Search Result
Results for "
wild
" in MedChemExpress (MCE) Product Catalog:
7
Biochemical Assay Reagents
28
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-148439
-
|
RMC-6236; RAS-IN-2
|
Ras
PERK
|
Cancer
|
|
Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors .
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-
-
- HY-100818
-
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TAS-120
|
FGFR
|
Cancer
|
|
Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
|
-
-
- HY-112306
-
|
DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
|
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
|
-
-
- HY-16305
-
|
1263W94; BW1263W94; GW257406X
|
EBV
CMV
|
Infection
|
|
Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).
|
-
-
- HY-164718
-
|
BAY 2927088
|
EGFR
|
Cancer
|
|
Sevabertinib (BAY 2927088) is an orally active and reversible dual EGFR-HER2 inhibitor (IC 50 <0.5 nM for wild-type HER2, HER2 A775insYVMA, wild-type EGFR, and EGFR D770_N771insSVD). Sevabertinib has anticancer activity against lung cancer .
|
-
-
- 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-13237
-
-
-
- HY-NP006
-
|
SPA
|
Endogenous Metabolite
Apoptosis
|
Inflammation/Immunology
|
|
Protein A (SPA) is an immunoglobulin (Ig)-binding protein that exists on the bacterial surface and can be freely secreted into the extracellular environment. Protein A blocks opsonophagocytosis and induces B cell apoptosis in vitro by binding to the Fc region of antibodies and the Fab region of B cell receptors. Protein A can form toxic immune complexes with IgG, thereby inducing leukocyte necrosis. Protein A contributes to the virulence expression of Staphylococcus aureus. Protein A triggers allergic reactions in IgG-pretreated mouse models. Protein A can be used in studies related to immune system diseases .
|
-
-
- HY-108917
-
|
GLS4
|
HBV
|
Infection
|
|
Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir (HY-B1826)-resistant HBV with an IC50 of 12 nM.
|
-
-
- HY-112256
-
|
|
Androgen Receptor
|
Inflammation/Immunology
|
|
ACP-105 is an orally available, selective amd potent androgen receptor modulator (SARM), with pEC50s of 9.0 and 9.3 for AR wild type and T877A mutant, respectively.
|
-
-
- HY-17603
-
-
-
- HY-17041
-
|
TMC114 Ethanolate
|
HIV
HIV Protease
|
Infection
|
|
Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
|
-
-
- HY-18343A
-
|
|
MDM-2/p53
|
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 .
|
-
-
- HY-16271
-
|
4-Isothioureidobutyronitrile hydrochloride; thioureidobutyronitrile hydrochloride; thioureido butyronitrile hydrochloride
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Kevetrin hydrochloride is a potent activator of p53, induces apoptosis in TP53 wild-type and mutant acute myeloid leukemia cells. Kevetrin a preferential cytotoxic activity against blast cells .
|
-
-
- HY-12928
-
|
|
Virus Protease
|
Infection
|
|
ML336 is quinazolinone-based inhibitor against venezuelan equine encephalitis virus (VEEV), with IC50s of 32, 20, and 42 nM for VEEV TC-83 CPE , VEEV V3526 CPE, VEEV Wild Type CPE, respectively. ML336 potently inhibits a VEEV-induced cytopathic effect in three strains of the virus (TC-83, V3526, and wild type Trinidad donkey) in the low nanomolar range .
|
-
-
- HY-119435
-
|
|
Herbicide
Environmental Pollutants
|
Others
|
|
Triallate is a selective thiocarbamate herbicide. Triallate regulates the biosynthesis of very-long-chain fatty acids and inhibits the elongation and division of plant cells. Triallate is used to control wild oats in barley, spring wheat, durum wheat, winter wheat and sugar beets .
|
-
-
- HY-18936
-
-
-
- HY-128888
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
(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 .
|
-
-
- HY-B1902
-
|
EGIS-5645
|
Antifolate
Bacterial
|
Infection
|
|
Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
|
-
-
- HY-16664
-
|
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MDM-2/p53
E1/E2/E3 Enzyme
|
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-160142
-
|
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PROTACs
Btk
Syk
MEK
ERK
|
Cancer
|
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UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers .
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-
-
- HY-15714
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NMS-859
1 Publications Verification
|
p97
|
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-W009811
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-
-
- HY-117273
-
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Raf
Autophagy
|
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-U00437
-
-
-
- HY-141715
-
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Antibiotic
|
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 .
|
-
-
- HY-120122
-
|
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MDM-2/p53
|
Cancer
|
|
PK7088 is a pyrazole and a specific peptide. PK7088 supports the reactivation of mutant p53 by converting it to a form exhibiting wild-type properties. PK7088 exhibit anticancer activity in cancer research .
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-
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- HY-N0308
-
|
|
Environmental Pollutants
Biochemical Assay Reagents
|
Cancer
|
|
Octyl acetate is an orally active aliphatic ester. Octyl acetate has certain antioxidant properties. Octyl acetate contributes to the formation of fruit aroma and affects the flavor of fruits such as strawberries. Octyl acetate can be used in the research of malignant melanoma, colon cancer and breast cancer .
|
-
-
- HY-177650
-
|
ALN-TTRsc04
|
Transthyretin (TTR)
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Others
|
|
Nucresiran is a siRNA that inhibits hepatic synthesis of both wild-type and variant TTR mRNA.
|
-
-
- HY-77113
-
|
|
Raf
|
Cancer
|
|
B-Raf IN 11 is a B-Raf V600E mutant kinase inhibitor with an IC50 of 76 nM, and exhibits an IC50 of 238 nM against wild-type B-Raf kinase. B-Raf IN 11 inhibits the kinase activities of B-Raf V600E mutant and wild-type B-Raf kinase. B-Raf IN 11 is applicable to relevant research on colorectal cancer .
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-
-
- HY-12083
-
|
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Bcr-Abl
|
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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-
-
- HY-19400
-
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DPH-153893
|
HIV Protease
HIV
|
Infection
|
|
DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.
|
-
-
- 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 .
|
-
-
- HY-126987
-
-
-
- HY-169311
-
|
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Ras
|
Cancer
|
|
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
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-
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- HY-E70404
-
|
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DNA/RNA Synthesis
Biochemical Assay Reagents
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Others
|
|
FastTaq DNA Polymerase (5'→3' exo-) is a modified DNA polymerase based on Taq DNA Polymerase. FastTaq DNA Polymerase (5'→3' exo-) lacks the 5'→3' exonuclease activity of wild-type Taq. It retains the 5'→3' DNA polymerase activity of wild-type Taq .
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-
-
- HY-14844
-
|
MIV-210
|
HBV
|
Infection
|
|
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-162590
-
|
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Bacterial
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Infection
|
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ECIN is a copper-responsive inhibitor of wild-type UPEC strains. ECIN inhibits Uropathogenic Escherichia coli (UPEC) with an IC50 value of 336 ng/mL in the absence of copper .
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-
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- HY-141566
-
|
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Histone Methyltransferase
|
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-111627
-
|
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Nucleoside Antimetabolite/Analog
|
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
-
|
|
PARP
Histone Methyltransferase
|
Cancer
|
|
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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-
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- HY-177650A
-
|
ALN-TTRsc04 sodium
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Transthyretin (TTR)
|
Others
|
|
Nucresiran sodium is a siRNA that inhibits hepatic synthesis of both wild-type and variant TTR mRNA.
|
-
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- HY-18936R
-
|
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
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Cancer
|
|
Alda-1 (Standard) is the analytical standard of Alda-1. This product is intended for research and analytical applications. Alda-1 is a potent and selective ALDH2 agonist, which activates wild-type ALDH2 and restores near wild-type activity to ALDH2*2.
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-
-
- HY-111050
-
|
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c-Met/HGFR
|
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.
|
-
-
- HY-P4391
-
-
-
- HY-15352
-
|
DPC 083
|
Reverse Transcriptase
HIV
|
Infection
|
|
BMS 561390 (DPC 083) is an orally available non-nucleoside reverse transcriptase inhibitor (NNRTI) with broad inhibitory effects on wild-type HIV-1 and mutant strains .
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-
-
- HY-186102
-
|
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Isocitrate Dehydrogenase (IDH)
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Others
|
|
IDH1 ligand 1 (Compound 18) can serve as a negative control for the IDH1 target, with no detectable affinity for wild-type IDH1 and an IC50 >10,000 nM .
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-
-
- HY-E70218
-
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Others
|
Others
|
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Cas9 Nuclease is cloned from wild-type Streptococcus pyogenes. Cas9 Nuclease can be used in the area of molecular diagnosis to achieve highly sensitive and specific detection of pathogens [1] .
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-
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- HY-147580
-
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Btk
|
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-W794670
-
|
|
Aminopeptidase
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Others
|
|
H-Ala-Pro-Ala-OH, tripeptide, is a substrate for Escherichia coli PepP (Xaa-Pro aminopeptidase). H-Ala-Pro-Ala-OH acts as a nitrogen source for wild-type Escherichia coli .
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- HY-175351
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1-IN-83 (Compound 18E) is a HIV-1 non-nucleoside reverse transcriptase inhibitor with an IC50 of 0.45 μM for wild-type HIV-1 non-nucleoside reverse transcriptase. HIV-1-IN-83 has potent antiviral activity against both HIV-1 wild-type and mutant strains and improves antidrug resistance for Y188L and RES056 mutant strains. HIV-1-IN-83 has no significant toxicity up to 11.088 μM .
|
-
- HY-106155
-
|
DAPD
|
HIV
Reverse Transcriptase
|
Infection
|
|
Amdoxovir (DAPD) is an orally active nucleoside reverse transcriptase inhibitor. Amdoxovir is active against wild-type and NRTl-resistant viruses. Amdoxovir is the prodrug of dioxolane guanosine. Amdoxovir can be used for research of HIV/AIDS .
|
-
- HY-P2319
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P2466
-
|
|
Apoptosis
|
Cancer
|
|
Bax BH3 peptide (55-74), wild type is a 20-amino acid Bax BH3 peptide (Bax 1) capable of inducing apoptosis in a variety of cell line models .
|
-
- HY-146262
-
|
|
EGFR
|
Cancer
|
|
LDC0496 is a potent and selective EGFR inhibitor. LDC0496 possesses intense inhibitory potency toward EGFR and Her2 exon20 insertion mutations, as well as selectivity over wild type EGFR and within the kinome .
|
-
- HY-171181
-
|
|
HBV
|
Infection
|
|
ZINC20451377 is a small molecule targeting hepatitis B (HBV) surface antigen (HBsAg) and can effectively inhibit wild-type hepatitis B and tenofovir (HY-13910)-resistant hepatitis B .
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-
- HY-116528
-
|
|
HIV
|
Infection
|
|
GCA-186 is a potent anti-HIV-1 agent. GCA-186 is highly active against both wild type and mutated HIV-1 strains with EC50s of 1, 180, 1, and 40 nM for IIIB, IIIB-R(Y181C), NL4-3 and NL4-3K103N of HIV-1 strains, respectively .
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-
- HY-119435R
-
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|
Herbicide
Reference Standards
Environmental Pollutants
|
Others
|
|
Triallate (Standard) is the analytical standard of Triallate (HY-119435). This product is intended for research and analytical applications. Triallate is a selective thiocarbamate herbicide. Triallate regulates the biosynthesis of very-long-chain fatty acids and inhibits the elongation and division of plant cells. Triallate is used to control wild oats in barley, spring wheat, durum wheat, winter wheat and sugar beets
|
-
- HY-121952
-
|
|
Drug Isomer
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Others
|
|
(9E,11E)-9,11-Octadecadienoic acid methyl ester is an isomer of 9(Z),11(E),13(E)-octadecatrienoic acid methyl ester and the methyl ester form of 9(Z),11(E),13(Z)-octadecatrienoic acid, which is found in wild growing pomegranate seed oil .
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-
- HY-142645
-
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RSV
|
Infection
|
|
TP0591816 is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus fusion proteins (wild-type, EC50 = 0.27 nM; D486N-mutant, EC50 = 0.70 nM).
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-
- HY-N0308R
-
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|
Reference Standards
Biochemical Assay Reagents
|
Cancer
|
|
Octyl acetate (Standard) is the analytical standard of Octyl acetate (HY-N0308). This product is intended for research and analytical applications. Octyl acetate is an orally active aliphatic ester. Octyl acetate has certain antioxidant properties. Octyl acetate contributes to the formation of fruit aroma and affects the flavor of fruits such as strawberries. Octyl acetate can be used in the research of malignant melanoma, colon cancer and breast cancer .
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-
- HY-N12533
-
|
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Others
|
Others
|
|
Quinquenoside R1 (Compound 12) is a saponin compound that can be isolated from wild ginseng .
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- HY-164469
-
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Bcr-Abl
Apoptosis
STAT
|
Cancer
|
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CHMFL-48 is an orally active BCR-ABL kinase inhibitor targeting both wild-type (wt) and various imatinib-resistant mutants. The IC50 values for CHMFL-48 against ABL wild-type and ABL T315I mutant are 1 nM and 0.8 nM, respectively. CHMFL-48 exerts its effects by blocking the autophosphorylation of BCR-ABL wild-type and mutant forms, which impacts downstream signaling mediators such as STAT5 and CRKL, leading to cell cycle arrest and induction of apoptosis. CHMFL-48 holds potential for research into chronic myeloid leukemia (CML) .
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-
- HY-150769
-
|
|
HIV
|
Inflammation/Immunology
|
|
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-153577
-
-
- HY-N12005
-
|
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Others
|
Others
|
|
6-Hydroxykaempferol 7-O-β-glucopyranoside (compound 5) is a flavonol isolated from wild marigold (Tagetes minuta) .
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-
- HY-146108
-
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RSV
|
Infection
|
|
RSV-IN-5 (Compound 4) is a potent dual inhibitor of wild-type and mutant respiratory syncytial virus (RSV) fusion proteins. RSV-IN-5 exhibits potent anti-RSV activities against not only wild-type A2 F protein (EC50=2.0 nM), but also D486N-mutant F protein (EC50=8.1 nM) .
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-
- HY-162680
-
|
|
Influenza Virus
|
Infection
|
|
OSC-GCDI(P) is a broad-spectrum orally active anti-influenza virus agent that exhibits significant inhibitory effects against both wild-type and Oseltamivir (HY-13317) resistant (H275Y) influenza virus strains in mouse infection models. OSC-GCDI(P) is capable of preventing not only wild-type influenza viruses but also OS-resistant variants with NA(H275Y) .
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-
- HY-122389
-
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Herbicide
|
Others
|
|
Difenzoquat methyl sulfate is a herbicide, which is used for post-emergence control of wild oats in cereal crops. Difenzoquat methyl sulfate is toxic to health and environment .
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-
- HY-142953
-
-
- HY-108917A
-
|
GLS4 mesylate
|
HBV
|
Infection
|
|
Morphothiadin (GLS4) mesylate is a potent inhibitor of wild-type and Adefovir (HY-B1826)-resistant HBV replication with an IC50 value of 12 nM .
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-
- HY-144215
-
|
|
HBV
|
Inflammation/Immunology
|
|
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-158241
-
|
|
Bacterial
|
Infection
|
|
GmhA-IN-1 (compound 17) is an inhibitor of GmhA with an IC50 value of 2.4 nM. GmhA-IN-1 enhances the activity of erythromycin and rifampicin on wild-type E. coli .
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-
- HY-N2894
-
|
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Parasite
|
Infection
|
|
Piperolactam A is a natural product that can be isolated from root of Piper betle. Piperolactam A exhibits promising leishmanicidal action against wild type and drug resistant strains of Leishmania donovani .
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-
- HY-13810
-
|
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Raf
|
Cancer
|
|
PF-04880594 is a potent and selective RAF inhibitor. PF-04880594 inhibits both wild-type and mutant BRAF and CRAF. PF-04880594 shows antitumor activity .
|
-
- HY-139631
-
|
|
HIV
|
Infection
|
|
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-N3113
-
|
|
Others
|
Cancer
|
|
Panaxyne is a polyacetylene, that can be isolated from the roots of cultivated-wild ginseng. Panaxyne shows significant and selective cytotoxicity against SK-OV-3, with an ED50 of 1.40 µM .
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-
- HY-111079
-
|
|
HIV
Reverse Transcriptase
|
Others
|
|
HIV-1 inhibitor-70 (compound 20) is a bifunctional inhibitor that inhibits both wild-type (WT) and K103N mutant reverse transcriptases (RTs) of HIV-1.
|
-
- HY-B1902R
-
|
EGIS-5645 (Standard)
|
Reference Standards
Antifolate
Bacterial
|
Infection
|
|
Diaveridine (Standard) is the analytical standard of Diaveridine. This product is intended for research and analytical applications. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.
|
-
- HY-171252
-
|
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EGFR
|
Cancer
|
|
EGFR-IN-145 (compound 7c) is an EGFR kinase inhibitor. At a concentration of 20 μM, EGFR-IN-145 has an inhibition rate of 52.7% on EGFR-wild type kinase .
|
-
- HY-108508
-
|
|
Smo
Hedgehog
|
Cancer
|
|
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 .
|
-
- HY-125144
-
|
|
Na+/H+ Exchanger (NHE)
|
Cardiovascular Disease
|
|
BIIB 513 is an inhibitor of NHE 1 that protects against myocardial ischemia. BIIB 513 inhibits acid load recovery with an IC50 of 27 nmol/L in cells expressing wild-type NHE 1 under acute acid load .
|
-
- HY-N18657
-
|
|
Others
|
Metabolic Disease
|
|
Wild Yam Extract is derived from the dried tubers of Dioscorea oppositae thunb. It has the functions of invigorating the spleen, tonifying the lungs, strengthening the kidney, and replenishing vital essence.
|
-
- HY-N18364
-
|
|
Others
|
Others
|
|
6'''-Sinapoylbaimaside is a flavonoid glycoside found in Hedyotis diffusa Wild .
|
-
- HY-W009811R
-
|
|
Insecticide
Reference Standards
|
Others
|
|
2-Tridecanone, a nonalkaloid insecticide, is isolated from the wild tomato Lycopersicon hirsutum f. glabratum. 2-Tridecanone is a volatile organic compound .
|
-
- HY-N0055A
-
|
trans-3-O-Caffeoylquinic acid; trans-Heriguard; trans-NSC-407296
|
Drug Derivative
|
Infection
|
|
trans-Chlorogenic acid (trans-3-O-Caffeoylquinic acid) is a caffeoyl ester derivative of quinic acid, as well as an oviposition stimulant. trans-Chlorogenic acid can be found in the leaves of carrot (Daucus carota) and wild parsnip (Pastinaca sativa) .
|
-
- HY-185276
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-204 (Example 1) is a HER2 exon 20 mutation inhibitor with selectivity for wild-type EGFR. EGFR-IN-204 exerts antiproliferative effects on cells dependent on HER2 exon 20 YVMA insertion mutation and wild-type HER2, and shows strong selectivity over cells dependent on wild-type EGFR. EGFR-IN-204 is applicable to non-small cell lung cancer research .
|
-
- HY-181052
-
|
|
PROTACs
Trk Receptor
|
Cancer
|
|
PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors .
|
-
- HY-183032
-
|
|
ATP-binding cassette (ABC) transporters
|
Metabolic Disease
|
|
ABC transporter modulator-1 (Compound I-5) is an ABC transporter expression enhancer. ABCC6 modulator-1 upregulates the expression of wild-type ABCC6, wild-type ABCB4, and ABCA4 P1380L mutant, with an EC50 of <1 μM for all .
|
-
- HY-181871
-
|
|
Trk Receptor
Akt
ERK
Apoptosis
|
Cancer
|
|
DZX19 (Compound C02) is an orally active, selective TRK inhibitor with a TRKA IC50 value of 1.32 nM, a TRKB IC50 of 2.28 nM, and a TRKC IC50 of 4.05 nM. DZX19 inhibits the kinase activities of wild-type TRKA, TRKA mutants (G595R, F589L, G667C), wild-type TRKB, and wild-type TRKC, and suppresses the phosphorylation of TRKA as well as its downstream AKT and ERK signaling pathways. DZX19 induces apoptosis. DZX19 inhibits tumor growth in a colorectal cancer xenograft mouse model. DZX19 is applicable for the research of colorectal cancer .
|
-
- HY-131570
-
|
|
Glycosidase
|
Neurological Disease
|
|
JZ-4109 is a β-Glucocerebrosidase (GCase) modulator with an IC50 of 8 nM for wild-type recombinant GCase. JZ-4109 binds to an allosteric site at the GCase dimer interface, stabilizes wild-type and GCase N370S mutant GCase, induces GCase dimerization. JZ-4109 increases GCase protein abundance. JZ-4109 can be used for the research of Parkinson's diseas .
|
-
- HY-183033
-
|
|
ATP-binding cassette (ABC) transporters
|
Metabolic Disease
|
|
ABC transporter modulator-2 (Compound I-200) is a ABC transporter expression modulator. ABC transporter modulator-2 upregulates the expression of wild-type ABCC6 with an EC50 of <1 μM. ABC transporter modulator-2 upregulates the expression of wild-type ABCB4 with an EC50 of <1 μM. ABC transporter modulator-2 upregulates the expression of wild-type ABCD2 with an EC50 of <1 μM. ABC transporter modulator-2 upregulates the expression of the ABCA4 P1380L mutant with an EC50 of <1 μM. ABC transporter modulator-2 can be used in the research of diseases associated with ABC transporter dysfunction .
|
-
- HY-N17966
-
|
|
Others
|
Others
|
|
Puerarin-6"-O-glucoside (Compound 2) is an isoflavonoid compound that can be isolated from the roots of Pueraria lobata (Wild.) Ohwi .
|
-
- HY-165532
-
|
SGX70393
|
Bcr-Abl
|
Cancer
|
|
SGX393 (SGX70393) is a Bcr-Abl kinase inhibitor. SGX393 binds to the active conformation of the kinase domains of both wild-type and T315I mutant Bcr-Abl, thereby inhibiting kinase activity. SGX393 exhibits antiproliferative effects in cells expressing wild-type or T315I mutant Bcr-Abl, and suppresses T315I-driven tumor growth. SGX393 can be used for the research of chronic myeloid leukemia .
|
-
- HY-125094
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
L-162782 is a high affinity AT1 receptor ligand for rat and human wild-type AT1 with IC50 values of 28.5 and 24.6 nM, respectively. L-162782 acts as a partial agonist (EC50 ≈ 30 nM) and insurmountable antagonist (IC50 = 6.5 μM) on wild-type rat AT1 receptors in COS-7 cells. L-162782 reduces Angiotensin II (HY-13948)-induced phosphatidylinositol turnover. L-162782 can be used for hypertension research .
|
-
- HY-112404
-
|
|
Src
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-13 is a dual c-Src and Abl inhibitor, with a Ki value of 0.55 μM against c-Src, 0.10 μM against wild-type Abl, and 0.40 μM against the Abl T315I mutant. BCR-ABL-IN-13 exerts competitive/mixed-type inhibitory effects on wild-type Abl, and non-competitive inhibitory effects on the drug-resistant Abl T315I mutant. BCR-ABL-IN-13 can be used for the research of chronic myeloid leukemia .
|
-
- HY-181263
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
Jun13698 is a SARS-CoV-2 main protease (M pro) inhibitor with Ki values of 65.6 nM, 510.0 nM, and 117.5 nM against the wild-type, E166V, and E166A mutants, respectively. Jun13698 forms stable complexes with wild-type and mutant M pro to mediate enzyme inhibition. Jun13698 exhibits antiviral activity against SARS-CoV-2 variants carrying the E166V/A mutation. Jun13698 is applicable to COVID-19-related research .
|
-
- HY-180979
-
|
|
PROTACs
Bcr-Abl
|
Cancer
|
|
P22D is a BCR-ABL PROTAC degrader based on Dasatinib (HY-10181), with a DC50 value of approximately 10 nM for the wild-type BCR-ABL protein. P22D cannot degrade the BCR-ABL T315I mutant. P22D has inhibitory activity against K562 cells (wild type), but is ineffective against BaF3-BCR-ABL (T315I) cells. P22D can be used for research on chronic myeloid leukemia and acute lymphocytic leukemia .
|
-
- HY-170830
-
|
|
Bacterial
|
Infection
|
|
Mtb against-1 (compound 17af) is an inhibitor of Mycobacterium tuberculosis, with IC90 values of 1.2 μM and 0.9 μM for the wild-type and LepB low-deformation strains, respectively .
|
-
- HY-P2360
-
|
Ras 5-17
|
Ras
|
Others
|
|
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
|
-
- HY-10468
-
NM107
1 Publications Verification
2'-C-Methylcytidine
|
HCV
|
Infection
|
|
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 .
|
-
- HY-P2319A
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P5437
-
|
|
PKC
|
Others
|
|
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
|
-
- HY-N12399
-
|
|
PKA
|
Inflammation/Immunology
|
|
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 .
|
-
- HY-10572
-
-
- HY-146394
-
|
|
HBV
DNA/RNA Synthesis
|
Infection
|
|
HBV-IN-22 (Compound LC5f) is an inhibitor of HBV DNA replication with IC50 values of 0.71 μM and 0.84 μM against wild-type and agent resistant HBV strains, respectively .
|
-
- HY-18634
-
|
ZMC1
|
MDM-2/p53
|
Cancer
|
|
NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.
|
-
- HY-147582
-
|
|
Btk
|
Cancer
|
|
BTK-IN-12 is a potent BTK inhibitor with IC50s of 1.2 nM and 0.8 nM for wild-type BTK or mutated BTK (C481S), respectively (WO2022037649A1; compound 8) .
|
-
- HY-W097867
-
|
8-Methoxy Ciprofloxacin; 8-Methoxy-cipro
|
Bacterial
|
Infection
|
|
3-Desmethyl Gatifloxacin (8-Methoxy Ciprofloxacin) induces DNA cleavage mediated by wild-type gyrase and Quinolone-resistant mutants. 3-Desmethyl Gatifloxacin can be used for research of drug resistance .
|
-
- HY-P4926
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research .
|
-
- HY-13223A
-
|
CP 868596-26
|
Autophagy
PDGFR
FLT3
|
Cancer
|
|
Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-121611
-
|
|
HIV
|
Inflammation/Immunology
|
|
HI-236 is a potent non-nucleoside inhibitor of HIV-1 reverse transcriptase.?
