Search Result
Results for "
Bax Inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
3
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P0081
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BIP-V5; Bax Inhibiting Peptide V5
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Bcl-2 Family
Apoptosis
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Cancer
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Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
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- HY-110031
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Apoptosis
Bcl-2 Family
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Cancer
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BAI1 hydrochloride is a selective apoptosis factor BAX allosteric inhibitors. BAI1 hydrochloride binds BAX and allosterically inhibits its activation. BAI1 hydrochloride has the potential to be used in the study of BAX dependent cell death-mediated diseases .
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- HY-120035
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Proteasome
Ribosomal S6 Kinase (RSK)
Apoptosis
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Cancer
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DD1, a proteasome inhibitor, targets Bax activation and P70S6K degradation during acute myeloid leukemia (AML) apoptosis. DD1 induces apoptosis in the caspase-dependent manner. DD1 induces mitochondrial membrane depolarization and Bad dephosphorylation .
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- HY-103269
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Bcl-2 Family
Apoptosis
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Cancer
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BAI1 is a selective and allosteric inhibitor of BAX, an apoptosis regulator. BAI1 directly binds to BAX and allosterically inhibits BAX activation. BAI1 has the potential for the research of diseases mediated by BAX-dependent cell death .
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- HY-161242A
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Bcl-2 Family
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Cancer
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CBI1 formic is a covalent BAX inhibitor. CBI1 formic selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 formic blocks t-2-hex lipidation and oligomerization of BAX. CBI1 formic inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
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- HY-157176
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Bcl-2 Family
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Others
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BAX-IN-1 is a potential, selective inhibitor of Bcl-2-associated X protein (BAX).
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- HY-103271
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Bcl-2 Family
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Cancer
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Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro .
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- HY-117136
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HDAC
Caspase
Bcl-2 Family
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Cancer
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AN-7 is an orally active histone deacetylase (HDAC) inhibitor that induces histone hyperacetylation and differentiation in vitro and in vivo, and inhibits the proliferation of human prostate 22Rv1 cancer cells. AN-7 can increase the expression of the pro-apoptotic protein Bax, reduce the expression of the anti-apoptotic protein Bcl-2, and promote apoptosis by activating caspase-3, and can be used in the study of prostate cancer .
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- HY-161242
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Bcl-2 Family
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Cancer
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CBI1 is a covalent BAX inhibitor. CBI1 selectively derivatizes BAX at C126 and inhibits BAX activation by triggering ligands or point mutagenesis. CBI1 blocks t-2-hex lipidation and oligomerization of BAX. CBI1 inhibits BAX activation induced by BH3 ligands, F116A mutagenesis or t-2-hex .
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- HY-172262
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Bcl-2 Family
Apoptosis
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Cancer
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WEHI-3773 is an inhibitor of the interaction between VDAC2 and BAK or BAX. WEHI-3773 inhibits BAX-mediated Apoptosis by blocking the VDAC2-mediated recruitment of BAX to mitochondria. Conversely, WEHI-3773 promotes BAK-mediated Apoptosis by limiting the inhibitory sequestration of BAK by VDAC2. WEHI-3773 is promising for research in the field of anti-cancer .
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- HY-162148
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EGFR
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Cancer
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HNPMI is an inhibitor of EGFR and has cytotoxic effects on tumor cells. HNPMI can downregulate the protein levels of osteopontin, survivin and cathepsin S, leading to apoptosis. HNPMI also regulates BCL-2/BAX and p53 in CRC cell lines to inhibit tumorigenesis .
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- HY-P1928
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Bcl-2 Family
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Neurological Disease
Endocrinology
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Humanin, an anti-apoptotic peptide of 24 amino acids, is a Bax inhibitor. Humanin prevents the translocation of Bax from cytosol to mitochondria, blocks Bax from the inactive to active conformation. Humanin is a mitochondria-associated peptide with a neuroprotective effect against AD-related neurotoxicity. Humanin also improves overall insulin sensitivity in animal. Humanin are related to aging . Humanin analogue, in which the serine at position 14 is replaced by glycine, names HNG .
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- HY-118119
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PGE synthase
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Cancer
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CAY10526 is a specific microsomal PGE2 synthase-1 (mPGES1) inhibitor. CAY10526 inhibits PGE2 production through the selective modulation of mPGES1 expression but does not affect COX-2. CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. CAY10526 reduces BCL-2 and BCL-XL (anti-apoptotic) protein levels and increases BAX and BAK (pro-apoptotic) as well as cleaved caspase 3 levels. CAY10526 inhibits cell viability (IC50<5 μM) in three melanoma cell lines expressing mPGES1 .
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- HY-120079
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MSN-125
2 Publications Verification
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Bcl-2 Family
Apoptosis
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Cancer
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MSN-125 is a potent Bax and Bak oligomerization inhibitor. MSN-125 prevents mitochondrial outer membrane permeabilization (MOMP) with an IC50 of 4 μM. MSN-125 potently inhibits Bax/Bak-mediated apoptosis in HCT-116, BMK Cells, and primary cortical neurons, protects primary neurons against glutamate excitotoxicity .
