Search Result
Results for "
wild type
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
11
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-12928
-
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Virus Protease
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Infection
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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 .
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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-146262
-
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EGFR
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Cancer
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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 .
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- HY-116528
-
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HIV
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Infection
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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 .
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-
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- HY-142645
-
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RSV
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Infection
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RSV-IN-2 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-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-resistant HBV with an IC50 of 12 nM.
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-
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- HY-128888
-
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Isocitrate Dehydrogenase (IDH)
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Cancer
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(R,R)-GSK321 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. (R,R)-GSK321 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity .
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-
-
- HY-B1902
-
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EGIS-5645
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Antifolate
Bacterial
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Infection
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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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-
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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
-
-
-
- HY-17603
-
-
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- HY-117273
-
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Raf
Autophagy
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Cancer
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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 .
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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-16664
-
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MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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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.
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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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-
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- HY-U00437
-
-
-
- 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-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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-
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- HY-142953
-
-
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- HY-121392
-
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5-HT Receptor
|
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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-
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- HY-111050
-
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c-Met/HGFR
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Cancer
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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.
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-
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- HY-128661
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-
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- HY-P4391
-
-
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- HY-15728
-
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IY-5511
|
Bcr-Abl
|
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-17041
-
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TMC114 Ethanolate
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HIV
HIV Protease
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Infection
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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.
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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-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-N2894
-
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Parasite
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Infection
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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 .
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-
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- HY-108721
-
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Others
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Metabolic Disease
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Velaglucerase alfa is produced through gene activation technology and is identical to wild-type enzyme. Velaglucerase alfa targets accumulated glucocerebroside primarily within the lysosome of the macrophages in the affected organs and systems. Velaglucerase alfa is an enzyme replacement therapy (ERT) for type 1 Gaucher disease (GD) .
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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-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-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-E70218
-
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Others
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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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-
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- HY-13237
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-
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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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- 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-16271
-
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4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
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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-112256
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ACP-105
5 Publications Verification
|
Androgen Receptor
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Inflammation/Immunology
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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.
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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-132885
-
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PARP
Histone Methyltransferase
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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
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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-120122
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Others
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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-118806
-
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mAChR
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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 .
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- HY-10035
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T-type calcium channel inhibitor
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Calcium Channel
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Neurological Disease
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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 .
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- HY-107123
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ASC-09
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HIV Protease
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Infection
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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 .
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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-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-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-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-112306
-
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DCC-2618
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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-10572
-
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- HY-18634
-
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ZMC1
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MDM-2/p53
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Cancer
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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-10468
-
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2'-C-Methylcytidine; NM-107
|
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
|
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-146394
-
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HBV
DNA/RNA Synthesis
|
Infection
|
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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-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-P5437
-
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PKC
|
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-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-12025
-
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JNJ-26854165
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
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Cancer
|
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Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.
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-
- HY-13223
-
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CP-868596
|
FLT3
PDGFR
Autophagy
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Cancer
|
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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.
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- HY-B0255
-
-
- HY-134877
-
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EGFR
|
Cancer
|
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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) .
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- HY-156712
-
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Antibody-Drug Conjugates (ADCs)
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Cancer
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Depatuxizumab MMAE is an antibody-drug conjugate (ADC) comprising an anti EGFR monoclonal antibody (Depatuxizumab) and the cytotoxic agent Monomethyl auristatin E (MMAE). Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR .
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- HY-121611
-
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HIV
|
Inflammation/Immunology
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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) .
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- HY-10542A
-
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Atg8/LC3
Raf
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Neurological Disease
|
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(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 .
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- HY-129943
-
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Bacterial
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Infection
|
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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) .
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- HY-136173
-
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TNO155
|
SHP2
Phosphatase
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Cancer
|
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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 .
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- HY-144105
-
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MDM-2/p53
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Cancer
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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 .
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- HY-147988
-
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DNA/RNA Synthesis
Bacterial
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Infection
|
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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 .