HI-236 inhibits HIV activity (wild type HTLVIIB IC50p24 < 0.001 μM) .
|
-
- HY-169427
-
|
|
EGFR
|
Cancer
|
|
FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively .
|
-
- HY-W591307
-
|
|
PROTAC Linkers
|
Cancer
|
|
P131 is a PROTAC molecule comprised of Pomalidomide-based cereblon ligand and IBT6A, linked by a PEG 3 chain. P131 can degrade both wild-type and C481S mutant BTK with nanomolar potencies.
|
-
- HY-179093
-
|
|
Potassium Channel
|
Neurological Disease
|
|
KCNT1-IN-3 (Compound 31) is a KCNT1 inhibitor with an IC50 value of 30 nM against the wild-type human KCNT1. KCNT1-IN-3 can be used in the research of epilepsy .
|
-
- HY-W558482
-
|
|
Biochemical Assay Reagents
|
Others
|
|
D-galactonic acid calcium is a CxaP ligand, with a Kd value of 6.6 µM for wild-type CxaP. D-galactonic acid calcium forms complexes with tungsten(VI). D-galactonic acid calcium can be used in the research of nutrient uptake .
|
-
- HY-13223
-
|
CP-868596
|
FLT3
PDGFR
Autophagy
|
Cancer
|
|
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-168151
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-128 (compund 28) is a potent and selective molecule targeting wild-type EGFR Ex20Ins that demonstrates efficacy in multiple human xenograft models and can cross the blood-brain barrier in preclinical species .
|
-
- HY-169428
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-138 (compound 19) is a potent EGFR inhibitor，with IC50s of 37，2.6 and 1.9 nM for Wild-type，L858R and T790M EGFR，respectively .
|
-
- HY-P2360A
-
|
Ras 5-17 TFA
|
Ras
|
Others
|
|
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12) .
|
-
- HY-108917R
-
|
GLS4 (Standard)
|
Reference Standards
HBV
|
Infection
|
|
Morphothiadin (Standard) is the analytical standard of Morphothiadin (HY-108917). This product is intended for research and analytical applications. Morphothiadin is a potent inhibitor on the replication of both wild-type and adefovir (HY-B1826)-resistant HBV with an IC50 of 12 nM.
|
-
- HY-B1902S
-
|
EGIS-5645-d6
|
Isotope-Labeled Compounds
Antifolate
Bacterial
|
Infection
|
|
Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
|
-
- HY-128596
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK-IN-6 (compound 11) is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK), with IC50 values of 71 nM, 18.72 nM and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L, respectively .
|
-
- HY-177534
-
|
|
MAGL
|
Metabolic Disease
|
|
MGL-IN-2 (Compound 1) is a MGL inhibitor with IC50 values of 0.006 μM and 0.0121 μM for mutant MGL and wild-type MGL, respectively. MGL-IN-2 can be used in the research of metabolic diseases .
|
-
- HY-10542A
-
|
|
Atg8/LC3
Raf
|
Neurological Disease
|
|
(Z)-GW 5074 is a compound which interacts with both mHTT (mutant huntingtin protein) and LC3, but not but not with the wild-type HTT protein. (Z)-GW 5074 inhibits c-Raf, shows no effect on autophagy, and is effective for neurodegenerative disorder .
|
-
- HY-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-16985
-
|
ODM-201; BAY-1841788
|
Androgen Receptor
|
Cancer
|
|
Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki of 11 nM for rat wild-type AR (wtAR) and IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
|
-
- HY-100818R
-
|
TAS-120 (Standard)
|
Reference Standards
FGFR
|
Cancer
|
|
Futibatinib (Standard) is the analytical standard of Futibatinib. This product is intended for research and analytical applications. Futibatinib (TAS-120) is an orally bioavailable, highly selective, and irreversible FGFR inhibitor, with IC50s of 3.9, 1.3, 1.6, and 8.3 nM for FGFR 1-4, respectively. Futibatinib inhibits mutant and wild-type FGFR2 with similar IC50s (wild-type FGFR2=0.9 nM; V5651=1-3 nM; N550H=3.6 nM; E566G=2.4 nM) .
|
-
- HY-149936
-
|
|
HIV Protease
|
Infection
|
|
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 .
|
-
- HY-136173
-
|
TNO155
|
SHP2
Phosphatase
|
Cancer
|
|
Batoprotafib (TNO155) is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). Batoprotafib has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors .
|
-
- HY-155048
-
|
|
Bacterial
|
Infection
|
|
BDM91270 (compound 29) is an E. coli AcrAB-TolC efflux pump inhibitor with an EC90 of 0.6 μM for wild-type E. coli AcrB. BDM91270 can be used in the study of Escherichia coli drug resistance .
|
-
- HY-105249
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
RDEA 806 is an orally active non-nucleoside reverse transcriptase inhibitor (NNRTI) that exhibits potent in vitro inhibitory activity against both wild-type HIV-1 (EC50 = 3.05 nM) and NNRTI-resistant HIV-1 .
|
-
- HY-182497
-
|
|
HIV
|
Infection
|
|
U 95133 is a non-nucleoside reverse transcriptase inhibitor. U 95133 exhibits activity against both wild-type and mutant HIV-1 reverse transcriptase. U 95133 can be used in studies related to HIV infection .
|
-
- HY-177375
-
|
|
MDM-2/p53
|
Cancer
|
|
dsP53-285 saRNA is a small activating RNA (saRNA) that readily activates wild-type p53 expression by targeting its promoter. dsP53-285 saRNA suppresses bladder cancer cells growth and metastasis .
|
-
- HY-144105
-
|
|
MDM-2/p53
|
Cancer
|
|
NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53 .
|
-
- HY-116833
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
4-Chloro-3,5-dimethylphenoxyacetic acid (compound 602 UC) is a product of masked amide bond hydrolysis of auxin analog 602 (compound 602). Auxin can effectively stimulate hypocotyl growth in wild-type seedlings .
|
-
- HY-151938
-
|
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-3 is a pyrimidine-5-carboxamide derivative, acts as an inhibitor of HIV-1. Reverse transcriptase-IN-3 shows potent activity against the HIV-1 wild-type and mutant strains .
|
-
- HY-129943
-
|
|
Bacterial
|
Infection
|
|
Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2) .
|
-
- HY-147988
-
|
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
DNA Gyrase-IN-5 (Compound 8I-w) is a potent DNA gyrase inhibitor with an IC50 of 0.10 μM. DNA Gyrase-IN-5 shows antibacterial activities against wild type and drug-resistant strains .
|
-
- HY-167948
-
|
|
EGFR
|
Cancer
|
|
Dacomitinib metabolite M1/2 is a potent inhibitor of both wild-type (WT) EGFR and the T790M mutation, demonstrating significant activity against acquired resistance mechanisms in EGFR-mutant non-small-cell lung cancer (NSCLC).
|
-
- HY-132609
-
|
|
Small Interfering RNA (siRNA)
Transthyretin (TTR)
|
Neurological Disease
|
|
Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis .
|
-
- HY-111396
-
|
|
Bacterial
|
Infection
|
|
PC58538 is a cell division inhibitor, targeting to FtsZ. PC58538 shows moderate antibacterial activity, and inhibits cell division in vegetative cells of wild-type B. subtilis. PC58538 is also known to modulate the rate of GTP hydrolysis .
|
-
- HY-174245
-
|
|
RET
|
Cancer
|
|
RET-IN-30 (Compound 28) is a RET inhibitor that exhibits inhibitory activity against both wild-type RET and some of its mutants. RET-IN-30 can inhibit the proliferation of A549 cells and has anti-tumor activity .
|
-
- HY-162698
-
|
|
Thymidylate Synthase
|
Cancer
|
|
JMF4073 is a thymidylate (TMP) and cytidylate (CMP) kinases inhibitor with IC50s of 0.16 μM and 0.17 μM, respectively. JMF4073 eliminates wild-type (WT)-Bcr-Abl-transformed myeloid cells in vitro and in vivo .
|
-
- HY-148742
-
|
|
RET
|
Cancer
|
|
RET-IN-21 (compound 5) is a selective RET V804M inhibitor with the IC50 of 0.02 μM. RET-IN-21 does not inhibit the wild type isoforms of RET or KDR. RET-IN-21 has antitumor activity .
|
-
- HY-112306R
-
|
DCC-2618 (Standard)
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
Reference Standards
|
Cancer
|
|
Ripretinib (Standard) is the analytical standard of Ripretinib. This product is intended for research and analytical applications. Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
|
-
- HY-185379
-
|
|
STING
|
Inflammation/Immunology
|
|
STING antagonist-3 is a potent STING antagonist with an IC50 of 2.3 nM against human wild-type STING. STING antagonist-3 inhibits human wild-type STING and the gain-of-function STING mutants N154S and V155M. STING antagonist-3 suppresses IFN‑α2a production in stimulated human whole blood. STING antagonist-3 inhibits IP-10 production in activated human dermal microvascular endothelial cells (HMVEC-d). STING antagonist-3 can be used for the research of autoimmune diseases, autoinflammatory diseases, interferonopathies, and fibrotic disorders .
|
-
- HY-136450
-
|
TCBZ-SO
|
Parasite
BCRP
|
Infection
Cancer
|
|
Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
|
-
- HY-16305S
-
|
1263W94-d6; BW1263W94-d6; GW257406X-d6
|
Isotope-Labeled Compounds
|
Others
|
|
Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
|
-
- HY-126987R
-
|
|
Acetolactate Synthase (ALS)
Reference Standards
|
Others
|
|
Mesosulfuron-methyl (Standard) is the analytical standard of Mesosulfuron-methyl. This product is intended for research and analytical applications. Mesosulfuron-methyl is a sulfonylurea herbicide that inhibits acetolactate synthase (ALS) and is used in research for post-emergence control of ryegrass and Avena spp. (wild oat) in wheat fields .
|
-
- HY-N5109
-
|
|
Parasite
|
Infection
|
|
Cheilanthifoline, an alkaloid, is isolated from Corydalis calliantha. Cheilanthifoline exhibits antiplasmodial activities against Plasmodium falciparum, with IC50s of 0.90 μg/mL and 1.22 μg/mL for wild type (TM4) and multidrug resistant (K1) strains, respectively .
|
-
- HY-162477
-
|
|
Cathepsin
Apoptosis
|
Cancer
|
|
TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
|
-
- HY-139884
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM).
|
-
- HY-B1838
-
Asulam
1 Publications Verification
|
Herbicide
|
Others
|
|
Asulam is a herbicide with control activity against wild oats. Asulam can be used for bulb production in spinach, tulips, daffodils and lilies. Maximum residue limits (MRLs) for Asulam were evaluated in spinach. The review of Asulam took into account its endocrine disrupting properties .
|
-
- HY-122389R
-
|
|
Herbicide
Reference Standards
|
Others
|
|
Difenzoquat methyl sulfate (Standard) is the analytical standard of Difenzoquat methyl sulfate. This product is intended for research and analytical applications. Difenzoquat methyl sulfate is a herbicide, which is used for post-emergence control of wild oats in cereal crops. Difenzoquat methyl sulfate is toxic to health and environment .
|
-
- 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-162461
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
HIV-1 inhibitor-66 is an orally active non-nucleoside reverse transcription inhibitor (NNRTI). HIV-1 inhibitor-66 shows inhibitory activity against wild-type HIV-1 reverse transcriptase with an IC50 of 40 nM .
|
-
- HY-160287
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
NVS MLLT-1 (compound 3), a chemical probe, is a potent and selective MLLT1 inhibitor with Kd values of 0.18 μM, 0.24 μM, and 0.22 μM for wild-type, T1 mutants, and T3 mutants, respectively .
|
-
- HY-N7433R
-
|
Ethylidene-glucose (Standard)
|
Reference Standards
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-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-186101
-
|
|
MDM-2/p53
|
Cancer
|
|
P53 mutant stabilizer-1 (compound 274) is a covalent mutant p53 stabilizer. P53 mutant stabilizer-1 can be used for the study of wild-type function of p53 mutants, such as cancers associated with p53 mutation .
|
-
- HY-16305R
-
|
1263W94 (Standard); BW1263W94 (Standard); GW257406X (Standard)
|
EBV
Reference Standards
CMV
|
Infection
|
|
Maribavir (Standard) is the analytical standard of Maribavir. This product is intended for research and analytical applications. Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM. Maribavir has potent antiviral activity against HCMV and Epstein-Barr virus (EBV).
|
-
- HY-16985R
-
|
ODM-201 (Standard); BAY-1841788 (Standard)
|
Reference Standards
Androgen Receptor
|
Cancer
|
|
Darolutamide (Standard) is the analytical standard of Darolutamide (HY-16985). This product is intended for research and analytical applications. Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
|
-
- HY-183667
-
|
|
Androgen Receptor
Kallikrein
|
Cancer
|
|
JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer .
|
-
- HY-N3354
-
|
8-prenylgenistein
|
Apoptosis
|
Cancer
|
|
Lupiwighteone is an isoflavone present widely in wild-growing plants, with antioxidant, antimicrobial and anticancer effects. Lupiwighteone induces caspase-dependent and -independent apoptosis on human breast cancer cells via inhibiting PI3K/Akt/mTOR pathway .
|
-
- HY-W005288
-
|
4-Hydroxystyrene
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
|
-
- 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-N9022
-
|
|
Others
|
Others
|
|
(S)-1-(4-Hydroxy-2,2-dimethylchroman-6-yl)ethanone is an enantiopure chiral alcohol. Stereoselective reduction of prochiral ketones is studied by using both cell cultures and wild tissues of various endemic plant species .
|
-
- HY-17041R
-
|
TMC114 Ethanolate (Standard)
|
Reference Standards
HIV
HIV Protease
|
Infection
|
|
Darunavir (Ethanolate) (Standard) is the analytical standard of Darunavir (Ethanolate). This product is intended for research and analytical applications. Darunavir ethanolate (TMC114 Ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
|
-
- HY-168344
-
|
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
CACPD2011a-0001278239 is a β2AR mixed agonist that shows a wide range of high-affinity binding to both wild-type and T164I β2AR variants, with no cytotoxicity or mutagenicity, making it suitable for asthma research .
|
-
- HY-103682
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PF-06726304 is a potent and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 displays robust antitumor growth activity .
|
-
- HY-135815B
-
|
TAK-788 mesylate; AP32788 mesylate
|
EGFR
|
Cancer
|
|
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research .
|
-
- HY-10572B
-
-
- HY-114636
-
|
|
Insecticide
|
Others
|
|
RG-102240 is a ligand for insect ecdysone receptor (EcR), with IC50 of 85 and 13 nM, in wildtype G:CfE(DEF) and its A110P mutant. RG-102240 induces the reporter gene activity of wild-type CfEcR and A110P mutant .
|
-
- HY-172762
-
|
|
HDAC
Molecular Glues
Histone Demethylase
|
Cancer
|
|
S234984 is a molecular glue degrader. S234984 forms a stable ternary complex with wild-type KBTBD4 E3 ligase and HDAC2 to drive neomorphic ubiquitination and degradation of CoREST1 and LSD1. S234984 can be used for the research of medulloblastoma .
|
-
- HY-145411
-
|
|
Liposome
|
Endocrinology
|
|
PEG2000-C-DMG, a pegylated lipid, can be used for the preparation of Onpattro. Onpattro, a hepatically directed investigational RNAi therapeutic agent, harnesses this process to reduce the production of mutant and wild-type transthyretin by targeting the 3′ untranslated region of transthyretin mRNA .
|
-
- HY-103682A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity .
|
-
- HY-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-172582
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-38 (compound 14) is a CDK9 inhibitor with IC50 values of 1.2 nM and 3.3 nM for CDK9 wild-type and L156F mutant, respectively. CDK9-IN-38 inhibits tumor growth in vivo and in vitro .
|
-
- HY-10364
-
|
|
Bcr-Abl
|
Cancer
|
|
AP24163 is a BCR-ABL kinase inhibitor. AP24163 inhibits wild-type (native) BCR-ABL and BCR-ABL-T315I with IC50 values of 7 nM and 511 nM, respectively. AP24163 can be used in the research of chronic myeloid leukemia (CML) .
|
-
- HY-164466A
-
|
|
Calcium Channel
Notch
|
Cancer
|
|
CAD204520 dihydrochloride, a SERCA inhibitor (IC50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). CAD204520 dihydrochloride can be used for T-ALL and MCL research .
|
-
- HY-146145
-
|
|
Fungal
Mitochondrial Metabolism
|
Infection
|
|
Metyltetraprole is a promising fungicide with EC50 values of both 0.002 ppm against sensitive wild-type and G143A mutant of Zymoseptoria tritici. Metyltetraprole is effective against QoI (quinone outside inhibitor) resistant strains. Metyltetraprole inhibits the respiratory chain via complex III .
|
-
- HY-159984
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-78 (compound 15f) is a potent and broad-spectrum non-nucleoside reverse transcriptase inhibitor, with an EC50 of 3 nM for wild-type HIV-1. HIV-1 inhibitor-78 can be used for the research of HIV infection .
|
-
- HY-16767
-
|
MK-1439
|
HIV
Reverse Transcriptase
|
Infection
Inflammation/Immunology
|
|
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-164466
-
|
|
Calcium Channel
Notch
|
Cancer
|
|
CAD204520, a SERCA inhibitor (IC50 = 0.34 μM), targets mutated over wild type NOTCH1 proteins in T-cell acute lymphoblastic leukemia (T-ALL) and mantle cell lymphoma (MCL). CAD204520 can be used for T-ALL and MCL research .
|
-
- 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-143734
-
|
|
EGFR
|
Cancer
|
|
HER2-IN-6 is a potent inhibitor of HER2. HER2-IN-6 has the potential for the research of wild and/or mutant EGFR and/or HER2 kinase mediated tumor (extracted from patent WO2021164697A1, compound 11) .
|
-
- HY-164529
-
|
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
|
-
- HY-136450R
-
|
TCBZ-SO (Standard)
|
Reference Standards
Parasite
BCRP
|
Infection
|
|
Triclabendazole sulfoxide (Standard) is the analytical standard of Triclabendazole sulfoxide. This product is intended for research and analytical applications. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
|
-
- HY-179506
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
P53 Activator 16 (Compound JC16) is a p53 activator. P53 Activator 16 exhibits selective cytotoxicity and pro-apoptotic (apoptosis) activity towards p53-Y220C mutant cancer cells, while having little effect on wild-type or P53-deficient cells. P53 Activator 16 induces the conformational transition of cell p53-Y220C from the mutant form to the wild-type form, accompanied by the transcriptional activation of p53 target genes, without increasing the overall level of p53 protein. P53 Activator 16 can be used for the study of p53 mutant cancers .
|
-
- HY-16985S
-
|
ODM-201-d4; BAY-1841788-d4
|
Isotope-Labeled Compounds
Androgen Receptor
|
Cancer
|
|
Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
|
-
- HY-179094
-
|
|
PROTACs
IRAK
NF-κB
Enolase
|
Inflammation/Immunology
Cancer
|
|
PSP-0119 is a highly efficient and effective PROTAC degrader targeting IRAK4 (IC50 = 2.83 nM). PSP-0119 can inhibit IRAK4 kinase activity, NF-κβ activity, and IL-1β-induced IRAK4 phosphorylation. PSP-0119 degrades IRAK4 in FLT3-mutant AML cell lines, sparing FLT3-wild-type AML cells, FLT3-wild-type samples, and normal bone marrow. PSP-0119 downregulates alpha-enolase (eNOS) of MOLM-13 cells. PSP-0119 can be used for the study of Acute Myeloid Leukemia (AML) .
|
-
- HY-136450S
-
|
TCBZ-SO-d3
|
Isotope-Labeled Compounds
Parasite
BCRP
|
Infection
|
|
Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
|
-
- HY-179507
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer .
|
-
- HY-162595A
-
|
|
Bacterial
|
Infection
|
|
BDM88855 hydrochloride is an allosteric inhibitor for the homolog AcrB protein. BDM88855 hydrochloride can boost the antibacterial effect of a panel of antibiotics (eg: Oxacillin (HY-B0925A), Linezolid (HY-10394), Novobiocin (HY-B0425), etc.) on wild-type E. coli .
|
-
- HY-117556
-
|
|
HIV
|
Infection
|
|
U-104489 is a HIV-1 inhibitor with the Ki values of 0.13, 0.12 and ＞ 100 μM aganist HIV-1 RT p66/p51 wild type (G190), G190A and G190E, respectively .
|
-
- HY-118742
-
|
|
Environmental Pollutants
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-118806
-
|
|
mAChR
|
Neurological Disease
|
|
AC-42 is a poent M1 muscarinic selective allosteric agonist with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 stimulates the IP-accumulation and calcium mobilization in CHO cells .
|
-
- 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-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-10572S1
-
-
- HY-111147
-
|
|
HIV
|
Infection
|
|
RDEA-427 is a pyrrolopyrimidine derivative and also a HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI). RDEA-427 acts on wild-type and NNRTI-resistant mutant HIV-1. RDEA-427 can be used in research related to HIV infection .
|
-
- HY-162595
-
|
|
Bacterial
|
Infection
|
|
BDM88855 is an allosteric inhibitor for the homolog AcrB protein. BDM88855 can boost the antibacterial effect of a panel of antibiotics (eg: Oxacillin (HY-B0925A), Linezolid (HY-10394), Novobiocin (HY-B0425), etc.) on wild-type E. coli .
|
-
- HY-P11465
-
|
|
Fungal
|
Infection
|
|
Histone H3 (73-83) is a histone H3 fragment. Histone H3 (73-83) can be obtained from incomplete tryptic digestion of underivatized wild-type histone H3. Histone H3 (73-83) can be used in the research of yeast infection .
|
-
- HY-179527
-
|
|
ROS Kinase
|
Cancer
|
|
LIG48 is ROS1 kinase domain and its mutant (G2032R ROS1 kinase domain) inhibitor. LIG48 remains within the mutated and wild-type ROS1 kinase domains. LIG48 can be used for the study of non-small cell lung cancer .
|
-
- 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-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-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)
|
Reference Standards
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-183034
-
|
|
ATP-binding cassette (ABC) transporters
|
Metabolic Disease
|
|
ABCC6 modulator-3 (Compound I-71) is a ABCC6 activator with an EC50 < 1 μM. ABCC6 modulator-3 upregulates the expression of wild-type ABCC6. ABCC6 modulator-3 is used in research on diseases associated with ABC transporter dysfunction .
|
-
- 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-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-170219
-
|
|
Parasite
Epigenetic Reader Domain
|
Infection
|
|
RMM23 is an inhibitor targeting PfBDP1 with a Kd value of 1.24 μM. RMM23 against the wild-type strains 3D7 and NF54, and the multidrug-resistant K1 strain in vitro blood stage, with EC50 values of 18 μM, 14 μM, 20 μM, respectively .
|
-
- HY-183702
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
BDM91531 is a AcrB inhibitor with an EC50 of 0.16 μM against E. coli. BDM91531 acts as an antibiotic potentiator to restore the sensitivity of wild-type Escherichia coli to multiple AcrB substrate antibiotics. BDM91531 exhibits antibacterial activity. BDM91531 can be used in the research of bacterial infections .
|
-
- 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-12580
-
|
|
MDM-2/p53
|
Cancer
|
|
RO5353 is an orally active inhibitor for p53-MDM2 with an IC50 of 7 nM for MDM2. RO5353 inhibits the proliferation of wild-type p53 cancer cells with an average IC50 of 7 nM. RO5353 exhibits antitumor efficacy and good pharmacokinetic characteristics in mice .
|
-
- HY-114737
-
|
|
Bacterial
|
Infection
|
|
L-573655 is a reversible inhibitor of UDP-3-O-[R-3-hydroxymyristoyl]-GlcNAc deacetylase with an IC50 value of 8.5 μM. L-573655 possesses antibacterial activity against a wild-type strain of E. coli. with MIC values of 200-400 μg/mL .
|
-
- HY-154966
-
|
|
RSV
|
Infection
|
|
RSV L-protein-IN-3 is a wild-type RSV polymerase inhibitor with an IC50 value of 10.4 μM and an EC50 value of 2.1 μM (against RSV). RSV L-protein-IN-3 has lesser cytotoxicity than the clinical agent, Ribavirin (HY-B0434) .
|
-
- HY-13223R
-
|
CP-868596 (Standard)
|
FLT3
PDGFR
Autophagy
Reference Standards
|
Cancer
|
|
Crenolanib (Standard) is the analytical standard of Crenolanib. This product is intended for research and analytical applications. Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-110094
-
BIMU 8
1 Publications Verification
|
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-59320
-
|
|
Biochemical Assay Reagents
Drug Intermediate
|
Metabolic Disease
|
|
4-Thiazolecarboxylic acid (Compound 1e) is an intermediate. 4-Thiazolecarboxylic acid can be used in the synthesis of MGL-IN-2 (HY-177534). MGL-IN-2 inhibits wild-type MGL enzyme activity with an IC50 of 0.0121 μM. 4-Thiazolecarboxylic acid can be used in the research of metabolic diseases .
|
-
- 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-147645
-
|
|
FBPase
|
Metabolic Disease
|
|
FBPase-IN-2 (Compound HS36) is a covalent FBPase inhibitor with an IC50 value of 0.15 μM for wild-type FBPase. FBPase-IN-2 inhibits glucose production in primary mouse hepatocytes via gluconeogenesis modulation. FBPase-IN-2 can be used for the research of type 2 diabetes mellitus .
|
-
- 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-109028
-
|
TR2-A
|
Cholecystokinin Receptor
Bacterial
|
Infection
Cardiovascular Disease
|
|
Ceclazepide (TR2-A), a CCK2R antagonist, is an orally active Mycobacterium abscessus inhibitor. Ceclazepide inhibits acid secretion in rats. Ceclazepide effectively suppresses the growth of M. abscessus wild-type strain and multiple subspecies. Ceclazepide inhibits M. abscessus growth within macrophages without causing harm .
|
-
- HY-161246
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
|
-
- HY-12025
-
|
JNJ-26854165
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes .
|
-
- HY-14852
-
-
- HY-W714171
-
|
BAY MKH 6561
|
Herbicide
|
Others
|
|
Propoxycarbazone sodium (BAY MKH 6561) is a herbicide. Propoxycarbazone sodium controls shepherd’s purse (Capsella bursa-pastoris L. Medicus), tumble mustard (Sisymbrium altissimum L.), field pennycress (Thlaspi arvense L.), and several Bromus species. Propoxycarbazone sodium also inhibits the growth of jointed goatgrass, wild oat (Avena fatua L.), and quackgrass (Elytrigia repens L. Nevski) .
|
-
- 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-W740378
-
|
AFN-941
|
EGFR
JAK
|
Others
|
|
1,2,3,4-Tetrahydrostaurosporine is a derivative of Staurosporine (HY-15141) and an inhibitor of mutant EGFR (IC50=74 nM for EGFRT790M). It is selective for EGFRT790M over wild-type EGFR (IC50=390 nM). It also binds to Janus kinase 3 (JAK3).
|
-
- HY-167135
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
DPC-082 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1. DPC-082 inhibits wild-type RF virus with an IC90 of 2.0 nM. DPC-082 inhibits various single and many multiple amino acid substituted HIV-1 mutant viruses .
|
-
- 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-183553
-
|
|
Ras
|
Cancer
|
|
AUBE00 is an orally active, selective cyclic peptide pan-KRAS inhibitor. AUBE00 selectively binds to the OFF state of KRAS. AUBE00 exhibits anticancer activity against RAS wild-type colorectal cancer. The combination of AUBE00 with Cetuximab (HY-P9905) produces a synergistic antiproliferative effect .
|
-
- HY-10468R
-
|
2'-C-Methylcytidine (Standard)
|
Reference Standards
HCV
|
Infection
|
|
NM107 (Standard) is the analytical standard of NM107. This product is intended for research and analytical applications. 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 .
|
-
- HY-153390
-
|
|
Histone Methyltransferase
|
Cancer
|
|
AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
|
-
- HY-139279
-
|
TPX-0131
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Zotizalkib (TPX-0131) is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). Zotizalkib has strong antitumor activities .
|
-
- HY-144297
-
|
|
HDAC
Parasite
|
Infection
|
|
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites .
|
-
- HY-135892
-
|
|
MAP4K
|
Inflammation/Immunology
|
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively .
|
-
- HY-157887
-
ADT-007
1 Publications Verification
|
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-108508R
-
|
|
Reference Standards
Smo
Hedgehog
|
Cancer
|
|
SMANT hydrochloride (Standard) is the analytical standard of SMANT (hydrochloride) (HY-108508). This product is intended for research and analytical applications. 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 .