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- HY-143235
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Epigenetic Reader Domain
Apoptosis
Bcl-2 Family
Caspase
c-Myc
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Cancer
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BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research .
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- HY-144778
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Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
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Cancer
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IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
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- HY-118948
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Bcl-2 Family
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Neurological Disease
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MSN-50 is a Bax and Bak oligomerization inhibitor. MSN-50 efficiently inhibits liposome permeabilization, prevents genotoxic cell death and promotes neuroprotection .
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- HY-148368
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Bcl-2 Family
Apoptosis
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Cancer
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CYD-4-61 is a novel Bax activator used for breast cancer research. CYD-4-61 inhibits triple-negative breast cancer MDA-MB-231 and ER-positive breast cancer MCF-7 cell lines proliferation. CYD-4-61 activates Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis .
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- HY-126741
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Apoptosis
Parasite
NF-κB
Bcl-2 Family
Caspase
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Infection
Inflammation/Immunology
Cancer
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Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells .
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- HY-161100
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Apoptosis
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Cancer
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BDM19 binds and activates cytosolic BAX dimers, and prompts cell apoptosis either alone or in combination with BCL-2/BCL-XL inhibitor Navitoclax (HY-10087) .
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- HY-50907
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ABT-737
Maximum Cited Publications
50 Publications Verification
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Bcl-2 Family
Apoptosis
Autophagy
Mitophagy
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Cancer
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ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
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- HY-12048
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- HY-162820
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Bcl-2 Family
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Cancer
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Bcl-2-IN-21 (compound C1) is an iridium compound with anticancer activity that targets and inhibits Bcl-2. Bcl-2-IN-21 inhibits colony formation of cancer cells and induces elevated levels of Bax and caspase 3 .
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- HY-111770
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2-Bromopalmitic acid; 2-Bromopalmitate
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Pyroptosis
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Infection
Inflammation/Immunology
Cancer
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2-Bromohexadecanoic acid (2-Bromopalmitate; 2-BP) is a palmitoylation inhibitor targeting DHHC (Asp-His-His-Cys) protein palmitoyltransferase. 2-Bromohexadecanoic acid inhibits palmitoylation of GSDME-C during pyroptosis and inhibits BAK/BAX-Caspase 3-GSDME pathway-mediated pyroptosis .
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- HY-50907S
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Biochemical Assay Reagents
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Cancer
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ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
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- HY-122481
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Topoisomerase
Apoptosis
Bcl-2 Family
Cytochrome P450
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Cancer
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Thaspine acetate, an alkaloid, is a topoisomerase I and II inhibitor. Thaspine acetate induces cancer cell apoptosis. Thaspine acetate induces Bak and Bax activation, mitochondrial cytochrome c release and mitochondrial membrane permeabilization. Thaspine acetate can be isoalted from the cortex of the South American tree Croton lechleri .
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- HY-128777
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VDAC
Apoptosis
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Cancer
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WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX .
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- HY-155012
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Bcl-2 Family
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Cancer
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Mcl-1 inhibitor 16 (Compound 9) is a mitochondrial targeting Platinum-based inhibitor of Mcl-1. Mcl-1 inhibitor 1 induces Bax/Bak-dependent apoptosis in cancer cells. Mcl-1 inhibitor 16 can be used alone or together with ABT-199 (HY-15531) and shows anti-tumor activity .
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- HY-W286906
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Bcl-2 Family
Apoptosis
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Cancer
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Mcl1-IN-15 (Compound 7) is the inhibitor for myeloid cell leukemia 1 (Mcl-1) with an IC50 of 8.73 μM. Mcl1-IN-15 inhibits Mcl1-BH3 peptide interaction, activates the Bak/Bax-mediated apoptosis and exhibits antitumor activity .
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- HY-12048R
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Reference Standards
PKC
Bcl-2 Family
Apoptosis
Autophagy
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Metabolic Disease
Inflammation/Immunology
Cancer
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Chelerythrine (chloride) (Standard) is the analytical standard of Chelerythrine (chloride). This product is intended for research and analytical applications. Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
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- HY-12875
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Ras
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Cancer
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BQU57 is a selective inhibitor of RalA/RalB small GTPases, with a binding potency (Kb) of 7.7 μM for RalB-GDP. BQU57 can block its interaction with effector proteins (such as SEC5 and EXO84), inhibiting tumor cell migration, invasion and non-adherent growth. BQU57 downregulates the NF-κB signaling pathway, reduces the expression of IL-6, IL-8 and MMP-13, and inhibits apoptosis by regulating the Bcl-2/Bax balance. BQU57 also protects the extracellular matrix by inhibiting the Ral/NF-κB pathway and can be used for the study of degenerative diseases. BQU57 exhibits significant antitumor activity in triple-negative breast cancer (TNBC) models, inhibiting orthotopic tumor growth and lung metastasis and enhancing paclitaxel chemotherapy sensitivity .