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- HY-151938
-
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HIV
|
Infection
|
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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 .
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- HY-155048
-
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Bacterial
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Infection
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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 .
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- HY-116833
-
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Others
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Metabolic Disease
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4-Chloro-3,5-dimethylphenoxyacetic acid (compound 602 UC) is a product of masked amide bond hydrolysis of auxin analog 602 (compound 602).602 can effectively stimulate hypocotyl growth in wild-type seedlings .
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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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- HY-132609
-
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Small Interfering RNA (siRNA)
Transthyretin (TTR)
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Neurological Disease
|
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Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis .
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- HY-111396
-
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Bacterial
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Infection
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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 .
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-
- HY-160287
-
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-N5109
-
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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 .
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- HY-139884
-
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EGFR
|
Cancer
|
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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-16305S
-
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1263W94-d6; BW1263W94-d6; GW257406X-d6
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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 .
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-
- HY-10035A
-
|
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Others
|
Neurological Disease
|
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(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 .
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-
- HY-50707
-
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(Rac)-T-type calcium channel inhibitor
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Others
|
Neurological Disease
|
|
(Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
|
-
- HY-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-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-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-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-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-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-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-P5819
-
|
|
Wnt
APC
PROTACs
β-catenin
|
Cancer
|
|
xStAx-VHLL is a PROTAC β-catenin degrader that manifests strong inhibition of Wnt signaling and sustains degradation of β-catenin in cancer cells and the intestinal organoids derived from wild-type and APC –/– mice. xStAx-VHLL can be used as a promising anticancer agent .
|
-
- 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 .
|
-
- 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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-14852
-
|
|
Transthyretin (TTR)
|
Neurological Disease
|
|
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 .
|
-
- 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-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-115282A
-
|
TRC-253
|
Androgen Receptor
|
Cancer
|
|
JNJ-63576253 (TRC-253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC) .
|
-
- HY-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-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-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-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-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.com/product_pic/hy-p1088.gif)
- HY-153342
-
|
ARV-766
|
PROTACs
Androgen Receptor
|
Cancer
|
|
ARV-766 is an orally active and potent proteolysis targeting chimera (PROTAC) protein degrader. ARV-766 degrades wild-type androgen receptor (AR) but also relevant AR LBD mutants, including the most prevalent AR L702H, H875Y, and T878A mutations .
|
-
- 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-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-161246
-
|
|
Others
|
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-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-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-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-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-136938
-
|
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-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-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-145268
-
|
|
Others
|
Cancer
|
|
SLEC-11 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 12.2 μM and 8.2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1 -/- .
|
-
- HY-145269
-
|
|
Others
|
Cancer
|
|
AL-GDa62 acts as a potential synthetic lethal lead for the research of gastric cancer. AL-GDa62 shows EC50 of 3.2 μM and 2 μM for isogenic mammary epithelial cells MCF10A-WT (wild-type) and MCF10A-CDH1 -/- .
|
-
- 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-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-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-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-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-152292
-
|
NVL-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-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-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-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-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-13001
-
|
AC220
|
FLT3
Ligands for Target Protein for PROTAC
Apoptosis
Autophagy
|
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-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-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-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-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-115282
-
|
TRC-253 free base
|
Androgen Receptor
|
Cancer
|
|
JNJ-63576253 (TRC-253) free base is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 free base can be used for the research of castration-resistant prostate cancer (CRPC) .
|
-
- HY-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-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-101985
-
BV02
1 Publications Verification
|
Bcr-Abl
|
Cancer
|
|
BV02 is a potent 4-3-3 PPI (14-3-3 protein–protein interaction) inhibitor. BV02 shows cytotoxicity for hematopoietic cells expressing the IM (imatinib mesylate)-sensitive wild type Bcr-Abl and the IM-resistant T315I mutation. BV02 has the potential for the research of chronic myeloid leukemia .
