Search Result
Results for "
wild-type
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
14
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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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-
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- HY-P2360
-
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Ras 5-17
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Ras
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Others
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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) .
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- HY-141715
-
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Antibiotic
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Infection
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BRD-8000.3, as a specific EfpA inhibitor, is a narrow-spectrum, bactericidal antimycobacterial agent with good wild-type activity. BRD-8000.3 can be used for the research of tuberculosis .
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-
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- HY-18936
-
-
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- HY-P2466
-
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Apoptosis
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Cancer
|
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Bax BH3 peptide (55-74), wild type is a 20-amino acid Bax BH3 peptide (Bax 1) capable of inducing apoptosis in a variety of cell line models .
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-
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- HY-108917A
-
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GLS4 mesylate
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HBV
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Infection
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Morphothiadin (GLS4) mesylate is a potent inhibitor of wild-type and Adefovir (HY-B1826)-resistant HBV replication with an IC50 value of 12 nM .
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-
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- HY-15352
-
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DPC 083
|
Reverse Transcriptase
HIV
|
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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-
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- HY-12083
-
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Bcr-Abl
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Cancer
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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) .
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-
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- HY-P2360A
-
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Ras 5-17 TFA
|
Ras
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Others
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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) .
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-
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- HY-118806
-
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mAChR
|
Neurological Disease
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AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
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-
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- HY-142645
-
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RSV
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Infection
|
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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).
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-
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- HY-149936
-
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HIV Protease
|
Infection
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HIV-1 protease-IN-8 (compound 34b) is a potent HIV-1 protease inhibitor with an IC50 value of 0.32 nM. HIV-1 protease-IN-8 displays IC50s of 0.29 μM and 1.90 μM for wild-type HIV-1 (HIV-1NL4-3) and drug-resistant variant (HIV-1MDR), respectively. HIV-1 protease-IN-8 displays robust antiviral activity against both wild-type HIV-1 and drug-resistant variant .
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-
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- HY-16271
-
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4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
|
MDM-2/p53
Apoptosis
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Cancer
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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 .
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- HY-14588
-
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ABT-378
|
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-E70404
-
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Biochemical Assay Reagents
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Others
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FastTaq DNA Polymerase (5'→3' exo-) is a modified DNA polymerase based on Taq DNA Polymerase. FastTaq DNA Polymerase (5'→3' exo-) lacks the 5'→3' exonuclease activity of wild-type Taq. It retains the 5'→3' DNA polymerase activity of wild-type Taq .
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- HY-115282A
-
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TRC-253
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Androgen Receptor
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Cancer
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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) .
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- HY-14588S2
-
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ABT-378-d7
|
HIV
SARS-CoV
HIV Protease
Isotope-Labeled Compounds
|
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-115282
-
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TRC-253 free base
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Androgen Receptor
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Cancer
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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) .
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- HY-164469
-
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Bcr-Abl
Apoptosis
STAT
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Cancer
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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) .
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- HY-150769
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HIV
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Inflammation/Immunology
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ZLM-66 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) with an IC50 of 41 nM for wild-type (WT) HIV-1 reverse transcriptase and an EC50 value of 13 nM for wild-type HIV-1. ZLM-66 is a Doravirine (HY-16767) analogs. ZLM-66 can be used for the research of AIDS .
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- HY-142952
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- HY-149480
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PROTACs
Estrogen Receptor/ERR
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Cancer
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ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
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- HY-108917
-
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GLS4
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HBV
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Infection
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Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir (HY-B1826)-resistant HBV with an IC50 of 12 nM.
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-
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- HY-10574
-
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R278474; TMC278; DB08864
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HIV
Reverse Transcriptase
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Infection
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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 .
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- HY-10574A
-
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TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride
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SARS-CoV
MMP
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Infection
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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 .
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- HY-19400
-
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DPH-153893
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HIV Protease
HIV
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Infection
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DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.
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- HY-153577
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-
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- HY-146108
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RSV
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Infection
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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) .
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- HY-17603
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-
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- HY-14844
-
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MIV-210
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HBV
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Infection
|
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Lagociclovir (FLG) is a nucleoside analogue that inhibits wild-type hepatitis B virus (HBV) replication in a human hepatoma cell line permanently expressing HBV .
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- HY-142953
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- HY-121392
-
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases .
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- HY-162680
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Influenza Virus
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Infection
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OSC-GCDI(P) is a broad-spectrum orally active anti-influenza virus agent that exhibits significant inhibitory effects against both wild-type and Oseltamivir (HY-13317) resistant (H275Y) influenza virus strains in mouse infection models. OSC-GCDI(P) is capable of preventing not only wild-type influenza viruses but also OS-resistant variants with NA(H275Y) .
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- HY-162590
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Bacterial
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Infection
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ECIN is a copper-responsive inhibitor of wild-type UPEC strains. ECIN inhibits Uropathogenic Escherichia coli (UPEC) with an IC50 value of 336 ng/mL in the absence of copper .
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- HY-128661
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-
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- HY-P4391
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-
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- HY-15728
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IY-5511
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Bcr-Abl
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Cancer
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Radotinib(IY-5511) is a novel and selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM for wild-type BCR-ABL1 kinase.
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- HY-10574AR
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SARS-CoV
MMP
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Infection
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Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. 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 .
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- HY-141807
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PROTACs
Akt
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Cancer
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MS21, a novel degrader of AKT, selectively inhibits the growth of PI3K/PTEN pathway-mutant cancers with wild-type KRAS and BRAF.
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- HY-144215
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HBV
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Inflammation/Immunology
|
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TLR8 agonist 4 showed effective inhibition on wild-type and drug-resistant (lamivudine and entecavir) HBV strains. The IC50 values are 0.15 and 0.10 respectively μM.
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- HY-18343A
-
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MDM-2/p53
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Cancer
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CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53 .
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- HY-158241
-
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Bacterial
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Infection
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GmhA-IN-1 (compound 17) is an inhibitor of GmhA with an IC50 value of 2.4 nM. GmhA-IN-1 enhances the activity of erythromycin and rifampicin on wild-type E. coli .
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- HY-114636
-
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Insecticide
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Others
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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 .
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- HY-13810
-
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Raf
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Cancer
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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 .
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- HY-139631
-
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HIV
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Infection
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HIV-1 inhibitor-9 is found to be potent inhibitor against the wild-type (WT) HIV-1 strain or multiple NNRTI-resistant strains at low nanomolar levels.
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- HY-16305
-
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1263W94; BW1263W94; GW257406X
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EBV
CMV
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Infection
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Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).
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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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-
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- HY-E70218
-
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Others
|
Others
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Cas9 Nuclease is cloned from wild-type Streptococcus pyogenes. Cas9 Nuclease can be used in the area of molecular diagnosis to achieve highly sensitive and specific detection of pathogens [1] .
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- HY-111079
-
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HIV
Reverse Transcriptase
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Others
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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.
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- HY-147580
-
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Btk
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Cancer
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BTK-IN-10 is a potent BTK inhibitor with IC50s of <5 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022012509A1; example 111) .
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- HY-13237
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- HY-W097867
-
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8-Methoxy-cipro
|
Bacterial
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Infection
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8-Methoxyciprofloxacin (8-Methoxy-cipro) induces DNA cleavage mediated by wild-type gyrase and Quinolone-resistant mutants. 8-Methoxyciprofloxacin can be used for research of drug resistance .
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- HY-132885
-
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PARP
Histone Methyltransferase
|
Cancer
|
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PARP/EZH2-IN-1 is a first-in-class dual PARP (IC50 6.87 nM) and EZH2 (IC50 36.51 nM) inhibitor for triple-negative breast cancer with wild-type BRCA.
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- HY-P99849
-
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ABT-806
|
EGFR
|
Cancer
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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 .
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- HY-120122
-
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MDM-2/p53
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Cancer
|
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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 .
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- HY-111627
-
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Nucleoside Antimetabolite/Analog
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Cancer
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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 .
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- HY-B0413
-
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Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
Cancer
|
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Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
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- HY-169428
-
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EGFR
|
Cancer
|
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EGFR-IN-138 (compound 19) is a potent EGFR inhibitor, with IC50s of 37, 2.6 and 1.9 nM for Wild-type, L858R and T790M EGFR, respectively .