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- HY-170648
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Thymidylate Synthase
Apoptosis
PI3K
STAT
Bcl-2 Family
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Cancer
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TS-IN-5 (Compound 15) is a thymidylate synthase (TS) inhibitor. TS-IN-5 induces Apoptosis by modulating Bax, BCL-2, PI3K, and STAT1 proteins. TS-IN-5 shows antitumor effects against liver, breast and colon cancers .
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- HY-W250111
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Biochemical Assay Reagents
Apoptosis
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
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Cancer
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Carboxymethyl chitosan is a derivative of chitosan. Carboxymethyl chitosan inhibits Apoptosis and ROS. Carboxymethyl chitosan increases the expression of Bcl-2 and reduces the expression of Bax, cytochrome c and caspase-3. Carboxymethyl chitosan inhibits the migration of various cells. Carboxymethyl chitosan exerts antitumor effects on Lewis tumors and hepatocarcinoma .
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- HY-162826
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Apoptosis
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Cancer
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Apoptosis inducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer (IC50: 12.8 μM) and can induce early apoptosis in breast cancer cells. Apoptosis inducer 27 can bind to DNA molecules, Bax and Bcl-2 proteins, and induce DNA damage .
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- HY-151429
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Apoptosis
Ferroptosis
Bcl-2 Family
COX
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Cancer
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Antitumor agent-77 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-77 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
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- HY-151428
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Ferroptosis
Apoptosis
Bcl-2 Family
COX
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Cancer
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Antitumor agent-78 is an antitumor agent, inhibits cancer cells growth and migration. Antitumor agent-78 triggers ferroptosis by inhibiting GPx-4 and elevating COX2. Antitumor agent-78 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process of cancer cells .
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- HY-111287
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DK-1-49
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Autophagy
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Cancer
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Autophagonizer (DK-1-49) is a small molecule autophagy inducer that results in an accumulation of autophagy-associated LC3-II and enhances levels of autophagosomes and acidic vacuoles. Autophagonizer inhibits cell viability and induces cell death in not only cancer cells but also Bax/Bak double-knockout cells with EC50 values of 3-4 μM .
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- HY-N0292
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Cytochrome P450
PPAR
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
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- HY-15191
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BI-97C1
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Bcl-2 Family
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Cancer
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Sabutoclax is a potent and effective Bcl-2 Family (Bcl-2, Bcl-XL, Mcl-1, Bfl-1) inhibitor with IC50s of 0.32 μM, 0.31 μM, 0.20 μM, and 0.62 μM, respectively. Sabutoclax increases Bax, Bim, PUMA and survivin expression .
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- HY-116204
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Caspase
CDK
Apoptosis
Bcl-2 Family
PARP
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Others
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SKLB70326 is a small molecule inhibitor of cell cycle progression that induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cells. SKLB70326 is involved in downregulating cyclin-dependent kinase (CDK) 2, CDK4, and CDK6, while also activating PARP, caspase-3, caspase-9, and Bax, and downregulating Bcl-2.
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- HY-N1414A
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Bcl-2 Family
Apoptosis
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Neurological Disease
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3′,6-Disinapoylsucrose is a type of oligosaccharide that's effective when taken orally, and it has antidepressant, anti-anxiety, and antioxidant properties. 3′,6-Disinapoylsucrose inhibits neuronal apoptosis by lowering the ratio of Bax to Bcl-2 in hippocampal neurons, and it enhances cognitive function in APP/PS1 transgenic mice by activating the CREB/BDNF signaling pathway .
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- HY-159938
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p38 MAPK
Apoptosis
Bcl-2 Family
MDM-2/p53
Caspase
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Cancer
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p38α inhibitor 6 (compound 19) is a p38α inhibitor with the IC50 of 0.68 μM. p38α inhibitor 6 induces cell apoptosis and arrests cell cycle at G0 and G2/M phase. p38α inhibitor 6 decreases the TNF-α concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7 .
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- HY-N2359
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Beta-lactamase
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Cancer
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Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM . Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity . Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy .
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- HY-167825
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-
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- HY-12286
-
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Proteasome
Apoptosis
Autophagy
Caspase
Bcl-2 Family
NF-κB
PARP
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Cancer
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PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α .
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- HY-149540
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Fatty Acid Synthase (FASN)
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Cancer
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CTL-06 is an inhibitor of Fatty Acid Synthase (FASN) (IC50: 3 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
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- HY-N2877
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Potassium Channel
Sodium Channel
Na+/K+ ATPase
Calcium Channel
Apoptosis
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Neurological Disease
Cancer
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Annonacin is an acetylgenin that is toxic by inhibiting the pathway of the mitochondrial complex. Annonacin increases tau phosphorylation in R406W +/+ mice. Annonacin acts as an inhibitor of the sodium/potassium and sarcoplasmic reticulum (SERCA) ATPase pumps. Annonacin has significant killing effect on ovarian cancer cell, cervical cancer cell, breast cancer cell, bladder cancer cell and skin cancer cell. Annonacin induces apoptosis through Bax and Caspase-3-related pathways .
