EGFR
|
Cancer
|
|
SOS1/EGFR-IN-2 (Compound 4) is a SOS1 and EGFR dual inhibitor with IC50s of 8.3 and 14.6 nM, respectively. SOS1/EGFR-IN-2 exhibits significant antiproliferative effect on the cancer cells haboring various KRAS mutants .
|
-
- HY-152560
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-55 (compound 4d) inhibits WT HIV-1 with an EC50 value of 8.6 nM. HIV-1 inhibitor-55 also shows inhibitory potency against single and double HIV-1 mutants. HIV-1 inhibitor-55 can be used for the research of virus infection .
|
-
- HY-101489A
-
|
|
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.
|
-
- HY-15519
-
|
|
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 .
|
-
- HY-143306
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 5 (compound 2) is an IDH1 (isocitrate dehydrogenase 1) inhibitor. IDH1 Inhibitor 5 inhibits MOG cells and wild-type IDH1 glioma cells with expressing exogenous mutant IDH1 R132H protein with IC50s of 64.4 and 34.9 nM, respectively .
|
-
- HY-115282
-
|
TRC-253 free base
|
Androgen Receptor
|
Cancer
|
|
JNJ-63576253 (TRC-253) free base 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 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
|
-
- HY-130616
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFR L858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1 .
|
-
- HY-122209
-
|
|
HBV
|
Infection
|
|
DVR-01 is a HBV inhibitor with EC50 values of 1.7 and 1.6 μM in AML12HBV10 and HepDES19 cells, respectively. DVR-01 shows antiviral activity against drug-resistant HBV mutants with EC50s of 2.403-3.273 μM. DVR-01 can be used for the research of HBV infection and related diseases .
|
-
- HY-16271
-
|
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 .
|
-
- HY-156158
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH2 R140Q-IN-2 (compound 36) is an an orally active IDH2 R140Q inhibitor (IC50: 29 nM). IDH2 R140Q-IN-2 reduces D2HG production in TF-1 cell lines expressing mutant IDH2 R140Q (IC50: 10 nM). IDH2 R140Q-IN-2 suppresses D2HG levels in tumor tissue. IDH2 R140Q-IN-2 can be used for research of acute myeloid leukemia (AML) .
|
-
- HY-111836
-
|
|
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 .
|
-
- HY-161654
-
|
|
PROTACs
Ras
|
Cancer
|
|
PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
|
-
- HY-122862
-
|
|
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 .
|
-
- HY-134813
-
|
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective 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 .
|
-
- HY-10574
-
|
R278474; TMC278; DB08864
|
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
|
-
- HY-10574A
-
|
TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride
|
SARS-CoV
MMP
|
Infection
|
|
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
|
-
- HY-153220
-
|
|
Btk
|
Cancer
|
|
NX-2127 is an orally and potent BTK inhibitor, inducing degradation of the mutated BTK C481S in cells. NX-2127 inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). NX-2127 catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. NX-2127 stimulates T cell activation and increases IL-2 production in primary human T Cells .
|
-
- HY-150754
-
|
|
Bacterial
|
Infection
|
|
FtsZ-IN-4 is an orally active FtsZ (filamenting temperature-sensitive mutant Z) inhibitor, exhibits excellent antibacterial activity. FtsZ-IN-4 shows good pharmaceutical properties with low cytotoxicity (CC50 >20 μg/mL) .
|
-
- 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 .
|
-
- HY-114491
-
|
|
ERK
Raf
|
Cancer
|
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-114491A
-
|
|
ERK
Raf
|
Cancer
|
|
Rineterkib hydrochloride (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-12083
-
|
|
Bcr-Abl
|
Cancer
|
|
PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba⁄F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
|
-
- HY-149880
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-124089
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
|
-
- HY-168580
-
|
|
PROTACs
c-Kit
|
Cancer
|
|
c-Kit-IN-7 (compound 104) is a potent inhibitor of c-Kit, with the IC50 of ≤10 nM. c-Kit-IN-7 plays an important role in cancer research .
|
-
- HY-P2265
-
|
|
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-157229
-
|
|
EGFR
|
Others
|
|
STX-721 is a mutant-selective inhibitor of EGFR and HER2 Exon 20 insertion (ex20ins) mutants .
|
-
- HY-19985
-
|
|
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 .
|
-
- HY-19803
-
|
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.
|
-
- HY-19729
-
|
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.
|
-
- HY-131066
-
|
|
EGFR
|
Cancer
|
|
EMI48, the derivative of EMI1, displays greater potency toward mutant EGFR than EMI1. EMI48 inhibits EGFR triple mutants .
|
-
- HY-12972
-
|
PF-06747775
|
EGFR
|
Cancer
|
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC) .
|
-
- HY-P2265A
-
|
|
Ras
|
Cancer
|
|
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-155046
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-14 (Compound 27i) is a FGFR4 inhibitor (IC50: 2.4 nM. FGFR4-IN-14 inhibits the proliferation of V550L and N535K mutant strains, with IC50s of 21 nM, 2.5 nM, 171 nM against huh7, BaF3/ETV6-FGFR4-V550L and BaF3/ETV6-FGFR4-N535K cells respectively. FGFR4-IN-14 has potent antitumor efficacy in the Huh7 xenograft model. FGFR4-IN-14 can be used for research of hepatocellular carcinoma (HCC) .
|
-
- HY-U00447
-
|
|
MDM-2/p53
DNA Alkylator/Crosslinker
|
Cancer
|
|
PK11000 is an alkylating agent, and stabilizes the DNA-binding domain of both WT and mutant p53 proteins by covalent cysteine modification without compromising DNA binding. PK11000 has anti-tumor activities .
|
-
- HY-164467
-
|
|
Wnt
|
Cancer
|
|
CCT070535 blocks TCF-dependent transcription at the TCF level, with GI50 values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively .
|
-
- HY-19980A
-
PRIMA-1
2 Publications Verification
NSC-281668
|
Autophagy
MDM-2/p53
Ferroptosis
Apoptosis
|
Cancer
|
|
PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.
|
-
- HY-122595
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-1 (compound 3) is a selective and SAM-competitive EZH2 and EZH1 inhibitor with an IC50s of 32 nM, 197 nM and 213 nM for EZH2wt, EZH2 Y641N mutant and EZH1, respectively. EZH2-IN-1 reduces bulk H3K27me3 and H3K27me2 levels. EZH2-IN-1 has the potential for diffuse large B cell lymphoma research .
|
-
- HY-78869
-
|
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.
|
-
- HY-12872
-
|
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.
|
-
- HY-12872A
-
|
EGF816 mesylate
|
EGFR
|
Cancer
|
|
Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min −1 on EGFR(L858R/790M) mutant, respectively.
|
-
- HY-142645
-
|
|
RSV
|
Infection
|
|
TP0591816 is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins (wild-type, EC50 = 0.27 nM; D486N-mutant, EC50 = 0.70 nM).
|
-
- HY-158151
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 12 (compound 510B) is a potent p53 activator. p53 Activator 12 binds to mutant p53 and restores the ability of the p53 mutant to bind DNA .
|
-
- HY-149359
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
|
-
- HY-W034419
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
STIMA-1 can stimulate mutant p53 DNA binding in vitro and induce expression of p53 target proteins and trigger apoptosis in mutant p53-expressing human tumor cells .
|
-
- HY-144104
-
-
- HY-19540
-
GSK864
4 Publications Verification
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
GSK864 is an isocitrate dehydrogenase 1 (IDH1) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC50 values of 8.8, 15.2 and 16.6 nM.
|
-
- HY-128860
-
|
|
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 .
|
-
- HY-145836
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
|
-
- HY-121708
-
|
|
Others
|
Cancer
|
|
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
|
-
- HY-19726
-
|
|
MDM-2/p53
|
Cancer
|
|
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling .
|
-
- HY-160287
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
NVS MLLT-1 (compound 3) 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 .
|
-
- HY-156671
-
|
|
Ras
PI3K
ERK
mTOR
Apoptosis
|
Cancer
|
|
RMC-4998 is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. RMC-4998 can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant, with an IC50 value of 28 nM. RMC-4998 can inhibit ERK signaling in KRAS G12C mutant cancer cells and induce apoptosis. RMC-4998 can be used for tumor research .
|
-
- HY-158115
-
|
|
Molecular Glues
Raf
MEK
|
Cancer
|
|
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
|
-
- HY-113843
-
|
|
Others
|
Cancer
|
|
RETRA (hydrobromide) is a mutant p53-dependent activator of p73 that can inhibit cancer cells carrying mutant p53. RETRA (hydrobromide) increases the expression level of p73, induces transcriptional activation of several common to transcriptional targets p53 and p73, which leads to mutant p53- and p73-dependent inhibition of tumor growth, reduction of colony formation and induction of effector caspases .
|
-
- HY-W423595
-
|
|
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 .
|
-
- HY-164142
-
|
|
HSP
|
Cancer
|
|
ETB is a potent Hsp60 chaperone activity inhibitor. ETB blockes the chaperone activities of the wild-type protein and of the C237A and C447A mutant proteins. ETB binds to Hsp60 Cys 442 and shows the resistance of the C442A mutant to ETB inhibition .
|
-
- HY-120331
-
|
|
HIV
HIV Protease
|
Infection
|
|
U-89360E is an inhibitor for HIV-1 protease. U-89360E inhibits the protease of HIV-1 wildtype, V82D mutant and V82N mutant with Ki of 20 nM, 560 nM and 2100 nM, respectively .
|
-
- HY-114636
-
|
|
Others
|
Others
|
|
RG-102240 is a ligand for insect ecdysone receptor (EcR), with IC50 of 85 and 13 nM, in wildtype G:CfE(DEF) and its A110P mutant. RG-102240 induces the reporter gene activity of wild-type CfEcR and A110P mutant .
|
-
- HY-112802A
-
|
|
c-Kit
|
Cancer
|
|
AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
|
-
- HY-100520
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.
|
-
- HY-117915
-
|
|
Bacterial
|
Infection
|
|
Averufin is a polyhydroxyanthraquinone that accumulates in large quantities in mutants of A. parasiticus deficient in aflatoxin biosynthesis .
|
-
- HY-156681A
-
|
|
Others
|
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 .
|
-
- HY-15003
-
|
|
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 .
|
-
- HY-18690A
-
-
- HY-100020
-
-
- HY-162440
-
|
|
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 .
|
-
- HY-162441
-
|
|
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 .
|
-
- HY-162442
-
|
|
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 .
|
-
- HY-162443
-
|
|
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 .
|
-
- HY-145020
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 23 is a KRAS G12C inhibitor. KRAS G12C inhibitor 23 inhibits H358 cells with an IC50 of 491 nM (WO2021218939A1, compound 1) .
|
-
- HY-153306
-
|
|
PI3K
|
Cancer
|
|
RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin .
|
-
- HY-19980
-
|
APR-246; PRIMA-1Met
|
MDM-2/p53
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance .
|
-
- HY-153008
-
|
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research .
|
-
- HY-121161C
-
|
|
Others
|
Metabolic Disease
|
|
Brassinazole (0.5, 1, 5 μM) causes markedly deformed seedlings, whose morphology is similar to that of BR-deficient mutants. Brassinazole causes cress dwarfism, altering leaf morphology such as the typical downward curl and dark green appearance of Arabidopsis BR-deficient mutants. However, administration of 10 nM BR reversed dwarfism .
|
-
- HY-161030
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-92 (compound 15) is an allosteric T790M/L858R double mutant EGFR inhibitor. EGFR-IN-92 shows antiproliferative activity against H1975 non-small lung cancer (NSCLC) cancer cells expressing double mutant EGFR .
|
-
- HY-122578
-
|
|
MDM-2/p53
|
Cancer
|
|
P53R3 is a potent p53 reactivator and restores sequence-specific DNA binding of p53 hot spot mutants, including p53 R175H, p53 R248W and p53 R273H. P53R3 induces p53-dependent antiproliferative effects with much higher specificity than PRIMA-1. P53R3 enhances the recruitment of wild-type p53 and p53 M237I to several target gene promoters. P53R3 strongly enhances the mRNA, total protein and cell surface expression of the death receptor death receptor 5 (DR5). P53R3 is used for cancer research .
|
-
- HY-122054
-
|
|
Others
|
Cancer
|
|
BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
|
-
- HY-122054A
-
|
|
Others
|
Cancer
|
|
BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells .
|
-
- HY-155742
-
|
|
CFTR
|
Others
|
|
CFTR corrector 12 (compound 17C) is a bithiazole derivative, serving as CFTR corrector. CFTR corrector 12 has the ability to correct some folding defective mutants of the channel responsible for the control of chloride transport across the plasma membrane. CFTR corrector 12 recovers the α-sarcoglycan (α-SG) content in mutant cells .
|
-
- HY-13897
-
|
|
EGFR
|
Cancer
|
|
CNX-2006 is a mutant-selective and irreversible EGFR inhibitor with an IC50 below 20 nM for EGFR T790M.
|
-
- HY-12408
-
|
|
Ras
|
Cancer
|
|
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
|
-
- HY-139891
-
|
|
Trk Receptor
|
Cancer
|
|
Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants (IC50 = 0.2-0.7 nM).
|
-
- HY-N3492
-
|
|
Others
|
Others
|
|
Isoderrone is a new isoflavone isolated from the methanol extractives from white lupin (cv. Kievskij Mutant) roots .
|
-
- HY-N3496
-
|
|
Others
|
Others
|
|
Isochandalone is a new isoflavone isolated from the methanol extractives from white lupin (cv. Kievskij Mutant) roots .
|
-
- HY-19896
-
COTI-2
2 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
COTI-2, an anti-cancer agent with low toxicity, is an orally available third generation activator of p53 mutant forms. COTI-2 acts both by reactivating mutant p53 and inhibiting the PI3K/AKT/mTOR pathway. COTI-2 induces apoptosis in multiple human tumor cell lines. COTI-2 exhibits antitumor activity in HNSCC through p53-dependent and -independent mechanisms. COTI-2 converts mutant p53 to wild-type conformation .
|
-
- HY-164469
-
|
|
Bcr-Abl
Apoptosis
STAT
|
Cancer
|
|
CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
|
-
- HY-16379
-
|
SB1518
|
JAK
FLT3
|
Cancer
|
|
Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM).
|
-
- HY-154313
-
|
Clospirazine
|
Ras
|
Cancer
|
|
Spiclomazine (Clospirazine) is a potent mutant KRAS(G12C) inhibitor that selectively inhibits mutant KRAS-driven pancreatic cancer. Spiclomazine can eliminate KRas-GTP levels in KRAS-driven pancreatic cancer and effectively inhibit RAS-mediated signaling. Spiclomazine significantly inhibits tumor progression in mouse renal capsule xenotransplantation models .
|
-
- HY-12408A
-
|
|
Ras
|
Cancer
|
|
6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
|
-
- HY-119177
-
|
|
Bcr-Abl
|
Others
|
|
PD173956 is a pyridopyrimidine Bcr-Abl kinase inhibitor with high selectivity for the P-loop mutant form of Bcr-Abl .
|
-
- HY-156967
-
|
|
MDM-2/p53
|
Cancer
|
|
BAY 1892005 is a regulator of p53 protein and acts on p53 condensates without causing mutant p53 reactivation .
|
-
- HY-134385
-
|
|
CFTR
|
Others
|
|
6-PhEt-dATP is an ATP analog that specifically enhances the function of certain CFTR mutants and is useful for studying cystic fibrosis .
|
-
- HY-153342
-
|
ARV-766
|
PROTACs
Androgen Receptor
|
Cancer
|
|
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
|
-
- HY-129550
-
|
|
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 .
|
-
- HY-18606
-
|
|
Ras
|
Cancer
|
|
K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
|
-
- 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.
|
-
- HY-143729
-
-
- HY-151571
-
|
|
Ras
|
Cancer
|
|
ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-161906
-
|
|
Acyltransferase
|
Cancer
|
|
SD-066-4 is an orally active acyltransferase inhibitor. SD-066-4 can be used in cancer research .
|
-
- HY-159476
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-26 (compound 194a) is a potent KRAS G12V inhibitor (IC50: ≤100 nM). KRAS inhibitor-26 can be used for cancer research .
|
-
- HY-10159A
-
|
AMN107 monohydrochloride monohydrate
|
Bcr-Abl
Autophagy
|
Cancer
|
|
Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
|
-
- HY-159795
-
|
PF-07799933; ARRY-440
|
Raf
|
Cancer
|
|
Claturafenib ( PF-07799933) is an inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in HT29 cells with an IC50 value of 1.6 nM .
|
-
- HY-101522
-
|
|
EGFR
BMX Kinase
Btk
MEK
|
Cancer
|
|
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
|
-
- HY-146108
-
|
|
RSV
|
Infection
|
|
RSV-IN-5 (Compound 4) is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. RSV-IN-5 exhibits potent anti-RSV activities against not only wild-type A2 F protein (EC50=2.0 nM), but also D486N-mutant F protein (EC50=8.1 nM) .
|
-
- HY-157389
-
|
|
Bcr-Abl
|
Cancer
|
|
AK-HW-90 (compound 2B) is a potent panBcr-Abl inhibitor with significant inhibitory activity against Imatinib (HY-15463)-resistant mutants. AK-HW-90 inhibits the resistance mutant Bcr-Abl T315I with an IC50 of 0.65 nM. AK-HW-90 has potential anticancer activity and can be used in the study of chronic myelogenous leukemia (CML) .
|
-
- HY-124153
-
|
|
Btk
|
Cardiovascular Disease
Inflammation/Immunology
|
|
GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases .
|
-
- HY-18082
-
-
- HY-P1004
-
|
|
Reactive Oxygen Species
|
Cancer
|
|
Luciferase from Vibrio fischeri has also been used in a study to investigate the sensitivity of dark mutants of various strains of luminescent bacteria to reactive oxygen species.