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- HY-171181
-
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HBV
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Infection
|
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ZINC20451377 is a small molecule targeting hepatitis B (HBV) surface antigen (HBsAg) and can effectively inhibit wild-type hepatitis B and tenofovir (HY-13910)-resistant hepatitis B .
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- HY-P2319
-
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p38 MAPK
JNK
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Inflammation/Immunology
|
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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 .
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- HY-170830
-
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Bacterial
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Infection
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Mtb against-1 (compound 17af) is an inhibitor of Mycobacterium tuberculosis, with IC90 values of 1.2 μM and 0.9 μM for the wild-type and LepB low-deformation strains, respectively .
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- HY-106155
-
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DAPD
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HIV
Reverse Transcriptase
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Infection
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Amdoxovir (DAPD) is an orally active nucleoside reverse transcriptase inhibitor. Amdoxovir is active against wild-type and NRTl-resistant viruses. Amdoxovir is the prodrug of dioxolane guanosine. Amdoxovir can be used for research of HIV/AIDS .
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- HY-108508
-
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Smo
Hedgehog
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Cancer
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SMANT hydrochloride is a Smoothened (Smo) signaling inhibitor. SMANT hydrochloride is antagonist of Smo accumulation within the primary cilium (PC). SMANT hydrochloride has an equivalent activity in inhibiting SmoM2 (oncogenic form of Smo) and wild-type Smo .
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- HY-125144
-
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Na+/H+ Exchanger (NHE)
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Cardiovascular Disease
|
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BIIB 513 is an inhibitor of NHE 1 that protects against myocardial ischemia. BIIB 513 inhibits acid load recovery with an IC50 of 27 nmol/L in cells expressing wild-type NHE 1 under acute acid load .
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- HY-15714
-
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p97
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Cancer
|
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NMS-859 is a potent, covalent VCP (p97) inhibitor, with IC50s of 0.37 and 0.36 μM for wild-type VCP in the presence of 60 μM and 1 mM ATP in cells, respectively.
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-
- HY-112306
-
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DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
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Cancer
|
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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 .
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- HY-100818
-
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TAS-120
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FGFR
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Cancer
|
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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) .
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- HY-10468
-
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2'-C-Methylcytidine
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HCV
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Infection
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NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC50 of NM107 in the wild-type replicon cells is 1.85 μM .
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- HY-P2319A
-
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p38 MAPK
JNK
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Inflammation/Immunology
|
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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 .
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- HY-N12399
-
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PKA
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Inflammation/Immunology
|
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Aplithianines A is a potent inhibitor against J-PKAcα with an IC50 of 1 μM , and inhibits wild-type PKA with an IC50 of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the ATP pocket .
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- HY-146394
-
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HBV
DNA/RNA Synthesis
|
Infection
|
|
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 μM and 0.84 μM against wild-type and agent resistant HBV strains, respectively .
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-
- HY-10572
-
-
- HY-18634
-
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ZMC1
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MDM-2/p53
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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.
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-
- HY-147582
-
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Btk
|
Cancer
|
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BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8) .
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-
- HY-P4926
-
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Amyloid-β
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Neurological Disease
|
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Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research .
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- HY-B0413S
-
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HIF/HIF Prolyl-Hydroxylase
Parasite
Microtubule/Tubulin
Antibiotic
|
Infection
|
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Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].
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-
- HY-13223A
-
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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.
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-
- HY-169427
-
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EGFR
|
Cancer
|
|
FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively .
|
-
- HY-134877
-
|
|
EGFR
|
Cancer
|
|
BAY 2476568 is a potent and selective EGFR inhibitor, with IC50s of < 0.2 nM for wild-type EGFR and several mutations (EGFRR ex20insSVD, EGFRR ex20insASV, EGFRR ex20insNPG) .
|
-
- 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-156712
-
|
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
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 .
|
-
- HY-168151
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-128 (compund 28) is a potent and selective molecule targeting wild-type EGFR Ex20Ins that demonstrates efficacy in multiple human xenograft models and can cross the blood-brain barrier in preclinical species .
|
-
- HY-N2894
-
|
|
Parasite
|
Infection
|
|
Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani .
|
-
- 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-B0413R
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-136173
-
|
TNO155
|
SHP2
Phosphatase
|
Cancer
|
Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors .
|
-
- HY-155048
-
|
|
Bacterial
|
Infection
|
|
BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC90 of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .
|
-
- 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-144105
-
|
|
MDM-2/p53
|
Cancer
|
|
NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53 .
|
-
- HY-105249
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
RDEA 806 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits potent in vitro inhibitory activity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistant HIV-1 .
|
-
- HY-116833
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
4-Chloro-3,5-dimethylphenoxyacetic acid (compound 602 UC) is a product of masked amide bond hydrolysis of auxin analog 602 (compound 602). Auxin can effectively stimulate hypocotyl growth in wild-type seedlings .
|
-
- 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-162698
-
|
|
Thymidylate Synthase
|
Cancer
|
|
JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC50s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo .
|
-
- HY-167948
-
|
|
EGFR
|
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-111396
-
|
|
Bacterial
|
Infection
|
|
PC58538 is a cell division inhibitor, targeting to FtsZ. PC58538 shows moderate antibacterial activity, and inhibits cell division in vegetative cells of wild-type B. subtilis. PC58538 is also known to modulate the rate of GTP hydrolysis .
|
-
- 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-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-16305S
-
|
1263W94-d6; BW1263W94-d6; GW257406X-d6
|
Isotope-Labeled Compounds
|
Others
|
|
Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
|
-
- 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-16305R
-
|
|
EBV
CMV
|
Infection
|
|
Maribavir (Standard) is the analytical standard of Maribavir. This product is intended for research and analytical applications. Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).
|
-
- HY-N7433
-
|
Ethylidene-glucose
|
GLUT
Endogenous Metabolite
|
Metabolic Disease
|
|
4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a Ki of 12 mM for wild-type 2-deoxy-D-glucose transport .
|
-
- HY-162461
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
|
-
- 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-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-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-135815
-
|
TAK-788; AP32788
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .
|
-
- HY-168344
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
CACPD2011a-0001278239 is a β2AR mixed agonist that shows a wide range of high-affinity binding to both wild-type and T164I β2AR variants, with no cytotoxicity or mutagenicity, making it suitable for asthma research .
|
-
- 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-135815B
-
|
TAK-788 mesylate; AP32788 mesylate
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research .
|
-
- HY-10572B
-
-
- HY-150697
-
|
|
HIV
|
Others
|
|
HIV-1 inhibitor-44 (compound 11l) is a HIV-1 reverse transcriptase inhibitor. HIV-1 inhibitor-44 shows inhibitory activity against wild-type HIV-1 strain with an EC50 value of 0.209 μM .
|
-
- 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-159984
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-78 (compound 15f) is a potent and broad-spectrum non-nucleoside reverse transcriptase inhibitor, with an EC50 of 3 nM for wild-type HIV-1. HIV-1 inhibitor-78 can be used for the research of HIV infection .
|
-
- HY-147650
-
|
|
HIV Protease
|
Infection
|
|
HIV-1 protease-IN-5 (Compound 13c) is a HIV-1 protease inhibitor with an IC50 of 1.64 nM. HIV-1 protease-IN-5 shows remarkable activity against wild-type and DRV-resistant HIV-1 variants .
|
-
- 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-162595A
-
|
|
Bacterial
|
Infection
|
|
BDM88855 hydrochloride is an allosteric inhibitor for the homolog AcrB protein. BDM88855 hydrochloride can boost the antibacterial effect of a panel of antibiotics (eg: Oxacillin (HY-B0925A), Linezolid (HY-10394), Novobiocin (HY-B0425), etc.) on wild-type E. coli .
|
-
- HY-162595
-
|
|
Bacterial
|
Infection
|
|
BDM88855 is an allosteric inhibitor for the homolog AcrB protein. BDM88855 can boost the antibacterial effect of a panel of antibiotics (eg: Oxacillin (HY-B0925A), Linezolid (HY-10394), Novobiocin (HY-B0425), etc.) on wild-type E. coli .