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- HY-170929
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Bcl-2 Family
Cytochrome P450
Apoptosis
Caspase
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Cancer
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EMT inhibitor-3 (compound 11i) is a epithelial-mesenchymal transition (EMT) inhibitor. EMT inhibitor-3 inhibits neuroblastoma SK-N-SH cells with an IC50 of 2.5 μM. EMT inhibitor-3 inhibits SK-N-SH cell proliferation, migration, and invasion. EMT inhibitor-3 increases the Bax/Bcl-2 protein expression ratio, promotes Cytochrome C ( HY-125857) release from mitochondria, and activates caspases 9 and caspases 3, inducing mitochondria-mediated endogenous tumor cell Apoptosis. EMT inhibitor-3 is potential for cancer research .
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- HY-171031
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GSK-3
Apoptosis
Caspase
Bcl-2 Family
Reactive Oxygen Species (ROS)
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Neurological Disease
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TFGF-18 is a GSK-3β inhibitor (IC50: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment .
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- HY-W001538
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SPRC
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STAT
MDM-2/p53
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Inflammation/Immunology
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S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca 2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties .
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- HY-122047
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Autophagy
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Cancer
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SW063058 is an autophagy inducer that specifically disrupts the binding of Beclin 1 to Bcl-2 while leaving the interaction between Bcl-2 and pro-apoptotic members like Bax and BIM unaffected. By inhibiting the negative regulatory effects of Bcl-2 on Beclin 1, which is crucial for the initiation of autophagy, SW063058 promotes autophagic activity without triggering cytotoxicity, apoptosis, or other forms of cell death in vitro.
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- HY-149541
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Fatty Acid Synthase (FASN)
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Cancer
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CTL-12 is an inhibitor of fatty acid synthase (FASN) (IC50: 2.5 μM) and can induce apoptosis. CTL-12 blocks the cell cycle in the Sub-G1/S phase, upregulates the expression of caspase-9 and the apoptosis marker Bax, and downregulates the anti-apoptotic marker Bcl-xL. CTL-12 inhibits de novo lipogenesis, blocks the metabolic demands of tumor cells, and is commonly used in breast and colorectal cancer research .
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- HY-N15449
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HSP
Caspase
Apoptosis
Reactive Oxygen Species (ROS)
Bcl-2 Family
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Cancer
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Vicanicin is a depsidone compound found in lichens. Vicanicin inhibits the expression of Hsp70, regulates the redox-sensitive mechanisms within cells, promotes the increase of reactive oxygen species (ROS) in cancer cells, changes the Bax/Bcl-2 ratio, activates caspase-3, and triggers apoptosis. Vicanicin inhibits cell growth and induces apoptosis in androgen-sensitive (LNCaP) and androgen-insensitive (DU-145) human prostate cancer cells. Vicanicin is promising for research of prostate cancer .
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- HY-124122
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VEGFR
Checkpoint Kinase (Chk)
Apoptosis
Caspase
Bcl-2 Family
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Cancer
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BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 µmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 µmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases .
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- HY-111329
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ILS-JGB-1741
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Sirtuin
Apoptosis
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Cancer
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JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research .
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- HY-100490
-
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Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Cancer
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Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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- HY-100490B
-
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Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
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Cardiovascular Disease
Cancer
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Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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- HY-161388
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Ferroptosis
Mitophagy
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Cancer
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NSCLC-IN-1 (Compound A10-2) induces mitophagy and ferroptosis through targeting transmembrane BAX inhibitor motif containing 6 (TMBIM6). NSCLC-IN-1 induces mitochondrial Ca 2+ imbalance, leading to mitochondrial damage. NSCLC-IN-1 reduces intracellular glutathione (GSH), increases the accumulation of lipid peroxides (LPO) and malondialdehyde (MDA) content. NSCLC-IN-1 is a potent anti-NSCLC agent .
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- HY-N0292R
-
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Cytochrome P450
Reference Standards
PPAR
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Oleuropein (Standard) is the analytical standard of Oleuropein. This product is intended for research and analytical applications. Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity . Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase .
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- HY-115529
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Bcl-2 Family
Apoptosis
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Cancer
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(-)BI97D6 is a broad-spectrum inhibitor of the Bcl-2 protein family, inhibiting Mcl-1, Bcl-2, Bcl-xL and Bcl-1 with IC50 values of 0.025, 0.031, 0.076 and 0.122 μM, respectively. (-)BI97D6 stimulates cell death through the Bak and Bax mediated mitochondrial apoptosis pathway. In addition, (-)BI97D6 inhibits Mcl-1 and can effectively induce apoptosis in acute myeloid leukemia (AML) cells .