|
-
- HY-136450S1
-
|
TCBZ-SO-13C,d3
|
Isotope-Labeled Compounds
Parasite
BCRP
|
Infection
|
|
Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast 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-126720
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
N-Lignoceroyl Taurine is an arachidonoyl amino acid and taurine conjugate with a fatty acid that can be isolated from bovine brain. N-Lignoceroyl Taurine is one of several novel taurine-conjugated fatty acids discovered during mass spectrometry lipidomic analysis of the brain and spinal cord of wild-type and fatty acid amide hydrolase (FAAH) knockout mice. N-Lignoceroyl Taurine levels were 23-26-fold higher in FAAH -/- mice compared to wild-type mice, suggesting that FAAH utilizes N-Lignoceroyl Taurine as a substrate. However, in vitro experiments with purified FAAH showed that N-Lignoceroyl Taurine was hydrolyzed 2,000-fold slower in FAAH compared to oleoylethanolamide. N-Acyl Taurines with polyunsaturated acyl chains can activate members of the transient receptor potential (TRP) calcium channel family, including TRPV1 and TRPV4.
|
-
- HY-186151
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53 null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer .
|
-
- HY-W419221
-
|
|
Herbicide
|
Others
|
|
Bixlozone, a proherbicide that requires in planta activation to its phytotoxic form, 5-ketobixlozone, is used to selectively control annual ryegrass (Lolium rigidum) in Australian cereal and canola crops. .
|
-
- HY-P991507
-
|
|
EGFR
|
Cancer
|
|
SCT200 is a fully humanized IgG1 anti-EGFR monoclonal antibody with a Kd of 0.08 nM. SCT200 can kill tumor cells by complement-dependent cytotoxicity (CDC) and antibody-dependent cellular cytotoxicity (ADCC) through the Fc. SCT200 can be used for the study of refractory RAS and BRAF wild-type metastatic colorectal cancer .
|
-
- 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-125258
-
|
|
Phosphatase
Filovirus
|
Infection
|
|
EBOV-IN-11 is a protein phosphatase 1 (PP1) inhibitor, with Kd values of 1.88 nM and 8.01 nM against wild-type and quadruple-mutant PP1, respectively. EBOV-IN-11 potently inhibits the replication and transcription of EBOV-eGFP virus. EBOV-IN-11 can be used in studies related to Ebola virus infection .
|
-
- HY-136938
-
NEO2734
4 Publications Verification
EP31670
|
Epigenetic Reader Domain
Histone Acetyltransferase
|
Cancer
|
|
NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains . NEO2734 is active in SPOP mutant and wild-type prostate cancer .
|
-
- HY-169903
-
|
|
Apoptosis
|
Cancer
|
|
SMIP34 is a PELP1 inhibitor. SMIP34 binds to PELP1 with a Kd of 37.4 μM. SMIP34 inhibits cancer cell proliferation and tumor progression. SMIP34 can be used for breast cancer research, and is active against wild-type (WT), mutant (MT) ER+ and therapy-resistant (TR)-ER+ breast cancer .
|
-
- HY-155285
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
YS-363 is a potent, selective, and orally active EGFR inhibitor, with IC50s of 0.96 nM and 0.67 nM for wild-type and L858R mutant forms of EGFR, respectively. YS-363 can induce G0/G1 cell cycle arrest and apoptosis .
|
-
- HY-15011
-
|
|
Oxytocin Receptor
|
Others
|
|
L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR .
|
-
- HY-103320
-
|
|
CaSR
|
Metabolic Disease
|
|
Calhex 231 is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- HY-152292
-
|
NVL-520; NUV-520
|
ROS Kinase
|
Cancer
|
|
Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer .
|
-
- HY-122753
-
|
|
MDM-2/p53
|
Cancer
|
|
SLMP53-1 is a wild-type and mutant p53 reactivator with promising antitumor activity. SLMP53-1 mediates the reprograming of glucose metabolism in cancer cells. SLMP53-1 depletes angiogenesis, decreasing endothelial cell tube formation and vascular endothelial growth factor (VEGF) expression levels .
|
-
- HY-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-P990282
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Anti-Mouse CD24 Antibody (M1/69) is a rat-derived anti-mouse CD24 IgG2b κ type antibody inhibitor. Anti-Mouse CD24 Antibody reduces heat stable antigen (HSA) expression level and delays wound healing in Wild-type HSA +/+ mice .
|
-
- 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-134823
-
MD-222
1 Publications Verification
|
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-W704348
-
|
|
Isotope-Labeled Compounds
MDM-2/p53
|
Cancer
|
|
Diphenyltin Dichloride-d10 is the deuterium labeled NSC405640 (HY-144105). NSC405640 is a potent inhibitor of the MDM2-p53 interaction. NSC405640 rescues structural p53 mutations. NSC405640 selectively inhibits the growth of cell lines with wild-type p53 .
|
-
- HY-167642
-
|
(Z)-R278474; (Z)-TMC278; (Z)-DB08864
|
Drug Isomer
HIV
Reverse Transcriptase
|
Infection
|
|
(Z)-Rilpivirine ((Z)-R278474) is the (Z)-isomer of Rilpivirine (HY-10574). Rilpivirine is an effective and selective diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). It exhibits potent antiviral activity against both wild-type HIV (EC50 = 0.4 nM) and mutant strains (EC50 = 0.1-2.0 nM) .
|
-
- HY-145702
-
|
|
MEK
ERK
|
Cancer
|
|
MAP855 is a highly potent, selective, ATP-competitive and orally active MEK1/2 kinase inhibitor (MEK1 ERK2 cascade IC50=3 nM, pERK EC50=5 nM). MAP855 shows equipotent inhibition of wild-type and mutant MEK1/2 .
|
-
- HY-103320A
-
|
|
CaSR
|
Metabolic Disease
|
|
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC50 = 0.39 μM) increases in [ 3H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca 2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- HY-183562
-
|
UIC-94003
|
HIV
HIV Protease
|
Infection
|
|
TMC-126 (UIC-94003) is a non-peptidic HIV-1 protease (HIV-1 protease) inhibitor. TMC-126 exhibits highly potent antiproliferative activity against wild-type HIV-1. TMC-126 can be used in studies related to HIV infection [1] .
|
-
- 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-149928
-
|
|
HIV
|
Infection
|
|
NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties .
|
-
- HY-105506
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
EXP-7711 is a non peptide angiotensin II (Ang II) AT1 receptor antagonist. EXP-7711’s affinity for wild-type AT1 receptor (Ki =180 nM) is lower than peptide antagonists, but higher than losartan (Ki = 12 nM). EXP-7711 can be used for research on cardiovascular conditions .
|
-
- 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-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-P99715
-
|
|
EGFR
|
Cancer
|
|
Losatuxizumab 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-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-135815R
-
|
TAK-788 (Standard); AP32788 (Standard)
|
EGFR
Reference Standards
|
Cancer
|
|
Mobocertinib (Standard) is the analytical standard of Mobocertinib. This product is intended for research and analytical applications. 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-15103
-
|
|
PTHR
Androgen 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-100131
-
GSK481
1 Publications Verification
|
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-182915
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-26 is an orally active FGFR inhibitor. FGFR-IN-26 inhibits FGFR2 wild-type and clinically relevant resistance mutations. FGFR-IN-26 inhibits tumor growth in FGFR2-amplified xenograft mouse models. FGFR-IN-26 can be used for the research of cancer, suah as gastric carcinoma .
|
-
- HY-146364
-
|
|
DNA/RNA Synthesis
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-W708304
-
|
|
Isotope-Labeled Compounds
Herbicide
|
Others
|
|
Asulam-d3 is the deuterium labeled Asulam (HY-B1838). Asulam is a herbicide with control activity against wild oats. Asulam can be used for bulb production in spinach, tulips, daffodils and lilies. Maximum residue limits (MRLs) for Asulam were evaluated in spinach. The review of Asulam took into account its endocrine disrupting properties .
|
-
- 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-186167
-
|
|
IKK
|
Cancer
|
|
CDDO-biotin is an IKKβ inhibitor with cancer cell inhibitory activity. CDDO-biotin directly interacts with and oxidizes Cys-179 in the activation loop of IKKβ, forming an adduct with wild-type IKKβ. CDDO-biotin can be used in the research of myeloid leukemia, osteosarcoma, multiple myeloma, lung cancer, breast cancer and pancreatic cancer .
|
-
- HY-178291
-
|
|
SARS-CoV
|
Infection
|
|
2-Chloro-2′-deoxyadenosine monophosphate is an anticoronavirus agent. It exhibits significant inhibitory effects against wild-type novel coronavirus, novel coronavirus variants (Beta, Delta, and Omicron strains), and other coronaviruses such as human coronavirus 229E, human coronavirus OC43, human coronavirus NL63, and mouse coronavirus MHV .
|
-
- HY-W110242A
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
(S)-CPP sodium serves as an inhibitor of the branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase, commonly referred to as BDK or keto acid dehydrogenase kinase. As a negative regulator of BCKDC activity, the inhibition of BDK by (S)-CPP (with an IC50 of 6.3 μM) results in the activation of the complex and a notable decrease in plasma levels of leucine/isoleucine and valine in wild-type mice.
|
-
- HY-168616
-
|
|
RSV
IGF-1R
|
Infection
|
|
CL-A3-7 is a virus-cell fusion inhibitor targeting the RSV F protein. It exerts its effect by blocking the interaction between the virus and the host IGF1R, effectively inhibiting infections of both wild-type RSV and the K394R variant. It is applicable to anti-RSV drug development and resistance-related research .
|
-
- HY-W050122
-
|
|
GABA Receptor
|
Neurological Disease
|
|
S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .
|
-
- HY-175829
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-119 (Compound A28) is a SARS-CoV-2 fusion inhibitor. SARS-CoV-2-IN-119 strongly inhibits Omicron entry with an EC50s of 1.95 and 1.08 μM for pOmicron (BA.2.86.1) and wild Omicron. SARS-CoV-2-IN-119 also has antiviral activities against wild SARS-CoV-2 and other variants, such as pseudotyped Delta SARS-CoV-2, pOmicron (BA.4) and (KP.3). SARS-CoV-2-IN-119 directly interferes with Omicron S2-mediated viral membrane fusion to block Omicron virus into host cells. SARS-CoV-2-IN-119 can be used for COVID-19 research .
|
-
- HY-181888
-
|
|
HIV
HIV Protease
|
Infection
|
GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC50=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND) .
|
-
- HY-176995
-
|
|
GHSR
|
Metabolic Disease
|
|
AZ-GHS-38 (compound 38) is an orally active CNS-penetrant inverse agonist of growth hormone secretagogue receptor (GHS-R1a) with an IC50 of 6.7 nM. AZ-GHS-38 results in acute reduction of food intake in wild-type mice. AZ-GHS-38 can be used for anti-obesity research .
|
-
- HY-118806A
-
|
|
mAChR
|
Neurological Disease
|
|
AC-42 hydrochloride is the hydrochloride salt form of AC-42 (HY-118806). AC-42 hydrochloride is an allosteric agonist for muscarinic M1 receptor with EC50s of 805 nM and 220 nM for human wild-type and Y381A mutated M1 receptors, respectively. AC-42 hydrochloride stimulates the inositol phosphate (IP)-accumulation and calcium mobilization in CHO cells .
|
-
- HY-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-121845
-
|
|
HSP
|
Metabolic Disease
|
|
4-Br-Bnlm is a selective inhibitor of glucose-regulated protein 94 (Grp94) with an EC50 value of 0.96 µM. 4-Br-Bnlm reduces the levels of mutant myocilin proteins as well as wild-type myocilin misfold in cells. 4-Br-Bnlm promotes the clearance of toxic formsof myocilin and reduces myocilin toxicity .
|
-
- HY-B0792
-
|
|
LRRK2
|
Neurological Disease
|
|
CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity .
|
-
- HY-161067
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-96 (compound 7a) is a thieno[2,3-d]pyrimidine EGFR inhibitor that can induce apoptosis. EGFR-IN-96 arrests the growth of HepG2 cells in the S phase and G2/M phase, and inhibits the growth of cancer cells bearing EGFR wild-type and EGFR T790M .
|
-
- HY-148106
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
MEL23 is a MDM2 E3 ligase inhibitor that blocks the E3 ligase activity of the MDM2-MDMX complex. MEL23 inhibits Mdm2 and p53 ubiquitination in cells, reduce viability of cells with wild-type p53. MEL23 stabilizes MDM2 via a mechanism independent of p53 transcription .
|
-
- HY-10574A
-
|
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-10572BR
-
|
(Rac)-DMP 266 (Standard); (Rac)-EFV (Standard); (Rac)-L-743726 (Standard)
|
Reference Standards
Autophagy
Parasite
HIV
Endogenous Metabolite
Reverse Transcriptase
|
Infection
Cancer
|
|
(Rac)-Efavirenz (Standard) is the analytical standard of (Rac)-Efavirenz. This product is intended for research and analytical applications. (Rac)-Efavirenz is the isomer of Efavirenz (HY-10572). Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture .
|
-
- HY-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 .
|
-
- 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-158987
-
|
APBADP
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Adenosine phosphonobutyric, 2'(3'), 5'-diposphate (APBADP) is an adenylosuccinate lyase substrate analog and competitive inhibitor. Adenosine phosphonobutyric, 2'(3'), 5'-diposphate binds to the tetramers of *Bacillus subtilis* adenylosuccinate lyase and wild-type human adenylosuccinate lyase. Adenosine phosphonobutyric, 2'(3'), 5'-diposphate can be used for research on adenylosuccinate lyase deficiency .
|
-
- 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-118742R
-
|
|
HPPD
Reference Standards
|
Others
|
|
Benzobicyclon (Standard) is the analytical standard of Benzobicyclon. This product is intended for research and analytical applications. Benzobicyclon is a 4-HPPD inhibitor and herbicide that reacts with water to form a hydrolysate of the active herbicide benzobicycline, causing bleaching and death of weeds. Benzobicyclon is effective against grass, sedge and broadleaf weeds. Benzobicyclon effectively targets sulfonylurea herbicide-resistant biotypes as well as wild-type weeds .
|
-
- HY-15041
-
|
|
Bradykinin Receptor
|
Inflammation/Immunology
|
|
NVP-SAA164 is an orally active nonpeptide kinin B1 receptor antagonist. NVP-SAA164 reverses CFA (Complete Freund's adjuvant) (HY-153808)-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, and is inactive in a model of inflammatory pain in wild-type mice .
|
-
- HY-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-19885
-
|
|
Bacterial
Dihydrofolate reductase (DHFR)
|
Infection
|
|
AR-102 has inhibitory activity towards Staphylococcus aureus. AR-102 exhibits a competitive potent inhibition of the F98Y mutant DHFR (Ki = 0.22 nM). AR-102 has been determined as ternary complex with NADPH in both wild-type S. aureus DHFR and the TMP-resistant F98Y mutant enzyme .
|
-
- HY-123153
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
GSK990 is an inactive mutant IDH1 inhibitor with no significant inhibitory activity against wild-type or mutant IDH1/IDH2 enzymes. In experiments, GSK990 can serve as an inactive negative control for the IDH1 inhibitor GSK321 (HY-18948). GSK990 is applicable to the research of acute myeloid leukemia .
|
-
- 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-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-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-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-E70893
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
α-Lytic Protease is an alternative specificity protease for proteomics applications, whose wild-type (WT) version cleaves after T, A, S, and V residues. α-Lytic Protease M190A Mutant has different cleavage specificities, and cleaves after M, F, and L residues. Both the WT and M190A forms of aLP geneRate peptides of similar average length as trypsin.
|
-
- HY-144053
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research .
|
-
- HY-107123
-
|
ASC-09
|
HIV Protease
|
Infection
|
|
TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity .
|
-
- HY-19816A
-
|
Abivertinib maleate; AC0010 maleate
|
EGFR
Btk
Apoptosis
|
Cancer
|
|
Avitinib (Abivertinib) maleate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate shows anticancer effects .
|
-
- HY-19925
-
|
|
HIV
|
Infection
|
|
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .
|
-
- HY-149991
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-56 (compound 12126065) is a potent HIV-1 non-nucleoside reverse transcriptase inhibitor. HIV-1 inhibitor-56 has antiviral activity against wild-type HIV-1 in TZM cells with an EC50 value of 0.24 nM. HIV-1 inhibitor-56 penetrates the blood-brain barrier .
|
-
- HY-149099
-
|
|
RET
|
Cancer
|
|
RET-IN-22 (compound 17b) is a potent, selective and orally active RET inhibitor with an IC50 of 20.9 nM and 18.3 nM for wild-type RET and RET-V804M, respectively. RET-IN-22 shows highly selective profile to most kinases, especially to EGFR and VEGFR2. RET-IN-22 has anticancer effects .
|
-
- HY-W747072
-
|
3-Sulfocholyl Taurine; TCA3S
|
Drug Metabolite
|
Neurological Disease
Metabolic Disease
|
|
3-Sulfo-taurocholic Acid Disodium Salt (3-Sulfocholyl Taurine; TCA3S) is a metabolite of the conjugated bile acid taurocholic acid. Plasma levels of 3-Sulfo-taurocholic Acid Disodium Salt are elevated in wild-type and Sortilin 1 (Sort1) knockout mice at 6 hours following bile duct ligation (BDL) and are further elevated in Sort1 knockout mice at 24 hours post-BDL.
|
-
- HY-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-18601
-
|
|
HIV
HIV Integrase
|
Infection
|
|
(±)-BI-D is a potent ALLINI (allosteric integrase inhibitor). (±)-BI-D binds integrase at the LEDGF/p75 binding site. (±)-BI-D inhibits HIV-Luc infection in cells (IC50: 0.16 μM in Psip1 knockout E9 mouse embryonic fibroblasts, 2.9 μM in wild-type E9 mouse embryonic fibroblasts) .
|
-
- HY-180653
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
c-Kit-IN-14 (Compound 1) is a c-kit kinase inhibitor. c-Kit-IN-14 inhibits the phosphorylation of wild-type c-kit, with an IC50 of 0.4 nM for pKIT. c-Kit-IN-14 inhibits Exon 11 KIT, with an IC50 of 0.4 nM. c-Kit-IN-14 can be used in the research of mast cell-mediated diseases such as urticaria .
|
-
- HY-180652
-
|
|
c-Kit
|
Inflammation/Immunology
|
|
c-Kit-IN-13 (Compound I) is a c-kit kinase inhibitor. c-Kit-IN-13 inhibits the autophosphorylation of wild-type c-kit, with an IC50 of 0.3 nM for pKIT. c-Kit-IN-13 inhibits Exon 11 KIT, with an IC50 of 0.9 nM. c-Kit-IN-13 can be used in the research of mast cell-mediated diseases such as urticaria .
|
-
- HY-182565
-
|
|
Plasminogen/Plasmin
|
Cancer
|
|
PSI-112 is a YO-class μPlm inhibitor, with IC50 values of 0.38 μM, 1.48 μM and 0.37 μM against the wild-type, F587A mutant and K607A mutant, respectively. PSI-112 shows low affinity for uPA. PSI-112 can be used in cancer research .
|
-
- HY-148089A
-
|
|
Transthyretin (TTR)
|
Neurological Disease
|
|
Eplontersen sodium the sodium salt form of Eplontersen (HY-148089). 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-161633
-
|
|
PROTACs
EGFR
FAK
|
Cancer
|
|
PROTAC EGFR degrader 11 (Compound B71) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 11 binds CRBN-DDB1 with a Ki of 36 nM. PROTAC EGFR degrader 11 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <100 nM.
|
-
- HY-124089
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
|
-
- HY-19815
-
|
CK-101; RX518
|
EGFR
|
Cancer
|
|
Olafertinib (CK-101) is an orally available, third generation and irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI). Olafertinib selectively inhibits both EGFR-TKI-sensitizing and resistance mutations with minimal activity on wild-type EGFR. Olafertinib can be used in research for non-small cell lung cancer (NSCLC) with EGFR mutations and other advanced malignancies .
|
-
- HY-169228
-
|
|
Btk
|
Cancer
|
|
WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds .
|
-
- HY-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-164427
-
|
|
SHP2
ERK
|
Cancer
|
|
SHP2-IN-31 is a SHP2 inhibitor, with IC50s of 13 nM (Wild-type SHP2), >10000 nM (SHP1), >10000 nM (SHP2 E76K) . SHP2-IN-31 inhibits pERK in a panel of tumor cells. SHP2-IN-31 inhibits tumor growth in RTK/KRAS-driven xenograft models .
|
-
- HY-138842
-
|
|
Insulin Receptor
Akt
ERK
|
Metabolic Disease
|
|
DDN is a selective insulin receptor (Insulin Receptor) activator, an insulin sensitizer, and a glucose-lowering insulin mimetic with oral bioavailability. DDN can directly bind to the receptor kinase domain and induce Akt and ERK phosphorylation, and it can also enhance insulin's effect on glucose uptake. DDN significantly reduces blood glucose levels in wild-type and diabetic ob/ob and db/db mice .
|
-
- HY-CE02028
-
|
Glutaconyl-coenzyme A
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaconyl-CoA (Glutaconyl-coenzyme A) is a key metabolic intermediate in the mitochondrial catabolic pathways of lysine, hydroxylysine and tryptophan. Glutaconyl-CoA competitively inhibits wild-type glutaryl-CoA dehydrogenase (GCDH) with a Ki value of 1.1 µM. Glutaconyl-CoA is generated via the oxidative decarboxylation of glutaryl-CoA catalyzed by GCDH, and is subsequently further metabolized. Glutaconyl-CoA can be used in the research of type I glutaric aciduria .
|
-
- HY-W841438
-
|
|
Amyloid-β
Tau Protein
|
Neurological Disease
|
|
Lithium orotate is an orally active lithium supplement with reduced binding that can bypass amyloid sequestration in AD mice models. Lithium orotate can prevent Aβ plaque deposition and phospho-tau accumulation and reverse AD pathology, neuroinflammatory changes and memory loss in AD mice models and ageing wild-type mice. Lithium orotate can be used for the research of alcoholism and Alzheimer’s disease .
|
-
- HY-155114
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-59 (Compound I-5b) is a HIV-1 inhibitor, with EC50s of 5.62-171 nM against the wild-type (WT) and mutant HIV-1 strains. HIV-1 inhibitor-59 has moderate RT enzyme inhibitory activity (IC50: 0.094-12.0 μM) .
|
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-16745A
-
|
KRP-AM1977 hydrochloride
|
Bacterial
|
Infection
|
|
Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitory activity against both wild-type and mutated target enzymes.
|
-
- HY-116804
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
|
-
- HY-153390A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
(R)-AMG-193 is an isomer of AMG 193 (HY-153390). AMG 193 is an orally active MTA-cooperative PRMT5 inhibitor with antitumor activity. AMG 193, when complexed with MTA, preferentially inhibits the growth of MTAP-deficient tumor cells by inhibiting PRMT5 (IC50=0.107 μM), thereby protecting normal cells with wild-type MTAP .
|
-
- HY-161632
-
|
|
PROTACs
EGFR
FAK
|
Cancer
|
|
PROTAC EGFR degrader 10 (Compound B56) is a PROTAC degrader for epidermal growth factor receptor (EGFR), with DC50 <100 nM. PROTAC EGFR degrader 10 binds CRBN-DDB1 with a Ki of 37 nM. PROTAC EGFR degrader 10 degrades EGFR, focal adhesion kinase (FAK), and RSK1, inhibits the proliferation of BaF3 wild type and EGFR mutants, with IC50 <150 nM .
|
-
- HY-153856
-
|
|
EGFR
|
Cancer
|
|
TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
- HY-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-135815AR
-
|
TAK-788 succinate (Standard); AP32788 succinate (Standard)
|
EGFR
Reference Standards
|
Cancer
|
|
Mobocertinib (succinate) (Standard) is the analytical standard of Mobocertinib (succinate). This product is intended for research and analytical applications. 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-19985A
-
|
|
EGFR
|
Cancer
|
|
(3S, 4S)-PF-06459988 is the S enantiomer of PF-06459988 with less active. PF-06459988 is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 has excellent selectivity against EGFR wild-type while possessing a minimally reactive electrophile that reduces the propensity of off-target labeling .
|
-
- HY-169327
-
|
|
PROTACs
MDM-2/p53
|
Cancer
|
|
MD-265 is a PROTAC degrader that can break down MDM2, leading to activation of p53 in cancer cells carrying wild-type p53. MD-265 achieves complete tumor regression and improves long-term survival of mice with leukemia. (Pink: MI-1063 (HY-133754); Black: linker; Blue: Lenalidomide (HY-A0003) .
|
-
- HY-18658B
-
|
NVP-HDM201 succinate; HDM201 succinate
|
MDM-2/p53
|
Cancer
|
|
Siremadlin (NVP-HDM201) succinate is an MDM2 inhibitor and cell cycle regulator. Siremadlin succinate blocks the p53-binding pocket of MDM2, inhibits MDM2-mediated ubiquitination and degradation of p53, thereby activating the p53 pathway in p53 wild-type cells. Siremadlin succinate can be used in the research of cutaneous melanoma .
|
-
- HY-W714171R
-
|
BAY MKH 6561 (Standard)
|
Herbicide
Reference Standards
|
Others
|
|
Propoxycarbazone (sodium) (Standard) is the analytical standard of Propoxycarbazone (sodium). This product is intended for research and analytical applications. Propoxycarbazone sodium (BAY MKH 6561) is a herbicide. Propoxycarbazone sodium controls shepherd’s purse (Capsella bursa-pastoris L. Medicus), tumble mustard (Sisymbrium altissimum L.), field pennycress (Thlaspi arvense L.), and several Bromus species. Propoxycarbazone sodium also inhibits the growth of jointed goatgrass, wild oat (Avena fatua L.), and quackgrass (Elytrigia repens L. Nevski) .
|
-
- HY-153856A
-
|
|
EGFR
|
Cancer
|
|
TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations .
|
-
- HY-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-181555
-
|
|
Ras
|
Endocrinology
Cancer
|
|
IACS-56676 is a selective NRAS G12D inhibitor with a target Kd of 0.031 μM. IACS-56676 stabilizes the p-loop, maintains key interactions with Asp12, Gly60 and Asp69, and achieves selectivity over wild-type KRAS through substitution targeting Leu95. IACS-56676 can be used for research on melanoma, hematologic malignancies and thyroid cancer .
|
-
- HY-139995
-
|
|
Drug Intermediate
|
Others
|
|
Spermine precursor-1 (Compound 1) is a redox-sensitive spermine precursor for the potential research of snyder robinson syndrome. Spermine precursor-1 inhibits wild-type (CMS-24949) and spermine synthase gene (SMS) mutant (CMS-26559, and CMS-6233) fibroblast cells with IC50s of 326.7, 198.5, and 244.1 μM, respectively .
|
-
- HY-181713
-
|
|
Bacterial
G-quadruplex
|
Infection
|
|
Antibiofilm agent-19 is an antibiofilm agent with iron-chelating activity. Antibiofilm agent-19 potently inhibits biofilm formation by wild-type PAO1 and the hyper-biofilm mutant strain PAO1-ΔwspF. Antibiofilm agent-19 promotes the formation of c-di-GMP G-quadruplexes and disrupts iron acquisition systems. It can be used in studies on antibacterial adjuvants .