|
-
- 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-118742
-
|
|
HPPD
|
Others
|
|
Benzobicyclon is a 4-HPPD inhibitor and herbicide that reacts with water to form a hydrolysate of the active herbicide benzobicycline, causing bleaching and death of weeds. Benzobicyclon is effective against grass, sedge and broadleaf weeds. Benzobicyclon effectively targets sulfonylurea herbicide-resistant biotypes as well as wild-type weeds .
|
-
- HY-164529
-
|
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
|
-
- HY-14361
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
MK-4965 is a nonnucleoside reverse transcriptase inhibitor (NNRTI). MK-4965 displays excellent activities against not only HIV-1 wild-type (WT) virus but also against a broad panel of NNRTI-resistant viruses and can be used for the research of HIV-1 infection .
|
-
- HY-135815A
-
|
TAK-788 succinate; AP32788 succinate
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research .
|
-
- HY-14267
-
|
UK-453061
|
HIV
Reverse Transcriptase
|
Infection
|
|
Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC50=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains .
|
-
- HY-10572S1
-
-
- HY-10572R
-
|
DMP 266 (Standard); EFV (Standard); L-743726 (Standard)
|
Reverse Transcriptase
HIV
Autophagy
Endogenous Metabolite
Parasite
|
Infection
Cancer
|
|
Efavirenz (Standard) is the analytical standard of Efavirenz. This product is intended for research and analytical applications. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture .
|
-
- 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-114737
-
|
|
Bacterial
|
Infection
|
|
L-573655 is a reversible inhibitor of UDP-3-O-[R-3-hydroxymyristoyl]-GlcNAc deacetylase with an IC50 value of 8.5 μM. L-573655 possesses antibacterial activity against a wild-type strain of E. coli. with MIC values of 200-400 μg/mL .
|
-
- HY-154966
-
|
|
RSV
|
Infection
|
|
RSV L-protein-IN-3 is a wild-type RSV polymerase inhibitor with an IC50 value of 10.4 μM and an EC50 value of 2.1 μM (against RSV). RSV L-protein-IN-3 has lesser cytotoxicity than the clinical agent, Ribavirin (HY-B0434) .
|
-
- 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-135184
-
|
CBR-2092; TNP-2092
|
Antibiotic
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
Rifaquizinone (CBR-2092) is a Rifamycin-Quinolone Hybrid Antibiotic. Rifaquizinone inhibits wild-type S. aureus RNA polymerase with an IC50 of 34 nM. Rifaquizinone is effective against S. aureus infections, with MICs ranged from 0.008 to 0.5 μg/mL for 300 clinical isolates of staphylococci and streptococci .
|
-
- HY-144279
-
|
|
Bacterial
|
Infection
|
|
MsbA-IN-1 is a highly potent MsbA inhibitor with IC50 of 4 nM. MsbA-IN-1 has activity against wild-type E. coli with MIC of 79 μM. MsbA-IN-1 possesses sufficient permeability across the fully intact outer membrane of Gram-negative bacteria to inhibit MsbA .
|
-
- HY-12580
-
|
|
MDM-2/p53
|
Cancer
|
|
RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
|
-
- HY-153390
-
|
|
Histone Methyltransferase
|
Cancer
|
|
AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
|
-
- HY-139279
-
|
TPX-0131
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities .
|
-
- 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 .
|
-
- HY-144297
-
|
|
HDAC
Parasite
|
Infection
|
|
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites .
|
-
- HY-135892
-
|
|
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 .
|
-
- 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-12025
-
|
JNJ-26854165
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes .
|
-
- HY-W740378
-
|
AFN-941
|
EGFR
JAK
|
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).
|
-
- HY-P1088
-
|
|
PKC
|
Others
|
|
[Ser25] Protein Kinase C (19-31) is a substrate of protein kinase C (PKC) (Km: 0.3 μM). [Ser25] Protein Kinase C (19-31) is derived from the pseudo-substrate regulatory domain of PKCα (19-31) with a Serine at position 25 replacing the wild-type Alanine .
|
-
![[Ser25] Protein Kinase C (19-31)](//file.medchemexpress.eu/product_pic/hy-p1088.gif)
- HY-157887
-
|
|
Ras
|
Cancer
|
|
ADT-007 is a potent and orally active pan-RAS inhibitor with strong anticancer effects. ADT-007 binds RAS in a nucleotide-free conformation to block GTP activation. ADT-007 potently and selectively inhibits the growth of cancer cells with mutated or hyper-activated wild-type RAS isozymes .
|
-
- HY-P99496
-
|
RPC 4046; ABT 308; CC-93538
|
Interleukin Related
|
Inflammation/Immunology
|
|
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
|
-
- HY-126720
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
N-Lignoceroyl Taurine is an arachidonoyl amino acid and taurine conjugate with a fatty acid that can be isolated from bovine brain. N-Lignoceroyl Taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of the brain and spinal cord of wild-type and fatty acid amide hydrolase (FAAH) knockout mice. N-Lignoceroyl Taurine levels were 23-26-fold higher in FAAH -/- mice compared to wild-type mice, suggesting that FAAH utilizes N-Lignoceroyl Taurine as a substrate. However, in vitro experiments with purified FAAH showed that N-Lignoceroyl Taurine was hydrolyzed 2,000-fold slower in FAAH compared to oleoylethanolamide. N-Acyl Taurines with polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) calcium channel family, including TRPV1 and TRPV4.
|
-
- HY-123450
-
|
|
Bcr-Abl
Apoptosis
PDGFR
|
Cancer
|
|
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies . S116836 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-134813
-
|
|
Ras
|
Cancer
|
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based 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-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-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-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-148089
-
|
|
Transthyretin (TTR)
|
Neurological Disease
|
|
Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases .
|
-
- HY-134823
-
|
|
MDM-2/p53
PROTACs
E1/E2/E3 Enzyme
|
Cancer
|
|
MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects .
|
-
- HY-152292
-
|
NVL-520; NUV-520
|
ROS Kinase
|
Cancer
|
|
Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer .
|
-
- 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-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-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-15011
-
|
|
Oxytocin Receptor
|
Others
|
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
|
-
- HY-103320
-
|
|
CaSR
|
Metabolic Disease
|
|
Calhex 231 is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- HY-148089A
-
|
|
Transthyretin (TTR)
|
Neurological Disease
|
|
Eplontersen sodium is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases .
|
-
- 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-103320A
-
|
|
CaSR
|
Metabolic Disease
|
|
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- 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-117764
-
|
|
mGluR
|
Neurological Disease
|
|
LSP4-2022 is a potent and brain-penetrant mGlu4-selective orthosteric agonist, with an EC50 of 0.11 μM. LSP4-2022 inhibits neurotransmission in cerebellar slices from wild-type but not mGlu4 receptor-knockout mice. LSP4-2022 shows pro-depressant activity .
|
-
- HY-W110242A
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
(S)-CPP sodium serves as an inhibitor of the branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase, commonly referred to as BDK or keto acid dehydrogenase kinase. As a negative regulator of BCKDC activity, the inhibition of BDK by (S)-CPP (with an IC50 of 6.3 μM) results in the activation of the complex and a notable decrease in plasma levels of leucine/isoleucine and valine in wild-type mice.
|
-
- HY-100131
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser 166 phosphorylation in wild-type human RIP1 (IC50=2.8 nM). GSK481 also exhibits excellent translation in the U937 cellular assay with an IC50 of 10 nM .
|
-
- 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-168616
-
|
|
RSV
IGF-1R
|
Infection
|
|
CL-A3-7 is a virus-cell fusion inhibitor targeting the RSV F protein. It exerts its effect by blocking the interaction between the virus and the host IGF1R, effectively inhibiting infections of both wild-type RSV and the K394R variant. It is applicable to anti-RSV drug development and resistance-related research .
|
-
- HY-W050122
-
|
|
GABA Receptor
|
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-118806A
-
|
|
mAChR
|
Neurological Disease
|
|
AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
|
-
- HY-113849
-
|
MLS000573151
|
Ras
|
Inflammation/Immunology
|
|
MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42 .
|
-
- HY-121845
-
|
|
HSP
|
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-B0792
-
|
|
LRRK2
|
Neurological Disease
|
|
CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity .
|
-
- HY-161067
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFR T790M .
|
-
- HY-118742R
-
|
|
HPPD
|
Others
|
|
Benzobicyclon (Standard) is the analytical standard of Benzobicyclon. This product is intended for research and analytical applications. Benzobicyclon is a 4-HPPD inhibitor and herbicide that reacts with water to form a hydrolysate of the active herbicide benzobicycline, causing bleaching and death of weeds. Benzobicyclon is effective against grass, sedge and broadleaf weeds. Benzobicyclon effectively targets sulfonylurea herbicide-resistant biotypes as well as wild-type weeds .
|
-
- HY-10572BR
-
|
|
Autophagy
Parasite
HIV
Endogenous Metabolite
Reverse Transcriptase
|
Infection
Cancer
|
|
(Rac)-Efavirenz (Standard) is the analytical standard of (Rac)-Efavirenz. This product is intended for research and analytical applications. (Rac)-Efavirenz is the isomer of Efavirenz (HY-10572). Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture .
|
-
- 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-128590
-
PHT-7.3
1 Publications Verification
|
Ras
|
Cancer
|
|
PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain (Kd=4.7 μM). PHT-7.3 inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling. PHT-7.3 has antitumor activity .
|
-
- HY-148106
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription .
|
-
- HY-15041
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
NVP-SAA164 is an orally active nonpeptide kinin B1 receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .
|
-
- HY-108704
-
|
|
Bcr-Abl
|
Cancer
|
|
CT-721 is a potent and time-dependent Bcr-Abl kinase inhibitor with an IC50 of 21.3 nM for wild-type Bcr-Abl kinase, and possesses anti-chronic myeloid leukemia (CML) activities . CT-721 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-B0792A
-
|
|
LRRK2
|
Neurological Disease
|
|
CZC-54252 hydrochloride is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 hydrochloride with an EC50 of ~1 nM.CZC-54252 hydrochloride has a neuroprotective activity .
|
-
- HY-P99715
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC50s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFR C271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers .
|
-
- HY-107123
-
|
ASC-09
|
HIV Protease
|
Infection
|
|
TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity .
|
-
- HY-19816A
-
|
Abivertinib maleate; AC0010 maleate
|
EGFR
Btk
Apoptosis
|
Cancer
|
|
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-149991
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-56 (compound 12126065) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC50 value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier .
|
-
- HY-149099
-
|
|
RET
|
Cancer
|
|
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
|
-
- HY-W747072
-
|
3-Sulfocholyl Taurine; TCA3S
|
Drug Metabolite
|
Metabolic Disease
|
|
3-Sulfo-taurocholic Acid Disodium Salt (3-Sulfocholyl Taurine; TCA3S) is a metabolite of the conjugated bile acid taurocholic acid. Plasma levels of 3-Sulfo-taurocholic Acid Disodium Salt are elevated in wild-type and Sortilin 1 (Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated in Sort1 knockout mice at 24 hours post-BDL.
|
-
- HY-19816
-
|
Abivertinib; AC0010
|
EGFR
Btk
Apoptosis
|
Cancer
|
|
Avitinib (Abivertinib) is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects .
|
-
- HY-164427
-
|
|
SHP2
ERK
|
Cancer
|
|
SHP2-IN-31 is a SHP2 inhibitor, with IC50s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .
|
-
- HY-138842
-
|
|
Insulin Receptor
Akt
ERK
|
Metabolic Disease
|
|
DDN is a selective insulin receptor (Insulin Receptor) activator, an insulin sensitizer, and a glucose-lowering insulin mimetic with oral bioavailability. DDN can directly bind to the receptor kinase domain and induce Akt and ERK phosphorylation, and it can also enhance insulin's effect on glucose uptake. DDN significantly reduces blood glucose levels in wild-type and diabetic ob/ob and db/db mice .
|
-
- HY-155114
-
|
|
HIV
|
Infection
|
|
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) .
|
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-16745A
-
|
KRP-AM1977 hydrochloride
|
Bacterial
|
Infection
|
|
Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitory activity against both wild-type and mutated target enzymes.
|
-
- 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-153390A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
(R)-AMG-193 is an isomer of AMG 193 (HY-153390). AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
|
-
- HY-153856
-
|
|
EGFR
|
Cancer
|
|
TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
- HY-139995
-
|
|
Drug Intermediate
|
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-153856A
-
|
|
EGFR
|
Cancer
|
|
TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
- 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-169327
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
MD-265 is a PROTAC degrader that can break down MDM2, leading to activation of p53 in cancer cells carrying wild-type p53. MD-265 achieves complete tumor regression and improves long-term survival of mice with leukemia. (Pink: MI-1063 (HY-133754); Black: linker; Blue: Lenalidomide (HY-A0003) .
|
-
- HY-168427
-
|
Abivertinib maleate dihydrate; AC0010 maleate dihydrate
|
EGFR
Btk
Apoptosis
|
Cancer
|
|
Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects .
|
-
- HY-51424
-
|
|
Raf
|
Cancer
|
|
PLX-4720 is a potent and selective inhibitor of B-Raf V600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-Raf V600E than wild-type B-Raf.
|
-
- HY-19840
-
|
GS-9857
|
HCV Protease
|
Infection
Cancer
|
|
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively . Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research .
|
-
- HY-168447
-
|
|
Bacterial
|
Infection
|
|
D-PheTrAP is a bisubstrate analog inhibitor of 1-Deoxy-d-xylulose 5-phosphate synthase (DXPS). D-PheTrAP inhibits Escherichia coli DXPS (EcDXPS) and Pseudomonas aeruginosa DXPS (PaDXPS) with IC50 values of 0.52 μM, 2.1 μM, 2.4 μM, and 1.7 μM for wild-type (WT) EcDXPS, EcA426E, WT PaDXPS, and PaE431A, respectively .
|
-
- 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-159479
-
|
|
Parasite
|
Infection
|
|
PfSUB1-IN-1 (compound 4c) is a plasmodium falciparum subtilisin-like serine protease 1 (PfSUB1) Inhibitor (IC50: 15 nM). PfSUB1 is an antimalarial target. PfSUB1-IN-1 inhibits the growth of a genetically modified P. falciparum line expressing reduced levels of PfSUB1 13-fold more efficiently compared to a wild-type parasite line .
|
-
- HY-151380
-
|
|
HSV
|
Infection
|
|
LANA-DNA-IN-1 is a potent LANA-DNA inhibitor. LANA-DNA-IN-1 has inhibition activity for LBS2, LBS1 and LBS3 with IC50 values of 8 μM, 9μM and 8μM. LANA-DNA-IN-1shows against wild-type LANA with IC50 value of 53 μM. LANA-DNA-IN-1 can be used for the research of infection .
|
-
- 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-131312A
-
|
LY3410738 (gentisate); Mutant IDH1-IN-6 (gentisate)
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes .
|
-
- HY-10035
-
TTA-P2
3 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-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-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-16999
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
|
-
- 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-145594
-
|
AB-291; DS-1001
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Safusidenib (AB-291; DS-1001) is an orally bioavailable, selective mutant IDH1 inhibitor. Safusidenib strongly inhibits mutant IDH1 but not wild-type IDH1. Safusidenib impairs tumor activity in chondrosarcoma . Safusidenib exhibits activity against IDH1R132H, and IDH1R132C with IC50s of 15, and 130 nM in assays without any preincubation, respectively .
|
-
- HY-116749
-
|
BBSKE
|
TrxR
|
Cancer
|
|
Ethaselen (BBSKE) is an orally active, selective thioredoxin reductase (TrxR) inhibitor with IC50s of 0.5 and 0.35 μM for the wild-type human TrxR1 and rat TrxR1, respectively. Ethaselen specifically binds to the unique selenocysteine-cysteine redox pair in the C-terminal active site of mammalian TrxR1. Ethaselen, an organoselenium compound, is a potent antitumor candidate that exerts potent inhibition on non-small cell lung cancer (NSCLC) by targeting TrxR .