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-
- HY-111237
-
Olomoucin
|
CDK
NF-κB
PERK
Bcl-2 Family
Reactive Oxygen Species (ROS)
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Butyrolactone I is an orally active and ATP-competitive inhibitor of CDK1. Butyrolactone I inhibits NF-κB, cdc2 kinase, Bax, ROS production, modulates the PERK/CHOP. Butyrolactone I mitigates heat-stress-induced Apoptosis. Butyrolactone I shows anti-inflammatory and intestinal protective activity. Butyrolactone I has antitumor effects against non-small cell lung, small cell lung, prostate cancer and leukemia. Butyrolactone I can be used in NASH research .
|
-
- HY-151443
-
|
HDAC
|
Cancer
|
HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC50s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo .
|
-
- HY-115974
-
|
Bombesin Receptor
|
Cancer
|
GRPR antagonist-1 is a potent gastrin releasing peptide receptor (GRPR) antagonist, having the cytotoxicity against certain cancer cells (IC50 of 4.97, 4.36 and 3.40 μM in PC3, Pan02 and HGC-27 cells, respectively). GRPR antagonist-1 inhibits HGC-27 cell viability by decreasing the Bcl-2 level and increasing the Bax level, causing apoptosis, with anticancer activity .
|
-
- HY-B0493
-
|
Chloride Channel
COX
|
Inflammation/Immunology
Cancer
|
Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-100490A
-
|
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na +/H + antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-155242
-
|
VEGFR
Bcl-2 Family
Apoptosis
|
Cancer
|
VEGFR-2-IN-36 (compound 15) is a VEGFR-2 inhibitor (IC50: 0.067 μM) and inducer of apoptosis with anticancer activity. VEGFR-2-IN-36 upregulates BAX levels and downregulates Bcl-2 levels. VEGFR-2-IN-36 is toxic to cancer cells, MCF-7 (IC50=0.42 μM) and HepG2 (IC50=0.22 μM) .
|
-
- HY-N15424
-
|
Apoptosis
Bcl-2 Family
|
|
Himachalol, a sesquiterpene, is an orally active antispasmodic and anticancer constituent found in the wood of Cedrus deodara. Himachalol has anti-proliferative activity against the melanoma cells, and induces apoptosis (decreases Bcl-2 level and increases Bax level). Himachalol has systemic hypotension and peripheral vasodilation effect. Himachalol inhibits Carbachol-induced spasm of the intestine. The LD50 of Himachalol in mice is 265 mg/kg (p.o.) and 247 mg/kg (i.p.) .
|
-
- HY-163527
-
|
FGFR
|
Cancer
|
FGFR-IN-13 (compound III-30) is an irreversible covalent fibroblast growth factor receptor (FGFR) inhibitor. FGFR-IN-13 regulates endogenous FGFR1(IC50=0.20±0.02 nM) and FGFR4(IC50=0.40±0.03 nM) mediated signaling pathways by inhibiting the expression of key proteins. FGFR-IN-13 inhibits total-PARP and Bcl-2 protein expressions, and promote Cleaved-PARP and Bax protein expressions in a dose-dependent manner. FGFR-IN-13 has significant antitumor activity and oral activity .
|
-
- HY-172092
-
|
Apoptosis
Ferroptosis
|
Cancer
|
BG11 induces the accumulation of Fe 2+ and intracellular lipid peroxides, induces ferroptosis. BG11 regulates the expression of Bax and Bcl-2 proteins, and induces apoptosis in MDA-MB-231 cell. BG11 arrests the cell cycle at G0/G1 and S phase, inhibits the proliferation of TNBC cancer cell (IC50 for MDA-MB-231 and BT549 is 0.49 μM and 0.52 μM), and inhibits the cell migration and invasion. BG11 exhibits antitumor efficacy in mouse models .
|
-
- HY-170366
-
|
VEGFR
Apoptosis
|
Cancer
|
VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with an IC50 of 42.5 nM. VEGFR-2-IN-58 displays selective cytotoxicity against cancer cells. VEGFR-2-IN-58 shows cellular growth arrest at the G2/M phase in cancer cells. VEGFR-2-IN-58 induces cancer cells Apoptosis, increasing BAX expression and reducing Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells .
|
-
- HY-N0060B
-
(E)-Coniferic acid
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
(E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
|
-
- HY-100490S
-
|
Isotope-Labeled Compounds
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-N8508
-
|
Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
|
Cancer
|
Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
|
-
- HY-150596
-
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-N2132
-
-
- HY-N6576
-
|
p38 MAPK
ERK
JNK
IAP
PARP
Apoptosis
Caspase
|
Cancer
|
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
|
-
- HY-136498AR
-
|
Reference Standards
Drug Metabolite
|
Infection
|
Rilmenidine (phosphate) (Standard) is the analytical standard of Rilmenidine (phosphate). This product is intended for research and analytical applications. Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-N3405
-
|
Glycosidase
Bcl-2 Family
Apoptosis
TGF-β Receptor
NF-κB
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Lariciresinol is an orally active ingredient. Lariciresinol can be isolated from Arabidopsis thaliana. Lariciresinol inhibits α-glucosidase activity (IC50 of 6.97 μM; Ki of 0.046 μM). Lariciresinol dereases Bcl-2, upregulates Bax and induces Apoptosis. Lariciresinol regulates TGF-β and NF-κB pathways. Lariciresinol has antitumor activity against liver cancer, gastric cancer, and breast cancer. Lariciresinol shows antifungal activity and anti-diabetic activity .