|
-
- HY-15103
-
|
|
Androgen Receptor
Thyroid Hormone Receptor
|
Cancer
|
|
AH3960 (compound 16c) is an antagonist of androgen receptor. AH3960 binds wild as well as T877 mutant type androgen receptors. AH3960 selectively inhibits T877 with an IC50 value of 0.82 μM. AH3960 also serves as an agonist of parathyroid hormone receptor-1 (PTHR1) .
|
-
- HY-10574
-
|
R278474; TMC278; DB08864
|
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
|
-
- HY-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-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-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-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-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-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-121845
-
|
|
Others
|
Metabolic Disease
|
|
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity .
|
-
- HY-10574A
-
|
TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride
|
SARS-CoV
MMP
|
Infection
|
|
Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
|
-
- HY-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-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-162363
-
|
|
PARP
|
Neurological Disease
|
|
MD6a is a melatonin derivative with inhibitroy activity towards PARP-1, which maintains proteins hemostasis and improves mitochondrial function through TOR/HSF-1 signaling. MD6a a neuroprotective effect .
|
-
- 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-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-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-19925
-
|
|
|
|
|
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-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-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-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-149480
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
|
-
- HY-156498
-
|
|
Ras
|
Cancer
|
|
RMC-7977 is a reversible, tri-complex RAS inhibitor with broad spectrum activity for both mutant and wild-type (WT) KRAS, NRAS, and HRAS variants.RMC-7977 can lead to tumor regressions and was well tolerated in diverse RAS-addicted preclinical cancer models. RMC-7977 also can inhibit the growth of KRAS G12C cancer models .
|
-
- HY-15814
-
|
|
Bcr-Abl
PDGFR
c-Kit
Src
JAK
Apoptosis
|
Cancer
|
|
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
|
-
- HY-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-14588
-
|
ABT-378
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
|
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-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-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-139995
-
|
|
Others
|
Others
|
|
Spermine precursor-1 (Compound 1) is a redox-sensitive spermine precursor for the potential research of snyder robinson syndrome. Spermine precursor-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively .
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-136910
-
|
|
Deubiquitinase
|
Cancer
|
|
USP7-IN-7 (compound 124) is a USP7 inhibitor with an IC50 value ＜10 nM. USP7-IN-7 shows cytotoxicity against p53-mutant cancer cell lines, p53 wild-type blood cancer and neuroblastoma cell lines with low nanomolar values. USP7-IN-7 can be used for cancer research .
|
-
- 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-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-19840
-
|
GS-9857
|
HCV Protease
|
Infection
|
|
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-151380
-
|
|
Others
|
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-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-10574S
-
|
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].
|
-
- HY-139590
-
|
BOS-172738; DS-5010
|
RET
PDGFR
|
Cancer
|
|
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RET V804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity .
|
-
- HY-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-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-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-B0413
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
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-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-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-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-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-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-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-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-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-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-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα .
|
-
- HY-136242
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy .
|
-
- HY-B0413S
-
|
|
HIF/HIF Prolyl-Hydroxylase
Parasite
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
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].
|
-
- 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-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-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-131312
-
|
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-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-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-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-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-162253
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-64 (Compound 7c) is a wild-type HIV-1 inhibitor that effectively suppresses the activity of HIV-1 mutants E138K/Q148K and G140S/Q148R with EC50 values of 62.5 nM and 11.3 nM, respectively. HIV-1 inhibitor-64 exhibits antiviral activity and can be used in the research of AIDS .
|
-
- HY-14588R
-
|
ABT-378 (Standard)
|
HIV
HIV Protease
SARS-CoV
|
Infection
Cancer
|
|
Lopinavir (Standard) is the analytical standard of Lopinavir. This product is intended for research and analytical applications. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-100218B
-
|
|
Others
|
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-14588S2
-
|
ABT-378-d7
|
HIV
SARS-CoV
HIV Protease
Isotope-Labeled Compounds
|
Infection
Cancer
|
|
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 .
|
-
- 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-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-14588S1
-
|
|
HIV
HIV Protease
SARS-CoV
|
Infection
|
|
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity[1][2]. Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM[3].
|
-
- HY-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-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-19617
-
|
|
|
|
|
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-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-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-16936
-
|
|
|
|
|
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-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-162033
-
|
|
Others
|
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-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-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-14588S
-
|
(rel)-ABT-378-d8
|
Isotope-Labeled Compounds
|
Others
|
|
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-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-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-13775
-
XL019
4 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-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-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-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-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-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-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-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-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
|
-
- 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-13803
-
Tazemetostat
Maximum Cited Publications
51 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-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-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-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-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-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-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-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-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 .