|
-
- HY-112929
-
|
|
Phosphatase
|
Cancer
|
|
DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
|
-
- HY-104036
-
IDH-305
1 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)) .
|
-
- HY-145785
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].
|
-
- HY-16379A
-
|
SB1518 hydrochloride
|
JAK
FLT3
|
Cancer
|
|
Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
|
-
- HY-16379R
-
|
|
JAK
FLT3
|
Cancer
|
|
Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
|
-
- HY-161885
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
SMARCA2-IN-6 is a SMARCA2 (also known as BRM) inhibitor, with IC50s less than 5 nM for SMARCA2 and SMARCA4. SMARCA2-IN-6 inhibits KRT80 gene expression in H1299 cells (IC50: 26 nM). SMARCA2-IN-6 inhibits proliferation in BRG1-mutant SKMEL5 cells (IC50: 13 nM) .
|
-
- HY-W998345
-
|
|
PROTACs
PDK-1
Akt
|
Cancer
|
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models.(Blue: CRBN ligand; Black: linker; Pink: Smurf1 ligand (Smurf1-L)) .
|
-
- HY-U00416
-
|
|
Ras
|
Cancer
|
|
ARS-1323, the racemate of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
|
-
- HY-111050
-
|
|
c-Met/HGFR
|
Cancer
|
|
JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC50s of 2 and 3 nM for wild type and mutant Met, respectively.
|
-
- HY-145126
-
|
|
CFTR
|
Others
|
|
CP-628006, a small molecule CFTR potentiator, restores ATP-dependent channel gating to the cystic fibrosis mutant G551D-CFTR.
|
-
- HY-154959
-
|
|
Ras
|
Cancer
|
|
AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS G12C inhibitor. AZD4747 has the potential to study cancer .
|
-
- HY-160020
-
|
|
Androgen Receptor
|
Cancer
|
|
ET516 is a potent inhibitor of Androgen Receptor. ET516 significantly inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants .
|
-
- HY-124089S
-
|
|
Isotope-Labeled Compounds
Cannabinoid Receptor
|
Metabolic Disease
|
|
Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant[1][2].
|
-
- HY-145785A
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
ADH-6 TFA is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 TFA targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 TFA has the potential for the research of cancer diseases .
|
-
- HY-157526
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-TK-IN-1 (compound 7o) is a potent mutant EGFR inhibitor with IC50 of 8.5 nM an 9.3 nM against EGFR L858R/T790M and EGFR Del19.EGFR-TK-IN-1 showes strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells and induces cell apoptosis .
|
-
- HY-161802
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 228 (Compound 8) inhibits the mycobacterial ribosome (IC50 for Mycobacterium smegmatis is 2.31 μM) and exhibits antibacterial activity against M. tuberculosis H37Rv (MIC=2 and 0.25 μg/mL for wildtype and Δ1258c mutant), M. abscessus ATCC 19977 (MIC=8 and 8 μg/mL for wildtype and Δ2780c mutant) and M. smegmatis (MIC=8 μg/mL) .
|
-
- HY-12090
-
|
MK-0859
|
PCSK9
|
Cardiovascular Disease
|
|
Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.
|
-
- HY-107977
-
-
- HY-128589
-
|
|
c-Kit
|
Cancer
|
|
CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM .
|
-
- HY-112802
-
|
|
c-Kit
|
Cancer
|
|
AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM .
|
-
- HY-N3920
-
|
|
Bacterial
|
Infection
|
|
Gancaonin G is a 6-prenylated isoflavanone that can be isolated from Glycyrrhiza uralensis. Gancaonin G has antibacterial activity against Streptococcus mutants and MRSA strains .
|
-
- HY-P4391
-
-
- HY-148901
-
|
|
COX
|
Neurological Disease
|
|
CMB-087229 is a mutant superoxide dismutase 1 (SOD1) protein aggregation inhibitor with IC50 of 67 nM, which can be used in the research of amyotrophic lateral sclerosis .
|
-
- HY-160167
-
|
|
Btk
|
Inflammation/Immunology
|
|
BTK-IN-30 (compound cpd15) is an inhibitor of Bruton's Tyrosine Kinase (BTK) and mutant BTK with IC50 values of 6.72 and 6.11nM respectively .
|
-
- HY-U00417
-
|
|
Ras
|
Cancer
|
|
ARS-1630, a less active enantiomer of ARS-1620, is a novel inhibitor of mutant K-ras G12C extracted from patent WO 2015054572 A1.
|
-
- HY-18343A
-
|
|
MDM-2/p53
|
Cancer
|
|
CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53 .
|
-
- HY-100002
-
-
- HY-141807
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
|
-
- HY-146223
-
|
|
Ras
|
Cancer
|
|
AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-120885
-
|
|
Ras
|
Cancer
|
|
(+)-Oxanthromicin (Compound 1) mislocalizes the oncogenic mutant K-Ras from the plasma membrane of intact Madin-Darby canine kidney (MDCK) cells, and exhibits thereby antitumor efficacy .
|
-
- HY-136379
-
|
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 .
|
-
- HY-114778
-
|
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 .
|
-
- HY-150699
-
|
|
Bacterial
|
Infection
|
|
TXA6101 is a bacterial protein FtsZ (filamentous temperature-sensitive protein Z) inhibitor that inhibits bacterial division. TXA6101 has antimicrobial activity against MRSA isolates expressing either the G193D or G196S mutant FtsZ with the MIC value of 1 μg/mL, retains significant activity against the TXA707-resistant FtsZ mutant. TXA6101 can be used as a potential method against Gram-negative bacterial infections .
|
-
- HY-148404
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 5 (compound 134A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 5 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 5 shows anti-tumor activity . p53 Activator 5 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-148402
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 3 (compound 87A) is a potent p53 activator with a SC150 value of <0.05 mM. p53 Activator 3 can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA. p53 Activator 3 shows anti-tumor activity . p53 Activator 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-16379B
-
|
SB1518 citrate
|
JAK
FLT3
|
Cancer
|
|
Pacritinib (SB1518) citrate is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib citrate also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
|
-
- HY-117540
-
|
|
Others
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
- HY-108637
-
|
|
MDM-2/p53
|
Cancer
|
|
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM. PhiKan 083 can be used for cancer research .
|
-
- HY-N5141
-
|
|
Others
|
Others
|
|
Isoscoparin-2′′O-glucoside is a flavonoid that can be found in yellow grain mutant of rice. Isoscoparin-2′′O-glucoside shows antioxidant activity .
|
-
- HY-13810
-
|
|
Raf
|
Cancer
|
|
PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity .
|
-
- HY-18205
-
-
- HY-121262
-
|
|
Others
|
Others
|
|
Bisabolene is a compound that can be synthesized by engineered bacteria. Bisabolene can be synthesized by heterologous expression of related genes in cyanobacteria. Its production and changes in related metabolites were studied in glycogen-deficient mutants.
|
-
- HY-P0222
-
|
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P0222A
-
|
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-134904
-
|
RM-006
|
mTOR
|
Cancer
|
|
RMC-6272 (RM-006) is a bi-steric mTORC1-selective inhibitor. RMC-6272 exhibits potent and selective (> 10-fold) inhibition of mTORC1 over mTORC2. RMC-6272 shows improved inhibition of mTORC1 in comparison to Rapamycin, and induces more cell death in TSC2 null tumors .
|
-
- HY-P3277
-
|
|
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 .
|
-
- HY-P3277A
-
|
|
Ras
|
Cancer
|
|
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
|
-
- HY-161655
-
-
- HY-161656
-
|
|
PROTAC Linkers
|
Cancer
|
|
PIP-C-3-Azaspiro[5.5]undecane-boc is the linker for PROTAC. PIP-C-3-Azaspiro[5.5]undecane-boc is utilized for synthesis of PROTAC SOS1 degrader-10 (HY-161654) .
|
-
![PIP-C-3-Azaspiro[5.5]undecane-boc](//file.medchemexpress.eu/product_pic/hy-161656.gif)
- HY-161819
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-29 (Compound B31) is a second-generation TRK inhibitor (IC50: 9 nM, 0.6 nM, 18 nM, 5 nM, 6 nM for TRKA G595R, TRKA F589L, TRKA G667C, TRKA and TRKC respectively). TRK-IN-29 inhibits the phosphorylation of TRKA. TRK-IN-29 has good antiproliferative activities against NTRK fusion positive cells. TRK-IN-29 has exellent plasma stability and moderate pharmacokinetic properties .
|
-
- HY-13237
-
-
- HY-18604
-
|
|
Ras
|
Cancer
|
|
K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
|
-
- HY-135805A
-
|
|
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 .
|
-
- HY-153007
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 shows anti-malaria activity .
|
-
- HY-149711
-
|
|
ICMT
|
Metabolic Disease
|
|
Farnesylcysteine (FC) is a competitive inhibitor of ICMT. The fcly mutant has quantitatively low farnesylcysteine (FC) lyase activity and an enhanced response to ABA. Farnesylcysteine induces an ABA hypersensitive phenotype in Arabidopsis thaliana .
|
-
- HY-111079
-
|
|
Others
|
Others
|
|
HIV-1 inhibitor-70 (compound 20) is a bifunctional inhibitor that inhibits both wild-type (WT) and K103N mutant reverse transcriptases (RTs) of HIV-1.
|
-
- HY-153007A
-
|
|
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-5 hydrochloride is a potent and orally active dihydrofolate reductase (DHFR) inhibitor with a Ki value of 0.54 nM for quadruple mutant Plasmodium falciparum DHFR. DHFR-IN-5 hydrochloride shows anti-malaria activity .
|
-
- HY-103369
-
|
|
CFTR
|
Endocrinology
|
|
PG01 is a potent CFTR Cl - channel potentiator. PG01 can correct gating defects of CFTR mutants, is effective on b>E193K, G970R and G551D (CFTR mutants) with Kd values of 0.22 μM, 0.45 μM and 1.94 μM, respectively. PG01 is also effective on ΔF508 (Ka of 0.3 μM). PG01 increases ΔF508-CFTR Cl - current after adding Forskolin .
|
-
- HY-161777
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SARS-CoV-2 Mpro-IN-23 (Compound 2) is an inhibitor for SARS-CoV-2 main protease (Mpro), which inhibits wildtype Mpro and mutant Mpro variants, with IC50 of 0.057-0.92 μM. SARS-CoV-2 Mpro-IN-23 inhibits the post-entry viral processes of wild-type SARS-CoV-2 single-round infectious particles (SRIPs), suppresses the viral replication of Mpro wildtype and Mpro mutants with EC50 of 0.02-0.52 μM .
|
-
- HY-162809
-
|
|
Ras
|
Cancer
|
|
XMU-MP-9 is a bifunctional compound that binds to the C2 domain of Nedd4-1 and the allosteric site of K-Ras. XMU-MP-9 enhances the interaction between Nedd4-1 and K-Ras, induces conformational changes in the Nedd4-1/K-Ras complex, promotes the ubiquitination and degradation of multiple K-Ras mutants, and inhibits the proliferation of cells carrying K-Ras mutants. XMU-MP-9 can be used in cancer research .
|
-
- HY-P99849
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
|
-
- HY-112256
-
ACP-105
5 Publications Verification
|
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.
|
-
- HY-111627
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
5-Aza-7-deazaguanine is a substrate for wild-type (WT) E. coli purine nucleoside phosphorylase and its Ser90Ala mutant in the synthesis of base-modified nucleosides .
|
-
- HY-130253
-
|
|
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 .
|
-
- HY-120122
-
|
|
Others
|
Cancer
|
|
PK7088 is a pyrazole and a specific peptide. PK7088 supports the reactivation of mutant p53 by converting it to a form exhibiting wild-type properties. PK7088 exhibit anticancer activity in cancer research .
|
-
- HY-162300
-
|
|
EGFR
|
Cancer
|
EGFR kinase inhibitor 4 (Compound 4) is a bivalent ATP-allosteric EGFR inhibitor (IC50: 1.8 nM for mutant EGFR (LRTMCS)). EGFR kinase inhibitor 4 can be used for research of NSCLC .
|
-
- HY-163636
-
|
|
Phosphodiesterase (PDE)
Ras
|
Cancer
|
|
Deltaflexin3 is a potent PDE6D inhibitor. Deltaflexin3 reduces the signaling of Ras and selectively decreases the KRAS mutant and PDE6D-dependent cancer cells growth .
|
-
- HY-164315
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 67 (example 35) is a KRAS G12C inhibitor that selectively inhibits the growth of many KRAS G12C mutant tumor cell lines .
|
-
- HY-18690
-
|
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.
|
-
- HY-108637A
-
|
|
MDM-2/p53
|
Cancer
|
|
PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM , and a relative binding affinity (Kd) of 150 μM in Ln229 cells .
|
-
- HY-122562
-
MT-802
1 Publications Verification
|
PROTACs
Btk
|
Inflammation/Immunology
Cancer
|
|
MT-802 is a potent BTK degrader based on Cereblon ligand, with a DC50 of 1 nM. MT-802 has potential to treat C481S mutant chronic lymphocytic leukemia (CLL) .
|
-
- HY-P2319
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-135914
-
|
|
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 .
|
-
- HY-107415
-
|
|
Raf
|
Cancer
|
|
PLX7922, a RAF inhibitor, can bind with BRAF V600E. PLX7922 inhibits pERK in BRAF V600E cell lines, and activates pERK in mutant NRAS cell lines .
|
-
- HY-112306
-
|
DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
|
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
|
-
- HY-112654A
-
|
|
Others
|
Cancer
|
|
GCN2iB acetate is a GCN2 inhibitor that enhances Gcn2 activity and Atf4 expression. GCN2iB can activate Gcn2 mutants lacking functional regulatory regions or certain kinase domain substitution mutants. GCN2iB increases eIF2 phosphorylation by Gcn2 at low concentrations, thereby enhancing the cellular response to nutritional stress. GCN2iB may have potential benefits for the inhibition of cancer cells expressing low basal levels of aspartate synthetase, enhancing their sensitivity to the anti-leukemic compound L-aspartase .
|
-
- HY-146243
-
|
|
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 .
|
-
- HY-18634
-
|
ZMC1
|
MDM-2/p53
|
Cancer
|
|
NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
|
-
- HY-P2319A
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P1974
-
|
WF11899A
|
Antibiotic
|
Infection
|
|
FR901379 (WF11899A) is a novel echinocandin-type lipopeptide antibiotic. FR901379 is primarily produced by mutant strain M-7 of Coleophoma empetri F-11899 (FERM BP-2635) .
|
-
- HY-161753
-
|
|
CFTR
|
Inflammation/Immunology
|
|
CFTR potentiator 1 (I1421) is a potent CFTR potentiator with an EC50 value of 64 nM. CFTR potentiator 1 allosterically activates a wide range of CF-causing mutants, such as ΔF508 and G551D CFTR .
|
-
- HY-169294
-
|
|
Others
|
Metabolic Disease
|
|
SLC6A8 corrector 1 is an orally active and brain-penetrant mutant SLC6A8 variant corrector. SLC6A8 corrector 1 can be used for the study of creatine transporter deficiency (CTD) .
|
-
- HY-13223
-
|
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.
|
-
- HY-B0282
-
|
ACh chloride
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
|
-
- HY-109061
-
|
YH25448; GNS-1480
|
EGFR
|
Cancer
|
|
Lazertinib (YH25448) is a potent, highly mutant-selective, blood-brain barrier permeable, orally available and irreversible third-generation EGFR tyrosine kinase inhibitor, and can be used in the research of non-small cell lung cancer .
|
-
- HY-111760
-
|
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCF β-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM .
|
-
- HY-13223A
-
|
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.
|
-
- HY-10542A
-
|
|
Atg8/LC3
Raf
|
Neurological Disease
|
|
(Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder .
|
-
- HY-142161
-
ABD957
1 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 .
|
-
- HY-B1907A
-
|
Rifamycin SV
|
Bacterial
Antibiotic
|
Infection
|
|
Rifamycin (Rifamycin SV) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .
|
-
- HY-156681
-
|
|
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 .
|
-
- HY-15217
-
|
|
Haspin Kinase
|
Cancer
|
|
CHR-6494 is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 inhibits histone H3T3 phosphorylation. CHR-6494 can be used in the research of cancer .
|
-
- HY-110350
-
|
|
Haspin Kinase
|
Cancer
|
|
CHR-6494 TFA is a potent inhibitor of haspin, with an IC50 of 2 nM. CHR-6494 TFA inhibits histone H3T3 phosphorylation. CHR-6494 TFA induces the apoptosis of cancer cells, including melanoma and breast cancer. CHR-6494 TFA can be used in the research of cancer .
|
-
- HY-132193
-
|
|
RET
|
Cancer
|
|
RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects .
|
-
- HY-116528
-
|
|
HIV
|
Infection
|
|
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively .
|
-
- HY-142680
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8) .
|
-
- HY-146710
-
|
|
RET
|
Cancer
|
|
RET-IN-16 is a potent and selective RET inhibitor with IC50s of 3.98 nM, 8.42 nM, 15.05 nM, 7.86 nM, 5.43 nM and 8.86 nM for RET(WT), RET(M918T), RET(V804L), RET(V804M), RET-CCDC6 and RET-KIF5B, respectively. RET-IN-16 has anticancer effects .
|
-
- HY-137191
-
|
|
EGFR
|
Cancer
|
|
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
|
-
- HY-164526
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
SH1573 is an orally active mIDH2 inhibitor. SH1573 has a strong and selective inhibitory effect on mIDH2 R140Q protein (IC50=4.78 nmol/L), and can effectively reduce the production of the carcinogenic metabolite 2-hydroxyglutarate (2-HG) in animal models, cell lines, serum and tumors. SH1573 can be used for the study of acute myeloid leukemia (AML) .