|
-
- HY-18343
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
|
-
- HY-131062
-
|
|
Others
|
Metabolic Disease
|
|
yGsy2p-IN-1 is a potent inhibitor for yeast glycogen synthase 2 (yGsy2p). yGsy2p-IN-1 is a competitive human glycogen synthase 1 (hGYS1) inhibitor with an IC50 of 2.75 μM and a Ki of 1.31 μM for wild-type hGYS1. yGsy2p-IN-H23 a pyrazole inhibitor, is used for glycogen storage diseases (GSDs) .
|
-
- 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-125028
-
|
|
Src
HIV
|
Infection
|
|
Hck-IN-1 (compound B9), a diphenylpyrazolo compound, is a selective Nef-dependent Hck inhibitor with IC50s of 2.8 μM, >20 μM for Nef:Hck complex and Hck, respectively. Hck-IN-1 is a direct and wide HIV-1 Nef antagonists with an IC50 of 100-300 nM for wild-type HIV-1 replication. Hck-IN-1 binds pocket residue Asn126 and has anti-retroviral activity .
|
-
- HY-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
|
-
- HY-17396R
-
|
|
Fungal
Antibiotic
|
Infection
|
|
Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. 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-10029
-
|
Rebemadlin
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
|
Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53?interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53?wild-type ovarian carcinomas .
|
-
- HY-149350
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-57 (Compound 12g) is a HIV inhibitor. HIV-1 inhibitor-57 is active against wild-type and five prevalent NNRTI-resistant HIV-1 strains with EC50 values ranging from 0.024 to 0.0010 μM. HIV-1 inhibitor-57 forms additional interactions with residues around the binding site in HIV-1 RT .
|
-
- HY-10029A
-
|
(Rac)-Rebemadlin
|
MDM-2/p53
Autophagy
Apoptosis
E1/E2/E3 Enzyme
|
Cancer
|
|
(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas .
|
-
- 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-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-13001
-
|
AC220; AC708
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
|
Cancer
|
|
Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
|
-
- 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-117540
-
|
|
Histone Methyltransferase
|
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-131312
-
|
LY3410738; Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
|
-
- 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-19617A
-
|
|
EGFR
|
Cancer
|
|
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 .
|
-
- 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-10572BS
-
|
|
Isotope-Labeled Compounds
Reverse Transcriptase
HIV
Autophagy
|
Infection
Cancer
|
|
(Rac)-Efavirenz-d4 is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. (Rac)-Efavirenz-d4 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-100218B
-
|
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
(1R,3S)-RSL3 is the less active (1R,3S)-enantiomer of RSL3 ((1S,3R)-RSL3). (1R,3S)-RSL3 and RSL3 induce cell death in HT22 wild-type cells with EC50 values of 5.2 µM and 0.004 µM, rspectively .
|
-
- 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-122038
-
|
|
MDM-2/p53
|
Cancer
|
|
NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines .
|
-
- HY-10412
-
|
KT7515
|
JNK
Mixed Lineage Kinase
MDM-2/p53
|
Neurological Disease
|
|
CEP-1347 is an inhibitor of the JNK/SAPK pathway with neuroprotective effects. CEP-1347 blocks JNK1 activation induced by members of the mixed lineage kinase (MLK) family (MLK3, MLK2, MLK1, dual leucine zipper kinase, and leucine zipper kinase). As an inhibitor of MDM4, CEP-1347 can more effectively inhibit the growth of glioma cells expressing wild-type p53 .
|
-
- HY-167710
-
|
|
Endogenous Metabolite
|
Cancer
|
|
CRCD2 is a small molecule NT5C2 nucleotidase inhibitor with enhanced 6-mercaptopurine cytotoxic activity. CRCD2 can effectively reverse 6-mercaptopurine resistance caused by mutations in the NT5C2 gene or non-genetic activation mechanisms. CRCD2 combined with 6-mercaptopurine can enhance its cytotoxic activity in NT5C2 wild-type leukemia, showing its potential in the treatment of acute lymphoblastic leukemia .
|
-
- HY-B1902
-
|
EGIS-5645
|
Antifolate
Bacterial
|
Infection
|
|
Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
|
-
- HY-136242
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
|
-
- HY-13488
-
|
|
LRRK2
MNK
|
Neurological Disease
|
|
HG-10-102-01 is a highly potent, selective, and brain-penetrable LRRK2 inhibitor, with IC50 values of 20.3 and 3.2 nM against wild-type LRRK2 and LRRK2[G2019S], respectively. HG-10-102-01 also inhibits MNK2 and MLK1, with IC50 values of 0.6 and 2.1 μM. HG-10-102-01 can be used for Parkinson's disease (PD) research .
|
-
- HY-14588S1
-
|
|
Isotope-Labeled Compounds
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-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-162033
-
|
|
Chloride Channel
|
Others
|
|
PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF .
|
-
- HY-51424S
-
|
|
Raf
|
Cancer
|
|
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-RafV600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
|
-
- 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-19617B
-
|
|
EGFR
|
Cancer
|
|
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 .
|
-
- HY-19617
-
|
|
EGFR
|
Cancer
|
|
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 .
|
-
- HY-10572S
-
|
|
Reverse Transcriptase
HIV
Autophagy
|
Infection
Cancer
|
|
Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. Efavirenz-d5 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-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-U00437
-
-
- HY-16664
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
|
-
- HY-50707
-
|
(Rac)-T-type calcium channel inhibitor
|
Calcium Channel
Drug Isomer
|
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-14588S
-
|
(rel)-ABT-378-d8
|
Isotope-Labeled Compounds
HIV Protease
SARS-CoV
HIV
|
Others
|
|
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium 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 .
|
-
- HY-141640
-
|
|
PROTACs
EGFR
|
Cancer
|
|
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 induces the degradation of mutant but not wild-type EGFR in an E3 ligase-dependent manner in cancer cell lines. MS154 potently inhibits cell proliferation in lung cancer cells (Blue: E3 Ligase ligand (HY-103596); Black: linker (HY-W096167); Pink: EGFR ligand (HY-168305)) .
|
-
- HY-13001R
-
|
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
Autophagy
|
Cancer
|
|
Quizartinib (Standard) is the analytical standard of Quizartinib. This product is intended for research and analytical applications. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .
|
-
- HY-137488
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
|
-
- 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 .
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-
- HY-10035A
-
|
|
Calcium Channel
|
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-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-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-14217
-
|
AC220 dihydrochloride
|
FLT3
Apoptosis
Ligands for Target Protein for PROTAC
|
Cancer
|
|
Quizartinib dihydrochloride (AC220 dihydrochloride) is the dihydrochloride salt form of Quizartinib (HY-13001). Quizartinib dihydrochloride is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib dihydrochloride inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib dihydrochloride can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib dihydrochloride induces apoptosis .
|
-
- HY-131864
-
|
|
EGFR
PROTACs
|
Cancer
|
|
SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 also degrades HER2 (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .
|
-
- HY-12928
-
|
|
Virus Protease
|
Infection
|
|
ML336 is quinazolinone-based inhibitor against venezuelan equine encephalitis virus (VEEV), with IC50s of 32, 20, and 42 nM for VEEV TC-83 CPE , VEEV V3526 CPE, VEEV Wild Type CPE, respectively. ML336 potently inhibits a VEEV-induced cytopathic effect in three strains of the virus (TC-83, V3526, and wild type Trinidad donkey) in the low nanomolar range .
|
-
- 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-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-143894
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM) .
|
-
- HY-13803
-
Tazemetostat
Maximum Cited Publications
65 Publications Verification
EPZ-6438; E-7438
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .
|
-
- 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-13775
-
XL019
5 Publications Verification
|
JAK
Apoptosis
|
Cancer
|
|
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
|
-
- HY-131909
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
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 .
|
-
- HY-155965
-
|
|
VEGFR
PARP
Apoptosis
|
Cancer
|
|
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC50s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC50: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .