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-
- HY-156292
-
|
|
Histone Methyltransferase
|
Cancer
|
|
IHMT-EZH2-426 (compound 38) is a potent and covalent EZH2 degrader with IC50s of 1.3 nM, 1.2 nM, and 1.7-3.5 nM against EZH2 wild-type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 exhibits potent antiproliferation effects against both B-cell lymphoma and triple negative breast cancer (TNBC) cell lines by reducing the levels of H3K27me3 and EZH2 .
|
-
- 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 .
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-
- HY-112363
-
|
RP107
|
CDK
GSK-3
ERK
JNK
CFTR
|
Inflammation/Immunology
Cancer
|
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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 .
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- HY-134813
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Ras
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Cancer
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|
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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-
- HY-123450
-
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Bcr-Abl
Apoptosis
PDGFR
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Cancer
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|
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.
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-
- HY-134851
-
|
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HIV
|
Infection
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|
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 .
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-
- 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) .
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- HY-W127393
-
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Biochemical Assay Reagents
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Others
|
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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.
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| Cat. No. |
Product Name |
Type |
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- 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 .
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-
- 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.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P2466
-
|
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Apoptosis
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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 .
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-
- HY-P3485
-
|
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Peptides
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Cancer
|
|
GAGGVGKSAL is a wild-type KRAS G12D 10mer peptide. GAGGVGKSAL can be used as an immunogenic neoantigen for cancer immunotherapy research .
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-
- HY-P3487
-
-
- 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 .
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-
- HY-P2360
-
|
Ras 5-17
|
Peptides
|
Others
|
|
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
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-
- HY-P2319A
-
|
|
p38 MAPK
JNK
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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 .
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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-P4926
-
|
|
Peptides
|
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 .
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-
- HY-P2360A
-
|
Ras 5-17 TFA
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Peptides
|
Others
|
|
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12) .
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-
- HY-P5819
-
|
|
Wnt
APC
PROTACs
β-catenin
|
Cancer
|
|
xStAx-VHLL is a PROTAC β-catenin degrader that manifests strong inhibition of Wnt signaling and sustains degradation of β-catenin in cancer cells and the intestinal organoids derived from wild-type and APC –/– mice. xStAx-VHLL can be used as a promising anticancer agent .
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-
- 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 .
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-
- 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-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 .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99849
-
|
ABT-806
|
EGFR
|
Cancer
|
|
Depatuxizumab is a brain-penetrant and humanized tumor-specific anti EGFR monoclonal antibody. Depatuxizumab inhibits the growth of xenograft models of mutant EGFRvIII and wild-type EGFR. Depatuxizumab can be used for research on cancer .
|
-
- HY-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-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 .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-16305S
-
|
|
|
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-10574S
-
|
|
|
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-B0413S
-
2 Publications Verification
|
|
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-10572S1
-
|
|
|
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].
|
-
-
- HY-14852S
-
|
|
|
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-10572BS
-
|
|
|
(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-14588S2
-
|
|
|
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 .
|
-
-
- HY-14588S1
-
|
|
|
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-51424S
-
|
|
|
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-10572S
-
|
|
|
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
-
|
|
|
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8)is the deuterium labeledLopinavir(HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-134813
-
|
|
|
Alkynes
|
|
MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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-
- HY-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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
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![[Ser25] Protein Kinase C (19-31)](http://file.medchemexpress.com/product_pic/hy-p1088.gif)