|
-
- HY-168221
-
|
|
PROTACs
|
Cancer
|
|
YD54 is a PROTAC based SMARCA2 degrader with a DC50 of 3.5 nM (Red: SMARCA2 degrader (HY-44012B), black: linker, Blue: E3 ligase ligand) .
|
-
- HY-10159AR
-
|
|
Bcr-Abl
Autophagy
|
Cancer
|
|
Nilotinib (monohydrochloride monohydrate) (Standard) is the analytical standard of Nilotinib (monohydrochloride monohydrate). This product is intended for research and analytical applications. Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly potent against BCR-ABL, and is active against many BCR-ABL mutants.
|
-
- HY-15734
-
|
|
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.
|
-
- HY-B1907
-
|
Rifamycin SV sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .
|
-
- HY-129943
-
|
|
Bacterial
|
Infection
|
|
Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2) .
|
-
- HY-N6674
-
|
ECO-4601; TLN-4601; BU 4664L
|
Ras
Apoptosis
|
Cancer
|
|
Diazepinomicin (TLN-4601) is a secondary metabolite produced by Micromonospora sp. Diazepinomicin (TLN-4601) inhibits the EGF-induced Ras-ERK MAPK signaling pathway and induces apoptosis. An anti-tumor agent for K-Ras mutant models .
|
-
- HY-145701
-
|
|
MEK
|
Cancer
|
|
MEK1/2-IN-2 is a potent ATP-competitive MEK1/2 inhibitor and shows equipotent inhibition of WT MEK1/2 and a panel of MEK1/2 mutant cell lines .
|
-
- HY-108639
-
|
NSC 19630
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
MIRA-1 is a maleimide analogue. MIRA-1 can induce apoptosis in mutant p53 cells via restoration of p53-dependent transcriptional transactivation. MIRA-1 has anticancer activity .
|
-
- HY-151938
-
|
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-3 is a pyrimidine-5-carboxamide derivative, acts as an inhibitor of HIV-1. Reverse transcriptase-IN-3 shows potent activity against the HIV-1 wild-type and mutant strains .
|
-
- HY-161031
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-93 (compound 18) is an allosteric inhibitor of T790M/L858R double mutant EGFR. EGFR-IN-93 can be used for non-small lung cancer (NSCLC) research .
|
-
- HY-161602
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-13 (Compd 38) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-13 can be used for cancer research .
|
-
- HY-161603
-
|
|
EGFR
|
Cancer
|
|
EGFR/HER2-IN-14 (Compd 46) is an inhibitor of mutant EGFR/HER2s which are resistant to other drugs. EGFR/HER2-IN-14 can be used for cancer research .
|
-
- HY-116572
-
|
|
APC
|
Cancer
|
|
TASIN-1 hydrochloride is a selective inhibitor of truncated APC gene (adenomatous polyposis coli gene) and exerts cytotoxic effects through inhibition of cholesterol biosynthesis. TASIN-1 hydrochloride represents a potential strategy for prevention and intervention in CRC with mutant APC .
|
-
- HY-126464
-
|
EoM
|
Androgen Receptor
|
Cancer
|
|
Estromustine (EoM) is the active metabolite of Estramustine phosphate (HY-13627A). Estromustine binds to mutant androgen receptor (m-AR) with EC50 of 2.6 μM in LNCaP, exhibits cytotoxicity in human prostate cells LNCaP with IC50 of 9.73 μM .
|
-
- HY-164464
-
|
|
EGFR
|
Cancer
|
|
BPI-15086 an orally active, potent, irreversible mutant-selective inhibitor of both EGFR and T790M resistance mutations tyrosine kinase. BPI-15086 can be used for the research of non-small-cell lung cancer .
|
-
- HY-101571A
-
-
- HY-117407
-
|
|
Smo
|
Cancer
|
|
ALLO-2 is a potent drug-resistant Smoothened (Smo) mutant antagonist that inhibits Smo agonist Hh-Ag1.5-induced luciferase expression in TM3-Gli-Luc cells with IC50 of 6 nM .
|
-
- HY-N2099
-
|
|
Autophagy
|
Neurological Disease
|
|
Onjisaponin B is a natural product derived from Polygala tenuifolia. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin in PC-12 cells, and exbibits potential therapeutic effects on Parkinson disease and Huntington disease .
|
-
- HY-132609
-
|
|
Small Interfering RNA (siRNA)
Transthyretin (TTR)
|
Neurological Disease
|
|
Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis .
|
-
- HY-145514
-
|
|
PROTACs
|
Cancer
|
|
dTAGV-1 TFA is a potent and selective degrader of mutant FKBP12 F36V fusion proteins. dTAGV-1 TFA can induce degradation of FKBP12 F36V-Nluc in vivo .
|
-
- HY-116572A
-
|
|
APC
|
Cancer
|
|
TASIN-1 is a selective inhibitor of truncated APC gene (adenomatous polyposis coli gene) and exerts cytotoxic effects through inhibition of cholesterol biosynthesis. TASIN-1 represents a potential therapeutic strategy for prevention and intervention in CRC with mutant APC .
|
-
- HY-150245
-
|
|
Huntingtin
|
Neurological Disease
|
|
mHTT-IN-1 (Example 1) is a potent mutant huntingtin (mHTT) inhibitor. mHTT is toxic and a major cause of the inherited autosomal dominant neurodegenerative disorder, Huntington's disease (HD). mHTT-IN-1 conducts the reduction of mHTT with an EC50 value of 46 nM .
|
-
- HY-155722
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-5 (compound (-)17j) is an isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity. Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
|
-
- HY-P5968
-
|
β(25-35)KA
|
Amyloid-β
|
Neurological Disease
|
|
[Ala28]-β Amyloid(25-35) (β(25-35)KA) is an electrically neutral mutant peptide of Aβ(25-35) that accelerates the aggregation of Firefly Luciferase .
|
-
![[Ala28]-β Amyloid(25-35)](//file.medchemexpress.eu/product_pic/hy-p5968.gif)
- HY-167948
-
|
|
Others
|
Cancer
|
|
Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
|
-
- HY-79077
-
|
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.
|
-
- HY-16905
-
|
|
Src
|
Cancer
|
|
T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
|
-
- HY-139884
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
|
-
- HY-P99701
-
|
BMS-986004
|
TNF Receptor
|
Inflammation/Immunology
|
|
Letolizumab (BMS-986004) is a monoclonal antibody targeting CD40L, which is produced to express mutant IgG1 lacking effector function, including Fc binding and complement fixation. Letolizumab reduces rejection, thromboembolism and prolongs the survival time .
|
-
- HY-120911
-
|
|
Phospholipase
|
Cancer
|
|
Palmostatin B is an Acyl protein thioesterase 1 and 2 (APT-1, APT-2) inhibitor. Palmostatin B reduces cell viability in a panel of NRAS mutant melanoma cell lines. Palmostatin B inhibits Ras depalmitoylation in cells .
|
-
- HY-P10610
-
|
|
MDM-2/p53
|
Cancer
|
|
Peptide 234CM is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. Peptide 234CM induces potent cytotoxic T cell (CTL) and antitumor immune responses against mutant p53 .
|
-
- HY-164482
-
|
|
RET
|
Cancer
|
|
HG-6-63-01 is a type II RET tyrosine kinase inhibitor (TKI). HG-6-63-01 also inhibits REarranged during Transfection (RET) kinase and signaling in human thyroid cancer cell lines carrying oncogenic RET alleles. HG-6-63-01 impairs phosphorylation and signalling of RET oncogenic mutants. HG-6-63-01 blunts proliferation of RET/C634R and RET/M918T-transformed fibroblasts and of RET mutant thyroid cancer cells, which is promising for research of cancers harboring oncogenic activation of RET .
|
-
- HY-15729
-
|
CO-1686; AVL-301; CNX-419
|
EGFR
|
Cancer
|
|
Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
|
-
- HY-110392
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively .
|
-
- HY-144882
-
-
- HY-100214
-
|
|
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 .
|
-
- HY-164488
-
|
|
PAK
|
Cancer
|
|
KT D606 is an inhibitor of the PAK kinase family, with an IC50 value of 4 μM. KT D606 selectively blocks the proliferation of cancer cells transformed by oncogenic RAS mutants and can be used for research on RAS/PAK1-induced cancers .
|
-
- HY-103682
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity .
|
-
- HY-103682A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity .
|
-
- HY-126143
-
|
|
Bcr-Abl
|
Cancer
|
|
CHMFL-ABL-039 is a type II native ABL kinase and drug-resistant V299L mutant BCR-ABL inhibitor with the IC50s of 7.9 nM and 27.9 nM, respectively. CHMFL-ABL-039 is used in the research of chronic myeloid leukemia .
|
-
- HY-145411
-
|
|
Liposome
|
Endocrinology
|
|
PEG2000-C-DMG, a pegylated lipid, can be used for the preparation of Onpattro. Onpattro, a hepatically directed investigational RNAi therapeutic agent, harnesses this process to reduce the production of mutant and wild-type transthyretin by targeting the 3′ untranslated region of transthyretin mRNA .
|
-
- HY-145468
-
|
|
GPR52
|
Neurological Disease
|
|
GPR52 antagonist-1 (Compound 43) is a GPR52 antagonist with an IC50 of 0.63 μM. GPR52 antagonist-1 reduces mHTT (mutant huntingtin protein) levels by targeting GPR52 and promotes survival of mouse primary striatal neurons .
|
-
- HY-168581
-
|
|
c-Kit
|
Cancer
|
|
c-Kit-IN-8 (Compound 53) is an inhibitor for c-Kit kinase, that inhibits uKIT kinase with an IC50 > 1 μM. c-Kit-IN-8 inhibits the proliferation of cancer cell GIST430 and BaF3 wildtype and mutants with IC50 > 0.1 μM .
|
-
- HY-153346
-
|
|
Ras
ERK
Apoptosis
|
Cancer
|
|
RMC-6291 is an orally active and covalent inhibitor of KRAS G12C(ON). RMC-6291 forms a tri-complex within tumor cells between KRAS G12C(ON) and cyclophilin A (CypA). Thus, RMC-6291 prevents KRAS G12C(ON) from signaling via steric blockade of RAS effector binding. RMC-6291 inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. RMC-6291 also inhibits the proliferation of KRAS G12C mutant cells with a median IC50 of 0.11 nM .
|
-
- HY-15729A
-
|
CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide
|
EGFR
|
Cancer
|
|
Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.
|
-
- HY-16767
-
|
MK-1439
|
HIV
Reverse Transcriptase
|
Infection
|
|
Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
|
-
- HY-N0328
-
|
α-Mangostin
|
Reactive Oxygen Species
Apoptosis
Bacterial
Fungal
Virus Protease
|
Cancer
|
|
alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
|
-
- HY-19851
-
|
GS-9131
|
Reverse Transcriptase
HIV
|
Cancer
|
|
Rovafovir etalafenamide (GS-9131), a proagent of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity .
|
-
- HY-143734
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11) .
|
-
- HY-146145
-
|
|
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Metyltetraprole is a promising fungicide with EC50 values of both 0.002 ppm against sensitive wild-type and G143A mutant of Zymoseptoria tritici. Metyltetraprole is effective against QoI (quinone outside inhibitor) resistant strains. Metyltetraprole inhibits the respiratory chain via complex III .
|
-
- HY-156819
-
|
KRAS G12D inhibitor 18
|
Ras
|
Cancer
|
|
RMC-9805 (KRAS G12D inhibitor 18) is a KRAS G12D inhibitor. RMC-9805 is orally active. RMC-9805 inhibits RAS signaling to induce apoptosis in KRAS G12D mutant cancer cells .
|
-
- HY-157808
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 185 (compound IP-01) is a potent antibacterial agent. Antibacterial agent 185 inhibits filamentous temperature-sensitive mutant Z (FtsZ) polymerization and bundling by increasing GTP hydrolysis. Antibacterial agent 185 inhibits Streptococcus pneumoniae and shows narrow-spectrum activity .
|
-
- HY-159163
-
|
|
Ras
|
Cancer
|
|
KRASG12C IN-12 (compound-1) is a KRAS G12C inhibitor. KRASG12C IN-12 (compound-1) can form a ternary complex with intracellular CYPA and the activated KRAS G12C mutant .
|
-
- HY-114604
-
|
|
Others
|
Others
|
|
Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacterium tuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
|
-
- HY-168512
-
|
|
Raf
|
Cancer
|
|
BRAFV600E-IN-1 (compound 9S) is a BRAF inhibitor. BRAFV600E-IN-1 has a significant apoptosis-inducing effect in cell lines expressing mutant KRAS and cancer cells expressing BRAFV600E .
|
-
- HY-163462
-
|
|
Fungal
|
Infection
|
|
Poacic Acid is a plant-derived stilbenoid with an antifungal activity. Poacic Acid localizes to the yeast cell wall and disrupts the production and assembly of β-1,3-glucan in the fungal cell walls. Poacic Acid exhibits fungicidal activity to Saccharomyces cerevisiae and plasma membrane-compromised Candida albicans mutants .
|
-
- HY-153951S
-
|
|
Btk
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research .
|
-
- HY-12343
-
|
CID-53347902
|
Potassium Channel
|
Cardiovascular Disease
|
|
ML277 (CID-53347902) is a potent and selective activator of K(v)7.1 (KCNQ1) potassium channel activator (EC50=270 nM), rescues function of pathophysiologically important mutant channel complexes in human induced pluripotent stem cell-derived cardiomyocytes .
|
-
- HY-121736
-
|
AGI-026
|
Isocitrate Dehydrogenase (IDH)
|
Neurological Disease
|
|
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
|
-
- HY-144605
-
|
|
EGFR
PROTACs
|
Cancer
|
|
PROTAC EGFR degrader 3 is a potent PROTAC EGFR degrader. PROTAC EGFR degrader 3 shows excellent cellular activity against the H1975 and HCC827 cells with high selectively. PROTAC EGFR degrader 3 shows that the lysosome is involved in the degradation process of EGFR mutant degradation .
|
-
- HY-126362
-
|
|
Glucosidase
|
Others
|
|
ML266 is glucocerebrosidase (GCase) molecule chaperone with IC50 of 2.5 µM. ML266 binds to GCase and transports of the mutant protein to the lysosome, and resume the activity of GCase. ML266 dose not inhibit the GCase enzyme’s action. ML266 has the potential for the research of gaucher disease .
|
-
- HY-151211
-
|
|
Btk
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-16 is a dual inhibitor of BTK wild type and C481S mutant of Bruton’s tyrosine kinase (BTK) with IC50s of 5.1 and 4.1 μM. BTK-IN-16 can be used for the research of autoimmune diseases and chronic lymphocytic leukemia .
|
-
- HY-P99823
-
|
TA-46; sFGFR3
|
FGFR
|
Others
|
|
Recifercept (TA-46) is a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule. Recifercept can be used as a decoy/ligand trap to decrease the amount of fibroblast growth factors that can bind to mutant FGFR3 receptors. Recifercept can be used for the research of achondroplasia .
|
-
- HY-153609
-
|
|
Transthyretin (TTR)
Small Interfering RNA (siRNA)
|
Neurological Disease
|
|
AS-Patisiran sodium is an antisense strand of Patisiran. Patisiran is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran can be used for the research of hereditary TTR amyloidosis .
|
-
- HY-154959A
-
|
|
Others
|
Cancer
|
|
(9R,12aR)-AZD4747 is a diastereomer of AZD4747 (HY-154959). AZD4747 is a selective mutant GTPase KRAS G12C inhibitor with blood-brain barrier permeability. AZD4747 has the potential to study cancer .
|
-
- HY-113646
-
|
|
FKBP
|
Others
|
|
Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
|
-
- HY-152161
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
|
-
- HY-B0282S
-
|
ACh-d4 (chloride)
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
|
-
- HY-B0282S1
-
|
ACh-d9(chloride)
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
|
-
- HY-151523
-
|
|
Ras
|
Cancer
|
|
KRas G12R inhibitor 1 (compound 3) is a KRas G12R selective covalent inhibitor that exploits the strong nucleophilicity of mutant cysteines and binds irreversibly in the Switch II region of K-Ras. KRas G12R inhibitor 1 can be used in cancer research .
|
-
- HY-E70219
-
|
|
Others
|
Others
|
|
SpCas9 D10A Nickase is a mutant of the Cas9 protein. SpCas9 D10A Nickase retains the function of a cleavage domain of Cas9 nuclease and specifically cleaves the target single strand to form a nick. SpCas9 D10A Nickase reduces off-target effects .
|
-
- HY-160678
-
|
|
Bacterial
|
Infection
|
|
InhA-IN-7 (Compound 11) is a Triclocan (HY-B1119) derivative with inhibitory activity towards enoyl-acyl carrier protein reductase (InhA) with an IC50 of 96 nM. InhA-IN-7 inhibits proliferations of Mycobacterium tuberculosis wildtype and mutant strains with MICs ranging from 19 to 75 μM .
|
-
- HY-164513
-
|
|
Ras
Phosphodiesterase (PDE)
|
Cancer
|
|
NHTD is a KRAS-PDEδ inhibitor. NHTD targets the prenyl-binding pocket of PDEδ, altering the cellular localization of KRAS, thereby inhibiting the proliferation of KRAS-mutant cancer cells and inducing apoptosis. NHTD can be used for research on KRAS-driven non-small cell lung cancer (NSCLC) .
|
-
- HY-18213
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-9 (Compound 8) is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kinase (L858R/T790M). EGFR-IN-9 has antitumor activity .
|
-
- HY-114277A
-
|
AMG-510 racemate
|
Ras
p38 MAPK
|
Cancer
|
|
Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib (HY-114277), a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research .
|
-
- HY-147098
-
|
|
PROTACs
FKBP
|
Cancer
|
|
dTAG-47, heterobifunctional dTAG molecule, targets mutant FKBP12 (FKBP12 F36V). FKBP12 F36V serves as a degradation tag (dTAG) and is fused to a protein of interest. dTAG-47 can be used for the research of basal-like breast cancers (BBC) .
|
-
- HY-W102456
-
|
L-4-Acetylphenylalanine
|
Others
|
Others
|
|
H-Phe(4-Ac)-OH is a keto-containing amino acid, which can be conversed from α-keto acids containing acetyl. H-Phe(4-Ac)-OH can be incorporated at the amber position to afford the mutant Z domain protein .
|
-
- HY-W127705
-
|
|
Fluorescent Dye
|
Others
|
|
Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes .
|
-
- HY-122958
-
|
|
α-synuclein
|
Neurological Disease
|
|
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research .
|
-
- HY-149928
-
|
|
HIV
|
Infection
|
|
NNRTIs-IN-1 is a potent non-nucleoside reverse transcriptase inhibitor featuring significantly anti-resistance efficacy. NNRTIs-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRTIs-IN-1 displays favorable pharmacokinetic properties .
|
-
- HY-155720
-
|
|
Bacterial
|
Infection
|
|
Mtb-IN-4 (compound 17h) is a nontoxic isoxazole, with anti-Mycobacterium tuberculosis (Mtb) activity (IC50=0.70 μM). Mtb-IN-4 inhibits Mtb respiration and biofilm formation in macrophage, and enhances antibiotic isoniazid (INH) inhibition against INH-resistant Mtb mutant .
|
-
- HY-B0282R
-
|
|
nAChR
Calcium Channel
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Acetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs) . Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro .
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-
- HY-163522
-
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Influenza Virus
|
Infection
|
|
Neuraminidase-IN-20 (Compound 5i) is a potent inhibitor of mutant neuraminidase (NA) (H5N1-H274Y) (IC50= 0.44 μM).Neuraminidase-IN-20 binds to the 430 cavity site of NA and disrupts the enzymatic activity of NA .
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-
- HY-101494
-
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LY3214996
|
ERK
|
Cancer
|
|
Temuterkib (LY3214996) is a highly selective inhibitor of ERK1 and ERK2, with IC50 of 5 nM for both enzymes in biochemical assays. Temuterkib potently inhibits cellular p-RSK1 in BRAF and RAS mutant cancer cell lines. Temuterkib shows potent antitumor activities in cancer models with MAPK pathway alterations.
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-
- HY-123921
-
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PROTACs
EGFR
|
Cancer
|
|
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively .
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-
- HY-135892
-
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MAP4K
|
Inflammation/Immunology
|
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively .
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-
- HY-114043
-
|
|
Glucosidase
|
Metabolic Disease
|
|
NCGC00092410 is a potent, selective, and nonsugar glucocerebrosidase (GC) inhibitor, with an IC50 of 31 nM. NCGC00092410 shows no activity against the related hydrolases at concentrations up to 77 μM. NCGC00092410, a GC chaperone, and increases the activity and lysosomal localization of glucocerebrosidase in mutant cell lines. NCGC00092410 can be used for the research of Gaucher disease .
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-
- HY-139047
-
|
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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 .
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-
- HY-110094
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors .
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-
- HY-151999
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 65 is a potent and covalent KRAS G12C inhibitor that traps KRAS G12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer .
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-
- HY-156529
-
|
|
Ras
|
Cancer
|
|
pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively .
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-
- HY-N12390
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Alternaphenol B2 is a selective IDH1 inhibitor from the coral-derived fungus Parengyodontium album SCSIO SX7W11. Alternaphenol B2 shows inhibitory activity against isocitrate dehydrogenase mutant R132H (IDH1m), with IC50 values of 41.9 μM .
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-
- HY-157287
-
|
|
Others
|
Inflammation/Immunology
|
|
(S)-Phe-A110/B319 is a selective binde that has 20-fold higher affinity towards the H1047R mutant of p110α in the p110α/p85α PI3K complex .
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-
- HY-160142
-
|
|
Btk
|
Cancer
|
|
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .
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-
- HY-160084
-
|
|
Others
|
Cancer
|
|
2′-Deoxy-4′-thiocytidine (T-dCyd) is a novel epigenetic agent. 2′-Deoxy-4′-thiocytidine administrations led to a significant p21 increase. 2′-Deoxy-4′-thiocytidine can eradicate of tumor cells in the double-mutant xenografts .
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-
- HY-123766
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-W740378
-
|
AFN-941
|
Others
|
Others
|
|
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
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-
- HY-14780
-
|
NXL 101
|
Antibiotic
Topoisomerase
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
Viquidacin (NXL 101) is an antibiotic with inhibitory activity against topoisomerase IV and DNA gyrase. Viquidacin exhibits antibacterial activity against gram positive bacterial by inhibiting the supercoiling, decatenation and relaxation in strains Staphylococcus aureus and Escherichia coli in micromolar levels. Viquidacin inhibits S. aureus wildtype and mutants with MIC of 2-128 mg/L .
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-
- HY-B1907R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Rifamycin (sodium) (Standard) is the analytical standard of Rifamycin (sodium). This product is intended for research and analytical applications. Rifamycin sodium (Rifamycin SV monosodium) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin sodium displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria .
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-
- HY-125540
-
|
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Saussureamine C shows gastroprotective effect on acidified ethanol-induced gastric mucosal lesions in rats. Saussureamine C inhibits H274Y and N294S mutants and can be used for research of influenza virus infection. Saussureamine C can be isolated from the dried roots of Saussurea lappa Clarke .
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-
- HY-10638
-
|
|
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 .
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-
- HY-168055
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation .
|
-
- HY-147183
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183A
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183B
-
|
|
EGFR
|
Cancer
|
|
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
|
-
- HY-126287
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
JND4135 is a Type II TRK inhibitor with IC50 values of 2.79, 3.19, and 3.01 nM against TRKA, TRKB, TRKC, respectively. JND4135 can overcome resistance from TRK xDFG and other mutant forms in the BaF3 stable model, inhibiting phosphorylation of both WT and xDFG mutant TRKs, along with their downstream signaling molecules. JND4135 can induce G0/G1 phase arrest and apoptosis in BaF3–CD74-TRKA-G667C cells. JND4135 shows tumor growth inhibition activity in the BaF3-CD74-TRKA-G667C mouse xenograft model .
|
-
- HY-18767
-
|
AG-120
|
Isocitrate Dehydrogenase (IDH)
|
Metabolic Disease
Cancer
|
|
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity .
|
-
- HY-128784
-
|
|
MDM-2/p53
Reactive Oxygen Species
|
Cancer
|
|
PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels .
|
-
- HY-16906
-
|
|
Src
|
Cancer
|
|
T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
|
-
- HY-130492
-
ARCC-4
1 Publications Verification
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARCC-4 is a low-nanomolar Androgen Receptor (AR) degrader based on PROTAC, with a DC50 of 5?nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy .
|
-
- HY-136938
-
NEO2734
1 Publications Verification
EP31670
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains . NEO2734 is active in SPOP mutant and wild-type prostate cancer .
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-122753
-
|
|
MDM-2/p53
|
Cancer
|
|
SLMP53-1 is a wild-type and mutant p53 reactivator with promising antitumor activity. SLMP53-1 mediates the reprograming of glucose metabolism in cancer cells. SLMP53-1 depletes angiogenesis, decreasing endothelial cell tube formation and vascular endothelial growth factor (VEGF) expression levels .
|
-
- HY-15772S1
-
|
AZD-9291-13C,d3; Mereletinib-13C,d3
|
EGFR
|
Cancer
|
|
Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
|
-
- HY-149318
-
|
|
Others
|
Others
|
|
VRT-534 targets connexin 26 (Cx26). Vrt-534 exhibits dose-responsive binding to recombinant WT Cx26 and mutant Cx26 K188N with EC50 value of 19 μM and 5 μM, respectively. Vrt-534 can be used in research related to hearing impairment .
|
-
- HY-155285
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis .
|
-
- HY-160426
-
|
|
Glucosidase
|
Neurological Disease
|
|
Gcase activator 3 (compound 9Q) is a glucosidase (Glucosidase, GCase) activator that can partially stabilize GCase and increase its activity. Gcase activator 3 reduces mutant GCase protein misfolding and degradation in fibroblasts and dopaminergic midbrain neurons. Gcase activator 3 can be used in the study of Parkinson's disease (PD) and related synucleinopathies .
|
-
- HY-158039
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors .
|
-
- HY-164389
-
|
|
Ras
|
Cancer
|
|
SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC50 of 26.6-47.6 μM .
|
-
- HY-169903
-
|
|
Apoptosis
|
Cancer
|
|
SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER+ and therapy-resistant (TR)-ER+ breast cancer .
|
-
- HY-135864
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A .
|
-
- HY-135866
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C .
|
-
- HY-135865
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B .
|
-
- HY-141450
-
|
|
β-catenin
|
Cancer
|
|
NRX-103095 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-103095 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 163 nM .
|
-
- HY-132979
-
|
|
Ras
|
Cancer
|
|
KRAS G12C inhibitor 18 is a potent and orally active KRAS G12C inhibitor. Anti-tumor activities .
|
-
- HY-142517
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively .
|
-
- HY-142519
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511) .
|
-
- HY-148234
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
M4K2234 (compound 26b) is an ALK2 inhibitor. M4K2234 inhibits ALK2 and ALK5 with IC50s of 5 and 2144 nM, respectively. M4K2234 can be used as a chemical probe for ALK1 and ALK2 protein kinases. M4K2234 can be used for the research of cancer .
|
-
- HY-168112
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-127 is an ATP-competitive EGFR inhibitor with IC50s of 136.3 nM and 161. 2 nM for EGFR del19 and EGFR del19/T790M/C797S, respectively. EGFR-IN-127 has the potential for the study of non-small-cell lung cancer (NSCLC) .
|
-
- HY-17040
-
|
TMC114; UIC-94017
|
HIV
HIV Protease
|
Infection
Inflammation/Immunology
|
|
Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity .
|
-
- HY-15772
-
|
AZD-9291; Mereletinib
|
EGFR
|
Cancer
|
|
Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15772A
-
|
AZD-9291 mesylate; Mereletinib mesylate
|
EGFR
|
Cancer
|
|
Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-100213
-
EAI045
1 Publications Verification
|
EGFR
|
Cancer
|
|
EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFR L858R, EGFR T790M and EGFR L858R/T790M at 10 μM ATP, respectively.
|
-
- HY-112601
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively . Anticancer activity .
|
-
- HY-134653
-
|
|
Others
|
Cancer
|
|
5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression .
|
-
- HY-100028
-
AT-130
1 Publications Verification
|
HBV
DNA/RNA Synthesis
|
Infection
Cancer
|
|
AT-130, a phenylpropenamide derivative, is a potent hepatitis B virus (HBV) replication non-nucleoside inhibitor. AT-130 inhibits the viral DNA synthesis with an EC50 of 0.13 μM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells .
|
-
- HY-141523
-
|
RMC-4630; SHP2-IN-7
|
SHP2
Phosphatase
|
Cancer
|
|
Vociprotafib (RMC-4630) is an orally active, selective and potent phosphatase SHP2 inhibitor, which blocks activation of the RAS-RAF-MEK-ERK signaling pathway with antitumor activity. Vociprotafib accelerates the time to, and increases the magnitude of, tumor regressions in Osimertinib (HY-15772)-sensitive EGFR-mutant tumors of mice .
|
-
- HY-147702
-
|
|
Others
|
Infection
Neurological Disease
|
|
BB 0305179 (compound 59) is a potent anti-prion agent, with an IC50 of 4.7 μM. BB 0305179 inhibits the toxicity of a specific PrP mutant carrying a deletion in the hydrophobic domain . BB 0305179 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-12847
-
|
|
Raf
Src
Apoptosis
|
Cancer
|
|
CCT241161 is an orally active pan-RAF inhibitor with IC50s of 3, 6, 10, 15 and 30 nM for LCK, CRAF, SRC, V600E-BRAF and BRAF, respectively. CCT241161 shows good activity to in BRAF and NRAS mutant melanomas. CCT241161 also exhibits anticancer cell proliferative activity .
|
-
- HY-138301
-
|
DS37262926
|
β-catenin
|
Cancer
|
|
Miclxin (DS37262926) is a potent inhibitor of mutant β-catenin, involving in Wnt signaling pathway. Miclxin induces β-catenin-dependent apoptosis, leads to severe mitochondrial damage with the loss of mitochondrial membrane. Miclxin kills tumor via targeting to MIC60, a major components of the mitochondrial contact site and cristae organizing system (MICOS) complex .
|
-
- HY-15103
-
|
|
Androgen Receptor
Thyroid Hormone Receptor
|
Cancer
|
|
AH3960 (compound 16c) is an antagonist of androgen receptor. AH3960 binds wild as well as T877 mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1) .
|
-
- HY-18690S
-
|
AG-221-d6
|
Isotope-Labeled Compounds
|
Others
|
|
Enasidenib-d6 (AG-221-d6)is the deuterium labeledEnasidenib(HY-18690) . 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 .
|
-
- HY-123985
-
|
|
Others
|
Others
|
|
MFN2 agonist-1 (B-A/l) potently stimulates mitochondrial fusion in mitofusin 2 (MFN2)-deficient cells. MFN2 agonist-1 reverses mitochondrial “clumping” (formation of static mitochondrial aggregates) and restores mitochondrial motility in cultured mouse neurons expressing the CMT2A mutant MFN2 T105M.
|
-
- HY-162265
-
|
|
Apoptosis
|
Cancer
|
|
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells, that can be used for the research of AML .
|
-
- HY-117187
-
|
|
CFTR
|
Others
|
|
Corr4A is a chemical corrector, which can be used for cystic fibrosis. Corr4A interacts directly with the cystic fibrosis transmembrane conductance regulator (CFTR) or affects indirectly its folding process. Corr4A increases the expression of CFTR ΔF508 on the cell surface, thereby improving its transport to the plasma membrane and increasing the stability of the rescued mutant protein .
|
-
- HY-119082A
-
|
|
Others
|
Others
|
|
VU0029767 is an allosteric enhancer of the M1 muscarinic receptor with the activity to modulate M1 receptor activity. VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
|
-
- HY-W050122
-
|
|
Others
|
Neurological Disease
|
|
S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .
|
-
- HY-164393
-
|
|
JAK
Bcr-Abl
Apoptosis
|
Cancer
|
|
ON044580, an α-benzoyl styryl benzyl sulfide, is a potent and non-ATP-competitive JAK2 kinase inhibitor with IC50s of 1.23 μM, 1.09 μM for WT and V617F mutant JAK2, respectively. ON044580 inhibits the JAK2 kinase activity either by binding to the STAT-5 binding domain of JAK2 or by binding to an allosteric site. ON044580 exerts its antiproliferative effect in JAK2 V617F-positive leukemic cells. ON044580 effectively induces apoptosis of Imatinib (HY-15463)-resistant chronic myelogenous leukemia (CML) cells. ON044580 also inhibits both WT and T315I mutant forms of the BCR-ABL kinase. ON044580 has the potential for myeloproliferative disorders typified by aberrant JAK/STAT signaling .
|
-
- HY-13912
-
|
|
Wnt
Porcupine
Casein Kinase
|
Cancer
|
|
IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ .
|
-
- HY-15801
-
|
|
Anaplastic lymphoma kinase (ALK)
EGFR
|
Cancer
|
|
HG-14-10-04 is a potent ALK and mutant EGFR inhibitor with IC50s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFR LR/TM, EGFR 19del/TM/CS and EGFR LR/TM/CS, respectively. HG-14-10-04 can be used to research anticancer .
|
-
- HY-112301
-
|
BLU-667
|
RET
|
Cancer
|
|
Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
|
-
- HY-N6790
-
-
- HY-128350A
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FGTI-2734 mesylate is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively. FGTI-2734 mesylate can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
|
-
- HY-139150
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity .
|
-
- HY-147942
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer .
|
-
- HY-121845
-
|
|
Others
|
Metabolic Disease
|
|
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity .
|
-
- HY-114365
-
|
UDP-N-acetyl-D-galactosamine disodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
UDP-GalNAc (UDP-N-acetyl-D-galactosamine) disodium is a sugar nucleotide and a substrate of EpsC115. EpsC115 is an exopolymeric substances (EPS) N-terminal deletion mutant with the residue 1-115 deletion. UDP-GalNAc UDP-GalNAc is the donor substrate of many N-acetylgalactosaminyltransferases, enzymes which transfer GalNAc from the nucleotide sugar to a saccharide or peptide acceptor .
|
-
- HY-15292
-
S107
1 Publications Verification
|
Others
|
Cardiovascular Disease
|
|
S107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca 2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold .
|
-
- HY-155537
-
|
|
EGFR
|
Cancer
|
|
YK-029A is an orally active inhibitor of mutant EGFR，targeting to both the T790M mutations (EGFR T790M) and exon 20 insertion of EGFR (EGFRex20ins). YK-029A exhibits significant antitumor activity，and results tumor regression in EGFRex20ins-driven PDX models .
|
-
- HY-146223A
-
|
|
Others
|
Cancer
|
|
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 (Compound 21) is a highly potent, selective, covalent and allosteric inhibitor of the mutant GTPase KRAS G12C. AZD4625 has high oral bioavailability .
|
-
- HY-149607
-
|
|
SHP2
|
Cancer
|
|
SHP2-IN-22 is SHP2 allosteric inhibitor with an IC50 value of 17.7 nM. SHP2-IN-22 inhibits the proliferation, migration, and invasion of MIA PaCa-2 pancreatic cancer cells. SHP2-IN-22 can be used for Kirsten rat sarcoma viral oncogene (KRAS) mutant cancer research .
|
-
- HY-163110
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
NNRT-IN-2 (compound 7w) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains. NNRT-IN-2 inhibits HIV-1 reverse transcriptase with an EC50 of 22 nM. NNRT-IN-2 is insensitive to CYP and hERG and has good safety and pharmacokinetic characteristics .