|
-
- HY-100490BR
-
|
Reference Standards
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine (phosphate) (Standard) is the analytical standard of Rilmenidine (phosphate). This product is intended for research and analytical applications. Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-101999
-
|
Bcl-2 Family
Caspase
Apoptosis
|
Cancer
|
EM20-25 is an inhibitor for Bcl-2, which interferes with the interaction between BCL-2 and BAX, activates caspase-9 and thus induces the apoptosis. EM20-25 affects the mitochondrial function, causes the open of permeability transition pore (PTP). EM20-25 enhances the sensitivity of cells to Staurosporine (HY-15141), and enhances the killing effect of BCL-2-expressing leukemia cells to Chlorambucil (HY-13593) and Fludarabine (HY-B0069) .
|
-
- HY-101310
-
|
iGluR
EAAT
Bcl-2 Family
Caspase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain .
|
-
- HY-100490R
-
|
Reference Standards
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine (Standard) is the analytical standard of Rilmenidine. This product is intended for research and analytical applications. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-161874
-
|
Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
PARP
Autophagy
|
Cancer
|
RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity .
|
-
- HY-169431
-
|
VEGFR
Akt
Caspase
Bcl-2 Family
Apoptosis
|
Cancer
|
VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells .
|
-
- HY-149517
-
|
EGFR
Raf
Caspase
Bcl-2 Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAF V600E, and EGFR T790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency .
|
-
- HY-100490AR
-
|
Reference Standards
Imidazoline Receptor
Adrenergic Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Cancer
|
Rilmenidine (hemifumarate) (Standard) is the analytical standard of Rilmenidine (hemifumarate). This product is intended for research and analytical applications. Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
|
-
- HY-168623
-
|
EGFR
Apoptosis
Necroptosis
Bcl-2 Family
Caspase
MDM-2/p53
|
Cancer
|
EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity .
|
-
- HY-B0493R
-
|
Reference Standards
Chloride Channel
COX
|
Inflammation/Immunology
|
Niflumic acid (Standard) is the analytical standard of Niflumic acid. This product is intended for research and analytical applications. Niflumic acid is a calcium-activated chloride channel blocker and COX-2 inhibitor with the IC50 value of 100 nM. Niflumic acid induces apoptosis through caspase-8/Bid/Bax pathway in lung cancer cells. Niflumic acide exhibits anti-tumor activity by affecting the expression of ERK1/2 and the activity of MMP2 and MMP9. Niflumic acid has orally bioactivity. Niflumic acid acts on rheumatoid arthritis .
|
-
- HY-168739
-
|
Topoisomerase
Reactive Oxygen Species (ROS)
Apoptosis
Survivin
Bcl-2 Family
IAP
DNA/RNA Synthesis
|
Cancer
|
Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
|
-
- HY-172393
-
|
β-catenin
Apoptosis
Caspase
MDM-2/p53
Bcl-2 Family
Cytochrome P450
|
Cancer
|
TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells .
|
-
- HY-N0060BR
-
(E)-Coniferic acid (Standard)
|
Reference Standards
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
(E)-Ferulic acid (Standard) is the analytical standard of (E)-Ferulic acid. This product is intended for research and analytical applications. (E)-Ferulic acid is an isomer of ferulic acid, an aromatic compound abundant in plant cell walls. (E)-Ferulic acid causes phosphorylation of β-catenin (β-catenin), leading to proteasome degradation, increasing the expression of pro-apoptotic factor Bax and reducing pro-apoptotic factor Expression of the survival factor survivin. (E)-Ferulic acid can effectively remove reactive oxygen species (ROS) and inhibit lipid peroxidation. (E)-Ferulic acid exerts antiproliferative and antimigratory effects in the human lung cancer cell line H1299.
|
-
- HY-172551
-
|
Apoptosis
Cadherin
MMP
Bcl-2 Family
|
Cancer
|
anti-TNBC agent-9 (Compound 3as) is an anti-cancer agent for triple-negative breast cancer (TNBC). anti-TNBC agent-9 exhibits significant inhibitory activity against MDA-MB-453 cells with an IC50 value of 8.5 μM. anti-TNBC agent-9 inhibits tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. anti-TNBC agent-9 induces apoptosis by increasing the expression of the pro-apoptotic protein BAX and decreasing the expression of the anti-apoptotic protein BCL-2, thereby inhibiting tumor cell proliferation .