|
-
- HY-17041
-
|
TMC114 Ethanolate
|
HIV
HIV Protease
|
Infection
|
|
Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
|
-
- HY-116973
-
|
|
HIV
|
Infection
|
|
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
|
-
- HY-131864A
-
|
|
PROTACs
EGFR
|
Cancer
|
|
SJF-1528 hemihydrate is the hemihydrate form of SJF-1528 (HY-131864). SJF-1528 hemihydrate is a EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 hemihydrate also degrades HER2. (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
|
-
- 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-153990
-
|
|
FKBP
|
Neurological Disease
|
|
FKBP51F67V-selective antagonist Ligand2 (example 3-3) is a potent FKBP51 F67V-selective antagonist ligand. FKBP51F67V-selective antagonist Ligand2 reverses the anxiogenic phenotype induced by overexpression of FKBP51 F67V in the amygdala. FKBP51F67V-selective antagonist Ligand2 binds to FKBP51 F67V, but not to wild-type FKBP51 or FKBP52 .
|
-
- 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-164694
-
|
|
EGFR
|
Cancer
|
|
Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively .
|
-
- HY-128131
-
|
|
Endogenous Metabolite
|
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-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-B1902R
-
|
|
Antifolate
Bacterial
|
Infection
|
|
Diaveridine (Standard) is the analytical standard of Diaveridine. This product is intended for research and analytical applications. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
|
-
- HY-171252
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase .
|
-
- 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-109014
-
|
CMX-157
|
HIV
HBV
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
|
-
- HY-13803R
-
|
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
Tazemetostat (Standard) is the analytical standard of Tazemetostat. This product is intended for research and analytical applications. Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .
|
-
- HY-P5437
-
|
|
PKC
|
Others
|
|
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
|
-
- HY-164466
-
|
|
Calcium Channel
Notch
|
Cancer
|
|
CAD204520, a SERCA inhibitor (IC50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL) .
|
-
- 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-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-121611
-
|
|
HIV
|
Inflammation/Immunology
|
|
HI-236 is a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase.?
HI-236 inhibits HIV activity (wild type HTLVIIB IC50p24 < 0.001 μM) .
|
-
- HY-146262
-
|
|
EGFR
|
Cancer
|
|
LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .
|
-
- HY-B0255
-
-
- HY-B1902S
-
|
EGIS-5645-d6
|
Isotope-Labeled Compounds
Antifolate
Bacterial
|
Infection
|
|
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
|
-
- 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-147988
-
|
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
DNA Gyrase-IN-5 (Compound 8I-w) is a potent DNA gyrase inhibitor with an IC50 of 0.10 μM. DNA Gyrase-IN-5 shows antibacterial activities against wild type and drug-resistant strains .
|
-
- 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-120828
-
|
CJC 1134PC
|
GLP Receptor
|
Metabolic Disease
|
|
Albenatide (CJC 1134PC) is a modified Exendin-4 (HY-13443) analogue conjugated to human recombinant albumin (HRA) in vitro to form a long-acting DPP-4-resistant GLP-1R agonist. Albenatide covalently binds through a low-molecular chemical linker (cys-C13H19O6N3-lys) to the cysteine residue in position 34 of HRA. Albenatide increases cyclic AMP (cAMP) production in vitro. Albenatide reduces glucose excursions, food intake, gastric emptying in wild-type mice and improves glucose tolerance and reduces body weight in high-fat diet mice .
|
-
- HY-173163
-
|
|
Bacterial
|
Infection
|
|
(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) (Compound 4a) is a Gram-negative outer membrane permeabilizer with synergistic antibacterial activity through the blockage on LptA/LptC interaction via targeting Met47 in LptA. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) potentiates pol B against both wild-typed and MDR A. baumannii and E. coli strains. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) can be used as antibiotic adjuvants against MDR Gram-negative bacteria .
|
-
- 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-N5109
-
|
|
Parasite
|
Infection
|
|
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively .
|
-
- HY-162477
-
|
|
Cathepsin
Apoptosis
|
Cancer
|
|
TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
|
-
- HY-119691
-
|
LY582563; MCC-478
|
HBV
|
Infection
|
|
Alamifovir (LY582563; MCC-478), a purine nucleotide analogue proagent, shows potent activity against wild type and lamivudine resistant hepatitis B virus (HBV). Alamifovir has high activity against HBV replication and sustained antiviral effect .
|
-
- HY-17041R
-
|
|
HIV
HIV Protease
|
Infection
|
|
Darunavir (Ethanolate) (Standard) is the analytical standard of Darunavir (Ethanolate). This product is intended for research and analytical applications. Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
|
-
- HY-119396
-
|
|
Endogenous Metabolite
|
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-112363
-
|
RP107
|
CDK
GSK-3
ERK
JNK
CFTR
|
Inflammation/Immunology
Cancer
|
|
Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research .
|
-
- HY-115701
-
|
1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-phosphoethanolamine; 15(S)-HpETE-SAPE; 15(S)-hydroperoxyeicostetraenoic acid-SAPE
|
Ferroptosis
|
Inflammation/Immunology
|
|
1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-Pe (SAPE) by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.
|
-
- 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-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-117556
-
|
|
HIV
|
Infection
|
|
U-104489 is a HIV-1 inhibitor with the Ki values of 0.13, 0.12 and ＞ 100 μM aganist HIV-1 RT p66/p51 wild type (G190), G190A and G190E, respectively .
|
-
- 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-142679
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-22 is a potent EGFR inhibitor with IC50s of 4.91 nM and 0.54 nM for wild type EGFR and EGFR L858R/T790M/C797S, respectively (CN112538072A, compound 243) .
|
-
- 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-N5005
-
|
Atisinium chloride
|
Parasite
|
Infection
|
|
Guanfu base H (Atisinium chloride) is a diterpenoid alkaloid isolated from Aconitum coreanum and has antiplasmodial activity against the malarial Plasmodium falciparum strains TM4/8.2 (wild type) and K1CB1 with IC50 values of 4 μM and 3.6 μM, respectively .
|
-
- HY-B0255R
-
|
|
HBV
Reverse Transcriptase
Orthopoxvirus
Endogenous Metabolite
|
Infection
Cancer
|
|
Adefovir dipivoxil (Standard) is the analytical standard of Adefovir dipivoxil. This product is intended for research and analytical applications. Adefovir dipivoxil, an adenosine analogue, is an oral proagent of the nucleoside reverse transcriptase inhibitor Adefovir. Adefovir dipivoxil inhibits both the wild type and HBV Lamivudine-resistant strains . Adefovir dipivoxil shows anti-orthopoxvirus activity.
|
-
- 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 .
|
-
- HY-147158
-
|
|
Molecular Glues
Ligands for E3 Ligase
|
Cancer
|
|
ZXH-1-161 is a potent cereblon (CRBN) modulator with an IC50 value of 39 nM in MM1.S wild type cells. ZXH-1-161 has selective degradation activity towards GSPT1. ZXH-1-161 can be used for researching multiple myeloma .
|
-
- HY-156284
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-89 (compound 13k) is a potent, fourth-generation EGFR mutation inhibitor with an IC50 of 10.1 nM against Del19/T790M/C797S mutations. EGFR-IN-89 shows higher selectivity over wild type .
|
-
- HY-14852
-
-
- HY-161246
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
|
-
- HY-153321
-
|
BTK-IN-24
|
Btk
PROTACs
|
Inflammation/Immunology
Cancer
|
|
NX-5948 (BTK-IN-24) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. NX-5948 mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. NX-5948 exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. NX-5948 is efficacious in a mouse collageninduced arthritis (CIA) model. NX-5948 can cross the blood brain barrier (BBB). NX-5948 is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: ligand for target protein; Blue: CRBN; Black: linker) .
|
-
- HY-134851
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
|
-
- HY-170926
-
|
|
RET
Apoptosis
|
Cancer
|
CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
|
-
- HY-150549
-
|
|
HIV Protease
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 protease-IN-6 (compound 17d) is a potent HIV-1 protease inhibitor, with an IC50 of 21 pM and a Ki of 4.7 pM, respectively. HIV-1 protease-IN-6 exhibits potent antiviral activity to DRV (darunavir)-resistant variant, even more than wild type virus .
|
-
- HY-146364
-
|
|
HIV
|
Infection
|
|
CI-39 is an antiviral natural product. CI-39 is an NNRTI (non-nucleoside reverse transcriptase inhibit) antiviral agent with an EC50 of 3.40 µM and an CC50 of >30 µM for wild type HIV-1. CI-39 inhibits HIV-1 RT DNA polymerase and ribonuclease H activitiessup .