|
-
- HY-162265A
-
|
|
Apoptosis
|
Cancer
|
|
UCM-13369 (Compound 4b) is a NPM1 inhibitor. UCM-13369 downregulates the pathway associated with mutant NPM1 C+, and specifically recognizes the C-end DNA-binding domain of NPM1 C+. UCM-13369 induces apoptosis in AML cell lines and primary cells. UCM-13369 can be used for leukemia research .
|
-
- HY-14829A
-
|
D-Isofagomine hydrochloride; Isofagomine hydrochloride
|
Glucosidase
|
Metabolic Disease
|
|
Afegostat hydrochloride (D-Isofagomine hydrochloride) is a potent β-galactosidase inhibitor with activity ameliorating GM1-gangliosidosis and Morquio B disease-associated mutations. Afegostat hydrochloride is able to induce the maturation of mutant β-galactosidase in fibroblasts from patients with GM1-gangliosidosis. Afegostat hydrochloride also promotes the reduction of keratin sulfate and oligosaccharide load in patient cells .
|
-
- HY-153663
-
|
|
Ras
|
Cancer
|
|
TH-Z827 is a mutant selective KRAS(G12D) inhibitor with an IC50 of 2.4 μM. TH-Z827 does not bind KRAS(WT) or KRAS(G12C). TH-Z827 blocked the KRAS(G12D)-CRAF interaction with an IC50 value of 42 μM .
|
-
- HY-12026
-
|
|
EGFR
|
Cancer
|
|
WZ4002 is a mutant selective EGFR inhibitor with IC50s of 2, 8, 3 and 2 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750 and EGFR E746_A750/T790M, respectively.
|
-
- HY-10206
-
|
MP470; HPK 56
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
Apoptosis
|
Cancer
|
|
Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
- HY-18161
-
|
|
FLT3
Aurora Kinase
|
Cancer
|
|
CCT241736 is a potent and orally bioavailable dual FLT3 and Aurora kinase inhibitor, which inhibits Aurora kinases (Aurora-A Kd, 7.5 nM, IC50, 38 nM; Aurora-B Kd, 48 nM), FLT3 kinase (Kd, 6.2 nM), and FLT3 mutants including FLT3-ITD (Kd, 38 nM) and FLT3(D835Y) (Kd, 14 nM).
|
-
- HY-117273
-
|
|
Raf
Autophagy
|
Cancer
|
|
AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity .
|
-
- HY-130608
-
|
|
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 .
|
-
- HY-10206A
-
|
MP470 hydrochloride; HPK 56 hydrochloride
|
c-Kit
PDGFR
RAD51
FLT3
c-Met/HGFR
RET
|
Cancer
|
|
Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair . Antineoplastic activity .
|
-
- HY-142452
-
|
|
Raf
|
Cancer
|
|
Pan-RAF kinase inhibitor 1 is a potent inhibitor of Pan-RAF kinase. Pan-RAF kinase inhibitor 1 regulates MAPK signaling by inhibiting RAF kinase, thereby exerting an effect on the proliferation of RAS-mutant tumor cells. Pan-RAF kinase inhibitor 1 has the potential for the research of cancer diseases (extracted from patent WO2021110141A1, compound 16B) .
|
-
- HY-144053
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .
|
-
- HY-136780
-
|
|
Amyloid-β
|
Neurological Disease
|
|
SEN177 is a potent glutaminyl cyclase (QPCT) inhibitor with an IC50 of 0.013μM for glutaminyl-peptide cyclotransferase-like (QPCTL). SEN177 has a Ki of 20 nM for human glutaminyl cyclase (hQC). SEN177 greatly reduces the early stages of mutant HTT oligomerisation and reduces the percentage of neurons with Q80 aggregates. SEN177 has the potential for Huntington’s disease research .
|
-
- HY-147941
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9427 is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer .
|
-
- HY-153386
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
CPD-1224 is an orally effective ALK inhibitor, a derivative of an ALK inhibitor that connects to the cereblon ligand. CPD-1224 targets the EML4-ALK oncogenic fusion protein and degrades both ALK and the mutant forms L1196M/G1202R. CPD-1224 can slow down tumor growth .
|
-
- HY-161633
-
|
|
PROTACs
EGFR
FAK
|
Cancer
|
|
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
|
-
- HY-158991
-
|
|
CFTR
|
Inflammation/Immunology
|
|
I1421 is an activator of the cystic fibrosis transmembrane conductance regulator (CFTR) with an EC50 of 64 nM for WT CFTR currents. I1421 also allosterically activates multiple mutants causing cystic fibrosis (CF) with good in vivo potency, with an oral bioavailability of 60% in mice corresponding to a half-life of 75 min. I1421 synergizes with Elexacaftor (HY-111772) to enhance CFTR currents .
|
-
- HY-125147
-
|
|
NAMPT
|
Cancer
|
|
A-1293201 is a substrate-independent NAMPT inhibitor with antitumor activity. A-1293201 effectively reduces the total cellular NAD +/NADH (NADt) level, subsequently leading to ATP depletion and cancer cell death. In addition, A-1293201 can effectively overcome the acquired resistance mechanism of the NAMPT Y18 mutant to CHS-828 (HY-10079) .
|
-
- HY-10358
-
|
MK-2206 (2HCl)
|
Organoid
Akt
Autophagy
Apoptosis
|
Cancer
|
|
MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
|
-
- HY-15244
-
|
BYL-719
|
PI3K
|
Cancer
|
|
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity .
|
-
- HY-137516
-
LC-2
1 Publications Verification
|
PROTACs
Ras
|
Cancer
|
|
LC-2 is a potent and first-in-class von Hippel-Lindau-based PROTAC capable of degrading endogenous KRAS G12C, with DC50s between 0.25 and 0.76 μM . LC-2 covalently binds KRAS G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS G12C degradation leading to suppression of MAPK signaling in both homozygous and heterozygous KRAS G12C cell lines .
|
-
- HY-141448
-
|
|
β-catenin
|
Cancer
|
|
NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 µM and a Kd of 54.8 nM .
|
-
- HY-141449
-
|
|
Molecular Glues
β-catenin
|
Cancer
|
|
NRX-103094 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCF β-TrCP. NRX-103094 enhances the binding of pSer33/Ser37 β-catenin peptide for β-TrCP with an EC50 of 62 nM and a Kd of 0.6 nM .
|
-
- HY-132842A
-
|
(S)-DZD9008
|
EGFR
Btk
|
Cancer
|
|
(S)-Sunvozertinib ((S)-DZD9008), the S-enantiomer of Sunvozertinib, shows inhibitory activity against EGFR exon 20 NPH and ASV insertions, EGFR L858R/T790M mutation and Her2 exon20 YVMA insertion (IC50=51.2 nM, 51.9 nM, 1 nM, and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK .
|
-
- HY-142512
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively .
|
-
- HY-152539
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-54 is a potent HIV-1 inhibitor. HIV-1 inhibitor-54 has anti-HIV activity in MT-4 cells against WT HIV-1 (strain IIIB) with an EC50 value of 0.032 μM. HIV-1 inhibitor-54 can be used for the research of virus infection .
|
-
- HY-12001
-
|
|
EGFR
|
Cancer
|
|
WZ3146 is a mutant selective EGFR inhibitor with IC50s of
2, 2, 5, 14 and 66 nM for EGFR L858R, EGFR L858R/T790M, EGFR E746_A750, EGFR E746_A750/T790M and EGFR, respectively.
|
-
- HY-19834
-
|
GDC-0853
|
Btk
|
Cancer
|
|
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research .
|
-
- HY-14174
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
MRK-560 is an orally active, brain barrier-penetrating γ-Secretase inhibitor, can potently reduce Aβ peptide in rat brain and cerebrospinal fluid. MRK-560 also decreases mutant NOTCH1 processing by selectively inhibiting PSEN1. MRK-560 can be used in studies of Alzheimer's disease and T-cell acute lymphoblastic leukaemia (T-ALL) .
|
-
- HY-128350
-
|
|
Farnesyl Transferase
|
Cancer
|
|
FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors .
|
-
- HY-128862
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers .
|
-
- HY-114358
-
|
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).
|
-
- HY-15772S
-
|
AZD-9291-d6; Mereletinib-d6
|
EGFR
|
Cancer
|
|
Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
|
-
- HY-19985A
-
|
|
EGFR
|
Cancer
|
|
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .
|
-
- HY-143218
-
TPE-MI
2 Publications Verification
Tetraphenylethene maleimide
|
Huntingtin
Parasite
|
Neurological Disease
|
|
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
|
-
- HY-139995
-
|
|
Others
|
Others
|
|
Spermine precursor-1 (Compound 1) is a redox-sensitive spermine precursor for the potential research of snyder robinson syndrome. Spermine precursor-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-146078
-
|
|
Bacterial
|
Infection
|
|
Antimicrobial agent-1 (compound 6C) possesses potent activity against TolC mutant E. coli with an MIC value of 2 μg/mL. Antimicrobial agent-1 and Colistin exhibit synergistic activity against Gram-negative bacteria. Antimicrobial agent-1 has no cytotoxicity on mammalian cell lines, with MICs > 128 μg/mL in Caco-2 and Vero cell lines .
|
-
- HY-147841
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 inhibitor-41 (Compound B23) is an orally active non-nucleoside HIV-1 reverse transcriptase inhibitor with EC50 values of 20.8 nM and 50 nM against HIV-1 WT and mutant E138K strain, respectively. HIV-1 inhibitor-41 shows low hERG, no apparent CYP enzymatic inhibition and no acute toxicity .
|
-
- HY-152160
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1 invistor-50 is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that targets HIV-1 reverse transcriptase (RT) (IC50=50 nM). HIV-1 inhibitor-50 shows significant antiviral activity, with EC50s of 2.22-53.3nM against HIV-1 IIIB and its mutant strains .
|
-
- HY-N0328R
-
|
α-Mangostin (Standard)
|
Fungal
Reactive Oxygen Species
Bacterial
Apoptosis
Virus Protease
|
Cancer
|
|
alpha-Mangostin (Standard) is the analytical standard of alpha-Mangostin. This product is intended for research and analytical applications. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
|
-
- HY-P10438
-
|
|
Raf
|
Cancer
|
|
Tat-braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by Tat-braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
|
-
- HY-161632
-
|
|
PROTACs
EGFR
FAK
|
Cancer
|
|
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
|
-
- HY-158409
-
|
|
Molecular Glues
Ras
Cyclophilin
|
Cancer
|
|
Pan-rasin-2 (compound 6A) is a molecular glues that targets RAS. Pan-rasin-2 has significant inhibitory activity on cell proliferation of RAS mutant cell lines. Pan-rasin-2 can form ternary complexes with cyclophilin A (CYPA) and RAS (ON) proteins and the formation of ternary complexes can block the binding of RAF downstream of RAS, which has anti-tumor effects .
|
-
- HY-161895
-
|
|
CFTR
|
Others
|
|
CFTR corrector 14 (Compound SVQ26) is a class 3 corrector for cystic fibrosis transmembrane conductance regulator (CFTR), that promotes the CFTR activity (EC50 of 3.08 μM with presence of C1 class corrector VX-809). CFTR corrector 14 regulates the mutant-caused misfolding and impaired function of the CFTR protein. CFTR corrector 14 can be used in research about cystic fibrosis .
|
-
- HY-119082
-
|
|
Others
|
Others
|
|
(E/Z)-VU0029767 is an allosteric enhancer of M1 muscarinic receptors with the activity to modulate M1 receptor activity. (E/Z)-VU0029767 can enhance M1 receptor activity by increasing agonist affinity, but exhibits different properties from other compounds under different experimental conditions, such as effects on mutant M1 receptors and effects on downstream signaling pathways.
|
-
- HY-10683
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-130258
-
|
|
Atg8/LC3
ATTECs
Autophagy
|
Neurological Disease
|
|
LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons .
|
-
- HY-130259
-
|
|
Atg8/LC3
ATTECs
Autophagy
|
Neurological Disease
|
|
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons .
|
-
- HY-130426
-
|
Mal-PEG3-acid
|
ADC Linker
PROTAC Linkers
|
Cancer
|
|
Maleimido-tri(ethylene glycol)-propionic acid is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Maleimido-tri(ethylene glycol)-propionic acid is used for the preparation of neolymphostin-based ADC precursors for site-specific cysteine mutant trastuzumab-A114C conjugation . Maleimido-tri(ethylene glycol)-propionic acid also can be used as a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-146112
-
|
|
IRAK
|
Cancer
|
|
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .
|
-
- HY-147941A
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS9427 TFA is a potent PROTAC EGFR degrader with Kds of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 TFA selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 TFA potently inhibits the proliferation of NSCLC cells. MS9427 TFA can be used for researching anticancer .
|
-
- HY-111517
-
|
|
Apoptosis
SF3B1
|
Cancer
|
|
H3B-8800 is a potent and orally active SF3B splicing modulator. H3B-8800 direct interaction with the SF3b complex and shows anti-cancer activity. H3B-8800 has the potential for the research of acute myeloid leukemia (AML) with SF3B1 mutant .
|
-
- HY-P10436
-
|
|
Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
|
-
- HY-15772AR
-
|
|
EGFR
|
Cancer
|
|
Osimertinib (mesylate) (Standard) is the analytical standard of Osimertinib (mesylate). This product is intended for research and analytical applications. Osimertinib mesylate (AZD9291 mesylate) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15772R
-
|
|
EGFR
|
Cancer
|
|
Osimertinib (Standard) is the analytical standard of Osimertinib. This product is intended for research and analytical applications. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer .
|
-
- HY-15164
-
|
BPI-2009H
|
EGFR
|
Cancer
|
|
Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-15164A
-
|
BPI-2009
|
EGFR
|
Cancer
|
|
Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-10574S
-
|
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
|
-
- HY-139590
-
|
BOS-172738; DS-5010
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
|
-
- HY-10035
-
TTA-P2
2 Publications Verification
T-Type calcium channel inhibitor
|
Calcium Channel
|
Neurological Disease
|
|
TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
|
-
- HY-146746
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-19 is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). HIV-1 inhibitor-19 maintains its inhibitory activity against L100I, K103N and V106A/ F227L mutant strains with EC50s of 7.3 nM, 9.2 nM and 21.0 nM, respectively[1].
|
-
- HY-146113
-
|
|
IRAK
|
Cancer
|
|
IRAK4-IN-15 (compound 35) is a potent and selective IRAK4 inhibitor with an IC50 of 0.002 µM. IRAK4-IN-15 shows good human PK predictions with low intrinsic clearance. IRAK4-IN-15 shows great synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib. .
|
-
- HY-123418
-
|
|
Phosphoglycerate Dehydrogenase (PHGDH)
|
Cancer
|
|
PKUMDL-WQ-2201 is a PHGDH non-NAD+-competing allosteric inhibitor (IC50=35.7 μM). PKUMDL-WQ-2201 also inhibits PHGDH mutants with IC50s of 69 μM (T59A) and >300 μM (T56AK57A), respectively. PKUMDL-WQ-2201 inhibits de novo serine synthesis in cancer cells, and reduces tumor growth .
|
-
- HY-164487
-
|
|
Others
|
Cancer
|
|
JBJ-08-178-01 is a mutant-selective tyrosine kinase inhibitor against human epidermal growth factor receptor 2 (HER2) with an antitumoral activity. JBJ-08-178-01 reduces both the kinase activity and protein levels of HER2 by inducing proteasomal degradation of the receptor in lung cancer. JBJ-08-178-01 is promising for research of non-small-cell lung cancer .
|
-
- HY-168069
-
|
|
Parasite
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
|
-
- HY-N12109
-
|
|
Others
|
Others
|
|
Albizziin is an amino acid analog with activity as a competitive inhibitor of asparagine synthetase. Albizziin has been used to isolate Chinese hamster ovary cell mutants with altered levels of the target enzyme. Several mutational classes of albizziin can be distinguished based on cross-resistance to β-aspartic hydroxamic acid. Studies on asparagine synthetase have shown that resistance to albizziin may be associated with altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification .
|
-
- HY-101119
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models .
|
-
- HY-112301R
-
|
|
RET
|
Cancer
|
|
Pralsetinib (Standard) is the analytical standard of Pralsetinib. This product is intended for research and analytical applications. Pralsetinib (BLU-667) is a highly potent, selective RET inhibitor. Pralsetinib (BLU-667) inhibits WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion with IC50s of 0.4, 0.3, 0.4, 0.4, and 0.4 nM, respectively .
|
-
- HY-17598
-
|
|
Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
|
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
|
-
- HY-18705
-
|
|
Apoptosis
Reactive Oxygen Species
Caspase
Bcl-2 Family
Mitochondrial Metabolism
|
Endocrinology
|
|
Azoramide is a potent, orally active small-molecule modulator of the unfolded protein response (UPR). Azoramide improves ER protein folding and elevates ER chaperone capacity, which together protects cells against ER stress. Azoramide alleviates PLA2G6 mutant-induced ER stress through modulating unfolded protein response, and enhances the CERB signaling to rescue mitochondrial function, thereby preventing apoptosis of DA neurons. Azoramide has antidiabetic activity .
|
-
- HY-101561
-
|
BLU-285
|
c-Kit
PDGFR
|
Cancer
|
|
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
|
-
- HY-112585
-
|
TMC114-d9; UIC-94017-d9
|
HIV
HIV Protease
|
Infection
Inflammation/Immunology
|
|
Darunavir-d9 (TMC114-d9) is the deuterium labeled Darunavir. Darunavir (TMC114), an orally active next generation HIV protease inhibitor, has a similar antiviral activity against the mutant and the wild-type viruses. Darunavir (TMC114) is potent against laboratory HIV-1 strains and primary clinical isolates (IC50 = 0.003 μM; IC90 = 0.009 μM) with minimal cytotoxicity .