|
-
- HY-14852R
-
|
|
Endoplasmic Reticulum Oxidoreductase 1 (ERO1)
Reference Standards
|
Neurological Disease
|
|
Tafamidis (Standard) is the analytical standard of Tafamidis. This product is intended for research and analytical applications. 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-168427
-
|
Abivertinib maleate dihydrate; AC0010 maleate dihydrate
|
EGFR
Btk
Apoptosis
|
Cancer
|
|
Avitinib (Abivertinib) maleate dihydrate is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC50 values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib maleate dihydrate is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib maleate dihydrate shows anticancer effects .
|
-
- HY-14588
-
|
ABT-378
|
HIV
HIV Protease
SARS-CoV
|
Infection
Neurological Disease
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-W005288S
-
|
4-Hydroxystyrene-d4
|
Apoptosis
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
|
4-Vinylphenol-d4 is deuterated labeled 4-Vinylphenol (HY-W005288). 4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
|
-
- HY-P99950
-
|
ALX148
|
CD47
|
|
|
Evorpacept (ALX148) is a high-affinity CD47-blocking fusion protein with an inactive human immunoglobulin Fc region. Evorpacept binds to CD47, blocks the interaction of the CD47-SIRPα immune checkpoint, and inhibits the binding of wild-type SIRPα to CD47. Evorpacept is applicable to research related to acute myeloid leukemia .
|
-
- HY-183292
-
|
|
EGFR
|
Cancer
|
|
SH-1092 is an orally active EGFR inhibitor with an IC50 of 0.96 nM against EGFR T790M/L858R and an IC50 of 6.1 nM against wild-type EGFR. SH-1092 exhibits anticancer activity against non-small cell lung cancer. SH-1092 can be used in studies related to non-small cell lung cancer .
|
-
- 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 .
|
-
- HY-19840
-
|
GS-9857
|
HCV Protease
|
Infection
Cancer
|
|
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively . Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research .
|
-
- HY-168447
-
|
|
Bacterial
|
Infection
|
|
D-PheTrAP is a bisubstrate analog inhibitor of 1-Deoxy-d-xylulose 5-phosphate synthase (DXPS). D-PheTrAP inhibits Escherichia coli DXPS (EcDXPS) and Pseudomonas aeruginosa DXPS (PaDXPS) with IC50 values of 0.52 μM, 2.1 μM, 2.4 μM, and 1.7 μM for wild-type (WT) EcDXPS, EcA426E, WT PaDXPS, and PaE431A, respectively .
|
-
- HY-P10596
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
Lasioglossin-III is an antimicrobial peptide that can be isolated from the venom of wild bees. Lasioglossin-III has high antibacterial activity against Gram-positive and Gram-negative bacteria, antifungal activity and antitumor activity. Lasioglossin-III has certain cytotoxicity against three cancer cell lines (HeLa S3, CRC SW 480 and CCRF-CEM T) with IC50 values of 4, 18 and 5 μM, respectively .
|
-
- HY-151380
-
|
|
HSV
|
Infection
|
|
LANA-DNA-IN-1 is a potent LANA-DNA inhibitor. LANA-DNA-IN-1 has inhibition activity for LBS2, LBS1 and LBS3 with IC50 values of 8 μM, 9μM and 8μM. LANA-DNA-IN-1shows against wild-type LANA with IC50 value of 53 μM. LANA-DNA-IN-1 can be used for the research of infection .
|
-
- HY-W177546
-
|
|
Phosphodiesterase (PDE)
Apoptosis
Caspase
DNA/RNA Synthesis
|
Cancer
|
|
CD00509 is a tyrosyl-DNA phosphodiesterase (PDE) Tdp1 inhibitor with an IC50 of 0.71 μM. CD00509 increases DNA damage and promotes apoptosis of MCF-7 cells. CD00509 can sensitize breast cancer cells and wild-type murine embryonic fibroblasts (MEFs) to Camptothecin (CPT) (HY-16560). CD00509 can be used for the study of cancers such as breast cancer .
|
-
- HY-175870
-
|
|
Ras
|
Cancer
|
|
Eras-4001 (Compound 14-1) is a pan-KRAS inhibitor. Eras-4001 has potent antitumor activities and significantly inhibits the proliferation of wild-type and mutant (such as KRAS G12D, KRAS G12V and KRAS G12C) cancer cells. Eras-4001 effectively inhibits tumor growth in GP2D and Panc0403 xenograft mouse models .
|
-
- HY-175652
-
|
|
PROTACs
Adenosine Receptor
|
Cancer
|
|
AZD9750 is an orally active, Cereblon (CRBN)-recruiting, androgen receptor (AR)-targeted PROTAC degrader. AZD9750 induces the proteasome-dependent degradation of both wild-type AR and the drug-resistant mutant AR L702H, thereby inhibiting the AR signaling pathway. AZD9750 suppresses tumor growth in mouse prostate cancer xenograft models and has been utilized in prostate cancer research .
|
-
- HY-124153
-
|
|
Btk
|
Cardiovascular Disease
Inflammation/Immunology
|
|
GNE-431 is a potent, selective and noncovalent “pan-BTK” inhibitor against C481R, T474I and T474Ms mutants. GNE-431 shows potency against wild-type BTK (IC50= 3.2 nM) and potency against C481S mutant (IC50= 2.5 nM). GNE-431 is proming for rasearch of haematological disorders and autoimmune diseases .
|
-
- HY-157469
-
|
NPD3064
|
HIV
|
Infection
|
|
TNT-i (NPD3064) is an inhibitor targeting M-Sec. TNT-i inhibits M-Sec-induced tunneling nanotube (TNT) formation reversibly. TNT-i reduces wild-type HIV-1 production in macrophages and M-Sec-expressing T cells. TNT-i shows low cytotoxic effects on macrophages and T cells. TNT-i can be used for the research of HIV-1 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-159479
-
|
|
Parasite
|
Infection
|
|
PfSUB1-IN-1 (compound 4c) is a plasmodium falciparum subtilisin-like serine protease 1 (PfSUB1) Inhibitor (IC50: 15 nM). PfSUB1 is an antimalarial target. PfSUB1-IN-1 inhibits the growth of a genetically modified P. falciparum line expressing reduced levels of PfSUB1 13-fold more efficiently compared to a wild-type parasite line .
|
-
- HY-131312A
-
|
LY3410738 gentisate; Mutant IDH1-IN-6 gentisate
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes .
|
-
- HY-174216
-
|
|
DNA/RNA Synthesis
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Neurological Disease
Metabolic Disease
|
|
PZL-A is a activator of mitochondrial DNA (mtDNA) synthesis. PZL-A restores wild-type-like activity to mutant forms of polymerase γ (POLγ) with AC50 s of 160 and 20 nM for A467T and G848S. PZL-A activates mtDNA synthesis in cells, enhancing biogenesis of the oxidative phosphorylation machinery and cellular respiration. PZL-A is promising for relieving POLG disease and other severe conditions linked to depletion of mtDNA .
|
-
- HY-B1268
-
|
Dioctyl sulfosuccinate sodium salt
|
Environmental Pollutants
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-P991221
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
ALD1613 is a potent neutralizing monoclonal antibody against adrenocorticotropic hormone (ACTH). ALD1613 neutralizes ACTH-induced signaling and inhibits ACTH-induced cyclic AMP accumulation in a mouse adrenal cell line (Y1) via all five melanocortin receptors. ALD1613 significantly reduces plasma corticosterone levels in wild-type rats. ALD1613 can be used in the study of diseases associated with elevated ACTH levels .
|
-
- HY-75368
-
|
|
LRRK2
|
Neurological Disease
|
|
SRI-31255 is an orally active LRRK2 inhibitor with IC50 values of 520 and 427 nM for human wild-type (WT) and mutant G2019S, respectively. SRI-31255 exerts neuroprotective effects by binding to the ATP-binding pocket of LRRK2, inhibiting kinase activity. SRI-31255 can be used as a lead compound for the development of LRRK2-targeted drugs for the treatment of Parkinson's disease .
|
-
- HY-168069
-
|
|
Parasite
Dihydrofolate reductase (DHFR)
|
Infection
|
|
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
|
-
- HY-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-16999
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
Apoptosis
|
Cancer
|
|
RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model .
|
-
- HY-17040R
-
|
TMC114 (Standard); UIC-94017 (Standard)
|
HIV
HIV Protease
Reference Standards
|
Infection
Inflammation/Immunology
|
|
Darunavir (Standard) is the analytical standard of Darunavir. This product is intended for research and analytical applications. 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-16379R
-
|
SB1518 (Standard)
|
Reference Standards
JAK
FLT3
|
Cancer
|
|
Pacritinib (Standard) is the analytical standard of Pacritinib. This product is intended for research and analytical applications. Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
|
-
- HY-131601A
-
|
3'-FdTTP tetrasodium
|
DNA/RNA Synthesis
Drug Derivative
|
Others
|
|
3'-Fluorothymidine-5'-triphosphate tetrasodium (3'-FdTTP tetrasodium) is a dTTP (HY-138615) analog. 3'-Fluorothymidine-5'-triphosphate tetrasodium inhibits the T4 DNA polymerases competitively with dTTP. 3'-Fluorothymidine-5'-triphosphate tetrasodium inhibits DNA synthesis by T4 wild-type, L98 and CB121 DNA polymerase .
|
-
- 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-125675
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
VPC-16606 is a selective inhibitor targeting the activation function 2 (AF2) domain of estrogen receptor α (ERα). VPC-16606 blocks the interaction between ERα and coactivators, inhibits the activity of both wild-type and clinically drug-resistant mutant ERα, and exerts inhibitory effects on hormone-resistant breast cancer cells. VPC-16606 can be used in breast cancer research .
|
-
- HY-175743
-
|
|
FGFR
|
Cancer
|
|
TYRA-200 is a potent and orally active FGFR2 inhibitor. TYRA-200 inhibits the kinase activity of wild-type FGFR2 and its mutants. TYRA-200 induces significant tumor regression in FGFR2-driven cancer models. TYRA-200 can be used for the research of FGFR2-altered advanced solid tumors, intrahepatic cholangiocarcinoma, and endometrial cancer .
|
-
- HY-181885
-
|
|
Influenza Virus
Drug Derivative
|
Infection
|
|
Antiviral agent 80 is a conjugate of Zanamivir (HY-13210) and Amantadine (HY-13317), acting as a dual inhibitor of influenza virus M2 ion channel/neuraminidase (NA). Antiviral agent 80 exhibits potent inhibitory activity against both wild-type and drug-resistant influenza neuraminidase mutants, with an IC50 value range of 1.50 nM to 120.4 nM. Antiviral agent 80 can be used in influenza-related research .
|
-
- HY-P11005
-
|
|
Dynamin
ATP Synthase
|
Neurological Disease
|
|
P259 is a Drp1-Mff inhibitor. P259 distinguishes physiological from pathological fission by specifically inhibiting Drp1-Mff interaction. P259 elongates cell mitochondria and disrupts mitochondrial function and motility. P259 reduces ATP levels and alters mitochondrial structure in the brain, resulting in behavioral deficits in wild-type mice and a short lifespan in Huntington's disease (HD) mice model .
|
-
- HY-156640
-
|
LP-168
|
EGFR
|
Cancer
|
|
Rocbrutinib is an orally available, highly selective Bruton's tyrosine kinase (BTK) inhibitor, with an IC50 of 0.11 nM against wild-type BTK and an IC50 of 1.0 nM against C481S-mutated BTK. Rocbrutinib reduces the viability of leukemia cells, induces cytotoxicity and inhibits cell migration. Rocbrutinib can be used in research related to chronic lymphocytic leukemia, non-Hodgkin's lymphoma and mantle cell lymphoma .
|
-
- 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-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-16767S1
-
|
MK-1439-13C,d3
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
|
-
- HY-178047
-
|
|
STING
IFNAR
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
UM-242 is a STING inhibitor, with an EC50 of 1.70 μM in THP1-Dual cells expressing wild-type STING. UM-242 blocks STING oligomerization and inhibits diABZI-induced phosphorylation of TBK1 and IRF3, thereby suppressing the transcription of IFNβ and IL6 and reducing IFNβ secretion. UM-242 can be used for the study of STING-dependent inflammatory and neurological diseases .
|
-
- HY-131062
-
|
|
Glycosyltransferase
|
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-178049
-
|
|
STING
IFNAR
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
UM-259 is a STING inhibitor, with an EC50 of 1.50 μM in THP1-Dual cells expressing wild-type STING. UM-259 blocks STING oligomerization and inhibits diABZI-induced phosphorylation of TBK1 and IRF3, thereby suppressing the transcription of IFNβ and IL6 and reducing IFNβ secretion. UM-259 can be used for the study of STING-dependent inflammatory and neurological diseases .
|
-
- HY-10574R
-
|
R278474 (Standard); TMC278 (Standard); DB08864 (Standard)
|
Reference Standards
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine (Standard) is the analytical standard of Rilpivirine. This product is intended for research and analytical applications. 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-103320AR
-
|
|
Reference Standards
CaSR
|
Metabolic Disease
|
|
Calhex 231 hydrochloride (Standard) is the analytical standard of Calhex 231 hydrochloride (HY-103320A). This product is intended for research and analytical applications. 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 Ca2+-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .
|
-
- HY-10574S1
-
|
R278474-13C6; TMC278-13C6; DB08864-13C6
|
Isotope-Labeled Compounds
HIV
Reverse Transcriptase
|
Infection
|
|
Rilpivirine- 13C6 (R278474- 13C6) is 13C 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 .
|
-
- HY-182809
-
|
|
Hsp-targeting Chimeras
Androgen Receptor
HSP
|
Neurological Disease
Cancer
|
|
Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research .
|
-
- HY-180981
-
|
|
PROTACs
Bcr-Abl
|
Cancer
|
|
P19As is a BCR-ABL PROTAC degrader based on Asciminib (HY-104010), with a DC50 value of approximately 200 nM for the wild-type BCR-ABL protein. P19As can degrade the T315I mutant and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19As can be used for the study of chronic myeloid leukemia and acute lymphoblastic leukemia .
|
-
- HY-14852AR
-
|
Fx-1006A (Standard)
|
Transthyretin (TTR)
Reference Standards
|
Neurological Disease
|
|
Tafamidis meglumine (Standard) is the analytical standard of Tafamidis meglumine. This product is intended for research and analytical applications. 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-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-B0413
-
|
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
Cancer
|
|
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-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
|
-
- HY-177208
-
|
|
Drug Derivative
MDM-2/p53
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
|
BW-AQ-113 is an Anthraquinone (HY-N0354) derivative. BW-AQ-113 can specifically degrade MDM2 and activate the p53 pathway. BW-AQ-113 can induce apoptosis by downregulating anti-apoptotic gene Bcl-2 and regulating pro-apoptotic gene Bax and CASP3. BW-AQ-113 can be used for research of p53 wild-type hematological malignancies .
|
-
- HY-17396R
-
|
KP363 Hydrochloride (Standard)
|
Reference Standards
Fungal
Antibiotic
|
Infection
|
|
Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
|
-
- HY-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-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 . (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-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-176250
-
|
|
Ras
ERK
|
Cancer
|
|
KRAS-IN-43 (Compound 9) is a pan-KRAS inhibitor with IC50 values of 0.15 μM, 0.14 μM, and 0.47 μM against KRAS G12V, KRAS G12C and wild-type KRAS, respectively. KRAS-IN-43 disrupts the interaction between KRAS and cRAF, and inhibits ERK phosphorylation. KRAS-IN-43 is promising for research of KRAS mutation-related cancers (such as pancreatic cancer, colorectal cancer, and lung cancer) .
|
-
- HY-181090
-
|
|
HIV
|
Infection
|
|
HIV-1-IN-92 is a non-nucleoside inhibitor of HIV-1 reverse transcriptase with an IC50 of 0.11 μM against HIV-1 reverse transcriptase. HIV-1-IN-92 exhibits activity against both wild-type HIV-1 IIIB and mutant HIV-1 strains. HIV-1-IN-92 can be used in research related to acquired immunodeficiency syndrome (AIDS) .
|
-
- 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-P10436
-
|
|
Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research .
|
-
- HY-159613
-
|
|
Apoptosis
Estrogen Receptor/ERR
|
Inflammation/Immunology
Cancer
|
|
PELP1-IN-1 is a PELP1 inhibitor and an apoptosis inducer with no cytotoxic activity against non-cancer cell lines. PELP1-IN-1 targets wild-type, mutant and drug-resistant ER + breast cancer, and promotes PELP1 degradation through the proteasome pathway. As an analog of SMIP34 (HY-169903), PELP1-IN-1 is applicable to the research of estrogen receptor α-positive breast cancer .
|
-
- 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-176210
-
|
|
Fungal
Cytochrome P450
|
Infection
|
|
CYP51-IN-24 (Compound 22) is a Sterol 14α-Demethylase (CYP51) inhibitor. CYP51-IN-24 exhibits potent inhibitory activity against wild-type and drug-resistant fungi. CYP51-IN-24 inhibits ergosterol biosynthesis by binding to the fungal CYP51 enzyme. CYP51-IN-24 can be used in research and drug development against drug-resistant fungal infections .
|
-
- 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-124089S
-
|
|
Isotope-Labeled Compounds
Cannabinoid Receptor
|
Metabolic Disease
|
|
Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
|
-
- HY-18343
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth .
|
-
- HY-10574AR
-
|
TMC-278 hydrochloride (Standard); TMC278 hydrochloride (Standard); TMC 278 hydrochloride (Standard)
|
Reference Standards
SARS-CoV
MMP
|
Infection
|
|
Rilpivirine (hydrochloride) (Standard) is the analytical standard of Rilpivirine (hydrochloride). This product is intended for research and analytical applications. Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV .
|
-
- HY-50703
-
MK-2461
1 Publications Verification
|
c-Met/HGFR
|
Cancer
|
|
MK-2461 is an ATP-competitive, selective and orally active wild-type and mutant c-Met inhibitor (IC50s: 0.4-2.5 nM). MK-2461 also inhibits Ron (IC50 of 7 nM) and Flt1 (IC50 of 10 nM), MK-2461 shows selective for c-MET over other kinases (lC50s = 22-7800 nM). MK-2461 can be used for the study of cancer, such as gastric cancer .
|
-
- HY-128661
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Metabolic Disease
|
|
IDH1 Inhibitor 2 (compound 13) is a potent wild-type IDH1 inhibitor that exerts its activity through covalent modification of His315 with an IC50 value of 110 nM. IDH1 Inhibitor 2 can dose-dependently reduce the intracellular reduced glutamine metabolic flux, thereby affecting cellular metabolic homeostasis. IDH1 Inhibitor 2 can be used to study the role of IDH1 in cellular metabolic regulation and cancer development .
|
-
- HY-128326
-
|
|
MAP3K
|
Cardiovascular Disease
|
|
ZAK-IN-1 is an orally active and selective selective leucine-zipper and sterile‑α motif kinase (ZAK) inhibitor with IC50 of 4 nM and KD of 8 nM. ZAK-IN-1 exhibits excellent selectivity against a panel of 403 wild-type kinases. ZAK-IN-1 blocks p38/GATA-4 and JNK/c-Jun signaling and shows promising anti antihypertrophic cardiomyopathy (HCM) efficacy. ZAK-IN-1 can be used for the study of HCM .
|
-
- HY-174303
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
NNRT-IN-9 (Compound EG28) is a non-nucleoside reverse transcriptase (NNRT) inhibitor. NNRT-IN-9 has potent antiviral and anti-resistance activity against wild-type (WT) HIV-1 and various clinically relevant mutations (E138K and K103N + Y181C) with EC50s of 55, 67 and 3910 nM, respectively. NNRT-IN-9 can be used for acquired immune deficiency syndrome (AIDS) research .
|
-
- HY-176083
-
|
|
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
|
ASTX295 is an orally active and selective MDM2 antagonist with an IC50 of <1 nM. ASTX295 inhibits the MDM2-p53 interaction, activates wild-type TP53, and thereby induces the expression of relevant transcriptional targets, leading to cell death. ASTX295 drives the transition of pancreatic cancer cells from senescence to apoptosis and regulates p53 and DNA damage biomarkers. ASTX295 can be used for the research of hematologic malignancies and pancreatic cancer .
|
-
- HY-162253
-
|
|
HIV
|
Infection
|
|
HIV-1 inhibitor-64 (Compound 7c) is a wild-type HIV-1 inhibitor that effectively suppresses the activity of HIV-1 mutants E138K/Q148K and G140S/Q148R with EC50 values of 62.5 nM and 11.3 nM, respectively. HIV-1 inhibitor-64 exhibits antiviral activity and can be used in the research of AIDS .
|
-
- HY-W587486
-
|
|
Endogenous Metabolite
Bacterial
|
Neurological Disease
|
|
N‑acetyltaurine is an orally active endogenous sulfonate that is synthesized from taurine and acetate in the renal cortex. N‑acetyltaurine supports bacterial growth as a sole fixed nitrogen or carbon source. N‑acetyltaurine buffers acetyl moieties of mitochondrial acetyl‑CoA in skeletal muscle. N‑acetyltaurine reduces food intake and body weight in obese and lean wild‑type mice in a GFRAL‑dependent manner. N‑acetyltaurine can be used for the research of diet‑induced obesity, hyperacetatemia and diabetes .
|
-
- 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-14588R
-
|
ABT-378 (Standard)
|
Reference Standards
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-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-16270
-
|
3-Cyanopropyl carbamimidothioate; 4-Isothioureidobutyronitrile
|
Apoptosis
MDM-2/p53
|
Cancer
|
|
Kevetrin (3-Cyanopropyl carbamimidothioate; 4-Isothioureidobutyronitrile) is an apoptosis inducer that exhibits p53-dependent and p53-independent antitumor activity. In TP53 wild-type models, Kevetrin activates and stabilizes the p53 protein by altering the processing of MDM2, thereby inducing cell cycle arrest and apoptosis. Kevetrin shows higher sensitivity in mutant models. Kevetrin is applicable for the research of various cancers including acute myeloid leukemia and breast cancer .
|
-
- HY-100218B
-
|
|
Glutathione Peroxidase
Ferroptosis
|
Cancer
|
|
(1R,3S)-RSL3 is the less active (1R,3S)-enantiomer of RSL3 ((1S,3R)-RSL3). (1R,3S)-RSL3 and RSL3 induce cell death in HT22 wild-type cells with EC50 values of 5.2 µM and 0.004 µM, rspectively .
|
-
- HY-169784
-
|
|
Drug Derivative
|
Metabolic Disease
|
|
PPI-1040 is an orally bioavailable vinyl ether synthetic plasmalogen. PPI-1040 acts as a precursor of plasmalogen. PPI-1040 increases plasmalogen levels in plasmalogen-deficient mice and normalizes hyperactive behaviors in these mice. In wild-type mice, PPI-1040 retains the sn-1 vinyl ether group and sn-3 phosphoethanolamine group, and is converted into endogenous ethanolamine plasmalogen. PPI-1040 can be used in studies related to rhizomelic chondrodysplasia punctata .
|
-
- HY-13464
-
|
Brigatinib analog
|
Anaplastic lymphoma kinase (ALK)
EGFR
|
Cancer
|
|
ALK-IN-1 is an orally active, blood-brain barrier-permeable ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
|
-
- HY-16379B
-
|
SB1518 citrate
|
JAK
FLT3
|
Cancer
|
|
Pacritinib (SB1518) citrate is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2 V617F mutant (IC50=19 nM). Pacritinib citrate also inhibits FLT3 (IC50=22 nM) and its mutant FLT3 D835Y (IC50=6 nM). Pacritinib citrate can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) .
|
-
- HY-122038
-
|
|
MDM-2/p53
|
Cancer
|
|
NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines .
|
-
- HY-N16422
-
|
|
HIV
HIV Protease
|
Infection
|
|
Mer-NF5003E is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1 reverse transcriptase (RT) (EC50=50 μM). Mer-NF5003E exhibits inhibitory activity against wild-type HIV-1 and multiple NNRTI-resistant strains (e.g., K103N, Y181C). Mer-NF5003E is promising for research of HIV infections .
|
-
- HY-126120
-
|
|
HIV
HIV Protease
|
Infection
|
|
BILA 1906 BS is a HIV protease inhibitor. BILA 1906 BS prevents HIV-1 replication via inhibition of viral protease-mediated cleavage of Gag and Gag-Pol polyprotein precursors during virion maturation. BILA 1906 BS blocks maturation of p24 proteins in wild-type HIV-1, impairing polyprotein processing and viral maturation. BILA 1906 BS can be used for the research of human immunodeficiency virus type 1 (HIV-1) infection .
|
-
- HY-19617A
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 hydrochloride is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 hydrochloride potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-112611
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations .
|
-
- HY-174427
-
|
|
LRRK2
|
Neurological Disease
|
|
RN341 is a specific type II kinase inhibitor of LRRK2 (IC50: 296 nM). RN341 inhibits LRRK2 phosphorylation and avoids S935 dephosphorylation by stabilizing the open conformation. RN341 rescues LRRK2-mediated kinesin motility block by preventing microtubule binding. RN341 effectively inhibits LRRK2 wild-type and G2019S mutant at the cellular level. RN341 provides a new direction for Parkinson's disease research.
|
-
- HY-117540
-
|
|
Histone Methyltransferase
|
Cancer
|
|
ZLD10A is a highly potent and selective EZH2 inhibitor with the activity of inhibiting H3K27 methylation. ZLD10A can inhibit wild-type and mutant EZH2 with nanomolar potency and has more than 1000-fold selectivity for the other 10 histone methyltransferases. ZLD10A inhibited cell proliferation of DLBCL cell lines in a concentration- and time-dependent manner, showing a potential antiproliferative effect. ZLD10A can be used in the study of EZH2 mutant lymphomas .
|
-
- HY-100131R
-
|
|
RIP kinase
Reference Standards
|
Inflammation/Immunology
|
|
GSK481 (Standard) is the analytical standard of GSK481 (HY-100131). This product is intended for research and analytical applications. GSK481 is a highly potent, selective, and specific receptor interacting protein 1 (RIP1) kinase inhibitor with an IC50 of 1.3 nM, which inhibits Ser166 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-131312
-
|
LY3410738; Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
|
-
- HY-14183
-
|
RSD1235 hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Vernakalant hydrochloride is a mixed voltage- and frequency-dependent Na + and atria-preferred K + channel blocker. IC50 for block by Vernakalant of wild-type and mutant Kv1.5 channels Fractional block is 13.35±0.93 μM, 0.61±0.03 μM, and 1.63±0.09 μM for Kv1.5 channel wt, Kv1.5 channel I508F, Kv1.5 channel T479A, respectively.
|
-
- HY-182043
-
|
|
c-Kit
PDGFR
|
Cancer
|
|
BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors .
|
-
- 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-51424R
-
|
|
Raf
|
Cancer
|
|
PLX-4720 (Standard) is the analytical standard of PLX-4720. This product is intended for research and analytical applications. PLX-4720 is a potent and selective inhibitor of B-RafV600E 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-RafV600E than wild-type B-Raf.
|
-
- 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 . 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-164056
-
|
|
EGFR
|
Cancer
|
|
EGFR T790M/L858R-IN-8 (Compound 9) is a selective EGFR T790M/L858R mutant kinase inhibitor with a IC50 of 56.8 μM, and it shows no inhibitory activity against wild-type EGFR. EGFR T790M/L858R-IN-8 can be used for the research of non-small cell lung cancer .