|
-
- HY-12333
-
|
G-749
|
FLT3
Apoptosis
|
Cancer
|
|
Denfivontinib (G-749) is a potent, oral active and ATP competitive FLT3 inhibitor, with IC50s of 0.4 nM and 0.6 nM for FLT3 wild type and FLT3-D835Y, respectively. Denfivontinib can be used for the research of agent resistance for acute myeloid leukemia (AML) .
|
-
- HY-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
|
-
- 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-14852A
-
|
Fx-1006A
|
Transthyretin (TTR)
|
Neurological Disease
|
|
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis .
|
-
- HY-169228
-
|
|
Btk
|
Cancer
|
|
WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds .
|
-
- HY-14852S
-
|
|
Transthyretin (TTR)
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis[1].
|
-
- 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-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-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-161270
-
|
|
HIV Protease
|
Infection
|
|
HIV-1 protease-IN-13 (compound 18d) is a potent HIV-1 protease inhibitor with an IC50 value of 0.54 nM. HIV-1 protease-IN-13 also shows potent activity against HIV-1DRVRS (DRV-resistant mutation) and HIV-1NL4_3 variant (wild type) .
|
-
- HY-123636
-
|
|
p97
|
Cancer
|
|
UPCDC-30245 is an allosteric p97 inhibitor with an IC50 of approximately 27 nM . UPCDC-30245 inhibits the p97 mutant N660K similar to wild type (WT; IC50=300 nM) and shows 3-fold resistance for p97 mutant T688A . UPCDC-30245 can be used in the research of cancer .
|
-
- HY-14391
-
|
GS-558093
|
HCV
|
Infection
|
|
PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes .
|
-
- HY-B1268
-
|
Dioctyl sulfosuccinate sodium salt
|
HSV
|
Others
|
|
Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
|
-
- 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-167690
-
|
|
Endogenous Metabolite
|
Infection
|
|
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 .
|
-
- HY-168384
-
|
|
STING
TNF Receptor
Interleukin Related
CD28
|
Inflammation/Immunology
|
|
M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases .
|
-
- 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-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-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-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-12475
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-1 is a mutant-selective IDH1 inhibitor with with IC50s of 4, 42, 80 and 143 nM against mutant IDH1 R132C/R132C, IDH1 R132H/R132H, IDH1 R132H/WT and wild type IDH1, respectively.
|
-
- HY-152098
-
|
|
EGFR
|
Cancer
|
|
HX103 is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor (TKI)-based fluorogenic probe. HX103 inhibits EGFR 19 del, EGFR L858R, EGFR wild type and EGFR T790M with IC50s of 1.3, 1.5, 4.0 and 977 nM, respectively. HX103 can be used for quantifying active-EGFR to predict agent sensitivity in NSCLC patients with EGFR-activating mutations .
|
-
- 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-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-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-W127393
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C9-HSL is a rare odd-numbered acyl carbon chain produced by wild-type Erwinia carotovora strain SCC 3193 grown in nutrient-rich Luria-Bertani broth (LB) medium.
|
-
- 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-B1268R
-
|
|
HSV
|
Others
|
|
Docusate (Sodium) (Standard) is the analytical standard of Docusate (Sodium). This product is intended for research and analytical applications. Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
|
-
- 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-121708
-
|
|
c-Kit
|
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-139458
-
|
|
MDM-2/p53
|
Cancer
|
|
MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer .
|
-
- HY-150620
-
|
|
MDM-2/p53
|
Cancer
|
|
BI-0282 (Compound 1) is a potent MDM2-p53 interaction inhibitor .
|
-
- 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-161066
-
|
|
Ras
|
Cancer
|
|
KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS G13D (IC50: 0.41 nM). The selectivity for KRAS G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .
|
-
- HY-169311
-
|
|
Ras
|
Cancer
|
|
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
|
-
- HY-112823A
-
|
HS-10296 mesylate
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer .
|
-
- HY-143873
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bcl-2-IN-5 is a BCL-2 inhibitor with IC50s of 0.12 nM, 0.14 nM and 0.22 nM for Bcl-2 wild type, Bcl-2 D103Y and Bcl-2 G101V, respectively. Bcl-2-IN-5 inhibits the cell growth with IC50 values of 0.2 nM and 0.44 nM for Bcl 2-G101V knock-in RS4; 11 and RS4; 11 cells, respectively (WO2021208963A1; Example 155) .
|
-
- HY-112823
-
|
HS-10296
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-145269
-
|
|
Cadherin
|
Cancer
|
|
AL-GDa62 is a derivative of the CDH1/E-cadherin modulator SLEC-11 (HY-145268) and induces apoptosis in CDH1 -/- cells. AL-GDa62 has an EC50 of 3.2 μM and 2 μM for isogenic mammary epithelial cells MCF10A-WT (wild type) and mutant MCF10A-CDH1 -/-, respectively. AL-GDa62 specifically inhibits TCOF1, ARPC5, and UBC9, and suppresses SUMOylation at low micromolar concentrations .
|
-
- HY-112823B
-
|
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-12215
-
|
PF-06463922
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-135509
-
|
PF-06463922 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-P99384
-
|
B-701; MFGR-1877S; RG-7444
|
FGFR
|
Cancer
|
|
Vofatamab (B-701) is an anti-FGFR3 monoclonal antibody (mAb). Vofatamab blocks activation of both the wildtype and genetically activated receptor. Vofatamab can be used in the research of metastatic urothelial carcinoma (mUC) .
|
-
- HY-112823R
-
|
|
EGFR
|
Cancer
|
|
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-156292
-
|
|
Histone Methyltransferase
|
Cancer
|
|
IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
|
-
- HY-146807
-
|
|
Trk Receptor
|
Cancer
|
|
Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 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-134813A
-
|
|
Ras
|
Cancer
|
|
MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic 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 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic shows efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-12215R
-
|
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- 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-170438
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
|
-
- HY-169329
-
|
|
PINK1/Parkin
E1/E2/E3 Enzyme
|
Neurological Disease
|
|
BIO-2007817 is a Parkin positive allosteric modulators (PAMs). BIO-2007817 enhances the activity of wildtype Parkin. BIO-2007817 stimulates Parkin (an E3 ligase)autoubiquitination and induces the appearance of monoubiquitinated forms of Miro1 (EC50: 0.17 μM) .
|
-
- HY-168860
-
|
|
Bacterial
|
Infection
Cancer
|
|
Antituberculosis agent-13 (Compound 11) inhibits Mycobacterium tuberculosis, that inhibits Mtb wildtype and mutated strains with IC50 of 4-62.5 nM. Antituberculosis agent-13 exhibits anti-leukemia activity that inhibits MOLM-13 with IC50 of 3.8 μM .
|
-
- 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-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-120110
-
-
- HY-P1115
-
|
|
Akt
|
Others
|
|
AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
|
-
- HY-N7484
-
|
|
Fungal
|
Cancer
|
|
(−)-Voacangarine is an indole alkaloid, which exhibits cytotoxic effects against cancer cells HepG2, A375, MDA-MB-231, SH-SY5Y, and CT26 with IC50 of 5~20 mg/mL. (−)-Voacangarine inhibits the cultivation of Saccharomyces cerevisiae wildtype and repair-deficient mutants .
|
-
- 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 .
|
-
- HY-P1115A
-
|
|
Akt
|
Others
|
|
AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
|
-
- 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 .
|
-
- HY-163817
-
|
|
PARP
|
Cancer
|
|
PARP1/2-IN-3 (Compound 29) is an orally active inhibitor for PARP 1 and PARP 2 with IC50 of 0.2235 nM and <0.001 nM. PARP1/2-IN-3 inhibits the proliferation of Capan-1 wildtype, AZD2281 or BMN673 resistant cells with IC50 of 1.82-9.98 nM. PARP1/2-IN-3 exhibits antitumor efficacy in mice .
|
-
- 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-172408
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
NNRT-IN-6 (Compound 13a) is the non-nucleoside reverse transcriptase inhibitor (NNRT) for HIV-1 reverse transcriptase (HIV-1 RT) with IC50 of 0.41 μM. NNRT-IN-6 inhibits HIV-1 wildtype and mutant strains L100I, K103N, Y181C, Y188L, E138K, F227L/V106A and RES056 with EC50 of 6.2-250 nM .