|
-
- HY-112929B
-
|
|
Phosphatase
|
Cancer
|
|
(1S,2S,3R)-DT-061 is an enantiomer of DT-061 (HY-112929). DT-061 is an orally active activator of protein phosphatase 2A (PP2A). (1S,2S,3R)-DT-061 can be used as a negative control in the research of KRAS-mutant and MYC-driven lung cancer tumorigenesis .
|
-
- HY-107779
-
|
|
Raf
|
Cancer
|
|
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
|
-
- HY-131003
-
|
DS-6051b; AB-106; IBI-344
|
ROS Kinase
|
Cancer
|
|
Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .
|
-
- HY-110088
-
|
|
MDM-2/p53
|
Cancer
|
|
SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC) .
|
-
- HY-139590A
-
|
BOS-172738 hemiadipate; DS-5010 hemiadipate
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity .
|
-
- HY-144069
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Pan-Trk-IN-3 (Compound 11g) is a potent inhibitor of pan-Trk and their drug-resistant mutants with IC50 values of 2, 3, 2, 21, 26, 5, 7 and 6 nM against TrkA, TrkB, TrkC, TrkA G595R, TrkA G667C, TrkA G667S, TrkA F589L and TrkC G623R, respectively. Pan-Trk-IN-3 displays excellent antitumor activity and induces apoptosis .
|
-
- HY-134050
-
|
Apt-1
|
RIP kinase
Autophagy
Apoptosis
Beclin1
Necroptosis
|
Inflammation/Immunology
|
|
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin .
|
-
- HY-149306
-
|
|
Histone Acetyltransferase
MDM-2/p53
|
Cancer
|
|
MS78 is an acetylation targeting chimera (AceTAC) that acetylates the p53 tumor suppressor protein. MS78 recruits histone acetyltransferase p300/CBP to acetylate the p53Y220C mutant. MS78 upregulates TRAIL apoptotic genes and downregulates DNA damage response pathways. MS78 contains a CBP/p300 binder, a p53Y220C binder and a linker .
|
-
- HY-149555
-
|
|
Eukaryotic Initiation Factor (eIF)
|
Neurological Disease
|
|
DNL343 is a potent, selective, orally active and brain-penetrant activator of eukaryotic initiation factor eIF2B. DNL343 inhibits the activity of the integrated stress response (ISR) in the central nervous system (CNS) and reverses neurodegeneration and neuroinflammation. DNL343 also prevents motor dysfunction and premature death in eIF2B loss-of-function (LOF) mutant mice. DNL343 can be used in the study of neurodegenerative diseases .
|
-
- HY-155227
-
|
|
Anaplastic lymphoma kinase (ALK)
EGFR
Apoptosis
|
Cancer
|
|
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research .
|
-
- HY-156103
-
|
|
Huntingtin
|
Neurological Disease
|
|
mHTT-IN-2 (compound 27) is a potent inhibitor (EC50=0.066 μM) of mutant huntingtin (mHTT). mHTT-IN-2 reduces canonical splicing of HTT RNA exons [49-50] and is a splicing regulator of the huntingtin (HTT) gene. mHTT-IN-2 exhibits inhibitory activity in vitro and in vivo in human HD stem cells and mouse BACHD models. mHTT-IN-2 may be used in the study of branaplam-related peripheral neuropathy .
|
-
- HY-156020
-
|
|
Glucosidase
|
Metabolic Disease
|
|
Glucocerebrosidase-IN-2 (compound 12) is a quinazoline analogue and an inhibitor of glucocerebrosidase (GC). Glucocerebrosidase-IN-2 has the potential to improve GC translocation to lysosomes in Gaucher disease patient-derived cells (mostly carrying the N370S mutation). Glucocerebrosidase-IN-2 inhibits the hydrolysis of 4-methylumbelliferone β-D-glucopyranoside (4MU) and fluorescent glycosylceramide (FlourGC) in N370S mutant tissues with an AC50 of 25.29 μM .
|
-
- HY-158325
-
|
|
PROTACs
FLT3
Apoptosis
|
Cancer
|
|
PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor) .
|
-
- HY-120181
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors .
|
-
- HY-101663
-
|
MK-8408
|
HCV
|
Infection
|
|
Ruzasvir (MK-8408) is an orally active inhibitor for genotypic HCV nonstructural protein 5A (NS5A), which inhibits the replication of NS5A mutants GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a and GT4a with EC90 ranging from 0.003 to 0.067 nM. Ruzasvir exhibits good pharmacokinetic characters in rhesus monkey model .
|
-
- HY-P1708
-
|
BRN 537924; NSC 657143
|
Bacterial
|
Infection
|
|
Enopeptin A, originally isolated from a culture broth of Streptomyces sp. RK-1051, is a depsipeptide antibiotic that contains two unusual amino acids (N-methylalanine and 4-methylproline) and features a pentaenone side chain. It is effective against Gram-positive bacteria, including methicillin-resistant S. aureus (MIC=25 μg/mL), and Gram-negative bacteria, including mutant forms of E. coli and P. aeruginosa (MICs=200 μg/mL); however, it is not inhibitory to fungi.
|
-
- HY-120667
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
DS-5272 is an orally acitve inhibitor for p53-MDM2 with an IC50 of 20 nM. DS-5272 inhibits the proliferation of SJSA-1 (wildtype p53, IC50=0.17 μM) and DLD-1 (mutant p53). DS-5272 arrest the cell cycle, and induces apoptosis in SJSA-1. DS-5272 exhibits antitumor efficacy in mice .
|
-
- HY-164492
-
|
|
Raf
|
Cancer
|
|
LSN3074753, an analog of LY3009120 (HY-12558), is a pan-RAF and Raf dimer inhibitor. LSN3074753 demonstrates activity against tumor cells with MAPK pathway activation driven by BRAF monomer or RAF dimers including BRAF- or KRAS-mutant colorectal cancer. LSN3074753 combined with Cetuximab (HY-P9905) shows additive and synergistic effects for colorectal cancer PDX models, particularly those with KRAS or BRAF mutation .
|
-
- HY-16767S1
-
|
MK-1439-13C,d3
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
|
-
- HY-402410
-
|
|
TET Protein
|
Cancer
|
|
TETi76 is an orally active TET family inhibitor with IC50 values ??of 1.5, 9.4 and 8.8 μM for TET1, TET2 and TET3, respectively. TETi76 competitively binds to the active site of TET enzymes, reduces cytosine hydroxymethylation and restricts clonal growth of TET2 mutants in vitro and in vivo, but does not affect the growth of normal hematopoietic precursor cells. TETi76 can be used for leukemia research .
|
-
- HY-114436
-
|
|
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 .
|
-
- HY-114436S
-
|
|
Isotope-Labeled Compounds
|
Cancer
|
|
MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). 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 .
|
-
- HY-14183
-
|
RSD1235 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
|
-
- HY-15666
-
|
GZD824; HQP1351
|
Bcr-Abl
|
Cancer
|
|
Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity . Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-19719
-
|
ARQ-092
|
Akt
Parasite
|
Infection
Cancer
|
|
Miransertib (ARQ-092) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib is effective against Leishmania .
|
-
- HY-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα .
|
-
- HY-123824
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GNE-0439 is a novel Nav1.7-selective inhibitor with IC50 of 0.34 uM and inhibits Nav1.5 with an IC50 of 38.3 μM. GNE-0439 inhibits mutant N1742K channels (IC50=0.37 uM) in membrane potential assays. GNE-0439 possesses a carboxylic acid group, binds outside of the channel pore, and is unique compared with known selective VSD4 binders .
|
-
- HY-112611
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations .
|
-
- HY-104066
-
|
Xiliertinib; HMPL-309
|
EGFR
|
Cancer
|
|
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-13811
-
|
|
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
|
-
- HY-125751
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has a high-affinity with a Ki value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole .
|
-
- HY-19719A
-
|
ARQ-092 hydrochloride
|
Akt
Parasite
|
Infection
Cancer
|
|
Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research . Miransertib hydrochloride is effective against Leishmania .
|
-
- HY-132842
-
|
DZD9008
|
EGFR
Btk
|
Cancer
|
|
Sunvozertinib (DZD9008) is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52) .
|
-
- HY-144269
-
|
|
Raf
|
Cancer
|
|
SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
|
-
- HY-146349
-
|
|
PROTACs
EGFR
Autophagy
|
Cancer
|
|
PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFR del19 and EGFR L858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy .
|
-
- HY-150602
-
|
|
Proteasome
|
Neurological Disease
|
|
20S Proteasome activator 1 is a potent 20S proteasome activator with EC200 values of 0.3 μM, 0.7 μM and 1.8 μM for trypsin-like site, chymotrypsin-like site and caspase-like site. 20S Proteasome activator 1 translates well in a cellular system, preventing the accumulation of the pathogenic A53T mutant of α-synuclein. 20S Proteasome activator 1 can be used for researching neurodegenerative diseases .
|
-
- HY-P99163
-
|
ABBV-8E12; C2N-8E12
|
Tau Protein
|
Neurological Disease
|
|
Tilavonemab (ABBV-8E12) is a humanized anti-tau antibody that targets the extracellular form of pathological tau protein aggregates by binding to the N-terminal 25-30 amino acid residues of tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates, reduces the loss of brain volume, slows the progression of tau pathology, and improves cognitive abilities in transgenic mice expressing mutant human tau. Tilavonemab is used in Alzheimer's disease research .
|
-
- HY-104066A
-
|
Xiliertinib tartrate; HMPL-309 tartrate
|
EGFR
|
Cancer
|
|
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-153341
-
|
|
PROTACs
Raf
|
Cancer
|
|
CFT1946 is an orally active, CRBN-based and mutant-selective bifunctional degradation activating compound (BiDAC ™) degrader of BRAF V600E with a DC50 of 14 nM in A375 cells. CFT1946 is capable of degrading BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations, and the p61-BRAF V600E splice variant. CFT1946 can be used in tumor research .
|
-
- HY-153202
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity .
|
-
- HY-149695
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFR L858R/C797S and EGFR exon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants .
|
-
- HY-157166
-
|
|
EGFR
|
Cancer
|
|
EGFR kinase inhibitor 2 (compound A-7) is a potent EGFR inhibitor targeting EGFR L858R/T790M/C797S and EGFR Del19/T790M/C797S mutants. EGFR kinase inhibitor 2 has the potential to address acquired resistance in the treatment of non-small cell lung cancer .
|
-
- HY-162253
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-64 (Compound 7c) is a wild-type HIV-1 inhibitor that effectively suppresses the activity of HIV-1 mutants E138K/Q148K and G140S/Q148R with EC50 values of 62.5 nM and 11.3 nM, respectively. HIV-1 inhibitor-64 exhibits antiviral activity and can be used in the research of AIDS .
|
-
- HY-14588R
-
|
ABT-378 (Standard)
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
|
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. 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 .
|
-
- HY-164056
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-8 (compound 9) is a potent inhibitor of EGFR, targeting mutant EGFR T790M/L858R with IC50 of 56.8 μM. The anti-proliferative effect of EGFR T790M/L858R-IN-8 on cancer cell lines A549, A431, and NHI-H1975 is not significant .
|
-
- HY-162577
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. FGFR-IN-14 inhibits FGFR1, FGFR2, FGFR3 and FGFR2 V564F gatekeeper mutant with IC50s of 46, 41, 99, and 62 nM, respectively. FGFR-IN-14 strongly suppresses NCI-H520 lung cancer cells, SNU-16 and KATO III gastric cancer cells proliferation with IC50s of 19, 59, and 73 nM, respectively .
|
-
- HY-101561R
-
|
|
c-Kit
PDGFR
|
Cancer
|
|
Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
|
-
- HY-15164AR
-
|
|
EGFR
|
Cancer
|
|
Icotinib (Standard) is the analytical standard of Icotinib. This product is intended for research and analytical applications. Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-12755
-
|
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-131003A
-
|
DS-6051b free base; AB-106 free base; IBI-344 free base
|
ROS Kinase
|
Cancer
|
|
Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .
|
-
- HY-14588S1
-
|
|
HIV
HIV Protease
SARS-CoV
|
Infection
|
|
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. 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[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
|
-
- HY-126247
-
|
|
Ras
|
Cancer
|
|
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-130122
-
|
|
Molecular Glues
PROTACs
Apoptosis
|
Cancer
|
|
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor based on Cereblon E3 ligand, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity .
|
-
- HY-17499
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-12 is a 4,6-disubstituted pyrimidine and is a potent, ATP-competitive, irreversible and highly selective EGFR inhibitor with an IC50of 21 nM. EGFR-IN-12 also inhibits mutant EGFR L858R and EGFR L861Q with IC50s of 63 nM and 4 nM, respectively. EGFR-IN-12 displays strong selectivity for EGFR over HER4 (IC50 = 7640 nM) and a panel of 55 other kinases. EGFR-IN-12 induces cells apoptosis and has antitumor activity .
|
-
- HY-15666A
-
|
GZD824 dimesylate; HQP1351 dimesylate
|
Bcr-Abl
|
Cancer
|
|
Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity . Olverembatinib (dimesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-135805
-
|
|
EGFR
|
Cancer
|
|
JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFR L858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFR L858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities .
|
-
- HY-130241
-
|
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme .
|
-
- HY-111545
-
|
|
FLT3
|
Cancer
|
|
BSc5371 is a potent and irreversible FLT3 inhibitor, with Kds of 1.3, 0.83, 1.5, 5.8 and 2.3 nM for mutant FLT3(D835H), FLT3(ITD, D835V), FLT3(ITD, F691L), FLT3-ITD and wild type FLT3wt, respectively. BSc5371 is cytotoxic to FLT3-dependent cell lines .
|
-
- HY-137458A
-
|
ARQ 751 trihydrochloride
|
Akt
|
Cancer
|
|
Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer .
|
-
- HY-16936
-
|
|
LRRK2
|
Neurological Disease
|
|
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
|
-
- HY-148416
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1) . p53 Activator 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155059
-
|
|
Bacterial
|
Infection
|
|
Antimycobacterial agent-6 (compound 25) is a potent inhibitor of Mycobacterium tuberculosis (Mtb)，targeting to both wild-type and fluoroquinolone-resistant Mtb strains. Antimycobacterial agent-6 inhibits Mtb DprE1-C387S mutant with MIC90s of 0.9 μM (H37Rv)，0.9 μM (MoxR)，0.5 μM (DprE1-P116S)，respectively .
|
-
- HY-P5395
-
|
|
HIV
|
Others
|
|
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
|
-
- HY-163393
-
|
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-18 (compound N5) is a novel polyheterocyclic neuraminidase (NA) inhibitor. Neuraminidase-IN-18 shows potency in inhibition of H5N1 NA with an IC50 of 0.14 μM and 0.27 μM against the wild-type H5N1 NA and H5N1-H274Y mutant NA, respectively. Neuraminidase-IN-18 inhibits influenza virus replication by binding to NAs in cell level .
|
-
- HY-17598R
-
|
|
Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
|
Rafoxanide (Standard) is the analytical standard of Rafoxanide. This product is intended for research and analytical applications. Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
|
-
- HY-164474
-
|
|
MEK
|
Cancer
|
|
DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy .
|
-
- HY-116191
-
|
|
PI3K
mTOR
|
Cancer
|
|
WJD008 is a potent dual phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor with antiproliferative and anticlonogenic activity in tumor cells and transformed cells with PIK3CA mutant. WJD008 inhibits kinase activity of PI3K α and mTOR and abrogates insulin-like growth factor-I-activated PI3K-Akt-mTOR signaling cascade. WJD008 is promising for research of cancers .
|
-
- HY-109142
-
|
AK0529; RO-0529
|
RSV
|
Infection
|
|
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species .
|
-
- HY-137497
-
|
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells .
|
-
- HY-122936
-
|
|
Histone Methyltransferase
Keap1-Nrf2
Sirtuin
|
Cardiovascular Disease
Cancer
|
|
Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research .
|
-
- HY-15666R
-
|
|
Bcr-Abl
|
Cancer
|
|
Olverembatinib (Standard) is the analytical standard of Olverembatinib. This product is intended for research and analytical applications. Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity . Olverembatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-100818
-
|
TAS-120
|
FGFR
|
Cancer
|
|
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
|
-
- HY-112289
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
|
-
- HY-15814
-
|
|
Bcr-Abl
PDGFR
c-Kit
Src
JAK
Apoptosis
|
Cancer
|
|
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
|
-
- HY-137460
-
|
K0706
|
Bcr-Abl
|
Cancer
|
|
Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research . Vodobatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-151903S
-
|
|
FGFR
|
Cancer
|
|
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
|
-
- HY-148597
-
|
|
FGFR
Cytochrome P450
|
Cancer
|
|
FGFR-IN-10 is an orally active inhibitor of FGFR and Cytochrome P450 (CYPs). FGFR-IN-10 inhibits wide type and V564F mutant FGFR2 with IC50s of 104.1 nM and 43.6 nM, respectively. FGFR-IN-10 also inhibits CYPs with IC50s of 3.33 μM (CYP2C9), 18.75 μM (CYP2C19), 4.34 μM (CYP2CD6), and 0.69 μM (CYP3A4), respectively .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-14588S
-
|
(rel)-ABT-378-d8
|
Isotope-Labeled Compounds
|
Others
|
|
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588) . 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 .
|
-
- HY-10035A
-
|
|
Others
|
Neurological Disease
|
|
(R)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
|
-
- HY-50707
-
|
(Rac)-T-Type calcium channel inhibitor
|
Others
|
Neurological Disease
|
|
(Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
|
-
- HY-15164AS
-
|
BPI-2009-d4
|
Isotope-Labeled Compounds
|
Others
|
|
Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-155356
-
|
|
PROTACs
Ras
|
Cancer
|
|
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.