|
-
- HY-16379S
-
|
SB1518-d4
|
Isotope-Labeled Compounds
JAK
FLT3
|
Cancer
|
|
Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). 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-178111
-
|
|
Bacterial
|
Infection
|
|
AcrB-IN-6 is an effective AcrB inhibitor. AcrB-IN-6 The compound inhibits the function of bacterial multidrug efflux pumps, thereby significantly enhancing the antibacterial activity of various antibiotics. AcrB-IN-6 achieves 32-fold MIC reductions in wild-type E. coli BW25113. AcrB-IN-6 exhibits excellent synergistic antibacterial effects, low cytotoxicity and hemolytic properties. AcrB-IN-6 can be used for researching anti-resistant bacteria .
|
-
- HY-14588S1
-
|
|
Isotope-Labeled Compounds
HIV
HIV Protease
SARS-CoV
|
Infection
|
|
Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-175183
-
|
|
Bacterial
|
Infection
|
|
Antituberculosis agent-15 (Compound 18c) is a selective antimycobacterial agent with MICs of 0.45 and 0.28 μM for M. tuberculosis H37Rv (ATCC 27294) and its wild-type H37Rv-LP (ATCC 25618), respectively. Antituberculosis agent-15 has potent intracellular inhibitory activities in macrophage infection models with IC50s of 0.16 μM. Antituberculosis agent-15 can be used for tuberculosis research .
|
-
- 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 .
|
-
- 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-179437
-
|
|
HIV
|
Infection
|
|
anti-HIV agent 1 (compound 10i) is a potent antiviral agent with anti-HIV activity (IC50 = 10.6 nM). anti-HIV agent 1 exhibits moderate to no inhibitory activity against RT mutant strains, but maintains their activity against wild-type viruses. anti-HIV agent 1 strongly shows dual inhibition of the viral attachment and reverse transcriptase phases of the viral life cycle. anti-HIV agent 1 can be used for HIV infection research .
|
-
- HY-167710
-
|
|
Endogenous Metabolite
|
Cancer
|
|
CRCD2 is a small molecule NT5C2 nucleotidase inhibitor with enhanced 6-mercaptopurine cytotoxic activity. CRCD2 can effectively reverse 6-mercaptopurine resistance caused by mutations in the NT5C2 gene or non-genetic activation mechanisms. CRCD2 combined with 6-mercaptopurine can enhance its cytotoxic activity in NT5C2 wild-type leukemia, showing its potential in the treatment of acute lymphoblastic leukemia .
|
-
- HY-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-182741
-
|
|
RET
|
Endocrinology
Cancer
|
|
RET-IN-32 is an orally active RET inhibitor with IC50 values of 0.285, 4.602 and 103.5 nM against wild-type, V804M and G810S mutant forms, respectively. RET-IN-32 inhibits the autophosphorylation of Tyr1062. RET-IN-32 completely suppresses tumor growth induced by BAF3-KIF3B-RET-WT xenografts. RET-IN-32 can be used in the research of thyroid cancer and lung cancer .
|
-
- HY-136242
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
Cancer
|
|
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
|
-
- HY-201256
-
|
|
Bacterial
MDM-2/p53
|
Infection
|
|
UCI-14 is a gltA1/lprQ modulator with in vitro anti-tuberculosis activity against drug-sensitive and multidrug-resistant mycobacteria. UCI-14 upregulates the expression of genes encoding citrate synthase I, downregulates the expression of genes encoding conserved mycobacterial lipoprotein, and alters the carbon metabolism of mycobacteria. UCI-14 reactivates the expression of wild-type p53 target genes in p53-mutated cells. UCI-14 can be used in the research of tuberculosis and cancer .
|
-
- HY-160167A
-
|
(R,R)-DZD8586
|
Btk
|
Cancer
|
|
(R,R)-Birelentinib ((R,R)-DZD8586) (Compound 14) is a potent BTK inhibitor with IC50 values for BTK WT and BTK C481S of 0.7 and 0.86 nM, respectively. (R,R)-Birelentinib inhibits the self-phosphorylation of BTK and its IC50 is 24.3 nM. (R,R)-Birelentinib exhibits significant anti-proliferative activity against wild-type and C481S mutant HEK293 cells. (R,R)-Birelentinib can be used for the study of drug-resistant B-cell malignancies .
|
-
- HY-P11109
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
RL-37 is an alpha-helical antimicrobial peptide. RL-37 can be isolated for rhesus monkey bone marrow. RL-37 rapidly permeabilizes the membranes of Escherichia coli ML-35p and lysed liposomes. RL-37 has effective antibacterial activity against staphylococci, such as wild-type and Methicillin (HY-121544)-resistant S. aureus strains and S. epidermidis ATCC 49741. RL-37 can be used for human skin infections research .
|
-
- HY-B1268R
-
|
Dioctyl sulfosuccinate sodium salt (Standard)
|
Reference Standards
HSV
|
Others
|
|
Docusate (Sodium) (Standard) is the analytical standard of Docusate (Sodium). This product is intended for research and analytical applications. Docusate Sodium (Dioctyl sulfosuccinate sodium salt) is one of the main components in stool softeners. Docusate Sodium is a sulfated surfactant and may inactivate viral pathogens by disrupting viral envelopes and/or denaturing/disassociating proteins. Docusate Sodium is effective in vitro against wild type and drug-resistant strains of HSV type 1 and 2. Docusate Sodium is an obesogen. Docusate Sodium with developmental exposure leads to increased adult adiposity, inflammation, metabolic disorder and dyslipidemia in offspring fed a standard diet in mice .
|
-
- HY-19980G
-
|
APR-246; PRIMA-1Met
|
MDM-2/p53
Apoptosis
Autophagy
Ferroptosis
|
Cancer
|
|
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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-163393
-
|
|
Influenza Virus
|
Infection
|
|
Neuraminidase-IN-18 (compound N5) is a novel polyheterocyclic neuraminidase (NA) inhibitor. Neuraminidase-IN-18 shows potency in inhibition of H5N1 NA with an IC50 of 0.14 μM and 0.27 μM against the wild-type H5N1 NA and H5N1-H274Y mutant NA, respectively. Neuraminidase-IN-18 inhibits influenza virus replication by binding to NAs in cell level .
|
-
- HY-19617B
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 TFA displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-136881
-
|
|
CCR
|
Inflammation/Immunology
|
|
CH0076989 is a specific CCR3 agonist. CH0076989 activates eosinophils and transfectants expressing both wild-type CCR3 and a CCR1:CCR3 chimaeric receptor lacking the CCR3 amino-terminus. CH0076989 has a direct interaction with the transmembrane helices of CCR3, supported by the complete loss of its activity due to mutations of the residues Y41, Y113 and E287. CH0076989 can be used for the study of inflammation and allergic diseases (such as asthma) .
|
-
- HY-B0413R
-
|
|
Reference Standards
Parasite
HIF/HIF Prolyl-Hydroxylase
Microtubule/Tubulin
Antibiotic
|
Infection
|
|
Fenbendazole (Standard) is the analytical standard of Fenbendazole. This product is intended for research and analytical applications. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent and acts on helminthes primarily by binding to tubulin and disrupting the tubulin microtubule equilibrium. Fenbendazole stabilizes the transcriptional activator HIF-1α. Fenbendazole possesses an efficient anti-proliferative activity and induces apoptosis. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
|
-
- HY-162033
-
|
|
Chloride Channel
|
Others
|
|
PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF .
|
-
- HY-51424S
-
|
|
Isotope-Labeled Compounds
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 .
|
-
- HY-183682
-
|
|
EGFR
p38 MAPK
ERK
Akt
|
Cancer
|
|
AZ14289671 is an orally active, blood-brain barrier-penetrant tyrosine kinase (tyrosine kinase) inhibitor (TKI) that specifically targets non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations (EGFR Exon20Ins), while largely sparing wild-type EGFR to reduce off-target toxicities such as rash and diarrhea. AZ14289671 inhibits the downstream MAPK/ERK/AKT pathway, suppressing tumor cell proliferation, survival and migration. AZ14289671 can be used for NSCLC research .
|
-
- HY-153268
-
|
BDTX-1535; EGFR-IN-76
|
EGFR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
|
-
- HY-156632
-
|
KIN-3248
|
FGFR
|
Cancer
|
|
Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer) .
|
-
- HY-123883
-
|
|
HIV
HIV Integrase
|
Infection
|
|
MK-0536 is a highly potent HIV-1 integrase inhibitor that effectively suppresses the replication of wild-type viruses. MK-0536 retains significant antiviral activity against multiple key drug-resistant mutants such as Y143R and N155H, and shows no toxicity to uninfected cells. MK-0536 selectively blocks the strand transfer reaction of integrase by chelating magnesium ions at the active site and interacting with viral DNA and enzyme residues. MK-0536 is applicable to the study of HIV infection mechanisms .
|
-
- HY-16936
-
|
|
LRRK2
|
Neurological Disease
|
|
JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
|
-
- HY-161777
-
|
|
SARS-CoV
Virus Protease
|
Infection
|
|
SARS-CoV-2 Mpro-IN-23 (Compound 2) is an inhibitor for SARS-CoV-2 main protease (Mpro), which inhibits wildtype Mpro and mutant Mpro variants, with IC50 of 0.057-0.92 μM. SARS-CoV-2 Mpro-IN-23 inhibits the post-entry viral processes of wild-type SARS-CoV-2 single-round infectious particles (SRIPs), suppresses the viral replication of Mpro wildtype and Mpro mutants with EC50 of 0.02-0.52 μM .
|
-
- HY-19617
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity .
|
-
- HY-121916
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
ML309 is a highly selective and potent inhibitor of the R132H mutant isocitrate dehydrogenase 1 (IDH1 R132H), with an IC50 of 96 nM. ML309 is a competitive inhibitor of α-KG, with a Ki value of 156 nM, and its inhibitory activity against the wild-type IDH1 is greater than 35 μM. ML309 effectively reduces the production of the tumor metabolite 2-HG in U87MG cells. ML309 can be used as a chemical probe to study the role of the mutant IDH1 in cancer .
|
-
- HY-P11003
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
PTD-N5-1 (N5-1) is an IRF5 inhibitory peptide. PTD-N5-1 blocks β-glucan-induced IL-12 production in IFN-γ primed wild-type and Clec2d-difecient bone-marrow-derived dendritic cells (BMDCs). PTD-N5-1 regulates antifungal immunity through suppression of IRF5-mediated IL-12 production .
|
-
- 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-B0255
-
|
GS 0840
|
HBV
Orthopoxvirus
HSV
DNA/RNA Synthesis
ATM/ATR
CDK
|
Infection
Cancer
|
|
Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer .
|
-
- HY-114625
-
|
|
Parasite
Mitochondrial Metabolism
|
Infection
|
|
Amquinate is a coccidiostat and a cytochrome b inhibitor. Amquinate blocks cytochrome-mediated electron transport near cytochrome b in mitochondria, acting downstream of coenzyme Q without affecting succinate dehydrogenase or NADH dehydrogenase. Amquinate inhibits succinate- and malate plus pyruvate-supported mitochondrial respiration in Eimeria tenella and does not affect L-ascorbate-supported respiration or any mitochondrial respiration in chicken liver mitochondria. Amquinate exhibits selective anticoccidial activity against wild-type Eimeria tenella. Amquinate can be used for the research of coccidiosis (Eimeria tenella infection) .
|
-
- 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-N12281
-
|
|
Apoptosis
MDM-2/p53
PAK
Calcium Channel
|
Endocrinology
Cancer
|
|
Sennoside is an orally active apoptosis inducer and stimulant laxative, found in Senna (Cassia angustifolia). Sennoside induces overexpression of wild-type p53 and p21/WAF as part of pathways mediating colonic epithelial cell apoptosis. Sennoside stimulates colonic peristalsis, reverses net water, sodium, chloride absorption to secretion and enhances potassium and calcium secretion. Sennoside increases paracellular permeability to small molecules, accelerates colon transit and softens fecal pellets. Sennoside can be used for the research of constipation, melanosis coli, and colorectal cancer .
|
-
- 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-178341
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
NNRT-IN-13 is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor that directly inhibiting HIV-1 reverse transcriptase (IC₅₀ = 0.25 μM). NNRT-IN-13 exhibits excellent antiviral activity against wild-type HIV-1 (EC₅₀ = 0.0046 μM) and a broad spectrum of drug-resistant mutants. NNRT-IN-13 exhibits favorable in vivo metabolic and safety profiles. NNRT-IN-13 can be used for human immunodeficiency virus (HIV) research .
|
-
- HY-107123R
-
|
ASC-09 (Standard)
|
Reference Standards
HIV Protease
|
Infection
|
|
TMC310911 (Standard) (ASC-09 (Standard)) is the analytical standard of TMC310911 (HY-107123). This product is intended for research and analytical applications. TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1. TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity .
|
-
- HY-171835
-
|
|
HIV
HIV Protease
|
Infection
|
|
DPC 684 is a potent and selective HIV-1 protease inhibitor (IC90 = 5.7-40 nM, Ki = 0.021 nM). DPC 684 competitively inhibits HIV-1 protease and blocks viral polyprotein cleavage. DPC 684 has low protein binding and broad-spectrum inhibition against a variety of wild-type and mutant HIV-1 proteases. DPC 684 has low protein binding and broad-spectrum inhibition (IC90 = 1.9-6.3 nM). DPC 684 has research significance for HIV .
|
-
- HY-101562R
-
|
GDC-0077 (Standard); RG6114 (Standard)
|
PI3K
Reference Standards
Apoptosis
|
Cancer
|
|
Inavolisib (Standard) is the analytical standard of Inavolisib (HY-101562). This product is intended for research and analytical applications. Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
|
-
- HY-114253
-
|
|
EGFR
|
Cancer
|
|
ODS-2004436 is a small molecule radiotracer that uses positron emission tomography (PET) imaging to measure the activity of the epidermal growth factor receptor (EGFR) in tumors. ODS-2004436 labeled with the radioactive isotope fluorine-18 shows significantly higher uptake in the xenograft models of lung cancer with EGFR mutations compared to the wild-type models, and could be used to distinguish the mutation status. ODS-2004436 can be used to identify EGFR-positive tumors and predict their response to certain reagent treatments, especially for non-small cell lung cancer (NSCLC) .
|
-
- HY-146223
-
|
|
Ras
p38 MAPK
PI3K
Apoptosis
|
Cancer
|
|
AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
|
-
- HY-141640
-
|
|
PROTACs
EGFR
|
Cancer
|
|
MS154 is a first-in-class E3 ligase cereblon-recruited EGFR degrader with Kd values of 1.8 nM and 3.8 nM for EGFR WT and EGFR L858R mutant, respectively. MS154 potently induces degradation of mutant, but not wild-type, EGFR in cancer cell lines in an E3 ligase-dependent manner. MS154 exhibits anticancer effects against lung cancer (blue: E3 ligase ligand (HY-103596); black: linker (HY-W096167); pink: EGFR ligand (HY-168305)) .
|
-
- HY-175769
-
|
|
VSV
|
Infection
|
|
SMU-V18 is a vesicular stomatitis virus (VSV) inhibitor, with an EC50 of 6.2 μM. SMU-V18 inhibits VSV-GFP fluorescence intensity, viral mRNA/protein expression, and progeny virus replication. SMU-V18 interferes with early viral infection stages, also effective against wild-type VSV (VSV-WT). SMU-V18 inhibits VSV-GFP in mouse tissues and prolongs survival. SMU-V18 can be used for the study of vesicular stomatitis virus (VSV) infection .
|
-
- HY-50707
-
|
(Rac)-T-Type calcium channel inhibitor
|
Calcium Channel
Drug Isomer
|
Neurological Disease
|
|
(Rac)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
|
-
- HY-14588S
-
|
(rel)-ABT-378-d8
|
Isotope-Labeled Compounds
HIV Protease
SARS-CoV
HIV
|
Others
|
|
(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
|
-
- HY-180562
-
|
|
Ras
|
Cancer
|
|
KARS-IN-1 (152) is a AKR1C3 dependent KARS inhibitor with an AC50 of 9.1 nM for human KARS. KARS-IN-1 shows anti-proliferative activity in H460 (NRF2 pathway mutant cell line with high AKR1C3 expression) and Hara (NRF2 pathway wild type cell line with low AKR1C3 expression), with AC50 values ??of 21 nM and 16 nM, respectively. KARS-IN-1 can be used for the study of non-small cell lung cancer (NSCLC) .
|
-
- HY-112974
-
|
GSK-2998728; ISIS-420915
|
Transthyretin (TTR)
|
Cardiovascular Disease
Neurological Disease
|
|
Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy .
|
-
- HY-157403
-
|
|
Virus Protease
SARS-CoV
|
Infection
|
|
Jun12682 is an orally active SARS-CoV-2 papain-like protease (PL pro) inhibitor, with a Ki value of 37.7 nM and an EC50 value of 1.1 μM in the FlipGFP PL pro assay. Jun12682 has efficacy in hindering PL pro both deubiquitination and deISGylation, with Ki values of 63.5 and 38.5 nM, respectively. Jun12682 exhibits resistance in multiple PL pro mutant strains, and its enzymatic activity is comparable to that of the wild-type. Jun12682 can be used for the study of the SARS-CoV-2 .
|
-
- HY-180115
-
|
|
Bacterial
MMP
|
Infection
|
|
LP07 is an antibacterial agent targeting Pseudomonas aeruginosa with MIC values for both wild-type and efflux pump-deficient P. aeruginosa PA14 of both 8 μg/mL. LP07 exerts its antibacterial effect by directly disrupting the structural integrity of the bacterial cell membrane. LP07 moderately inhibits MMP-17 and MMP-19, but has no significant inhibitory effect on other MMP subtypes. LP07 does not inhibit the activity of LpxC enzyme. LP07 can be used for research on Pseudomonas aeruginosa infections .
|
-
- HY-P11829
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer .
|
-
- HY-182916
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
NNRT-IN-16, Rilpivirin (HY-10574) analogue, is a non-nucleoside reverse transcriptase inhibitor (NNRTI). NNRT-IN-16 inhibits recombinant WT HIV-1 RT with an IC50 of 0.07 μM. NNRT-IN-16 exerts antiviral activity against wild-type and drug-resistant HIV-1 mutants, shows attenuated CYP isoenzyme and hERG inhibition, reduced cytotoxicity, and improved metabolic stability in human liver microsomes. NNRT-IN-16 can be used for the research of HIV-1 infection .
|
-
- HY-137488
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC BRAF-V600E degrader-2 (compound 12) is a potent BRAF-V600E degrader with Kds of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-2 selectively degraded the kinase domain of BRAF-V600E but not the wild-type BRAF. PROTAC BRAF-V600E degrader-2 inhibits melanoma cell growth .
|
-
- HY-15814
-
|
|
Bcr-Abl
PDGFR
c-Kit
Src
JAK
Apoptosis
|
Cancer
|
|
HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression .
|
-
- HY-10035A
-
|
|
Calcium Channel
|
Neurological Disease
|
|
(R)-TTA-P2 is the isomer of TTA-P2 (HY-10035), and can be used as an experimental control. TTA-P2 (T-Type calcium channel inhibitor) is a potent inhibitor of T-Type calcium channel. TTA-P2 penetrates well the CNS and blocks the native T-type currents in deep cerebellar nuclear neurons, the window current is completely abolished both for wild-type and mutant Cav3.1 channels. TTA-P2 has the potential for the research of neurology disease .
|
-
- HY-P2265
-
|
|
SOS1
Ras
|
Cancer
|
|
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS .
|
-
- HY-136910
-
|
USP7-IN-7
|
Deubiquitinase
MDM-2/p53
|
Cancer
|
|
USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines .
|
-
- HY-B1588
-
|
|
Amyloid-β
Gap Junction Protein
|
Neurological Disease
Metabolic Disease
|
|
Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis .
|
-
- HY-19896
-
COTI-2
4 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-19869
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
VRX-480773 is an efficient non-nucleoside reverse transcriptase inhibitor (NNRTI), used for HIV infection. VRX-480773 has high specificity for HIV-1, with an EC50 for wild-type HIV-1 being 0.14 nM. VRX-480773 does not inhibit HIV-2, HBV or HCV, and has no effect on human DNA polymerase α/β. VRX-480773 retains inhibitory activity against Efavirenz (HY-10572) resistant strains, with EC50s mostly < 1 nM. VRX-480773 can be used for research on AIDS .
|
-
- HY-186122
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CCK2R agonist-1 (Compound 2S) is a CCK2R agonist, with an IC50 of 48 nM against wild-type CCK-2R and an IC50 of 450 nM against mutant CCK-2R (N353L). CCK2R agonist-1 stimulates the production of inositol phosphate. The changes in pH and HDC induced by CCK2R agonist-1 in mice are comparable to those induced by the full-length peptide agonist Gastrin. CCK2R agonist-1 can be used in studies of gastric diseases and pain .
|
-
- HY-143894
-
|
|
FLT3
|
Cancer
|
|
FLT3-IN-11 (compound 30) is a potent, selective and orally active FLT3 kinase inhibitor with IC50s of 7.22 nM and 4.95 nM for wild-type FLT3 and FLT3-D835Y, respectively. FLT3-IN-11 high selectivity for FLT3 over c-KIT (>1000-fold). FLT3-IN-11has excellent anti-acute myeloid leukemia (AML) activity (MV4-11 cells, IC50 of 3.2 nM) .
|
-
- HY-13803
-
Tazemetostat
Maximum Cited Publications
89 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-174850
-
|
|
Btk
|
Cancer
|
|
CFON-026 is a selective, orally active and non-covalent BTK inhibitor with an IC50 of 0.27 nM. CFON-026 has significant antitumor activity against wild-type BTK (TMD8 and REC-1) and all clinically relevant BTK resistance mutations (BTK C481S, T474I, L528W and V416L). CFON-026 induces complete tumor regression in TMD8 xenograft mice model. CFON-026 can be used for research of hematological cancers like chronic lymphocytic leukemia and waldenström macroglobulinemia .
|
-
- HY-19337
-
|
BAY 1896953; ORM-15341
|
Androgen Receptor
|
Cancer
|
|
Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
|
-
- HY-181647
-
|
|
Bacterial
Elastase
|
Infection
|
|
LasB-IN-3 is a protease elastase (LasB) inhibitor of Pseudomonas aeruginosa with an IC50 value of 8.5 nM. LasB-IN-3 shows an IC50 of 58.9 nM for the Met128Val mutant. LasB-IN-3 binds to active sites of wild-type and Met128Val mutant LasB, coordinates zinc ions, forms hydrogen bonds and CH-π interactions, and inhibits LasB proteolytic activity. LasB-IN-3 increases survival rate in LasB-induced acute lung injury mice models. LasB-IN-3 can be used for the research of Pseudomonas aeruginosa infection .
|
-
- 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-180273
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 309 (Compound C9) is an antibacterial agent, substrate of AcrB efflux pump. Antibacterial agent 309 promotes FtsZ polymerization. Antibacterial agent 309 demonstrates antibacterial activity against Erythromycin (HY-B0220)-resistant S. pyogenes 2 (MIC = 0.25 μg/mL), Penicillin-resistant S. aureus CI (MIC = 0.125 μg/mL), Penicillin-resistant S. epidermidis (MIC = 2 μg/mL). Antibacterial agent 309 exhibits weak antibacterial activity against the wild-type E. coli BW25113 MIC = 256 μg/mL) .
|
-
- HY-112823
-
|
HS-10296
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-145269
-
|
|
Cadherin
|
Cancer
|
|
AL-GDa62 is a derivative of the CDH1/E-cadherin modulator SLEC-11 (HY-145268) and induces apoptosis in CDH1 -/- cells. AL-GDa62 has an EC50 of 3.2 μM and 2 μM for isogenic mammary epithelial cells MCF10A-WT (wild type) and mutant MCF10A-CDH1 -/-, respectively. AL-GDa62 specifically inhibits TCOF1, ARPC5, and UBC9, and suppresses SUMOylation at low micromolar concentrations .
|
-
- HY-112823B
-
|
HS-10296 hydrochloride
|
EGFR
|
Cancer
|
|
Almonertinib (HS-10296) hydrochloride is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib hydrochloride shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib hydrochloride is used for the research of the non-small cell lung cancer .
|
-
- HY-13775
-
XL019
5 Publications Verification
|
JAK
Apoptosis
|
Cancer
|
|
XL019?is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2 .
|
-
- HY-P11092
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
TLQP-62 (mouse,rat) is a secreted C-terminal peptide that can be derived from protein VGF. TLQP-62 activates the BDNF-TrkB signaling pathway, inducing acute, transient phosphorylation of TrkB receptor and downstream CREB (Ser133) phosphorylation. TLQP-62 demonstrates excellent efficacy in promoting long-term fear memory formationin wild-type mice and reversing memory impairment in VGF heterozygous knock-out mice. TLQP-62 can be used for the study of memory-related neurological disorders (e.g., Alzheimer’s disease, frontotemporal dementia) .
|
-
- HY-178031
-
|
|
HIV
Reverse Transcriptase
|
Infection
|
|
HIV-1-IN-87 (Compound 11x) is a dual-site HIV-1 inhibitor targeting the non-nucleoside reverse transcriptase inhibitor binding pocket (NNIBP) and its adjacent site (NNIAS). HIV-1-IN-87 has potent antiviral activities against wild-type and mutant strains (such as L100I, K103N and Y181C) (EC50: 4.1-150 nM). HIV-1-IN-87 can be used for HIV-1 infections like acquired immune deficiency syndrome (AIDS) research .
|
-
- HY-156498
-
|
|
Ras
ERK
Raf
Ribosomal S6 Kinase (RSK)
AMPK
Apoptosis
PARP
|
Cancer
|
|
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
|
-
- HY-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-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-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-13464R
-
|
Brigatinib analog (Standard)
|
Reference Standards
Anaplastic lymphoma kinase (ALK)
EGFR
|
Cancer
|
|
ALK-IN-1 (Standard) is the analytical standard of ALK-IN-1 (Brigatinib analog) (HY-13464). This product is intended for research and analytical applications. ALK-IN-1 is an ALK and EGFR inhibitor. ALK-IN-1 binds to and inhibits ALK kinase, ALK fusion proteins, and wild-type and mutant EGFR variants, thereby disrupting their corresponding signaling pathways. ALK-IN-1 can suppress the growth and proliferation of tumor cells and exhibits potential inhibitory activity against mutant EGFR. ALK-IN-1 can be used in the research of non-small-cell lung cancer .
|
-
- HY-10029R
-
|
Rebemadlin (Standard)
|
MDM-2/p53
Reference Standards
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
|
Nutlin-3a (Standard) is the analytical standard of Nutlin-3a (HY-10029). This product is intended for research and analytical applications. 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-171884
-
|
|
EGFR
|
Cancer
|
|
BI-8128 is a potent EGFR inhibitor, with IC50 values of 12, 6.7, 22, 10, and 3 nM against wild-type, T790M, C797S, T790M/C797S, and L858R/T790M/C797S mutant EGFR, respectively. BI-8128 significantly inhibits the proliferation of Ba/F3 and PC-9 drug-resistant mutant cells. BI-8128 is applicable for the research of non-small cell lung cancer .
|
-
- HY-B0255R
-
|
GS 0840 (Standard)
|
Reference Standards
HBV
Reverse Transcriptase
Orthopoxvirus
Endogenous Metabolite
|
Infection
Cancer
|
|
Adefovir dipivoxil (Standard) is the analytical standard of Adefovir dipivoxil. This product is intended for research and analytical applications. Adefovir dipivoxil is an orally active adenosine analog and Adefovir prodrug. Adefovir dipivoxil inhibits DNA synthesis, activates the ATR signaling pathway, and disrupts the KCTD12-CDK1 interaction. Adefovir dipivoxil has antiviral activity against PRV, HBV, and orthopoxviruses. Adefovir dipivoxil has inhibitory effects on both lamivudine-resistant and wild-type strains. Adefovir dipivoxil has antitumor activity against lung and colon cancer .
|
-
- HY-W587486R
-
|
|
Reference Standards
Endogenous Metabolite
Bacterial
|
Neurological Disease
|
|
N-Acetyltaurine (Standard) is the analytical standard of N-Acetyltaurine (HY-W587486). This product is intended for research and analytical applications. N‑acetyltaurine is an orally active endogenous sulfonate that is synthesized from taurine and acetate in the renal cortex. N‑acetyltaurine supports bacterial growth as a sole fixed nitrogen or carbon source. N‑acetyltaurine buffers acetyl moieties of mitochondrial acetyl‑CoA in skeletal muscle. N‑acetyltaurine reduces food intake and body weight in obese and lean wild‑type mice in a GFRAL‑dependent manner. N‑acetyltaurine can be used for the research of diet‑induced obesity, hyperacetatemia and diabetes .
|
-
- HY-149591
-
|
|
TGF-β Receptor
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
M4K-2009 is an orally bioactive ALK2 inhibitor with an IC50 of 13 nM. M4K-2009 exerts comparable inhibitory potency against wild-type and mutant ALK2 G328V, ALK2 R206H, and ALK2 R258G. M4K-2009 exhibits moderate off-target inhibitory activity against hERG potassium channels. M4K-2009 can be used in studies related to diffuse intrinsic pontine glioma .
|
-
- HY-165381
-
|
|
MDM-2/p53
|
Cancer
|
|
ZMC2 is a thiosemicarbazone-class metal ion chelator and zinc ionophore with a human mutant p53 R175H binding Ka of 27.4 nM.ZMC2 binds Fe, Cu, Mn, Zn, and other transition metals.ZMC2 facilitates zinc transport across membranes.ZMC2 restores zinc binding to zinc-deficient p53 mutants, restoring wild-type structure and function, including site-specific DNA binding.ZMC2 generates reactive oxygen species (ROS).ZMC2 can be used for the research of cancer .