|
-
- HY-169096
-
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
DPP-21 is an inhibitor of tubulin polymerization (IC50: 2.4 μM). DPP-21 shows anti-proliferative activity against cancer cell lines, with IC50s of 0.38 nM (HCT116), 11.69 nM (B16), 5.37 nM (HeLa), 9.53 nM (MCF7), 8.94 nM (H23) and 9.37 nM (HepG2) respectively. DPP-21 arrests the cell cycle in the G2/M phase of mitosis, subsequently inducing tumor cell apoptosis (decreases Bcl-2 but upregulates the pro-apoptotic protein Bax) .
|
-
- HY-N0060BS
-
(E)-Coniferic acid-d3
|
β-catenin
Bcl-2 Family
Ferroptosis
Endogenous Metabolite
|
Cancer
|
(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299 .
|
-
- HY-146253
-
|
CDK
Apoptosis
Bcl-2 Family
Caspase
|
Cancer
|
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research .
|
-
- HY-174232
-
|
EGFR
Carbonic Anhydrase
Caspase
|
Cancer
|
EGFR/CA-IX-IN-1 (Compound 14) is a dual inhibitor against epidermal growth factor receptor (EGFR) and carbonic anhydrase IX (CA-IX) with IC50 values of 5.92 nM and 63 nM, respectively. EGFR/CA-IX-IN-1 shows strong cytotoxicity against breast cancer cells (MDA-MB-231, MCF-7) with IC50 values of 5.78 μM and 8.05 μM, respectively. EGFR/CA-IX-IN-1 inhibits the catalytic activity of CA-IX, up-regulates BAX/Bcl-2, activates caspases, and arrests the cell cycle at the G1 phase. EGFR/CA-IX-IN-1 is promising for research of breast cancer .
|
-
- HY-168338
-
|
Cannabinoid Receptor
Caspase
|
Cancer
|
CB2 receptor agonist 8 (Compound 17) is an agonist for cannabinoid receptor 2 (CB2 receptor). CB2 receptor agonist 8 exhibits cytotoxicity in cells U87, RPMI 8226, HL-60, and L929 with IC50s of 91.03, 16.29, 23.51 and 564.6 μM, respectively. CB2 receptor agonist 8 activates caspase 3/7, increases the expressions of pro-apoptotic genes BAX, BAD, BIM and tumor suppressor genes p53, and induces apoptosis in U87. CB2 receptor agonist 8 inhibits the migration of U87 .
|
-
- HY-128483
-
|
TGF-beta/Smad
PI3K
NF-κB
Akt
Apoptosis
Dopamine β-hydroxylase
mTOR
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer .
|
-
- HY-144791
-
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-144792
-
|
Bcl-2 Family
MDM-2/p53
Caspase
Apoptosis
|
Cancer
|
Bcl-2-IN-7 (compound 6) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.17, 22.64, 45.57, and 51.50 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively .
|
-
- HY-147826
-
|
EGFR
Apoptosis
|
Cancer
|
EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFR WT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio .
|
-
- HY-128483R
-
|
TGF-beta/Smad
PI3K
NF-κB
Akt
Apoptosis
Dopamine β-hydroxylase
mTOR
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
Cancer
|
Fusaric acid (Standard) is the analytical standard of Fusaric acid (HY-128483). This product is intended for research and analytical applications. Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer .
|
-
- HY-170932
-
|
EGFR
COX
Apoptosis
|
Cancer
|
EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
|
-
- HY-172886
-
|
PI3K
Bcl-2 Family
Apoptosis
|
Cancer
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PI3K-IN-58 (Compound 17f) is a PI3Kα inhibitor (IC50: 0.039 μM). PI3K-IN-58 exhibits significant antiproliferative effects on PC-3, 22RV1, MDA-MB-231 and MDA-MB-453 cell lines with IC50s of 3.48 μM, 1.06 μM, 2.21 μM and 0.93 μM, respectively. PI3K-IN-58 induces apoptosis by downregulating the expression levels of anti-apoptotic proteins Bcl-XL and Bcl-2 and upregulating the expression of anti-apoptosis protein BAX. PI3K-IN-58 can be used in PI3K-targeted cancer research .
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- HY-173309
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MDM-2/p53
Toll-like Receptor (TLR)
Apoptosis
MyD88
Bcl-2 Family
Interleukin Related
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Cancer
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P53/TLR2 modulator-1 (Compound Z9) is a modulator that targets both the P53 pathway and TLR2 simultaneously, exhibiting anti-radiation activity. P53/TLR2 modulator-1 reduces apoptosis by inhibiting the radiation-induced expression of P53 and Bax. At the same time, it activates the TLR2 pathway, upregulates the expression of downstream proteins MyD88 and P65, and promotes the secretion of cytokines such as IL-6, thus exerting an anti-radiation effect. P53/TLR2 modulator-1 shows significant anti-radiation activity against both AHH-1 cells and HUVECs. It can also increase the survival rate of C57BL/6J mice irradiated with a lethal dose of radiation and reduce the damage to their hematopoietic system, the villous structure of the small intestine, and the spleen caused by radiation. P53/TLR2 modulator-1 can be used in the research of radiation injury-related diseases .