|
-
- HY-134850
-
|
|
PROTACs
Tau Protein
|
Neurological Disease
|
|
QC-01-175 is a heterobifunctional molecule, which degrades aberrant tau. QC-01-175 reduces the levels of A152T and P301L mutant tau protein and protects neurons from tau-mediated toxicity and improve cell survival (Pink: ligand for target protein Aberrant tau ligand 1 (HY-W453397); Black: linker NH2-PEG3 (HY-W007545); Blue: ligand for E3 ligase Pomalidomide (HY-10984)) .
|
-
- HY-162720
-
|
|
HIV
Potassium Channel
Reverse Transcriptase
|
Infection
|
|
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
|
-
- HY-160023
-
|
|
Ras
|
Cancer
|
|
D3S-001 is an orally active inhibitor for KRAS. D3S-001 inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. D3S-001 exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
|
-
- HY-164373
-
|
|
Androgen Receptor
Apoptosis
|
Cancer
|
|
SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
|
-
- HY-130149
-
|
MRTX849
|
Ras
|
Cancer
|
|
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
|
-
- HY-155302
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .
|
-
- HY-156498
-
|
|
Ras
ERK
Raf
Ribosomal S6 Kinase (RSK)
AMPK
Apoptosis
PARP
|
Cancer
|
|
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
|
-
- HY-163799
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
|
-
- HY-164477
-
|
|
Androgen Receptor
|
Cancer
|
|
FL442 is an Androgen Receptor (AR) modulator. FL442 exhibits strong inhibitory effects in AR-dependent prostate cancer cells, showing similar inhibitory efficiency to traditional antiandrogen drugs Bicalutamide (HY-14249) and Enzalutamide (HY-70002), while maintaining antiandrogenic activity against the AR mutant F876L, which is highly resistant to Enzalutamide. Pharmacokinetic studies of FL442 in mice reveal a long half-life (8 hours), good targeting (prostate tissue), and metabolic stability, and it effectively inhibits LNCaP tumor growth at low plasma concentrations (30 ng/mL) .
|
-
- HY-169076
-
|
|
FLT3
HDAC
Apoptosis
|
Cancer
|
FLT3/HDAC-IN-1 is a dual inhibitor of FLT3/HDAC, with IC50 values of 30.4, 52.4, and 14.7 nM for FLT3, HDAC1, and HDAC3, respectively. FLT3/HDAC-IN-1 can induce apoptosis in MV-4-11 cells and has anti-proliferative effects on FLT3 mutant-transformed BaF3 cells. FLT3/HDAC-IN-1 is being researched for its potential in treating hard-to-treat solid tumors and hematological malignancies .
|
-
- HY-100818R
-
|
|
FGFR
|
Cancer
|
|
Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
|
-
- HY-13238
-
|
S/GSK1349572
|
HIV Integrase
HIV
|
Infection
|
|
Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
- HY-111373
-
|
|
mTOR
Autophagy
|
Cancer
|
|
RapaLink-1, the third-generation bivalent mTOR inhibitor, combines Rapamycin (HY-10219) with MLN0128 (HY-13328, a second-generation mTOR kinase inhibitor) by an inert chemical linker. RapaLink-1 shows better efficacy than Rapamycin or mTOR kinase inhibitors (TORKi), potently blocking cancer-derived, activating mutants of mTOR. RapaLink-1 can cross the blood-brain barrier. RapaLink-1 binding to FKBP12 results in targeted and durable inhibition of mTORC1. RapaLink-1 plays an antithrombotic role in antiphospholipid syndrome by improving autophagy. Anticancer activity .
|
-
- HY-150926
-
|
|
Ras
|
Cancer
|
|
G12Si-1 is a selective K-Ras(G12S) covalent inhibitor, which can inhibit oncogenic signaling of K-Ras(G12S). G12Si-1 shows good ability to covalently engage recombinant K-Ras(G12S) at the mutant serine residue. G12Si-1 can also affect nucleotide cycling of K-Ras by blocking Sos-catalyzed exchange and decreasing the rate of EDTA promoted exchange .
|
-
- HY-150652
-
|
|
FGFR
Apoptosis
|
Cancer
|
|
FGFR-IN-8 (Compound 17a) is a highly potent and orally active panFGFR inhibitor against wild-type and mutant FGFRs. FGFR-IN-8 shows inhibition with IC50 values of <0.5, 189.1, <0.5, 22.6, <0.5 and 7.30 nM against FGFR1, V564F-FGFR2, N549H-FGFR2, V555M-FGFR3, FGFR3 and FGFR4, respectively. GFR-IN-8 induces cancer cell apoptosis and shows anticancer activities .
|
-
- HY-148409
-
|
|
Ferroptosis
Apoptosis
Autophagy
MDM-2/p53
|
Cancer
|
|
MMRi62, a ferroptosis inducer targeting MDM2-MDM4 (negative regulators of tumor suppressor p53). MMRi62 shows a P53-independent pro-apoptotic activity against pancreatic ductal adenocarcinoma (PDAC) cells and induce autophagy. MMRi62 inducesferroptosis, resulting in a increase of reactive oxygen and lysosomal degradation of ferritin heavy chain (FTH1). MMRi62 also leads to proteasomal degradation of mutant p53, also inhibits orthotopic xenograft PDAC mouse model in vivo with high frequency mutation characteristics of KRAS and TP53.12 .
|
-
- HY-152233
-
|
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-116762
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. The control of bacterial infection by quenching the quorum sensing system of bacteria is a promising research area. The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR protein family, is coordinated by the synthesis of diffusible acyl homoserine lactone (AHL) molecules. N-butyryl-L-Homocysteine thio-lactone is an analog of N-butyryl-L-homoserine lactone, a small, diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and cellular metabolism . N-butyryl-L-homocysteine thiolactone induces violacein expression in Viola viola mutants that normally fail to produce AHL.
|
-
- HY-153857
-
|
|
FLT3
|
Cancer
|
|
PHI-101 is an orally active FLT3 inhibitor that overcomes resistance to multiple drug-resistant mutations. PHI-101 potently inhibits FLT3 single activating mutations (ITD or TKD mutants) and has inhibitory activity against FLT3 double (ITD/D835Y or ITD/F691L) and triple (ITD/D835Y/F691L) resistance mutations. PHI-101 has potential for research in relapsed or refractory acute myeloid leukemia (AML) .
|
-
- HY-157288
-
|
|
Others
|
Metabolic Disease
|
|
(R)-Phe-A110/B319, a hapten, is a selective binder to tumor-associated antigens. (R)-Phe-A110/B319 has a 20-fold higher affinity towards the H1047R mutant of p110α in the p110α/p85α PI3K complex. (R)-Phe-A110/B319 can be used for the research of conditional chimeric antigen receptor T (CAR-T) cell activation and tumor targeting .
|
-
- HY-161536
-
|
|
PROTACs
EGFR
Apoptosis
|
Cancer
|
|
PROTAC EGFR degrader 9 (Compound C6) is an orally active CRBN-based PROTAC EGFR degrader. PROTAC EGFR degrader 9 exhibits a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 9 exhibits potent degradation activity against various EGFR mutants, while sparing the EGFRWT. (Blue: CRBN ligand (HY-A0003), Black: linker (HY-161613); Pink: EGFR inhibitor (HY-161537)) .
|
-
- HY-159190
-
|
|
MAPKAPK2 (MK2)
|
Cancer
|
|
HRX-0233 is a small-molecule MAP2K4 inhibitor. HRX-0233 results in strong tumor shrinkage without any apparent toxicity in H358 KRASG12C-mutant non-small cell lung cancers (NSCLC) in vivo. HRX-0233 efficiently prevents feedback activation of receptor tyrosine kinases (RTKs) upon monotherapy KRAS inhibitor Sotorasib (HY-114277) and causes a more sustained and complete inhibition of MAPK signaling. HRX-0233 is promising for research of AR-negative prostate cancer, lung and colon cancers .
|
-
- HY-164473
-
|
|
ERK
Akt
STAT
Apoptosis
|
Cancer
|
|
DETD-35 is an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways, which promotes cancer cell apoptosis (Apoptosis) and reduces cancer cell resistance to Vemurafenib (HY-12057). The IC50 values of DETD-35 against wild-type and mutant melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c are 2.7, 6.0, 3.9, 3.1, and 2.5 μM, respectively. DETD-35 holds promise for research in the field of anti-melanoma therapy .
|
-
- HY-149127
-
|
ASC-JM17; ALZ-003
|
Keap1-Nrf2
Androgen Receptor
HSP
Mitophagy
|
Metabolic Disease
|
|
Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
|
-
- HY-128131
-
|
|
Others
|
Others
|
|
UCCF-029 Free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. UCCF-029 Free base exhibits enhanced activity through benzannulation of the flavone A-ring at the 7,8-position. UCCF-029 Free base serves as a structural guide for the development of more effective flavonoid analogues. UCCF-029 Free base demonstrates improved potency compared to apigenin in activating wild-type CFTR. UCCF-029 Free base also exhibits potential for activating the mutant CFTR (G551D-CFTR) though not as robustly as apigenin.
|
-
- HY-13238A
-
|
S/GSK1349572 sodium
|
HIV Integrase
HIV
|
Infection
|
|
Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
- HY-104042
-
|
AG-881
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K .
|
-
- HY-128888B
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
(S,R)-GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. (S,R)-GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. (S,R)-GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
|
-
- HY-126247B
-
|
|
Others
|
Cancer
|
|
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
|
-
- HY-158684
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
YX-02-030M is a PROTAC MDM2 degrader. YX-02-030M inhibits MDM2-p53 binding and VHL-HIF1α binding with IC50s of 63 nM and 1.35 μM respectively. YX-02-030M binds MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, and effectively kills p53 mutant or deleted Triple-negative breast cancers (TNBC) cells. (Blue: VHL ligand; Black: linker; Pink: MDM2 inhibitor) .
|
-
- HY-13238R
-
|
|
HIV Integrase
HIV
|
Infection
|
|
Dolutegravir (Standard) is the analytical standard of Dolutegravir. This product is intended for research and analytical applications. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM) .
|
-
- HY-136265
-
|
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research .
|
-
- HY-13238S1
-
|
S/GSK1349572-d3
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
|
Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
|
-
- HY-139920
-
|
SH-1028
|
EGFR
|
Cancer
|
|
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR WT, EGFR L858R, EGFR L861Q, EGFR L858R/T790M, EGFR d746-750 and EGFR d746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively .
|
-
- HY-13238S2
-
|
S/GSK1349572-d5
|
Isotope-Labeled Compounds
HIV Integrase
HIV
|
Infection
|
|
Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
|
-
- HY-112289B
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
(1R)-IDH889 is the isomer of IDH889 (HY-112289), and can be used as an experimental control. IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM .
|
-
- HY-W744699
-
|
(+)-Larixol
|
Src
ERK
Akt
|
Inflammation/Immunology
|
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-W745090
-
|
|
Formyl Peptide Receptor (FPR)
Src
ERK
Akt
p38 MAPK
|
Others
|
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-161785
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-117 (Compound 8h) exhibits inhibitory activity against EGFR mutation, targets the tumor environment, and induces apoptosis of cancer cells. EGFR-IN-117 inhibits proliferations of H1975, PC-9, and EGFR mutant cells BaF3-EGFR L858R/T790M/C797S and BaF3– C797S/Del19/T790M, with IC50 of 13 nM, 19 nM, 1.2 nM and 1.3 nM, respectively. EGFR-IN-117 exhibits antitumor efficacy in mouse models .
|
-
- HY-168012
-
|
|
Ras
Phosphatase
|
Cancer
|
|
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively .
|
-
- HY-15800A
-
|
|
LRRK2
|
Neurological Disease
Inflammation/Immunology
|
|
CZC-25146 is a potent and orally active LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 can be used to research Parkinson's disease and liver diseases .
|
-
- HY-D0098
-
|
N-(5-Fluoresceinyl)maleimide
|
Fluorescent Dye
|
Others
|
Fluorescein-5-maleimide (N-(5-Fluoresceinyl)maleimide) is a fluorescent dye. Fluorescein-5-maleimide can be used to detect the redox state of thiols in eukaryotic cells. Fluorescein-5-maleimide can label peptides and is used to detect negatively charged nanoparticles. Fluorescein-5-maleimide can also label actin to explore its interaction with cardiac myosin-binding protein C (cMyBP-C), which helps in developing small molecule modulators for heart failure. Fluorescein-5-maleimide can screen mutant proteins that contain cysteine residues. The excitation wavelength of Fluorescein-5-maleimide is 494 nm, and the emission wavelength is 519 nm .
|
-
- HY-15800
-
|
|
LRRK2
|
Neurological Disease
Inflammation/Immunology
|
|
CZC-25146 hydrochloride is a potent LRRK2 inhibitor with IC50 values of 4.76 nM and 6.87 nM for wild-type LRRK2 and G2019S LRRK2, respectively. CZC-25146 hydrochloride inhibits PLK4, GAK, TNK1, CAMKK2 and PIP4K2C as well. CZC-25146 hydrochloride prevents mutant LRRK2-induced injury of neurons in vitro. CZC-25146 hydrochloride exhibits relatively favorable pharmacokinetic properties in mice. CZC-25146 hydrochloride can increase normal α-1-antitrypsin (AAT) secretion and reduce inflammatory cytokines. CZC-25146 hydrochloride can be used to research Parkinson's disease and liver diseases .
|
-
- HY-156086
-
|
|
Trk Receptor
|
Cancer
|
|
TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
|
-
- HY-164476
-
|
|
EGFR
GSK-3
PD-1/PD-L1
|
Cancer
|
|
ES-072 is an orally effective selective EGFR mutant (EGFR-T790M) inhibitor. ES-072 activates GSK3α by inhibiting EGFR-T790M activity, which promotes phosphorylation of PD-L1 at Ser279 and Ser283. The phosphorylated PD-L1 recruits the E3 ubiquitin ligase ARIH1, leading to ubiquitination and proteasomal degradation of PD-L1. This mechanism not only reduces cancer cell growth but also enhances anti-tumor immune response by lowering PD-L1 levels. ES-072 can be used to inhibit proliferation in non-small cell lung cancer (NSCLC) cells .
|
-
- HY-102069
-
|
|
Polo-like Kinase (PLK)
CDK
DAPK
|
Others
|
|
3MB-PP1, a bulky purine analog, is a Polo-like kinase 1 (Plk1) inhibitor. 3MB-PP1 blocks mitotic progression and cell division arise through target Plk1 in in cells expressing analog-sensitive Plk1 alleles. 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits Leu93 Mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used for the research of hypha formation of Candida albicans and cell division .
|
-
- HY-119396
-
|
|
Others
|
Cancer
|
|
DY3002 is a selective and highly potent EGFR inhibitor with activity in overcoming T790M-mediated drug resistance in non-small cell lung cancer. DY3002 exhibited superior inhibitory effects against EGFR T790M mutants in kinase assays (IC50 = 0.71 nM), compared to weaker inhibitory effects against wild-type EGFR (IC50 = 448.7 nM). DY3002 was significantly superior to rociletinib and osimertinib in selectivity, showing an extremely high selectivity index (SI = 632.0). In cell experiments, DY3002 had an IC50 value of 0.037 μM against H1975 cells, showing enhanced inhibitory potency. In addition, DY3002 was superior to other alternative compounds in terms of biological properties and did not cause hyperglycemia .
|
-
- HY-146019A
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS .
|
-
- HY-164490
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
LS-106 is an orally active and potent inhibitor against epidermal growth factor receptor (EGFR) . LS-106 exhibits antitumor activities both in vitro and in vivo. LS-106 inhibits the kinase activities of EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, which is more potent than Osimertinib (HY-15772). LS-106 induces Apoptosis, suppresses cell proliferation of tumor cells harboring EGFR 19del/T790M/C797S and leas to significant tumor regression in a C797S-mutant xenograft model .
|
-
- HY-126077
-
|
LXI-15029
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .
|
-
- HY-148369
-
|
|
PROTACs
Deubiquitinase
Apoptosis
MDM-2/p53
|
Cancer
|
|
U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells .
|
-
- HY-164392
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
|
-
- HY-W251428
-
|
Egg PG
|
Biochemical Assay Reagents
|
Others
|
|
Phosphatidylglycerol is a naturally occurring anionic phospholipid that is a component of plant, animal and bacterial cell membranes. It is present in prokaryotes and eukaryotes less than phosphatidylethanolamine, and in eukaryotes less than phosphatidylcholine. It is formed by the reaction between CDP-diglyceride and L-α-glycerol 3-phosphate followed by dephosphorylation and is the metabolic precursor of cardiolipin. Phosphatidylglycerols containing polyunsaturated and monounsaturated fatty acyl chains inhibit and promote the proliferation of murine keratinocytes, respectively. Phosphatidylglycerol is the second-largest lipid component of mammalian lung surfactant, accounting for 10% of lipids, and has reduced levels of pulmonary surfactant in infants with respiratory distress syndrome. Phosphatidylglycerol (egg) is a mixture of phosphatidylglycerols isolated from eggs with various fatty acyl groups at the sn-1 and sn-2 positions. References: [1]. Ohtsuka, T., Nishijima, M., and Akamatsu, Y. Phosphatidylglycerol phosphate synthase-deficient somatic mutants with impaired phosphatidylglycerol and cardiolipin biosynthesis J. Biol. Chemical. 268(30), 22908-22913 (1993).[2]. Furse, S. Are phosphatidylglycerols essential for terrestrial life J. Chemistry. biology. 10(1), 1-9 (2016).[3]. Xie, D., Seremwe, M., Edwards, JG, et al. Different effects of different phosphatidylglycerols on the proliferation of mouse keratinocytes PLoS One 9(9), e107119 (2014).