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-
- HY-177554
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
KB05yne is a site-selective, alkyne-functionalized electrophilic "probe" fragment probe designed for covalent ligand discovery, with preferential reactivity toward specific cysteine residues in proteins. KB05yne strongly labels wild-type target proteins (e.g., CDKN2AIP, HPCAL1) but does not label their cysteine-to-alanine mutants, confirming site-specific cysteine reactivity. KB05yne can be used for the discovery and optimization of site-specific covalent ligands, and is applicable to proteins with diverse structures and functions, especially in studies targeting cysteine residues in cancer-related or difficult-to-purify proteins .
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-
- HY-164473
-
|
|
ERK
Akt
STAT
Apoptosis
|
Cancer
|
|
DETD-35 is an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways, which promotes cancer cell apoptosis (Apoptosis) and reduces cancer cell resistance to Vemurafenib (HY-12057). The IC50 values of DETD-35 against wild-type and mutant melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c are 2.7, 6.0, 3.9, 3.1, and 2.5 μM, respectively. DETD-35 holds promise for research in the field of anti-melanoma therapy .
|
-
- HY-128131
-
|
|
Endogenous Metabolite
|
Others
|
|
UCCF-029 Free base is a potent activator of the cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel. UCCF-029 Free base exhibits enhanced activity through benzannulation of the flavone A-ring at the 7,8-position. UCCF-029 Free base serves as a structural guide for the development of more effective flavonoid analogues. UCCF-029 Free base demonstrates improved potency compared to apigenin in activating wild-type CFTR. UCCF-029 Free base also exhibits potential for activating the mutant CFTR (G551D-CFTR) though not as robustly as apigenin.
|
-
- HY-180229
-
|
|
SARS-CoV
|
Infection
|
|
GK730 is a potent and selective SARS-CoV-2 main protease inhibitor with an IC50 of 5.75 nM. GK730 does not inhibit cathepsin B, while exhibits weak inhibition of cathepsin L (IC50 = 11 μM). GK730 can simultaneously block the replication of the virus and the entry pathways for variants such as Omicron into cells. GK730 demonstrates an EC50 value of 5.70 μM against a wild-type SARS-CoV-2 strain in Vero E6 cells and CC50 value greater than 100 μM. GK730 can be used for the research of COVID-19 .
|
-
- 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-174458
-
|
|
PROTACs
MDM-2/p53
IKZF Family
Casein Kinase
|
Cancer
|
|
MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
|
-
- HY-176942
-
|
ROS1-IN-3
|
ROS Kinase
Trk Receptor
|
Cancer
|
|
YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-164694
-
|
TAS3351
|
EGFR
|
Cancer
|
|
Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively .
|
-
- HY-156619
-
|
EVT-8565072; THB335
|
c-Kit
PDGFR
|
Metabolic Disease
Inflammation/Immunology
|
|
Labuxtinib (EVT-8565072; THB335) is a potent dual inhibitor of c-Kit and PDGFR. Labuxtinib exhibits potent inhibitory activity against wild-type c-Kit (IC50 = 0.005 μM). Labuxtinib inhibits SCF-dependent and PDGF-dependent cell proliferation, and blocks the proliferation of cells dependent on c-Kit or PDGFR signaling pathways. In animal models of skin allergy, Labuxtinib depletes skin mast cells and significantly alleviates anaphylactic shock responses. Labuxtinib can be used in research on mast cell-related diseases, respiratory diseases, inflammatory diseases, fibrotic diseases, metabolic diseases, and other related conditions .
|
-
- HY-145743
-
|
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
CP-17 is a potent and selective IDH2/R140Q inhibitor with an IC50 of 40.75 nM. CP-17 exhibits excellent selectivity of >55-fold against the wild-type IDH2. CP-17 exhibits robust D-2-HG suppression activity in TF-1 (IDH2/R140Q) cells and reverses the cellular differentiation block induced by the R140Q mutation. CP-17 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-152233
-
|
|
HIV
|
Infection
|
|
Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-116973
-
|
|
HIV
|
Infection
|
|
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
|
-
- HY-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-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
-
- HY-135509
-
|
PF-06463922 acetate
|
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-180172
-
|
|
Trk Receptor
Apoptosis
|
Cancer
|
|
TRK-IN-33 is a TRK inhibitor. TRK-IN-33 exhibits excellent TRKA G667C degradation (DC50 = 24.69 nM; Dmax > 90%), while sparing the wild-type protein in virto. TRK-IN-33 shows antiproliferative activities against Ba/F3-LMNA-NTRK1 G667C cells with an IC50 value of 2.48 nM. TRK-IN-33 effectively inhibits tumor growth and enhances apoptosis in tumor tissues with no apparent toxicity in vivio. TRK-IN-33 can be used for NTRK fusion−positive cancers research .
|
-
- HY-112823R
-
|
HS-10296 (Standard)
|
Reference Standards
EGFR
|
Cancer
|
|
Almonertinib (Standard) is the analytical standard of Almonertinib. This product is intended for research and analytical applications. Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib is used for the research of the non-small cell lung cancer .
|
-
- HY-156292
-
|
|
Histone Methyltransferase
|
Cancer
|
|
IHMT-EZH2-426 (compound 38) is an effective covalent EZH2 degrader, with IC50 values of 1.3 nM, 1.2 nM, and 1.7-3.5 nM for EZH2 wild type, EZH2-A687V, and EZH2-Y641F/Y641N/Y641S, respectively. IHMT-EZH2-426 reduces H3K27me3 and EZH2 levels and shows effective anti-proliferative effects in B-cell lymphoma and TNBC cell lines.
|
-
- HY-W099725
-
|
|
Herbicide
Photosystem II
|
Cardiovascular Disease
Infection
|
|
Sarmentine is a broad-spectrum contact herbicide and PSII inhibitor, with an IC50 of 3.0 μM and a Ki of 1.5 μM against spinach, an IC50 of 1.72 μM against wild-type Amaranthus retroflexus, and an IC50 of 0.97 μM against triazine-resistant Amaranthus retroflexus. Sarmentine competitively binds to the QB binding site of plastoquinone on PSII, thereby blocking photosynthetic electron transport. Sarmentine inhibits enoyl-ACP reductase in Arabidopsis thaliana by targeting the early fatty acid synthesis process, with an IC50 of 18.3 μM. Sarmentine induces light-independent loss of plasma membrane integrity and electrolyte leakage. Sarmentine also exhibits antiplasmodial, antimycobacterial, antituberculous, and antiplatelet aggregation activities .
|
-
- HY-12879
-
IWP-4
2 Publications Verification
|
Wnt
Casein Kinase
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure .
|
-
- HY-109014
-
|
CMX-157
|
HIV
HBV
Nucleoside Antimetabolite/Analog
|
Infection
|
|
Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV .
|
-
- HY-13803R
-
|
EPZ-6438 (Standard); E-7438 (Standard)
|
Reference Standards
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
Tazemetostat (Standard) is the analytical standard of Tazemetostat. This product is intended for research and analytical applications. Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat also inhibits EZH1 with an IC50 of 392 nM. Tazemetostat induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells .
|
-
- HY-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-16639
-
|
|
GPR35
Neurotensin Receptor
|
Neurological Disease
Endocrinology
|
|
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
|
-
- HY-131864
-
|
|
PROTACs
EGFR
|
Cancer
|
|
SJF-1528 (PROTAC 1) 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 mutant EGFR in HeLa cells. SJF-1528 also degrades HER2. SJF-1528 promotes ubiquitination and degradation of EGFR and can be used in breast cancer research (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .
|
-
- HY-131864A
-
|
|
PROTACs
EGFR
|
Cancer
|
|
SJF-1528 (PROTAC 1) hemihydrate 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 mutant EGFR in HeLa cells. SJF-1528 hemihydrate also degrades HER2. SJF-1528 hemihydrate promotes ubiquitination and degradation of EGFR and can be used in breast cancer research (Pink: ligand for target protein (HY-159047); Black: linker Tos-PEG2-CH2-Boc (HY-130532); Blue: ligand for E3 ligase (S,R,S)-AHPC (HY-125845)) .
|
-
- HY-183622
-
|
|
MDM-2/p53
|
Cancer
|
|
UCI-1014 is a mutant p53 (p53 R175H) corrector/reactivator. UCI-1014 restores the wild-type-like DNA-binding activity of p53 R175H, promotes the redistribution of the mutant protein to chromatin, and induces the expression of p53-dependent target genes. UCI-1014 inhibits the proliferation of p53 R175H-mutant cancer cells through an SLC7A11-independent mechanism. UCI-1014 can be used for research related to p53-mutant cancers .
|
-
- HY-183080
-
|
|
Bacterial
Penicillin-binding protein (PBP)
|
Infection
|
|
VNRX-14079 is an antibacterial agent and PBP2 inhibitor, with an IC50 value of 1.7 μM against wild-type Neisseria gonorrhoeae PBP2. VNRX-14079 forms a covalent bond with Ser310 of PBP2, interacts with multiple residues of PBP2 to stabilize the complex, and induces an inward conformational change of the β3-β4 loop in chimeric PBP2. VNRX-14079 exhibits antibacterial activity against Ceftriaxone (HY-B0712)-resistant Neisseria gonorrhoeae strains. VNRX-14079 can be used in the research of gonorrhea .
|
-
- HY-403733A
-
|
|
Androgen Receptor
|
Cancer
|
|
(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
|
-
- HY-153228
-
|
PBI-0451
|
SARS-CoV
|
Infection
|
|
Pomotrelvir is a selective, competitive, orally active covalent inhibitor of the SARS-CoV-2 main protease (M pro), with an IC50 of 24 nM for wild-type SARS-CoV-2 M pro. Pomotrelvir inhibits viral polyprotein processing, thereby preventing viral replication. Pomotrelvir has shown broad antiviral activity against multiple SARS-CoV-2 variants (including Omicron) in cell-based experiments, and has an additive effect when combined with nucleoside analogs that target viral RNA synthesis. Pomotrelvir is primarily used for the research and development of COVID-19 antiviral drugs, especially for infections caused by SARS-CoV-2 and its variants .
|
-
- HY-185443
-
|
|
Bacterial
Dihydrofolate reductase (DHFR)
|
Infection
|
|
UCP1172 is an antibacterial (Antibacterial) agent and Dihydrofolate reductase inhibitor, with an IC50 of 0.0089 μM against Staphylococcus aureus DfrB, 0.22 μM against DfrG, 0.41 μM against DfrA, and 0.030 μM against DfrK. UCP1172 potently inhibits the growth of MRSA/MSSA isolates carrying dfrG and dfrK (MIC values of 0.3125-0.625 μg/mL), shows weak activity against MRSA carrying dfrA (MIC of 5 μg/mL), and exerts extremely potent inhibitory effects on wild-type S. aureus ATCC 43300 (MIC of 0.0098 μg/mL). UCP1172 can be used in studies related to tuberculosis and Staphylococcus aureus infections .
|
-
- 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. KRAS G13D-IN-1 can be used in the research of colon cancer .
|
-
- HY-12215R
-
|
PF-06463922 (Standard)
|
Reference Standards
Anaplastic lymphoma kinase (ALK)
ROS Kinase
Apoptosis
|
Cancer
|
|
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
|
-
- HY-175541
-
|
|
PROTACs
Btk
|
Cancer
|
|
TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545)) .
|
-
- HY-116572A
-
|
|
Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
|
Cancer
|
|
TASIN-1 is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 can be used to prevent and intervene in APC mutant colorectal cancer .
|
-
- HY-P2265A
-
|
|
SOS1
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-116572
-
|
|
Reactive Oxygen Species (ROS)
JNK
Apoptosis
Caspase
|
Cancer
|
|
TASIN-1 hydrochloride is a selective inhibitor of truncated APC TR (adenomatous polyposis coli gene) that exerts cytotoxic effects by inhibiting cholesterol biosynthesis. TASIN-1 hydrochloride specifically targets colorectal cancer (CRC) cells carrying APC truncated mutations, while having no significant toxicity to wild-type APC cells. TASIN-1 hydrochloride exerts cytotoxic effects by targeting Emopamil binding protein (EBP) to inhibit cholesterol biosynthesis, triggering endoplasmic reticulum (ER) stress, reactive oxygen species (ROS) generation, and JNK-mediated apoptosis, and inhibiting Akt survival signaling. TASIN-1 hydrochloride can be used to prevent and intervene in APC mutant colorectal cancer .
|
-
- HY-175804
-
|
|
SARS-CoV
|
Infection
|
|
M2 ion channel blocker-2 (Compound 10) is a M2 channel blocker. M2 ion channel blocker-2 significantly blocks wild-type and mutant M2 (L27F and V27A) ion channels. M2 ion channel blocker-2 has potent antiviral activity against HCoV-229E (EC50: 4.7 μM in cytopathic effect) but not against influenza A virus. M2 ion channel blocker-2 has no significant inhibition of hERG and cytochrome P450 (CYP1A2, CYP2C19, and CYP3A4) activity .
|
-
- 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-178497
-
|
|
PROTACs
Ras
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
ZJK-807 is a highly effective and selective PROTAC degrader targeting KRASG12D (DC50 = 79.5 nM in AsPC-1 cells). ZJK-807 shows minimal impact on wild-type KRAS or other mutants (G12C/S/V, G13D), inducing mutant-specific cytotoxicity. ZJK-807 suppresses RAS/MAPK signaling and uniquely modulates TNF signaling and eukaryotic ribosome biogenesis. ZJK-807 can be used for the study of KRAS-driven pancreatic cancer. Yellow: KRASG12D ligand (HY-W087383); Green: E3 ligase CRBN ligand (HY-178507); Black: Linker (HY-178506) .
|
-
- HY-115443
-
|
|
FLT3
|
Cancer
|
|
MZH29 is a potent and orally active FLT3 inhibitor. MZH29 shows inhibitory effects on wild-type and mutant FLT3, including the FLT3-ITD, FLT3-D835H/Y/V and FLT3-K663Q mutants. MZH29 retains its potent inhibitory effect against the FLT3-ITD/F691L mutation, a drug resistance mutation against the well-known FLT3 inhibitor, AC220 (HY-13001). MZH29 can be used for the research of cancer, such as acute myeloid leukemia (AML) .
|
-
- HY-W778649
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Isotope-Labeled Compounds
Herbicide
Photosystem II
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Others
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Sarmentine-d8 is the deuterium labeled Sarmentine. Sarmentine is a broad-spectrum contact herbicide and PSII inhibitor, with an IC50 of 3.0 μM and a Ki of 1.5 μM against spinach, an IC50 of 1.72 μM against wild-type Amaranthus retroflexus, and an IC50 of 0.97 μM against triazine-resistant Amaranthus retroflexus. Sarmentine competitively binds to the QB binding site of plastoquinone on PSII, thereby blocking photosynthetic electron transport. Sarmentine inhibits enoyl-ACP reductase in Arabidopsis thaliana by targeting the early fatty acid synthesis process, with an IC50 of 18.3 μM. Sarmentine induces light-independent loss of plasma membrane integrity and electrolyte leakage. Sarmentine also exhibits antiplasmodial, antimycobacterial, antituberculous, and antiplatelet aggregation activities .
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- HY-170438
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EGFR
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Cancer
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EGFR-IN-139 (compound PD 18) is an epidermal growth factor receptor (EGFR) inhibitor, with IC50s of 12.88 (wild type), 10.84 (L858R/T790M), 42.68 (L858R/T790M/C797S) nM, respectively. EGFR-IN-139 displays strong anticancer activity against A549 and H1975 cancer cell lines, which are highly expressed EGFR. EGFR-IN-139 has a strong selectivity to cancer cells. EGFR-IN-139 can be used for nonsmall cell lung cancer (NSCLC) research[1].
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- HY-171906
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1-Arachidonoyl-sn-glycerol 3-phosphate; 1-Arachidonoyl LPA; LPA (20:4)
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LPL Receptor
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Inflammation/Immunology
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1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid containing arachidonic acid at the sn-1 position. It is a precursor to 1-arachidonoyl glycerol (1-Monoarachidin; HY-130567) . 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA binds to the LPA2/EDG4 receptor with an EC50 value of approximately 10 nM . It prevents TNF-α and IL-6 secretion in wild-type but not Lpa2-/- dendritic cells stimulated by LPS . It also decreases differentiation of HT-29 human colon carcinoma cells to goblet cells in the presence of sodium butyrate .
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- HY-122562
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MT-802
4 Publications Verification
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PROTACs
Btk
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Cancer
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MT-802 is a BTK PROTAC degrader. MT-802 degrades wild-type BTK (DC50 = 14.6 nM) and BTK mutants including E41K, C481S (DC50 = 14.9 nM), C481R, C481Y, C481T, C481F, L528W, and inhibits their Y223 phosphorylation. BI-4732 can be used for the study of Ibrutinib (HY-10997)-resistant chronic lymphocytic leukemia (CLL). (Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-141371), E3 ligase ligand-linker conjugate (HY-176340)) .
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- HY-12879G
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Wnt
Casein Kinase
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Cardiovascular Disease
Neurological Disease
Cancer
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IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure .
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- HY-175302
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Trk Receptor
Apoptosis
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Cancer
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TRK-IN-32 is a potent TRK inhibitor. TRK-IN-32 potently inhibits TRK WT, TRK G595R and TRK G667C with IC50 values of 0.08 nM, 2.14 nM and 0.68 nM, respectively. TRK-IN-32 also demonstrates antiproliferative activity against a panel of Ba/F3 cell lines transformed with wild type, xDFG, solvent-front as well as gatekeeper mutant TRK fusion proteins. TRK-IN-32 induces apoptosis of Ba/F3-TRKA WT and Ba/F3-TRKA G667C cells.TRK-IN-32 can be used for the study of various cancers (such as thyroid cancer, secretory breast carcinoma) .
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- HY-19337S1
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BAY 1896953-d6; ORM-15341-d6
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Isotope-Labeled Compounds
Androgen Receptor
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Cancer
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Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-179497
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FLT3
VEGFR
Akt
STAT
ERK
Apoptosis
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Cancer
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FLT3-IN-37 (Compound 6z) is a potent inhibitor of FLT3-ITD, with IC50 values of 1.5 and 3.4 nM for FLT3-ITD and TEL-VEGFR2, respectively. FLT3-IN-37 exhibits high selectivity for wild-type FLT3 (WT) and c-Kit. FLT3-IN-37 inhibits FLT3 phosphorylation and downregulates the expression of p-Akt, p-STAT5, and p-ERK. FLT3-IN-37 exerts anti-leukemia effects by blocking the cell cycle and inducing apoptosis (apoptosis). FLT3-IN-37 can be used for research on acute myeloid leukemia (AML) .
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- HY-180561
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Deubiquitinase
JAK
STAT
Apoptosis
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Cancer
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WWQ-03-012 is a selective deSUMOylating isopeptidases DESI2 inhibitor with an IC50 of 47.3 μM. WWQ-03-012 cans induce JAK2-V617F ubiquitination-proteasome degradation with no significant effect on wild-type JAK2. WWQ-03-012 can block JAK2-STAT3/5 signaling, inhibit cell proliferation and induce apoptosis. WWQ-03-012 has a synergistic effect in combination with Ruxolitinib (HY-50856), further enhancing its killing effect on JAK2 mutant cells. WWQ-03-012 can be used for the research of cancer, such as myeloproliferative neoplasms .
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- HY-159834
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SLC-D011
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DNA/RNA Synthesis
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Others
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Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in Lmna G609G/G609G mice and Lmna G609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS) .
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- HY-181659
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EGFR
Apoptosis
Akt
ERK
Caspase
Bcl-2 Family
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Cancer
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EGFR-IN-201 is a potent EGFR inhibitor, with an IC50 of 0.091 μM against wild-type EGFR; for mutant EGFR variants, the IC50 values of EGFR T790M, EGFR L858R and EGFR C797S are 0.147 μM, 0.221 μM and 0.703 μM, respectively. EGFR-IN-201 inhibits EGFR downstream signaling proteins AKT1 (IC50 = 0.225 μg/mL) and ERK1 (IC50 = 0.705 μg/mL). EGFR-IN-201 induces G0/G1 cell cycle arrest, apoptosis and low-level necrosis in cancer cells. EGFR-IN-201 is applicable to research on cancers such as colon cancer .
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- HY-173163
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Bacterial
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Infection
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(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) (Compound 4a) is a Gram-negative outer membrane permeabilizer with synergistic antibacterial activity through the blockage on LptA/LptC interaction via targeting Met47 in LptA. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) potentiates pol B against both wild-typed and MDR A. baumannii and E. coli strains. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) can be used as antibiotic adjuvants against MDR Gram-negative bacteria .
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- HY-181004
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CDK
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Cancer
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PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer .
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- HY-161275
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EGFR
Akt
ERK
Ribosomal S6 Kinase (RSK)
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Cancer
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BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
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- HY-181661
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SARS-CoV
Virus Protease
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Infection
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YL1004 is a potent, selective and orally active noncovalent inhibitor of SARS-CoV-2 papain-like protease (PL pro). YL1004 shows an IC50 of 17.5 nM and a Ki of 2.3 nM against PL pro, with an in vitro anti-SARS-CoV-2 EC50 of 0.08 μM-1.37 μM. YL1004 suppresses the proteolytic activity of PL pro and blocks its deubiquitinating and deISGylating effects to restore host innate antiviral immune signaling. YL1004 inhibits the replication of wild-type, Delta, Omicron variants and nirmatrelvir-resistant strains of SARS-CoV-2. YL1004 can be used for the research of COVID-19 (SARS-CoV-2 infection) .
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- HY-N18649
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Others
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Inflammation/Immunology
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Rosa canina extract, derived from the wild rose (often known as rose hip), is rich in vitamin C, flavonoids, carotenoids, and essential fatty acids, contributing to its numerous health benefits. The extract is primarily known for its anti-inflammatory, antioxidant, and immune-boosting properties. Rosa canina extract is commonly used to boost the immune system, particularly during cold and flu seasons, due to its high vitamin C content. It also has joint health benefits, as it helps reduce inflammation and pain in conditions like arthritis. The extract's antioxidant properties help protect cells from oxidative stress and may contribute to skin health by promoting collagen synthesis, reducing the appearance of wrinkles, and supporting overall skin elasticity.
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- HY-182924
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PROTACs
Enterovirus
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Infection
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Jun15702 is a PROTAC degrader targeting the capsid protein VP1 of enterovirus D68. Jun15702 recruits the Cereblon (CRBN) E3 ligase and activates the ubiquitin-proteasome pathway. Jun15702 inhibits viral entry and exerts inhibitory effects during the early, middle and late stages of viral replication. Jun15702 exhibits antiviral activity against multiple wild-type enterovirus D68 strains, and also shows submicromolar antiviral activity against the Pleconaril (HY-19952)-resistant enterovirus D68 variant rMO-VP1 F159V. Jun15702 can be used in studies related to enterovirus D68 (EV-D68) infection .
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- HY-109014R
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CMX-157 (Standard)
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HIV
HBV
Nucleoside Antimetabolite/Analog
Reference Standards
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Infection
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Tenofovir exalidex (Standard) is the analytical standard of Tenofovir exalidex. This product is intended for research and analytical applications. 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 .
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- HY-182500A
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Toll-like Receptor (TLR)
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Neurological Disease
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(S,S)-SARM1-IN-9 (Compound MY-13A) is a stereoselective SARM1 inhibitor with covalent binding properties. (S,S)-SARM1-IN-9 covalently modifies Cys311 in the autoregulatory ARM domain of wild-type SARM1, thereby blocking NADase activity, without inhibiting the SARM1 C311A or SARM1 C311S mutants. (S,S)-SARM1-IN-9 blocks vacor- and vincristine-induced axon degeneration in primary rodent dorsal root ganglion neurons. (S,S)-SARM1-IN-9 can be used for research on axon degeneration-dependent neurological disorders, including chemotherapy-induced peripheral neuropathy .
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- HY-403733C
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Androgen Receptor
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Cancer
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JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
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- HY-174499
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mRNA
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Others
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Cas9 Nickase D10A mRNA expresses a version of the Streptococcus pyogenes SF370 Cas9 protein (CRISPR Associated Protein 9) that contains a D10A amino acid substitution. This mRNA also contains a C-terminal nuclear localization signal followed by a HA tag.Cas9 functions as part of the CRISPR (clustered regularly interspaced short palindromic repeats) genome editing system. In the CRISPR system, an RNA guide sequence targets the site of interest and the Cas9 protein is employed to perform the DNA cleavage. While wild-type Cas9 creates a double-stranded break at the target site, Cas9 nickase creates a single-stranded break. This favors homology-directed repair and decreases the occurrence of non-homologous end joining.