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Cat. No. |
Product Name |
Type |
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- HY-W250111
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Biochemical Assay Reagents
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Carboxymethyl chitosan is a derivative of chitosan. Carboxymethyl chitosan inhibits Apoptosis and ROS. Carboxymethyl chitosan increases the expression of Bcl-2 and reduces the expression of Bax, cytochrome c and caspase-3. Carboxymethyl chitosan inhibits the migration of various cells. Carboxymethyl chitosan exerts antitumor effects on Lewis tumors and hepatocarcinoma .
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Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P0081
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BIP-V5; Bax Inhibiting Peptide V5
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Bcl-2 Family
Apoptosis
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Cancer
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Bax inhibitor peptide V5 (BIP-V5) is a Bax-mediated apoptosis inhibitor, used for cancer treatment.
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- HY-P1928
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Bcl-2 Family
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Neurological Disease
Endocrinology
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Humanin, an anti-apoptotic peptide of 24 amino acids, is a Bax inhibitor. Humanin prevents the translocation of Bax from cytosol to mitochondria, blocks Bax from the inactive to active conformation. Humanin is a mitochondria-associated peptide with a neuroprotective effect against AD-related neurotoxicity. Humanin also improves overall insulin sensitivity in animal. Humanin are related to aging . Humanin analogue, in which the serine at position 14 is replaced by glycine, names HNG .
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- HY-103271
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Bcl-2 Family
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Cancer
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Bax inhibitor peptide, negative control is a inhibitor of Bax. Bax inhibitor peptide, negative control inhibits Bax translocation to mitochondria and Bax-mediated apoptosis in vitro .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-126741
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- HY-12048
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- HY-N0292
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- HY-N1414A
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- HY-N0292R
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- HY-12048R
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- HY-N2359
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- HY-167825
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- HY-N2877
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- HY-N15449
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- HY-N15424
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- HY-N0060B
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- HY-N8508
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Structural Classification
Natural Products
Microorganisms
Source classification
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Apoptosis
Cytochrome P450
PARP
JNK
Bcl-2 Family
Caspase
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Myrothecine A is a trichothecene mycotoxin found in M. roridum. Myrothecine A induces apoptosis, promotes the cytochrome c release, PARP-cleavage and phosphorylation of JNK, increases Bax and cleaved caspase-3, -5, and -8 levels. Myrothecine A has anticancer activities and promotes the maturation of DC cells in the microenvironment. Myrothecine A inhibits proliferation of A549, MCF-7, HepG2, and SMMC-7721 cancer cells with IC50s of 95, 70, 60, and 25 µM, respectively .
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- HY-N2132
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- HY-N6576
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Structural Classification
Animals
Classification of Application Fields
Source classification
Disease Research Fields
Steroids
Cancer
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p38 MAPK
ERK
JNK
IAP
PARP
Apoptosis
Caspase
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Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
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- HY-N3405
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- HY-N0060BR
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- HY-128483
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Infection
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Disease Research Fields
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TGF-beta/Smad
PI3K
NF-κB
Akt
Apoptosis
Dopamine β-hydroxylase
mTOR
Adrenergic Receptor
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Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer .
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- HY-128483R
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
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TGF-beta/Smad
PI3K
NF-κB
Akt
Apoptosis
Dopamine β-hydroxylase
mTOR
Adrenergic Receptor
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Fusaric acid (Standard) is the analytical standard of Fusaric acid (HY-128483). This product is intended for research and analytical applications. Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β1/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-50907S
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ABT 737-d8 is the deuterium labeled ABT-737. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research .
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- HY-N0060BS
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(E)-Ferulic acid-d3 is the deuterium labeled (E)-Ferulic acid. (E)-Ferulic acid is a isomer of Ferulic acid which is an aromatic compound, abundant in plant cell walls. (E)-Ferulic acid causes the phosphorylation of β-catenin, resulting in proteasomal degradation of β-catenin and increases the expression of pro-apoptotic factor Bax and decreases the expression of pro-survival factor survivin. (E)-Ferulic acid shows a potent ability to remove reactive oxygen species (ROS) and inhibits lipid peroxidation. (E)-Ferulic acid exerts both anti-proliferation and anti-migration effects in the human lung cancer cell line H1299 .
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- HY-100490S
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Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
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Cat. No. |
Product Name |
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Classification |
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- HY-W001538
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SPRC
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Alkynes
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S-Propargylcysteine (SPRC), a structural analog of S-allyl cysteine (SAC), is a slow H2S-releasing compound. S-Propargylcysteine reduces Ca 2+ accumulation and inflammatory cytokines, inhibits STAT3, and elevates p53 and Bax. S-Propargylcysteine has anti-inflammatory activity and protects mice against acute pancreatitis. S-Propargylcysteine also has cardioprotective, neuroprotective acitivties .
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