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-114491
-
|
|
Fluorescent Dyes/Probes
|
|
Rineterkib (compound B) is an orally available ERK1 and ERK2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer. Rineterkib hydrochloride can also inhibit RAF .
|
-
- HY-P1004
-
|
|
Fluorescent Dyes/Probes
|
|
Luciferase from Vibrio fischeri has also been used in a study to investigate the sensitivity of dark mutants of various strains of luminescent bacteria to reactive oxygen species.
|
-
- HY-W127705
-
|
|
Fluorescent Dyes/Probes
|
|
Quinacrine mustard dihydrochloride is a fluorochrome. Quinacrine mustard dihydrochloride as a polycyclic aromatic agent can be used as mutagenic agent induces the mutants of bacteria. Quinacrine mustard dihydrochloride induces cell cycle arrest at G2/M-phase. Quinacrine mustard dihydrochloride has the potential for the research of plant, animal, or human chromosomes .
|
-
- HY-143218
-
TPE-MI
2 Publications Verification
Tetraphenylethene maleimide
|
Fluorescent Dyes/Probes
|
|
TPE-MI (Tetraphenylethene maleimide) is a thiol probe for measuring unfolded protein load and proteostasis in cells. TPE-MI can report imbalances in proteostasis in induced pluripotent stem cell models of Huntington disease, as well as cells transfected with mutant Huntington exon 1 before the formation of visible aggregates. TPE-MI also detects protein damage following dihydroartemisinin research of the malaria parasitesPlasmodium falciparum .
|
-
- HY-D0098
-
|
N-(5-Fluoresceinyl)maleimide
|
Fluorescent Dyes/Probes
|
Fluorescein-5-maleimide (N-(5-Fluoresceinyl)maleimide) is a fluorescent dye. Fluorescein-5-maleimide can be used to detect the redox state of thiols in eukaryotic cells. Fluorescein-5-maleimide can label peptides and is used to detect negatively charged nanoparticles. Fluorescein-5-maleimide can also label actin to explore its interaction with cardiac myosin-binding protein C (cMyBP-C), which helps in developing small molecule modulators for heart failure. Fluorescein-5-maleimide can screen mutant proteins that contain cysteine residues. The excitation wavelength of Fluorescein-5-maleimide is 494 nm, and the emission wavelength is 519 nm .
|
| Cat. No. |
Product Name |
Type |
-
- HY-145411
-
|
|
Drug Delivery
|
|
PEG2000-C-DMG, a pegylated lipid, can be used for the preparation of Onpattro. Onpattro, a hepatically directed investigational RNAi therapeutic agent, harnesses this process to reduce the production of mutant and wild-type transthyretin by targeting the 3′ untranslated region of transthyretin mRNA .
|
-
- HY-114365
-
|
UDP-N-acetyl-D-galactosamine disodium
|
Gene Sequencing and Synthesis
|
|
UDP-GalNAc (UDP-N-acetyl-D-galactosamine) disodium is a sugar nucleotide and a substrate of EpsC115. EpsC115 is an exopolymeric substances (EPS) N-terminal deletion mutant with the residue 1-115 deletion. UDP-GalNAc UDP-GalNAc is the donor substrate of many N-acetylgalactosaminyltransferases, enzymes which transfer GalNAc from the nucleotide sugar to a saccharide or peptide acceptor .
|
-
- HY-W251428
-
|
Egg PG
|
Drug Delivery
|
|
Phosphatidylglycerol is a naturally occurring anionic phospholipid that is a component of plant, animal and bacterial cell membranes. It is present in prokaryotes and eukaryotes less than phosphatidylethanolamine, and in eukaryotes less than phosphatidylcholine. It is formed by the reaction between CDP-diglyceride and L-α-glycerol 3-phosphate followed by dephosphorylation and is the metabolic precursor of cardiolipin. Phosphatidylglycerols containing polyunsaturated and monounsaturated fatty acyl chains inhibit and promote the proliferation of murine keratinocytes, respectively. Phosphatidylglycerol is the second-largest lipid component of mammalian lung surfactant, accounting for 10% of lipids, and has reduced levels of pulmonary surfactant in infants with respiratory distress syndrome. Phosphatidylglycerol (egg) is a mixture of phosphatidylglycerols isolated from eggs with various fatty acyl groups at the sn-1 and sn-2 positions. References: [1]. Ohtsuka, T., Nishijima, M., and Akamatsu, Y. Phosphatidylglycerol phosphate synthase-deficient somatic mutants with impaired phosphatidylglycerol and cardiolipin biosynthesis J. Biol. Chemical. 268(30), 22908-22913 (1993).[2]. Furse, S. Are phosphatidylglycerols essential for terrestrial life J. Chemistry. biology. 10(1), 1-9 (2016).[3]. Xie, D., Seremwe, M., Edwards, JG, et al. Different effects of different phosphatidylglycerols on the proliferation of mouse keratinocytes PLoS One 9(9), e107119 (2014).
|
-
- HY-116762
-
|
|
Microbial Culture
|
|
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. The control of bacterial infection by quenching the quorum sensing system of bacteria is a promising research area. The expression of specific target genes, such as transcriptional regulators belonging to the LuxIR protein family, is coordinated by the synthesis of diffusible acyl homoserine lactone (AHL) molecules. N-butyryl-L-Homocysteine thio-lactone is an analog of N-butyryl-L-homoserine lactone, a small, diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and cellular metabolism . N-butyryl-L-homocysteine thiolactone induces violacein expression in Viola viola mutants that normally fail to produce AHL.
|
-
- HY-W745090
-
|
|
Biochemical Assay Reagents
|
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2361
-
|
|
Peptides
|
Others
|
|
S12 is a mutant RAS peptide containing the Gly (G) to Ser (S12) substitution. The sequence of the peptide is KLVVVGASGVGKS .
|
-
- HY-P2360
-
|
Ras 5-17
|
Peptides
|
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) .
|
-
- HY-P2265A
-
|
|
Ras
|
Cancer
|
|
SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-P2670
-
|
|
Peptides
|
Others
|
|
SN50M, a mutant peptide of SN50 (HY-P0151), is a cell membrane-permeable inactive control peptide .
|
-
- HY-P2250
-
|
ELA-32 negative control
|
Peptides
|
Others
|
|
ELA RR>GG (ELA-32 negative control), an ELABELA (ELA-32 human) mutant peptide, is inactive. ELA RR>GG is a negative control for ELABELA (HY-P2196) .
|
-
- HY-P2360A
-
|
Ras 5-17 TFA
|
Peptides
|
Others
|
|
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12) .
|
-
- HY-P10425
-
|
|
Peptides
|
Cancer
|
|
T2857W is a mutant peptide that has inhibitory effect on KIX-MLL interaction (IC50=5.67 μM). T2857W can be used for protein-protein interaction (PPI) and for the study of diseases related to KIX-MLL interaction, such as leukemia, cancer, etc .
|
-
- HY-P5082
-
|
|
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 .
|
-
- HY-P2265
-
|
|
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-P10456
-
|
|
Peptides
|
Inflammation/Immunology
|
|
[Leu144,Arg147]-PLP (139-151) is a mutant peptide fragment of myelin proteolipid protein (PLP), with the tryptophan and histidine at positions 144 and 147 respectively replaced by leucine and arginine. [Leu144,Arg147]-PLP (139-151) also serves as a T cell receptor (TCR) antagonist for encephalitogenic Th1 clones, blocking their activation in vitro. Furthermore, [Leu144,Arg147]-PLP (139-151) can inhibit the development of experimental autoimmune encephalomyelitis (EAE) .
|
-
- HY-129028
-
-
- HY-129028A
-
|
|
Peptides
|
Others
|
|
H-Ala-Ala-Tyr-OH TFA can be synthesized mutant peptides .
|
-
- HY-P5192
-
-
- HY-P3488
-
-
- HY-P3486
-
-
- HY-P4391
-
-
- HY-P0222
-
|
|
PKA
|
Others
|
|
PKI(5-24) is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P0222A
-
|
|
PKA
|
Others
|
|
PKI(5-24) TFA is a potent, competitive, and synthetic peptide inhibitor of PKA (cAMP-dependent protein kinase), with a Ki of 2.3 nM. PKI(5-24) TFA corresponds to residues 5-24 in the naturally occurring heat-stable protein kinase inhibitor .
|
-
- HY-P3277
-
|
|
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 .
|
-
- HY-P3277A
-
|
|
Ras
|
Cancer
|
|
KRpep-2d (TFA) is a potent K-Ras inhibitor and inhibits proliferation of K-Ras-driven cancer cells. KRpep-2d can be used for cancer research .
|
-
- HY-P2319
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P2319A
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P1974
-
|
WF11899A
|
Antibiotic
|
Infection
|
|
FR901379 (WF11899A) is a novel echinocandin-type lipopeptide antibiotic. FR901379 is primarily produced by mutant strain M-7 of Coleophoma empetri F-11899 (FERM BP-2635) .
|
-
- HY-P5968
-
|
β(25-35)KA
|
Amyloid-β
|
Neurological Disease
|
|
[Ala28]-β Amyloid(25-35) (β(25-35)KA) is an electrically neutral mutant peptide of Aβ(25-35) that accelerates the aggregation of Firefly Luciferase .
|
-
- HY-P10610
-
|
|
MDM-2/p53
|
Cancer
|
|
Peptide 234CM is a peptide containing isoleucine at position 3, corresponding to the sequence of a point mutation in p53 codon 234. Peptide 234CM induces potent cytotoxic T cell (CTL) and antitumor immune responses against mutant p53 .
|
-
- HY-P4528
-
|
|
Peptides
|
Others
|
|
Ala-Phe-Pro-βNA is the subsrate of prolyl tripeptidyl aminopeptidase, which is from Porphyromonas gingivalis. Ala-Phe-Pro-βNA binds to H-Ala-Ile-pyrrolidin-2-yl boronic acid for PTP39 and the E636A mutant with Ki values of 88.1 nM and 48.8 nM, respectivley .
|
-
- HY-P10438
-
|
|
Raf
|
Cancer
|
|
Tat-braftide is a peptide inhibitor designed to block the dimerization of BRAF, thereby inhibiting its kinase activity. The destruction of BRAF dimer by Tat-braftide makes BRAF protein more susceptible to proteasome degradation, directly inhibits the activity of BRAF kinase, and reduces the activation of MAPK signaling pathway. Tat-braftide can be used for the role of RAF kinase in MAPK signaling pathway and for the study of BRAF mutant cancers .
|
-
- HY-P10436
-
|
|
Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
|
-
- HY-P5395
-
|
|
HIV
|
Others
|
|
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
|
-
- HY-K0233
-
|
|
|
MCE Anti-RFP Affinity Gel can be used for the detection and purification of native RFP, RFP mutants, and IP assays.
|
-
- HY-KE8004
-
|
|
|
Reverse Transcriptase is a reverse transcriptase that clones and expresses the deletion mutant RNase H- of M-MuLV through genetic recombination technology.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99849
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
|
-
- HY-P99701
-
|
BMS-986004
|
TNF Receptor
|
Inflammation/Immunology
|
|
Letolizumab (BMS-986004) is a monoclonal antibody targeting CD40L, which is produced to express mutant IgG1 lacking effector function, including Fc binding and complement fixation. Letolizumab reduces rejection, thromboembolism and prolongs the survival time .
|
-
- HY-P99823
-
|
TA-46; sFGFR3
|
FGFR
|
Others
|
|
Recifercept (TA-46) is a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule. Recifercept can be used as a decoy/ligand trap to decrease the amount of fibroblast growth factors that can bind to mutant FGFR3 receptors. Recifercept can be used for the research of achondroplasia .
|
-
- HY-P99163
-
|
ABBV-8E12; C2N-8E12
|
Tau Protein
|
Neurological Disease
|
|
Tilavonemab (ABBV-8E12) is a humanized anti-tau antibody that targets the extracellular form of pathological tau protein aggregates by binding to the N-terminal 25-30 amino acid residues of tau protein. Tilavonemab blocks the ability of human and mouse neurons to take up tau aggregates, reduces the loss of brain volume, slows the progression of tau pathology, and improves cognitive abilities in transgenic mice expressing mutant human tau. Tilavonemab is used in Alzheimer's disease research .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-P1004
-
-
-
- HY-P99849
-
-
-
- HY-N10502
-
-
-
- HY-117915
-
-
-
- HY-N3492
-
-
-
- HY-N3496
-
-
-
- HY-N3920
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- HY-120885
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- HY-N5141
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- HY-121262
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- HY-P1974
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- HY-B0282
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- HY-B1907
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- HY-N2099
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- HY-N0328
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- HY-114604
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Structural Classification
Natural Products
Microorganisms
Source classification
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Others
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Propioxatin B is a tricyclic sesquiterpenoid compound isolated from the root of vetiver grass. It has anti-tuberculosis activity and inhibitory effects on a variety of drug-resistant mutants of Mycobacterium tuberculosis. In computer simulation docking studies, it showed binding affinity with bacterial DNA gyrase and has a certain safety in vivo.
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- HY-122958
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- HY-B0282R
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- HY-N12390
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- HY-B1907R
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- HY-125540
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- HY-N6790
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- HY-114365
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- HY-N0328R
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- HY-130259
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- HY-N12109
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
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Albizziin is an amino acid analog with activity as a competitive inhibitor of asparagine synthetase. Albizziin has been used to isolate Chinese hamster ovary cell mutants with altered levels of the target enzyme. Several mutational classes of albizziin can be distinguished based on cross-resistance to β-aspartic hydroxamic acid. Studies on asparagine synthetase have shown that resistance to albizziin may be associated with altered regulation of asparagine synthetase, structural mutations of the enzyme, and gene amplification .
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- HY-122936
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- HY-W744699
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(+)-Larixol
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Larix decidua Miller
Structural Classification
Natural Products
Pinaceae
Source classification
Plants
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Src
ERK
Akt
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Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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Optimized version of product available:
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Chemical Structure |
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- HY-124089S
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Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant[1][2].
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- HY-B0282S
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Acetylcholine-d4 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
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- HY-B0282S1
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Acetylcholine-d9 (chloride) is the deuterium labeled Acetylcholine chloride. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs)[1][2]. Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro[5].
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- HY-15772S1
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Osimertinib- 13C,d3 is the deuterium and 13C labeled Osimertinib. Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively.
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- HY-15772S
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Osimertinib-d6 is a deuterium labeled osimertinib. Osimertinib is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].
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- HY-14588S2
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Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). 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 .
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- HY-153951S
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BTK-IN-26 (compound 18) is a potent inhibitor of Bruton's tyrosine kinase (BTK) and its C481 mutant, with IC50 values of 0.7 and 0.8 nM for BTK and BTK C481S, respectively. BTK-IN-26 can be used for cancer and autoimmune diseases research .
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- HY-18690S
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Enasidenib-d6 (AG-221-d6)is the deuterium labeledEnasidenib(HY-18690) . 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 .
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- HY-10574S
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Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
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- HY-16767S1
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Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
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- HY-114436S
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MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). 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 .
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- HY-14588S1
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Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. 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[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
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- HY-151903S
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FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively[1].
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- HY-14588S
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(rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588) . 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 .
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- HY-15164AS
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Icotinib-d4 is the deuterium-labeled Icotinib (HY-15164A). Icotinib-d4 (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib-d4 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-13238S1
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Dolutegravir-d3 is the deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
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- HY-13238S2
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Dolutegravir-d5 is deuterium labeled Dolutegravir. Dolutegravir (S/GSK1349572) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir (S/GSK1349572) inhibits HIV-1 viral replication with an IC50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC50=3.6-5.8 nM)[1][2].
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- HY-134813
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MRTX1133
Maximum Cited Publications
13 Publications Verification
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective 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 .
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- HY-15164
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BPI-2009H
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Alkynes
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Icotinib Hydrochloride (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib (Hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-15164A
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BPI-2009
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Alkynes
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Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFR L858R, EGFR L858R/T790M, EGFR T790M and EGFR L861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-104066
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Xiliertinib; HMPL-309
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Alkynes
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Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-131033
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Azide
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L-Azidonorleucine hydrochloride, an unnatural amino acid, is A Methionine surrogate. L-Azidonorleucine hydrochloride can be used to label mammalian cell proteins and identify a diverse set of methionyl-tRNA synthetase (MetRS) mutants . L-Azidonorleucine (hydrochloride) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-159493
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Azide
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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 .
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- HY-149880
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Alkynes
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c-Met-IN-18 is ATP competitive type-III c-MET inhibitor of WT and D1228V mutant c-MET. c-Met-IN-18 has inhibitory for WT/D1228V with an IC50 value of 0.013/0.20 e.c-Met-IN-18 can be used for the research of c-MET driven cancers . c-Met-IN-18 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-167690
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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- HY-159476
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Azide
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KRAS inhibitor-26 (compound 194a) is a potent KRAS G12V inhibitor (IC50: ≤100 nM). KRAS inhibitor-26 can be used for cancer research .
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- HY-104066A
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Xiliertinib tartrate; HMPL-309 tartrate
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Alkynes
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Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-152233
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Azide
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Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-132609
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siRNAs
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Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis .
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- HY-145411
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Pegylated Lipids
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PEG2000-C-DMG, a pegylated lipid, can be used for the preparation of Onpattro. Onpattro, a hepatically directed investigational RNAi therapeutic agent, harnesses this process to reduce the production of mutant and wild-type transthyretin by targeting the 3′ untranslated region of transthyretin mRNA .
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- HY-153609
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siRNAs
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AS-Patisiran sodium is an antisense strand of Patisiran. Patisiran is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran can be used for the research of hereditary TTR amyloidosis .
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- HY-160044
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Aptamers
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Apt-M13 aptamer sodium is a mutant 33 nt aptamer based on the original aptamer for dexamethasone (HY-14648). Apt-M13 aptamer sodium can be combined with other nanomaterials for rapid detection of dexamethasone (HY-14648) .
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![PIP-C-3-Azaspiro[5.5]undecane-boc](http://file.medchemexpress.eu/product_pic/hy-161656.gif)
![[Ala28]-β Amyloid(25-35)](http://file.medchemexpress.eu/product_pic/hy-p5968.gif)