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- HY-N0475
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Hypolide; (+)-Triptophenolide
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Androgen Receptor
Pyroptosis
Caspase
Bcl-2 Family
Apoptosis
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Inflammation/Immunology
Cancer
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Triptophenolide (Hypolide) is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
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- HY-19337S
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BAY 1896953-d3; ORM-15341-d3
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Isotope-Labeled Compounds
Androgen Receptor
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Cancer
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Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-145836
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FGFR
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Cancer
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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-134421
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HMG-CoA Reductase (HMGCR)
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Metabolic Disease
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2-Butenoyl coenzyme A lithium is an inactivator and a substrate of Plasmodium falciparum enoyl-β-hydroxyacyl-acyl carrier protein (ACP) reductase and other enoyl-CoA reductases, and it is also the lithium salt of trans-2-methyl-2-butenoyl coenzyme A. 2-Butenoyl coenzyme A lithium acts on short-chain and medium-chain coenzyme A dehydrogenases as well as glutaryl-CoA dehydrogenase, and shows no activity against wild-type isovaleryl-CoA dehydrogenase. 2-Butenoyl coenzyme A lithium functions as a metabolite in the L-isoleucine catabolic pathway, and can serve as a substrate in the activity assay of 3-ketothiolase. 2-Butenoyl coenzyme A lithium is applicable to research related to 3-ketothiolase deficiency .
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- HY-15800
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TNK1
LRRK2
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-175491
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HIV
Reverse Transcriptase
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Infection
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HIV-1-IN-85 is an orally active HIV-1 inhibitor (IC50 = 72 nM). HIV-1-IN-85 exhibits strong inhibitory activity against wild-type (WT) HIV-1 and NNRTI-resistant single mutant strains (L100I, K103N, Y181C, Y188L, E138K) and moderate efficacy against double mutant strains (F227L+V106A, RES056). HIV-1-IN-85 shows good in vivo safety in ICR mice. HIV-1-IN-85 can be used for the study of HIV-1 infection .
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- HY-153605
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EGFR
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Cancer
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EGFR-IN-77 (Compound 4a) is a selective EGFR T790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFR T790M/L858R, 0.477 μM against EGFR L858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFR L858R/T790M double-mutant non-small cell lung cancer .
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- HY-182946
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PI3K
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Cancer
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PI3Kα-IN-31 is an orally active and selective PI3Kα inhibitor. PI3Kα-IN-31 shows potent preference for mutant PI3Kα over wild-type PI3Kα. PI3Kα-IN-31 exerts antiproliferative effects in PI3Kα-mutant cancer cells. PI3Kα-IN-31 suppresses tumor growth in xenograft models. PI3Kα-IN-31 can be used for the research of breast cancer .
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- HY-108029
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ACH-2684 sodium; Neceprevir sodium
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HCV
HCV Protease
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Infection
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Deldeprevir (ACH-2684; Neceprevir) sodium is a HCV NS3/4A protease inhibitor and resistance inhibitor. Deldeprevir sodium exhibits activity against wild-type genotype 1a and 1b HCV, including mutant strains resistant to other NS3 protease inhibitors. Deldeprevir sodium blocks the emergence of HCV mutant strains resistant to ACH-3422 in vitro, with enhanced efficacy when used in triple combination with ACH-3422 and ACH-3102 (HY-124182). Deldeprevir sodium shows additive antiviral potency when combined with ACH-3422, and exerts antiviral activity against HCV replicons carrying ACH-3102. Deldeprevir sodium is applicable to research related to hepatitis C .
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- HY-15800A
-
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TNK1
LRRK2
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-146223A
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Ras
PI3K
p38 MAPK
Apoptosis
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Cancer
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(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
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- HY-181954
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EGFR
Apoptosis
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Cancer
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ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer .
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- HY-119396
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Endogenous Metabolite
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Cancer
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DY3002 is a selective and highly potent EGFR inhibitor with activity in overcoming T790M-mediated drug resistance in non-small cell lung cancer. DY3002 exhibited superior inhibitory effects against EGFR T790M mutants in kinase assays (IC50 = 0.71 nM), compared to weaker inhibitory effects against wild-type EGFR (IC50 = 448.7 nM). DY3002 was significantly superior to rociletinib and osimertinib in selectivity, showing an extremely high selectivity index (SI = 632.0). In cell experiments, DY3002 had an IC50 value of 0.037 μM against H1975 cells, showing enhanced inhibitory potency. In addition, DY3002 was superior to other alternative compounds in terms of biological properties and did not cause hyperglycemia .
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- HY-112363
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RP107
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CDK
GSK-3
ERK
JNK
CFTR
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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-174453
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PROTACs
Estrogen Receptor/ERR
Apoptosis
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Cancer
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PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310)) .
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- HY-122578
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MDM-2/p53
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Cancer
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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-176786
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PROTACs
Ras
Apoptosis
PERK
p38 MAPK
Caspase
TNF Receptor
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Cancer
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MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
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- HY-180977
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PROTACs
Bcr-Abl
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Cancer
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P19P is a BCR-ABL PROTAC degrader based on Ponatinib (HY-12047), with a DC50 value of approximately 20 nM for the wild-type BCR-ABL protein. P19P can effectively degrade various drug-resistant mutants such as T315I, E255K, H396R, and V468F, and exhibits potent anti-proliferative activity in BaF3-BCR-ABL (T315I) cells. P19P maintains strong inhibitory activity against ABL (T315I), with a IC50 of 13.1 nM. P19P does not inhibit the formation of vascular lumens in HUVEC. P19P can be used for research on chronic myeloid leukemia and acute lymphoblastic leukemia .
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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 alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-181991
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Virus Protease
Flavivirus
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Infection
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IRBM-Z-2 is a non-competitive, orally active Zika virus (ZIKV) NS2B-NS3 protease inhibitor, with IC50 values of 0.04 μM and 3.1 μM against the wild-type and I156T mutant strains, respectively. IRBM-Z-2 exhibits broad-spectrum anti-flavivirus potential, with IC50 values of 2.1 μM and 0.09 μM against the NS2B-NS3 proteases of dengue virus 2 (DENV2) and West Nile virus (WNV), respectively. IRBM-Z-1 inhibits ZIKV replication and alleviates virus-induced cytopathic effects. IRBM-Z-1 can be used in studies related to ZIKV infection .
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- HY-115701
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1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-phosphoethanolamine; 15(S)-HpETE-SAPE; 15(S)-hydroperoxyeicostetraenoic acid-SAPE
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Ferroptosis
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Inflammation/Immunology
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1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe is a phospholipid that contains stearic acid (HY-B2219) at the sn-1 position and 15(S)-HpETE at the sn-2 position. It is produced via oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-Pe (SAPE) by 15-lipoxygenase (15-LO). 1-Stearoyl-2-15(S)-HpETE-sn-glycero-3-Pe (0.6 and 0.9 μM) increases ferroptotic cell death in wild-type and Acsl4 knockout Pfa1 mouse embryonic fibroblasts (MEFs) treated with the GPX4 inhibitor RSL3.
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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-153321
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NX-5948; BTK-IN-24
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PROTACs
Btk
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Inflammation/Immunology
Cancer
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Bexobrutideg (NX-5948) 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. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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- HY-W013403
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IFNAR
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Infection
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2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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- HY-172733S
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Isotope-Labeled Compounds
Histone Methyltransferase
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Cancer
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|
PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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- HY-175213
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Isocitrate Dehydrogenase (IDH)
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Cancer
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Mutant IDH1-IN-7 is a highly selective Isocitrate Dehydrogenase 1 (IDH1) R132H (IC50 = 0.26 μM, Kd = 2.1 μM)/R132C (IC50 = 1.1 μM) inhibitor. Mutant IDH1-IN-7 has no inhibitory effect on wild-type IDH1, IDH2-wt, and IDH2 R140Q. Mutant IDH1-IN-7 inhibits 2-Hydroxyglutarate (2-HG) production in U87-MG R132H cells (EC50 = 0.55 μM). Mutant IDH1-IN-7 exhibits moderate antiproliferative effects on U87-MG R132H and HT-1080 cells .
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- HY-N0475R
-
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Hypolide (Standard); (+)-Triptophenolide (Standard)
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Reference Standards
Androgen Receptor
Pyroptosis
Caspase
Bcl-2 Family
Apoptosis
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Inflammation/Immunology
Cancer
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Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
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- HY-165298
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PROTACs
FGFR
ERK
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Cancer
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DGY-09-192 is a PROTAC FGFR1/2 degrader (FGFR1: DC50 = 4.35 nM; FGFR2: DC50 = 70 nM). DGY-09-192 preferentially degrades wild-type FGFR1/2 and multiple FGFR2 fusion proteins (including FGFR2-PHGDH and FGFR2-OPTN). DGY-09-192 suppresses downstream FGFR signaling (reducing phosphorylation of FRS2 Y196 and ERK1/2 T202/Y204) in vitro and vivo. DGY-09-192 can be used for the study of FGFR-driven cancers. (Pink: FGFR1/2 ligand (HY-160013), Blue: VHL Ligand (HY-112078), Black: Linker (HY-W020017)) .
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- HY-159591
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Ras
Akt
ERK
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Cancer
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YK-8S is a dual-targeted K-Ras (G12D/G12C) covalent inhibitor. YK-8S shows no significant binding to wild-type K-Ras and other mutants (G12R, G13D, Q61R/K). YK-8S exhibits anti-proliferative activity against H358 (G12C) and AGS (G12D) cells. YK-8S inhibits the phosphorylation of p-AKT/p-ERK in BaF3/G12D and G12C cells. YK-8S can be used for pancreatic cancer, colorectal cancer and other tumors with high incidence of G12D .
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- HY-D1737
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Bacterial
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Infection
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RADA is a fluorescent D-amino acid (FDAA) with high photostability and thermostability, which emits yellow-to-orange fluorescence. RADA shows low outer membrane permeability in wild-type Gram-negative Escherichia coli, but it targets penicillin-binding proteins and L,D-transpeptidases, mimics the interaction between acyl acceptors and enzyme intermediates, and integrates into peptidoglycan during biosynthesis. As a peptidoglycan labeling reagent, RADA metabolically integrates into the nascent peptidoglycan of live bacterial cells, labels the peptidoglycan at the poles and lateral walls of mycobacteria, and enables visualization of peptidoglycan synthesis and remodeling processes. RADA serves as a non-specific stain for fixed cells, is non-toxic to bacterial cells, and its red-shifted excitation/emission spectra reduce phototoxicity. RADA also supports virtual pulse-chase labeling experiments and stochastic optical reconstruction microscopy for sub-diffraction-limited imaging of bacterial cell walls .
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- HY-178938
-
|
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Molecular Glues
Androgen Receptor
Caspase
Apoptosis
|
Endocrinology
Cancer
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AR Degrader-3 is an orally active molecular glue that targets AR/ARV7 and induces the degradation of AR and ARV7 through the ubiquitin-proteasome pathway (UPP). AR Degrader-3 directly interacts with the ligand-binding domain (LBD) and the N-terminal domain (NTD) of AR. AR Degrader-3 effectively suppresses the transcriptional activity of wild-type AR (AR-WT), AR mutants, and ARV7. AR Degrader-3 downregulates the mRNA and protein levels of downstream AR target genes, thereby overcoming antiandrogen resistance mediated by ARV7 and AR point mutations. AR Degrader-3 induces apoptosis in Enzalutamide (HY-70002) (ENZa)-resistant cells and increases cleaved caspase-3 protein levels. AR Degrader-3 can be used for the study of castration-resistant prostate cancer (CRPC) .
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- HY-P11075
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Neurokinin Receptor
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Metabolic Disease
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[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research .
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![[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10)](//file.medchemexpress.com/product_pic/hy-p11075.gif)
- HY-176785S
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Ras
Apoptosis
p38 MAPK
Caspase
TNF Receptor
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Cancer
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MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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- HY-176547
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FGFR
Cytochrome P450
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Endocrinology
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|
FGFR2/3-IN-3 is a dual-target FGFR2/3 inhibitor with IC50s of 2.7 nM (TEL-FGFR2) and 3.9 nM (TEL-FGFR3), respectively. FGFR2/3-IN-3 has effective activity against both wild-type and mutant FGFR3. FGFR2/3-IN-3 has low CYP3A4 inhibitory effect and hERG toxicity. FGFR2/3-IN-3 improves the imbalance between chondrocyte proliferation and differentiation and promotes bone growth by inhibiting the signaling pathway mediated by mutant FGFR3. FGFR2/3-IN-3 shows a growth-promoting effect in a dwarfism mouse model and has the potential to study bone development disorder-related diseases such as achondroplasia (ACH) .
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- HY-153321A
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(R,R)-NX-5948; (R,R)-BTK-IN-24
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Drug Isomer
PROTACs
Btk
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Inflammation/Immunology
Cancer
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|
(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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- HY-145939
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|
BRD5846
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Casein Kinase
|
Cancer
|
|
BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
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-
- HY-134851
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HIV
|
Infection
|
|
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM .
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-
- HY-153356
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Molecular Glues
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
MRT-2359 is an orally active and selective GSPT1 molecular glue degrader, with a DC50 of 5 nM. MRT-2359 induces CRBN/GSPT1 ternary complex formation to drive CRBN- and degron-dependent proteasomal GSPT1 degradation, with selectivity for wild-type GSPT1 over the GSPT1G575N mutant. MRT-2359 disrupts protein translation, induces ribosome stalling, downregulates MYC family proteins and their transcriptional output, reduces proliferation, and induces apoptosis in cancer cells. MRT-2359 can be used for the research of non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), neuroendocrine lung cancer, high grade neuroendocrine cancers, diffuse large B-cell lymphoma, prostate cancer, and MYC-driven solid tumors .
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- HY-P991641
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|
LY3012218
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FLT3
p38 MAPK
STAT
PI3K
Akt
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Cancer
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|
IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research .
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- HY-180976
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|
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PROTACs
α-synuclein
|
Neurological Disease
|
|
Arg-PEG1-Tαsyn is an α-syn PROTAC degrader with a DC50 of 0.28 μM in U251 cells. Arg-PEG1-Tαsyn employs the amino acid arginine (Arg) as the E3 ligase UBR1 ligand and a benzothiazole-aniline variant as the warhead for α-syn. Arg-PEG1-Tαsyn significantly reduces α-syn aggregates and improves the dopaminergic neuronal impairment and the locomotion with safety profile in vivo.Arg-PEG1-Tαsyn shows the high degradation effect in mammalian cells for both wild-type α-syn and the α-syn (A53T) mutant. Arg-PEG1-Tαsyn can be used for Parkinson’s disease research .
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-
- HY-170926
-
|
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RET
Apoptosis
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Cancer
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CQ1373 is a potent RET inhibitor, demonstrating cellular potency with IC50 values of 13.0, 25.7 and 28.4 nM against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C and CCDC6-RET-G810R, respectively. CQ1373 exhibits good selectivity toward wild-type RET and solvent front mutants G810C/R with IC50 values of 4.2, 7.1 and 32.4 nM, respectively. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. CQ1373 induces Apoptosis and cell cycle arrest in BaF3 cells. CQ1373 exhibits anti-tumor efficacy and can be used for cancer research .
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-
- HY-139062
-
|
C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
|
Apoptosis
Ceramidase
Autophagy
β-catenin
|
Cancer
|
|
C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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-
- HY-178057
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|
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EGFR
Akt
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant). EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR 19del/T790M/C797S and EGFR L858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 < 0.5 nM). EGFR-IN-176 can be used for the study of non-small cell lung cancer (NSCLC) .
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- HY-175864
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|
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EGFR
Apoptosis
p38 MAPK
ERK
Akt
STAT
|
Inflammation/Immunology
Cancer
|
|
EGFR-IN-173 is an orally active, pan-mutant EGFR tyrosine kinase inhibitor that targets EGFR 19del, L858R/T790M and C797S triple-mutations, potently inhibiting EGFR 19del/T790M/C797S with an IC50 of 1.19 nM while showing over 100-fold selectivity for mutant over wild-type EGFR (IC50 = 19.362 μM against WT). EGFR-IN-173 significantly inhibits cell migration, induces apoptosis in non-small cell lung cancer (NSCLC) cells. EGFR-IN-173 inhibits EGFR phosphorylation and suppresses the downstream pathways (MAPK/ERK, AKT, STAT3). EGFR-IN-173 exhibits antitumor efficacy in NSCLC and Ba/F3 xenograft models. EGFR-IN-173 can be used for NSCLC research .
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- HY-167690
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|
|
Endogenous Metabolite
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Infection
|
|
MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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- HY-168384
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STING
TNF Receptor
Interleukin Related
CD28
|
Inflammation/Immunology
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|
M04 is an agonist of STING. It induces the expression of the IFN reporter gene in HEK293T cells expressing wild-type human STING, but does not induce this expression in HEK293T cells expressing the R71H-G230A-R293Q (HAQ) STING variant or in mouse RAW 264.7 cells, indicating that its activity is dependent on allelic and species variations. M04 induces the production of TNF-α, IL-10, IL-1β, and IL-12p70 in human peripheral blood mononuclear cells (PBMCs). At a concentration of 50 µM, M04 stimulates dendritic cells isolated from PBMCs to express the MHC class II cell surface receptor HLA-DR and co-stimulatory molecules CD40, CD80, and CD86, and also enhances their ability to activate T cells in an ex vivo assay. M04 can be used in research on inflammatory immune diseases .
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- HY-170316
-
|
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Ras
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Cancer
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Ibetazol is a Importin β1 (KPNB1) inhibitor and nucleocytoplasmic transport disruptor. Ibetazol binds covalently to Cys585 of Importin β1, blocks both Importin β1-mediated direct transport and Importin α-dependent nuclear import processes, without affecting transport mediated by other nucleocytoplasmic transport proteins. Ibetazol induces cytoplasmic accumulation of Importin α1, and inhibits nuclear import of substrates carrying nuclear localization signals (NLS), including the NLS-cMyc reporter gene, RelA/p65 and SREBP1. Ibetazol triggers spindle malformation and chromosome misalignment by disrupting the mitotic function of Importin β1. Ibetazol inhibits the proliferation of cells expressing wild-type Importin β1. Ibetazol has a high activity-cytotoxicity window, lacks intrinsic fluorescence, and acts rapidly on nucleocytoplasmic transport processes. Ibetazol serves as a tool compound for investigating nuclear import processes specifically mediated by Importin β1 .
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- HY-W013403S
-
|
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IFNAR
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Infection
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|
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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- HY-164392
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EGFR
Apoptosis
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Cancer
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TAS-121 is an orally active, selective, covalent, third-generation mutant EGFR-tyrosine kinase inhibitor (EGFR-TKI). TAS-121 inhibits the L858R mutation (IC50=1.7 nM), Ex19del mutation (IC50=2.7 nM), L858R/T790M mutation (IC50=0.56 nM) and Ex19del/T790M mutation (IC50=1.1 nM) and wild-type EGFR (IC50=8.2 nM). TAS-121 inhibits HER2 and HER4 with IC50s of 110 and 2.6 nM, respectively. TAS-121 inhibits phosphorylation of EGFR and its downstream signaling targets to block cell proliferation. TAS-121 induces apoptosis and displays antitumor activity in SW48 (EGFR G719S) and NCI-H1975 (EGFR L858R/T790M) xenograft models .
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- HY-153803
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|
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PROTACs
Molecular Glues
Btk
|
Cancer
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GBD-9 is a degrader based on the E3 ubiquitin ligase CRBN that targets BTK and the G1 to S phase transition protein GSPT1. GBD-9 has both PROTAC and molecular glue properties by inducing ubiquitination and proteasomal degradation of target proteins. GBD-9 can efficiently degrade wild-type and mutant BTK (such as C481S mutation) and GSPT1. GBD-9 significantly inhibits tumor cell proliferation by inducing G1 phase arrest in cancer cells, downregulating anti-apoptotic proteins (BCL-2, MCL-1) and activating Caspase-3 to induce apoptosis. GBD-9 is mainly used in the research of hematological tumors such as diffuse large B-cell lymphoma (DLBCL) and acute myeloid leukemia (AML) .
GBD-9 is composed of E3 ubiquitin ligase ligand (pink part) 5-Aminothalidomide (HY-W023573), target protein ligand (blue part) Btk Inhibitor: IBT6A (HY-13036A), and PROTAC linker (black part) Nonanoic acid (HY-N7057).
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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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- HY-121708
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c-Kit
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Cancer
|
|
KI-328 is a novel inhibitor targeting KIT kinase that has selective activity against some KIT mutant kinases commonly found in acute myeloid leukemia (AML). KI-328 showed specificity for KIT kinase in in vitro kinase assays and inhibited the growth of wild-type (Wt) and mutant KIT-expressing cells, but had lower activity against D816V-KIT. Comparative analysis of the inhibitory effects of several potent KIT inhibitors on the growth of multiple mutant KIT-expressing cells showed that the multi-kinase inhibitors had comparable activity against D816V-KIT as against other mutant KITs; however, heat shock protein 90 (HSP90) inhibitors showed significant activity against D816V-KIT, inhibiting the growth of D816V-KIT-expressing cells at concentrations that did not affect the growth of other mutant KIT-expressing cells. These results suggest that potent KIT inhibitors have different activities against different types of KIT mutant kinases. Therefore, in clinical development, KIT inhibitors need to validate their activity against multiple types of KIT mutant kinases.
|
-
- HY-171906A
-
|
1-Arachidonoyl-sn-glycerol 3-phosphate sodium; 1-Arachidonoyl LPA sodium; LPA (20:4) sodium
|
LPL Receptor
|
Cancer
|
|
1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) (1-Arachidonoyl-sn-glycerol 3-phosphate (sodium)) is a phospholipid with arachifonic acid at the sn-1 position. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) binds to the LPA2/EDG4 receptor (EC50 of 10 nM). 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can be found in rat brain as 37% of the arachidoinic acid-containing lysophosphatidic acid species. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) is the precursor to 1-arachidonoyl glycerol. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) can prevent TNF-α and IL-6 secretion in wild type LPS-stimulated dendritic cells. 1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA (sodium) reduces differentiation of HT-29 colon carcinoma cells into goblet cells when sodium butyrate is present .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-19980G
-
|
APR-246; PRIMA-1Met
|
Fluorescent Dye
|
|
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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-12879G
-
|
|
Fluorescent Dye
|
|
IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure .
|
-
- HY-D1737
-
|
|
Fluorescent Dye
|
|
RADA is a fluorescent D-amino acid (FDAA) with high photostability and thermostability, which emits yellow-to-orange fluorescence. RADA shows low outer membrane permeability in wild-type Gram-negative Escherichia coli, but it targets penicillin-binding proteins and L,D-transpeptidases, mimics the interaction between acyl acceptors and enzyme intermediates, and integrates into peptidoglycan during biosynthesis. As a peptidoglycan labeling reagent, RADA metabolically integrates into the nascent peptidoglycan of live bacterial cells, labels the peptidoglycan at the poles and lateral walls of mycobacteria, and enables visualization of peptidoglycan synthesis and remodeling processes. RADA serves as a non-specific stain for fixed cells, is non-toxic to bacterial cells, and its red-shifted excitation/emission spectra reduce phototoxicity. RADA also supports virtual pulse-chase labeling experiments and stochastic optical reconstruction microscopy for sub-diffraction-limited imaging of bacterial cell walls .
|
| Cat. No. |
Product Name |
Type |
-
- HY-NP006
-
|
SPA
|
Biochemical Assay Reagents
|
|
Protein A (SPA) is an immunoglobulin (Ig)-binding protein that exists on the bacterial surface and can be freely secreted into the extracellular environment. Protein A blocks opsonophagocytosis and induces B cell apoptosis in vitro by binding to the Fc region of antibodies and the Fab region of B cell receptors. Protein A can form toxic immune complexes with IgG, thereby inducing leukocyte necrosis. Protein A contributes to the virulence expression of Staphylococcus aureus. Protein A triggers allergic reactions in IgG-pretreated mouse models. Protein A can be used in studies related to immune system diseases .
|
-
- HY-145411
-
|
|
Biochemical Assay Reagents
|
|
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-134421
-
|
|
Biochemical Assay Reagents
|
|
2-Butenoyl coenzyme A lithium is an inactivator and a substrate of Plasmodium falciparum enoyl-β-hydroxyacyl-acyl carrier protein (ACP) reductase and other enoyl-CoA reductases, and it is also the lithium salt of trans-2-methyl-2-butenoyl coenzyme A. 2-Butenoyl coenzyme A lithium acts on short-chain and medium-chain coenzyme A dehydrogenases as well as glutaryl-CoA dehydrogenase, and shows no activity against wild-type isovaleryl-CoA dehydrogenase. 2-Butenoyl coenzyme A lithium functions as a metabolite in the L-isoleucine catabolic pathway, and can serve as a substrate in the activity assay of 3-ketothiolase. 2-Butenoyl coenzyme A lithium is applicable to research related to 3-ketothiolase deficiency .
|
-
- 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.
|
-
- HY-59320
-
|
|
Biochemical Assay Reagents
|
|
4-Thiazolecarboxylic acid (Compound 1e) is an intermediate. 4-Thiazolecarboxylic acid can be used in the synthesis of MGL-IN-2 (HY-177534). MGL-IN-2 inhibits wild-type MGL enzyme activity with an IC50 of 0.0121 μM. 4-Thiazolecarboxylic acid can be used in the research of metabolic diseases .
|
-
- HY-19980G
-
|
APR-246; PRIMA-1Met
|
Biochemical Assay Reagents
|
|
Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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-12879G
-
|
|
Biochemical Assay Reagents
|
|
IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3485
-
-
- HY-P3487
-
-
- HY-P2265A
-
|
|
SOS1
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-P2319A
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide TFA, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P11005
-
|
|
Dynamin
ATP Synthase
|
Neurological Disease
|
|
P259 is a Drp1-Mff inhibitor. P259 distinguishes physiological from pathological fission by specifically inhibiting Drp1-Mff interaction. P259 elongates cell mitochondria and disrupts mitochondrial function and motility. P259 reduces ATP levels and alters mitochondrial structure in the brain, resulting in behavioral deficits in wild-type mice and a short lifespan in Huntington's disease (HD) mice model .
|
-
- HY-P10436
-
|
|
Raf
|
Cancer
|
|
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence. Braftide can be used for cancer research .
|
-
- HY-P5437
-
|
|
PKC
|
Others
|
|
PKCε (85-92) is a biological active peptide. (This peptide is the e-PKC specific activator, it also activates MARCKS phosphorylation in wild type cells, and has no effect on MARCKS phosphorylation in the cells derived from knockout mice.)
|
-
- HY-P1088
-
|
|
PKC
|
Others
|
|
[Ser25] Protein Kinase C (19-31) is a substrate of protein kinase C (PKC) (Km: 0.3 μM). [Ser25] Protein Kinase C (19-31) is derived from the pseudo-substrate regulatory domain of PKCα (19-31) with a Serine at position 25 replacing the wild-type Alanine .
|
-
- HY-P11003
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
PTD-N5-1 (N5-1) is an IRF5 inhibitory peptide. PTD-N5-1 blocks β-glucan-induced IL-12 production in IFN-γ primed wild-type and Clec2d-difecient bone-marrow-derived dendritic cells (BMDCs). PTD-N5-1 regulates antifungal immunity through suppression of IRF5-mediated IL-12 production .
|
-
- HY-P2265
-
|
|
SOS1
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-P4525
-
|
|
Peptides
|
Others
|
|
Ala-Ala-Ala-Ala is a poly-L-alanine (PLA) sequences. PLA is a kind of key element of the crystalline domains of spider dragline and wild silkworm silks .