|
-
- HY-170497
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
|
-
- HY-111434
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases . UAA crosslinker 1 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-111434A
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases . UAA crosslinker 1 (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.
|
-
- HY-164350
-
|
|
Ras
ERK
p38 MAPK
|
Cancer
|
|
KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .
|
-
- 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-170799
-
|
|
DNA/RNA Synthesis
SARS-CoV
Arenavirus
|
Infection
|
|
HNC-1664 is the orally active inhibitor for RNA-dependent RNA polymerase (RdRP). HNC-1664 exhibits broad-spectrum antiviral activity against coronavirus (SARS-CoV-2 wildtype and its mutants XBB.1.18, HK.3.1, BF.7.14, BA.1HCoV-229E, HCoV-OC43) and arenavirus. HNC-1664 exhibits anti-infectious activity in SARS-CoV-2 Delta infected mouse 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-155995
-
|
MK-905
|
Biochemical Assay Reagents
|
Cancer
|
|
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
|
-
- HY-169309
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-133 (Compound 24) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 0.1, 0.044, 0.036, 0.04, and 0.054 nM. EGFR-IN-133 exhibits good pharmacokinetics characteristics with high oral exposure .
|
-
- HY-169308
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-132 (Compound 23) is an inhibitor for EGFR, that inhibits the EGFR wildtype, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S mutans with IC50 of 1.6, 0.025, 0.019, 0.022, and 0.029 nM. EGFR-IN-132 exhibits good pharmacokinetics characteristics with high oral exposure .
|
-
- HY-P10854
-
|
|
NF-κB
Interleukin Related
STAT
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
TAT-N15 is a p55PIK inhibitor with remarkable anti-inflammatory activity and neuroprotective effects. TAT-N15 can significantly inhibit the activation of IL-6, IL-8, Akt, and NF-κB pathways, as well as suppress the protein expression of phosphorylated STAT3 and NF-κB. By inhibiting the activation of Akt, STAT3, and NF-κB pathways, TAT-N15 is used in research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke .
|
-
- HY-163030
-
|
|
Elastase
NF-κB
p38 MAPK
Bacterial
|
Infection
Inflammation/Immunology
|
|
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
|
-
- 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-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-W127393
-
|
|
Biochemical Assay Reagents
|
|
Quorum sensing is a regulatory system used by bacteria to control gene expression in response to increased cell density. This regulatory process manifests itself in a variety of phenotypes, including biofilm formation and virulence factor production. Coordinated gene expression is achieved through the production, release and detection of small diffusible signaling molecules called autoinducers. N-acylated homoserine lactones (AHLs) comprise a class of such autoinducers, each of which generally consists of a fatty acid coupled to a homoserine lactone (HSL). Modulation of bacterial quorum-sensing signaling systems to suppress pathogenesis represents a new approach to antimicrobial research for infectious diseases. AHLs differ in acyl length (C4-C18), C3 substitution (hydrogen, hydroxyl, or oxo group), and the presence or absence of one or more carbon-carbon double bonds in the fatty acid chain. These differences confer signaling specificity through the affinity of the LuxR family of transcriptional regulators. C9-HSL is a rare odd-numbered acyl carbon chain produced by wild-type Erwinia carotovora strain SCC 3193 grown in nutrient-rich Luria-Bertani broth (LB) medium.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2360
-
|
Ras 5-17
|
Ras
|
Others
|
|
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
|
-
- HY-P3485
-
|
|
Peptides
|
Cancer
|
|
GAGGVGKSAL is a wild-type KRAS G12D 10mer peptide. GAGGVGKSAL can be used as an immunogenic neoantigen for cancer immunotherapy research .
|
-
- 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-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-P2466
-
|
|
Apoptosis
|
Cancer
|
|
Bax BH3 peptide (55-74), wild type is a 20-amino acid Bax BH3 peptide (Bax 1) capable of inducing apoptosis in a variety of cell line models .
|
-
- HY-P2360A
-
|
Ras 5-17 TFA
|
Ras
|
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-P4391
-
-
- 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-P4926
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research .
|
-
- HY-P1088
-
|
|
PKC
|
Others
|
|
[Ser25] Protein Kinase C (19-31) is a substrate of protein kinase C (PKC) (Km: 0.3 μM). [Ser25] Protein Kinase C (19-31) is derived from the pseudo-substrate regulatory domain of PKCα (19-31) with a Serine at position 25 replacing the wild-type Alanine .
|
-
- 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 .
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- HY-P3487
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-
- HY-P5437
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PKC
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Others
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PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
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- HY-P2265A
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Ras
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Cancer
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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 .
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- HY-P1115
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Akt
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Others
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AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
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- HY-P1115A
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Akt
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Others
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AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
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- HY-P10854
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NF-κB
Interleukin Related
STAT
Akt
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Neurological Disease
Inflammation/Immunology
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TAT-N15 is a p55PIK inhibitor with remarkable anti-inflammatory activity and neuroprotective effects. TAT-N15 can significantly inhibit the activation of IL-6, IL-8, Akt, and NF-κB pathways, as well as suppress the protein expression of phosphorylated STAT3 and NF-κB. By inhibiting the activation of Akt, STAT3, and NF-κB pathways, TAT-N15 is used in research on acute conjunctivitis, allergic rhinitis, chronic obstructive pulmonary disease (COPD), and stroke .
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- HY-KE8011
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Phi29 DNA polymerase is a protein-engineered Phi29 DNA polymerase expressed in E. coli and then purified and isolated multiple times. Compared with wild-type Phi29 DNA polymerase, it has higher amplification efficiency and sensitivity, and can greatly shorten the reaction time.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P99849
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ABT-806
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EGFR
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Cancer
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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 .
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- HY-P99496
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RPC 4046; ABT 308; CC-93538
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Interleukin Related
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Inflammation/Immunology
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Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a high affinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
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- HY-P99715
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ABT-806
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EGFR
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Cancer
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Losatuxizumab (ABT-806) is an anti-EGFR monoclonal antibody. Losatuxizumab binds to EGFR with EC50s of 0.96 nM for EGFR wild-type, 0.09 nM for EGFR C271A,C283A, 0.12 nM for EGFRvIII, 0.66 nM for EGFR1-501. Losatuxizumab can be used for research of EGFR-expressing cancers .
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- HY-P99384
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B-701; MFGR-1877S; RG-7444
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FGFR
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Cancer
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Vofatamab (B-701) is an anti-FGFR3 monoclonal antibody (mAb). Vofatamab blocks activation of both the wildtype and genetically activated receptor. Vofatamab can be used in the research of metastatic urothelial carcinoma (mUC) .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0413S
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3 Publications Verification
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Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53[1][2][3][4].
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-
-
- HY-16305S
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Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
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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-10572S1
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Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
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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-10572BS
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(Rac)-Efavirenz-d4 is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. (Rac)-Efavirenz-d4 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-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-51424S
-
|
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PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of B-RafV600E with an IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
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-
-
- HY-10572S
-
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Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1]. Efavirenz-d5 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-14588S
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(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium 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-B1902S
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Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
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-
-
- HY-14852S
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Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis[1].
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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-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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-
| Cat. No. |
Product Name |
|
Classification |
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- HY-134813
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|
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Alkynes
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|
MRTX1133 is a noncovalent, potent, and selective alkyne-based 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-111434
-
|
|
|
Azide
|
|
UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases . UAA crosslinker 1 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-111434A
-
|
|
|
Azide
|
|
UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases . UAA crosslinker 1 (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-152233
-
|
|
|
Azide
|
|
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-167690
-
|
|
|
Alkynes
|
|
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 .
|
| Cat. No. |
Product Name |
|
Classification |
-
- HY-132609
-
|
|
|
siRNAs
siRNA drugs
|
|
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-145411
-
|
|
|
Pegylated Lipids
|
|
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-153609
-
|
|
|
siRNAs
siRNA drugs
|
|
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-148089A
-
|
|
|
Antisense Oligonucleotides
|
|
Eplontersen sodium is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases .
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-
- HY-148089
-
|
|
|
Antisense Oligonucleotides
|
|
Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases .
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