|
-
- HY-P4391
-
-
- HY-W794670
-
|
|
Aminopeptidase
|
Others
|
|
H-Ala-Pro-Ala-OH, tripeptide, is a substrate for Escherichia coli PepP (Xaa-Pro aminopeptidase). H-Ala-Pro-Ala-OH acts as a nitrogen source for wild-type Escherichia coli .
|
-
- HY-P2360
-
|
Ras 5-17
|
Ras
|
Others
|
|
G12 (Ras 5-17) is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 can be used as a control of mutant Ras peptides studies (such V12) .
|
-
- HY-P2319
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
OVA-E1 peptide, is an antagonist variant of SIINFEKL [OVA (257-264). OVA-E1 peptide, activates the p38 and JNK cascades similarly in mutant and wild-type thymocytes .
|
-
- HY-P4926
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research .
|
-
- HY-P2466
-
|
|
Apoptosis
|
Cancer
|
|
Bax BH3 peptide (55-74), wild type is a 20-amino acid Bax BH3 peptide (Bax 1) capable of inducing apoptosis in a variety of cell line models .
|
-
- HY-142953
-
-
- HY-P2360A
-
|
Ras 5-17 TFA
|
Ras
|
Others
|
|
G12 (Ras 5-17) TFA is a wild-type Ras peptide consisted of amino acids 5-17 (KLVVVGAGGVGKS). G12 TFA can be used as a control of mutant Ras peptides studies (such V12) .
|
-
- HY-P10596
-
|
|
Bacterial
Fungal
|
Infection
Cancer
|
|
Lasioglossin-III is an antimicrobial peptide that can be isolated from the venom of wild bees. Lasioglossin-III has high antibacterial activity against Gram-positive and Gram-negative bacteria, antifungal activity and antitumor activity. Lasioglossin-III has certain cytotoxicity against three cancer cell lines (HeLa S3, CRC SW 480 and CCRF-CEM T) with IC50 values of 4, 18 and 5 μM, respectively .
|
-
- HY-P11109
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
RL-37 is an alpha-helical antimicrobial peptide. RL-37 can be isolated for rhesus monkey bone marrow. RL-37 rapidly permeabilizes the membranes of Escherichia coli ML-35p and lysed liposomes. RL-37 has effective antibacterial activity against staphylococci, such as wild-type and Methicillin (HY-121544)-resistant S. aureus strains and S. epidermidis ATCC 49741. RL-37 can be used for human skin infections research .
|
-
- HY-P11092
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
TLQP-62 (mouse,rat) is a secreted C-terminal peptide that can be derived from protein VGF. TLQP-62 activates the BDNF-TrkB signaling pathway, inducing acute, transient phosphorylation of TrkB receptor and downstream CREB (Ser133) phosphorylation. TLQP-62 demonstrates excellent efficacy in promoting long-term fear memory formationin wild-type mice and reversing memory impairment in VGF heterozygous knock-out mice. TLQP-62 can be used for the study of memory-related neurological disorders (e.g., Alzheimer’s disease, frontotemporal dementia) .
|
-
- HY-P11075
-
|
|
Neurokinin Receptor
|
Metabolic Disease
|
|
[Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) (ID 305) is a selective NK2R agonist with an EC50 of 3.7 nM for hNK2R. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) significantly inhibits weight loss in diet-induced obese (DIO) mice model and improves Loperamide (HY-156131)-induced dysfunctional voiding in wild-type mice. [Lys5,Tyr6,mLeu9,Nle10]-Neurokinin A (4-10) can be used for neurokinin receptor mediated disorders, such as obesity, insulin resistance and type 2 diabetes research .
|
-
- HY-P11465
-
|
|
Fungal
|
Infection
|
|
Histone H3 (73-83) is a histone H3 fragment. Histone H3 (73-83) can be obtained from incomplete tryptic digestion of underivatized wild-type histone H3. Histone H3 (73-83) can be used in the research of yeast infection .
|
-
- HY-P11829
-
|
|
Histone Acetyltransferase
|
Cancer
|
|
ACTR-AD1 2L is a ACTR-AD1 peptide. ACTR-AD1 2L inhibits CBP/p300-NCOA3 complex formation, modulates gene transcription, inhibits CBP/p300 acetylase activity, reduces acetylation levels, and exhibits antiproliferative activity. ACTR-AD1 2L binds with stronger affinity to its target proteins than the wild-type peptide. ACTR-AD1 2L can be used for the research of breast cancer .
|
-
- HY-P10989
-
|
|
Peptides
|
Cancer
|
|
NG2 binding peptide is a short peptide that specifically recognizes NG2 proteoglycan and can be obtained by phage screening technology. NG2 binding peptide interacts with NG2 binding sites to achieve precise targeting of tumor angiogenesis in vitro and in vivo. NG2 binding peptide exhibits significant homing ability in wild-type tumor-bearing mice, but has no localization effect in NG2 knockout mice. Due to the tissue specificity of NG2 expression, NG2 binding peptide can be used in scenarios such as tumor targeted therapy, drug delivery, and molecular imaging diagnosis .
|
-
- HY-KE8011
-
|
|
|
Phi29 DNA polymerase is a protein-engineered Phi29 DNA polymerase expressed in E. coli and then purified and isolated multiple times. Compared with wild-type Phi29 DNA polymerase, it has higher amplification efficiency and sensitivity, and can greatly shorten the reaction time.
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- 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 .
|
-
(5)
-
- 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) .
|
-
(5)
-
- HY-P99950
-
|
ALX148
|
CD47
|
|
|
Evorpacept (ALX148) is a high-affinity CD47-blocking fusion protein with an inactive human immunoglobulin Fc region. Evorpacept binds to CD47, blocks the interaction of the CD47-SIRPα immune checkpoint, and inhibits the binding of wild-type SIRPα to CD47. Evorpacept is applicable to research related to acute myeloid leukemia .
|
-
(5)
-
- HY-P990282
-
|
|
Transmembrane Glycoprotein
|
Cancer
|
|
Anti-Mouse CD24 Antibody (M1/69) is a rat-derived anti-mouse CD24 IgG2b κ type antibody inhibitor. Anti-Mouse CD24 Antibody reduces heat stable antigen (HSA) expression level and delays wound healing in Wild-type HSA +/+ mice .
|
-
(5)
-
- HY-P991221
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
ALD1613 is a potent neutralizing monoclonal antibody against adrenocorticotropic hormone (ACTH). ALD1613 neutralizes ACTH-induced signaling and inhibits ACTH-induced cyclic AMP accumulation in a mouse adrenal cell line (Y1) via all five melanocortin receptors. ALD1613 significantly reduces plasma corticosterone levels in wild-type rats. ALD1613 can be used in the study of diseases associated with elevated ACTH levels .
|
-
(5)
-
- HY-P991571
-
|
GC-1118A
|
EGFR
PERK
Akt
|
Cancer
|
|
GC1118 (GC-1118A) is a fully human anti-EGFR monoclonal antibody with binding affinity of 0.16 nM (KD) to EGFR. GC1118 displays potent inhibitory effects on high- and low-affinity EGFR ligand-induced signaling. GC1118 shows potent anti proliferative activity in KRAS wild-type and KRAS mutant cells. GC1118 can reach the tumor by crossing both BBB (blood-brain barrier) and BTB (brain-tumor barrier) and shows superior anti-tumor effects in various mice xenograft models. GC1118 can be used for the researches of cancer, such as colorectal cancer .
|
-
(5)
-
- HY-P99715
-
|
|
EGFR
|
Cancer
|
|
Losatuxizumab 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 .
|
-
(5)
-
- HY-P991641
-
|
LY3012218
|
FLT3
p38 MAPK
STAT
PI3K
Akt
|
Cancer
|
|
IMC-EB10 (LY3012218) is an anti-FLT3 monoclonal antibody. IMC-EB10 binds to FLT3 with high affinity (Kd = 158 pM) and blocks the binding of FLT3 ligand to FLT3 (IC50 ≈ 10 nM), thereby inhibiting MAPK, STAT5, and PI3K/Akt signaling in leukemia cells. IMC-EB10 can enhance the anti-leukemic effect of Methotrexate (HY-14519) and inhibit leukemias expressing wild-type or ITD-mutated FLT3 receptors. IMC-EB10 prolongs the survival of acute lymphoblastic leukemia (ALL) cells and primary leukemia samples and reduces engraftment in non-obese diabetic/severe combined immunodeficiency patients. IMC-EB10 is indicated for leukemia research .
|
-
(5)
-
- HY-P991507
-
|
|
EGFR
|
Cancer
|
|
SCT200 is a fully humanized IgG1 anti-EGFR monoclonal antibody with a Kd of 0.08 nM. SCT200 can kill tumor cells by complement-dependent cytotoxicity (CDC) and antibody-dependent cellular cytotoxicity (ADCC) through the Fc. SCT200 can be used for the study of refractory RAS and BRAF wild-type metastatic colorectal cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-10572
-
-
-
- HY-B0255
-
-
-
- HY-W005288
-
-
-
- HY-134421
-
|
|
Human Gut Microbiota Metabolites
Microorganisms
Endogenous metabolite
Source Classification
|
HMG-CoA Reductase (HMGCR)
|
|
2-Butenoyl coenzyme A lithium is an inactivator and a substrate of Plasmodium falciparum enoyl-β-hydroxyacyl-acyl carrier protein (ACP) reductase and other enoyl-CoA reductases, and it is also the lithium salt of trans-2-methyl-2-butenoyl coenzyme A. 2-Butenoyl coenzyme A lithium acts on short-chain and medium-chain coenzyme A dehydrogenases as well as glutaryl-CoA dehydrogenase, and shows no activity against wild-type isovaleryl-CoA dehydrogenase. 2-Butenoyl coenzyme A lithium functions as a metabolite in the L-isoleucine catabolic pathway, and can serve as a substrate in the activity assay of 3-ketothiolase. 2-Butenoyl coenzyme A lithium is applicable to research related to 3-ketothiolase deficiency .
|
-
-
- HY-N3354
-
-
-
- HY-N0475
-
-
-
- HY-W009811
-
-
-
- HY-N5109
-
-
-
- HY-N7433
-
-
-
- HY-N0308
-
-
-
- HY-N5005
-
-
-
- HY-N12281
-
|
|
Quinones
Structural Classification
Leguminosae
Anthraquinones
Plants
Senna alexandrina Milll
Source Classification
|
Apoptosis
MDM-2/p53
PAK
Calcium Channel
|
|
Sennoside is an orally active apoptosis inducer and stimulant laxative, found in Senna (Cassia angustifolia). Sennoside induces overexpression of wild-type p53 and p21/WAF as part of pathways mediating colonic epithelial cell apoptosis. Sennoside stimulates colonic peristalsis, reverses net water, sodium, chloride absorption to secretion and enhances potassium and calcium secretion. Sennoside increases paracellular permeability to small molecules, accelerates colon transit and softens fecal pellets. Sennoside can be used for the research of constipation, melanosis coli, and colorectal cancer .
|
-
-
- HY-10572R
-
-
-
- HY-N16422
-
|
|
Microorganisms
Terpenoids
Sesquiterpenes
Source Classification
|
HIV
HIV Protease
|
|
Mer-NF5003E is a non-nucleoside reverse transcriptase inhibitor targeting HIV-1 reverse transcriptase (RT) (EC50=50 μM). Mer-NF5003E exhibits inhibitory activity against wild-type HIV-1 and multiple NNRTI-resistant strains (e.g., K103N, Y181C). Mer-NF5003E is promising for research of HIV infections .
|
-
-
- HY-B0255R
-
-
-
- HY-N0308R
-
-
-
- HY-N12533
-
-
-
- HY-N12005
-
-
-
- HY-N2894
-
-
-
- HY-N3113
-
-
-
- HY-N12399
-
-
-
- HY-N7433R
-
-
-
- HY-N9022
-
-
-
- HY-146364
-
-
-
- HY-N0475R
-
|
Hypolide (Standard); (+)-Triptophenolide (Standard)
|
Structural Classification
Monophenols
Terpenoids
Celastraceae
Phenols
Diterpenoids
Tripterygium wilfordii Hook. f.
Plants
Source Classification
|
Reference Standards
Androgen Receptor
Pyroptosis
Caspase
Bcl-2 Family
Apoptosis
|
|
Triptophenolide (Standard) (Hypolide) is the analytical standard of Triptophenolide (HY-N0475). This product is intended for research and analytical applications. Triptophenolide is a colorless crystal isolated from the ethyl acetate extract of Tripterygium wilfordii. Triptophenolide is an orally active pan‑antagonist of the androgen receptor (AR) with an IC50 of 467 nM against human wild‑type AR. Triptophenolide reduces AR expression, inhibits AR nuclear translocation, downregulates prostate‑specific antigen mRNA levels, and suppresses the growth of AR‑positive prostate cancer cells. Triptophenolide shows anti-tumor effects against breast cancer by inhibiting cell proliferation and migration, inducing G1-phase arrest and apoptosis, repressing xenograft tumor growth. Triptophenolide inhibits pyroptosis, alleviates tissue inflammation, and ameliorates synovial injury. Triptophenolide can be used for the study of prostate cancer, rheumatoid arthritis and breast cancer .
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- HY-N18657
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Structural Classification
Extract
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Others
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Wild Yam Extract is derived from the dried tubers of Dioscorea oppositae thunb. It has the functions of invigorating the spleen, tonifying the lungs, strengthening the kidney, and replenishing vital essence.
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- HY-N18364
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- HY-W009811R
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- HY-N0055A
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- HY-N17966
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- HY-114625
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Structural Classification
Human Gut Microbiota Metabolites
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
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Parasite
Mitochondrial Metabolism
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Amquinate is a coccidiostat and a cytochrome b inhibitor. Amquinate blocks cytochrome-mediated electron transport near cytochrome b in mitochondria, acting downstream of coenzyme Q without affecting succinate dehydrogenase or NADH dehydrogenase. Amquinate inhibits succinate- and malate plus pyruvate-supported mitochondrial respiration in Eimeria tenella and does not affect L-ascorbate-supported respiration or any mitochondrial respiration in chicken liver mitochondria. Amquinate exhibits selective anticoccidial activity against wild-type Eimeria tenella. Amquinate can be used for the research of coccidiosis (Eimeria tenella infection) .
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- HY-W099725
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Piper longum Linn.
Structural Classification
Alkaloids
Pyrrole Alkaloids
Piperaceae
Plants
Source Classification
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Herbicide
Photosystem II
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Sarmentine is a broad-spectrum contact herbicide and PSII inhibitor, with an IC50 of 3.0 μM and a Ki of 1.5 μM against spinach, an IC50 of 1.72 μM against wild-type Amaranthus retroflexus, and an IC50 of 0.97 μM against triazine-resistant Amaranthus retroflexus. Sarmentine competitively binds to the QB binding site of plastoquinone on PSII, thereby blocking photosynthetic electron transport. Sarmentine inhibits enoyl-ACP reductase in Arabidopsis thaliana by targeting the early fatty acid synthesis process, with an IC50 of 18.3 μM. Sarmentine induces light-independent loss of plasma membrane integrity and electrolyte leakage. Sarmentine also exhibits antiplasmodial, antimycobacterial, antituberculous, and antiplatelet aggregation activities .
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- HY-N18649
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Structural Classification
Extract
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Others
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Rosa canina extract, derived from the wild rose (often known as rose hip), is rich in vitamin C, flavonoids, carotenoids, and essential fatty acids, contributing to its numerous health benefits. The extract is primarily known for its anti-inflammatory, antioxidant, and immune-boosting properties. Rosa canina extract is commonly used to boost the immune system, particularly during cold and flu seasons, due to its high vitamin C content. It also has joint health benefits, as it helps reduce inflammation and pain in conditions like arthritis. The extract's antioxidant properties help protect cells from oxidative stress and may contribute to skin health by promoting collagen synthesis, reducing the appearance of wrinkles, and supporting overall skin elasticity.
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0413S
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5 Publications Verification
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Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole-d3 is a HIF-1α agonist and activates the HIF-1α-related GLUT1 pathway. Fenbendazole is an orally active benzimidazole anthelmintic agent, with a broad antiparasitic range. Fenbendazole is a microtubule destabilizing agent. Fenbendazole causes cell-cycle arrest and mitotic cell death, and has antitumor activity in mice xenografted with wild-type p53 .
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- HY-16305S
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Maribavir-d6 (1263W94-d6) is a deuterium labeled Maribavir (HY-16305). Maribavir is a potent inhibitor of histone phosphorylation catalyzed by wild-type pUL97 in vitro, with an IC50 of 3 nM .
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- HY-176785S
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MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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- HY-16767S1
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Doravirine-13C,d3 (MK-1439-13C,d3) is the deuterium labeled Doravirine (HY-16767). Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 4.5 nM, 5.5 nM and 6.1 nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively .
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- HY-16985S
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Darolutamide-d4 (ODM-201-d4) is deuterium labeled Darolutamide (HY-16985). Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist, with a Ki of 11 nM for rat wild-type AR (wtAR) and an IC50 of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation . Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation . Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants . Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer .
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- HY-W005288S
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4-Vinylphenol-d4 is deuterated labeled 4-Vinylphenol (HY-W005288). 4-Vinylphenol is found in the medicinal herb Hedyotis diffusa Willd, wild rice and is also the metabolite of p-coumaric and ferulic acid by lactic acid bacteria in wine. 4-Vinylphenol induces apoptosis and inhibits blood vessels formation and suppresses invasive breast tumor growth in vivo .
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- HY-16379S
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Pacritinib-d8 (SB1518-d8) is the deuterium labeled Pacritinib (HY-16379). 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).
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- HY-10572S1
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Efavirenz- 13C6 is the 13C-labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture .
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- HY-14852S
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Tafamidis-d3 is deuterium labeled Tafamidis. Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis .
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- HY-10574S
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Rilpivirine-d6 is the deuterium labeled Rilpivirine. Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV .
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- HY-10572S
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Efavirenz-d5 (DMP 266-d5) is the deuterium labeled Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture . 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-14588S1
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Lopinavir-d8 (ABT-378-d8) is the deuterium labeled Lopinavir. Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 14.2 μM .
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- HY-51424S
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PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of?B-RafV600E?with?an IC50?of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf .
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- HY-B1902S
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Diaveridine-d6 (EGIS-5645-d6) is deuterium labeled Diaveridine. Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent .
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- HY-136450S
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Triclabendazole sulfoxide-d3 is the deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
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- HY-136450S1
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Triclabendazole sulfoxide- 13C,d3 is the 13C- and deuterium labeled Triclabendazole sulfoxide. Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
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- HY-W704348
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Diphenyltin Dichloride-d10 is the deuterium labeled NSC405640 (HY-144105). 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-W708304
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Asulam-d3 is the deuterium labeled Asulam (HY-B1838). Asulam is a herbicide with control activity against wild oats. Asulam can be used for bulb production in spinach, tulips, daffodils and lilies. Maximum residue limits (MRLs) for Asulam were evaluated in spinach. The review of Asulam took into account its endocrine disrupting properties .
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- HY-10572BS
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(Rac)-Efavirenz-d4 is a labelled racemic Efavirenz. Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture . (Rac)-Efavirenz-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-124089S
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Eicosapentaenoyl ethanolamide-d4 is the deuterium labeled Eicosapentaenoyl ethanolamide. Eicosapentaenoyl ethanolamide, an omega-3 fatty acid, is one of N-acylethanolamines (NAEs). Eicosapentaenoyl ethanolamide is cannabinoid CB1/CB2 receptor agonist. Eicosapentaenoyl ethanolamide acts as a metabolic signal. Eicosapentaenoyl ethanolamide inhibits dietary restriction (DR)-induced lifespan extension in wild type animals and suppresses lifespan extension in a TOR pathway mutant .
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- HY-10574S1
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Rilpivirine- 13C6 (R278474- 13C6) is 13C 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 .
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- HY-14588S2
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Lopinavir-d7 is deuterated labeled Lopinavir (HY-14588). Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
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- HY-14588S
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(rel)-Lopinavir-d8 ((rel)-ABT-378-d8) is the deuterium labeled Lopinavir (HY-14588) . Lopinavir (ABT-378) is a highly potent, selective peptidomimetic inhibitor of the HIV-1 protease, with Kis of 1.3 to 3.6 pM for wild-type and mutant HIV protease. Lopinavir acts by arresting maturation of HIV-1 thereby blocking its infectivity . Lopinavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 14.2 μM .
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- HY-W778649
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Sarmentine-d8 is the deuterium labeled Sarmentine. Sarmentine is a broad-spectrum contact herbicide and PSII inhibitor, with an IC50 of 3.0 μM and a Ki of 1.5 μM against spinach, an IC50 of 1.72 μM against wild-type Amaranthus retroflexus, and an IC50 of 0.97 μM against triazine-resistant Amaranthus retroflexus. Sarmentine competitively binds to the QB binding site of plastoquinone on PSII, thereby blocking photosynthetic electron transport. Sarmentine inhibits enoyl-ACP reductase in Arabidopsis thaliana by targeting the early fatty acid synthesis process, with an IC50 of 18.3 μM. Sarmentine induces light-independent loss of plasma membrane integrity and electrolyte leakage. Sarmentine also exhibits antiplasmodial, antimycobacterial, antituberculous, and antiplatelet aggregation activities .
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- HY-172733S
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PRMT5-MTA-IN-3-d3 (compound P22) is the deuterium labeled PRMT5-MTA-IN-3 (HY-172733). PRMT5-MTA-IN-3-d3 is an orally active PRMT5-MTA inhibitor. PRMT5-MTA-IN-3-d3 has antiproliferative effects on HTC116-MTAP del and wild type colorectal cancer HCT-116 cell lines, with IC50 values of 6 nM and 961 nM, respectively. PRMT5-MTA-IN-3-d3 has anticancer effects, especially for MTAP-deficient tumors, such as non-small cell lung cancer (NSCLC), pancreatic cancer .
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- HY-W013403S
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2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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- HY-19337S1
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Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-19337S
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Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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Optimized version of product available:
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| Cat. No. |
Product Name |
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Classification |
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- HY-134813
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-176786
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Alkynes
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MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader without affecting KRAS transcription. MCB-36 exhibits minimal effects on HRAS and NRAS protein levels. MCB-36 binds to the GDP-loaded state of G12D, G12C, G12V, and wild-type KRAS with high affinities Kd ≈ 1 pM). MCB-36 decreases p-ERK levels, leading to cell apoptosis. MCB-36 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-36 can be used for the study of colorectal cancer and lung cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-112078); Black: Linker (HY-W091879)) .
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- HY-176785S
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Alkynes
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MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRAS G12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer .
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- HY-164694
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TAS3351
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Alkynes
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Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively .
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- HY-152233
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Azide
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Reverse transcriptase-IN-4 (compound F10) is a potent and selective non-nucleoside reverse transcriptase (NNRT) inhibitor with an EC50 value of 0.053 μM for wild-type HIV-1 and an EC50 value of 0.26 μM for HIV-1 mutant E138K . Reverse transcriptase-IN-4 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-167690
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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- HY-153605
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PROTAC Synthesis
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EGFR-IN-77 (Compound 4a) is a selective EGFR T790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFR T790M/L858R, 0.477 μM against EGFR L858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFR T790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFR L858R/T790M double-mutant non-small cell lung cancer .
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| Cat. No. |
Product Name |
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Classification |
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- HY-132609
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siRNAs
siRNA drugs
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Patisiran sodium is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran sodium specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran sodium can be used for the research of hereditary TTR amyloidosis .
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- HY-145411
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Pegylated Lipids
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PEG2000-C-DMG, a pegylated lipid, can be used for the preparation of Onpattro. Onpattro, a hepatically directed investigational RNAi therapeutic agent, harnesses this process to reduce the production of mutant and wild-type transthyretin by targeting the 3′ untranslated region of transthyretin mRNA .
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- HY-148089
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Antisense Oligonucleotides
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Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases .
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- HY-112974
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GSK-2998728; ISIS-420915
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Antisense Oligonucleotides
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Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy .
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- HY-148089A
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Antisense Oligonucleotides
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Eplontersen sodium the sodium salt form of Eplontersen (HY-148089). Eplontersen sodium is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases .
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- HY-153609
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siRNAs
siRNA drugs
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AS-Patisiran sodium is an antisense strand of Patisiran. Patisiran is a double-stranded small interfering RNA that targets a sequence within the transthyretin (TTR) messenger RNA. Patisiran specifically inhibits hepatic synthesis of mutant and wild-type TTR. Patisiran can be used for the research of hereditary TTR amyloidosis .
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- HY-177650
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ALN-TTRsc04
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siRNAs
siRNA drugs
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Nucresiran is a siRNA that inhibits hepatic synthesis of both wild-type and variant TTR mRNA.
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- HY-158987
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APBADP
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Nucleotide Analogs
Adenine Nucleotide
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Adenosine phosphonobutyric, 2'(3'), 5'-diposphate (APBADP) is an adenylosuccinate lyase substrate analog and competitive inhibitor. Adenosine phosphonobutyric, 2'(3'), 5'-diposphate binds to the tetramers of *Bacillus subtilis* adenylosuccinate lyase and wild-type human adenylosuccinate lyase. Adenosine phosphonobutyric, 2'(3'), 5'-diposphate can be used for research on adenylosuccinate lyase deficiency .
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- HY-111627
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Nucleoside Analogs
Guanosine
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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-109014
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CMX-157
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Phospholipids
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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 .
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- HY-177650A
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ALN-TTRsc04 sodium
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siRNAs
siRNA drugs
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Nucresiran sodium is a siRNA that inhibits hepatic synthesis of both wild-type and variant TTR mRNA.
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- HY-174499
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mRNA
Gene Editing
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Cas9 Nickase D10A mRNA expresses a version of the Streptococcus pyogenes SF370 Cas9 protein (CRISPR Associated Protein 9) that contains a D10A amino acid substitution. This mRNA also contains a C-terminal nuclear localization signal followed by a HA tag.Cas9 functions as part of the CRISPR (clustered regularly interspaced short palindromic repeats) genome editing system. In the CRISPR system, an RNA guide sequence targets the site of interest and the Cas9 protein is employed to perform the DNA cleavage. While wild-type Cas9 creates a double-stranded break at the target site, Cas9 nickase creates a single-stranded break. This favors homology-directed repair and decreases the occurrence of non-homologous end joining.
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- HY-177375
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saRNAs
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dsP53-285 saRNA is a small activating RNA (saRNA) that readily activates wild-type p53 expression by targeting its promoter. dsP53-285 saRNA suppresses bladder cancer cells growth and metastasis .
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-19980G
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APR-246; PRIMA-1Met
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MDM-2/p53
Apoptosis
Autophagy
Ferroptosis
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Cancer
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Eprenetapopt (GMP) (APR-246(GMP)) is Eprenetapopt (HY-19980) in GMP grade. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. 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 .
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- HY-12879G
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Wnt
Casein Kinase
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Cardiovascular Disease
Neurological Disease
Cancer
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IWP-4 (GMP) is the GMP-grade form of IWP-4 (HY-12879). IWP-4 is a Wnt inhibitor with an IC50 of 25 nM. IWP-4 specifically inhibits casein kinase 1δ/ε (CK1δ/ε), with an IC50 of 1.06 μM against wild-type CK1δ, 1.02 μM against the CK1δ kinase domain, and 7.07 μM against CK1ε; it shows enhanced inhibitory activity against the M82F CK1δ mutant (IC50 = 0.14 μM). IWP-4 is applicable to research related to cancer, Alzheimer's disease (AD), and heart failure .
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