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NCI-H226

" in MedChemExpress (MCE) Product Catalog:

標的別:	Apoptosis (2) c-Myc (1) Caspase (1) Dihydroorotate Dehydrogenase (1) E3 Ligase Ligand-Linker Conjugates (1) Ferroptosis (1) Glycosidase (1) HBV (1) IAP (2) JAK (1) JNK (1) Ligands for Target Protein for PROTAC (2) NADPH Oxidase (1) PARP (1) PROTACs (7) Radionuclide-Drug Conjugates (RDCs) (1) Reactive Oxygen Species (ROS) (1) SARS-CoV (1) SNIPERs (3) STAT (1) Transmembrane Glycoprotein (1) Tyrosinase (2) YAP (22)
研究分野別:	Cancer (30) Infection (1) Inflammation/Immunology (3) Neurological Disease (2)
クリックケミストリー:	Alkynes (1)

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製品番号	製品名	Target	研究分野	構造式

HY-134955

VT103 5 Publications Verification	YAP	Cancer
VT103, an analog of VT101, is an orally active and selective TEAD1 protein palmitoylation inhibitor. VT103 inhibits YAP/TAZ-TEAD promoted gene transcription, blocks TEAD auto-palmitoylation, and disrupts interaction between YAP/TAZ and TEAD. VT103 can be used for the research of cancer .

HY-175357

YAP/TEAD-IN-2	YAP	Cancer
YAP/TEAD-IN-2 (Compound T-1) is a YAP/TEAD inhibitor. YAP/TEAD-IN-2 inhibits the luciferase activity driven by YAP/TEAD in 293T cells. YAP/TEAD-IN-2 exhibits strong anti-proliferative activity against human pleural mesothelioma NCI-H226 cells. YAP/TEAD-IN-2 can be used for the study of diseases associated with Hippo pathway dysregulation, particularly cancers .

HY-N2278

Kushenol A 4 Publications Verification Leachianone E	Tyrosinase Glycosidase	Cancer
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC₅₀ and K_ivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC₅₀: 45 μM; K_i: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .

HY-172113

H122	PROTACs YAP c-Myc Apoptosis	Cancer
H122 is a PROTAC degrader for TEAD that degrades TEAD1 with a DC₅₀ of 3 nM. H122 exhibits good affinity to TEAD2, TEAD3, and TEAD4 with K_i values of 2.0, 3.6 and 1.6 nM, respectively. H122 relies on binding to TEAD1 and CRBN, functional E3 ligase activity, and a functional proteasome for degradation.H122 induces degradation of TEAD3 and forms a ternary complex with TEAD4 and CRBN/DDB1 to mediate degradation.H122 downregulates expression of Myc target genes. H122 exhibits antitumor efficacy in MSTO-211H mouse xenograft models.H122 can be used for the research of malignant mesothelioma .

HY-147322

YAP/TAZ inhibitor-2 1 Publications Verification	YAP	Cancer
YAP/TAZ inhibitor-2 is a potent and orally active TEAD-YAP/TAZ inhibitor with an EC₅₀ value of 3 nM. YAP/TAZ inhibitor-2 shows anti-proliferative activity. YAP/TAZ inhibitor-2 shows antitumor activity .

HY-174275

TEAD1/3/4-IN-1	YAP	Inflammation/Immunology Cancer
TEAD1/3/4-IN-1 is an orally active inhibitor of TEAD1/3/4. TEAD1/3/4-IN-1 inhibits the YAP/TAZ-TEAD interaction, with its EC₅₀ being 2 nM. TEAD1/3/4-IN-1 has anti-proliferative activity against NCI-H226 cells. TEAD1/3/4-IN-1 can be used in the research of lung squamous cell carcinoma .

HY-168016

PROTAC YAP degrader-1	PROTACs YAP	Cancer
PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC₅₀=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma .

HY-147208

MSC-4106	YAP	Cancer
MSC-4106 is an orally active and potent inhibitor of YAP/TAZ-TEAD. MSC-4106 inhibits TEAD1 or TEAD3 auto-palmitoylation and shows inhibitory effect on NCI-H226 tumor xenograft model .

HY-N3239

Mulberrofuran G	Tyrosinase NADPH Oxidase HBV SARS-CoV Reactive Oxygen Species (ROS) JAK STAT Apoptosis Caspase PARP	Infection Neurological Disease Inflammation/Immunology Cancer
Mulberrofuran G is a NOX inhibitor (IC₅₀: 6.9 μM) and tyrosinase inhibitor. Mulberrofuran G exhibits anti-inflammatory, antioxidant, antiviral, antitumor, and neuroprotective effects. Mulberrofuran G can be used in the research of tumors, nervous system diseases, and other conditions .

HY-158342

PROTAC TEAD degrader-1	PROTACs YAP	Cancer
PROTAC TEAD degrader-1 is a TEAD2 degrader and antiproliferative agent with selective activity toward TEAD2 relative to other TEAD family members. PROTAC TEAD degrader-1 relies on CRBN and the proteasome system for TEAD2 degradation; disruption of CRBN binding attenuates this activity. PROTAC TEAD degrader-1 decreases expression of YAP target genes CYR61 and CTGF. PROTAC TEAD degrader-1 can be used for the research of NF2-deficient cancer .

HY-179395

TEAD-IN-23	YAP	Cancer
TEAD-IN-23 (Compound 22) is an efficient pan-TEAD inhibitor with an IC₅₀ of 10 nM. TEAD-IN-23 exhibits potent anti-proliferative activity in both NCI-H226 and MSTO-211H. TEAD-IN-23 causes complete tumor regression in the MSTO-211H xenograft tumor model. TEAD-IN-23 can be used for the study of mesothelioma and hepatocellular carcinoma .

HY-170764

M3686	YAP	Cancer
M3686 (Compound 29) is a potent, selective TEAD1 inhibitor with an IC₅₀ value of 51 nM. M3686 also shows weaker binding activity on TEAD3. M3686 potently inhibits cell viability against YAP-dependent NCI-H226 cell line with an IC₅₀ value of 0.06 uM. M3686 shows strong anti-tumor effects in the NCI-H226 xenograft model .

HY-169021

JNK-1-IN-3	JNK	Cancer
JNK-1-IN-3 (Compound 9e) is an inhibitor of JNK1 that downregulates JNK1 gene expression and inhibits the protein levels of its phosphorylated form, concurrently reducing the expression of its downstream targets, c-Jun and c-Fos, in tumors while restoring p53 activity. JNK-1-IN-3 exhibits broad-spectrum antiproliferative activity, particularly with high inhibitory activity against renal and breast cancer cell lines, demonstrating both in vivo and in vitro anticancer activity .

HY-N12004

19-Hydroxy-10-deacetylbaccatin III	Others	Cancer
19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively .

HY-159119

hDHODH-IN-15	Dihydroorotate Dehydrogenase Ferroptosis	Cancer
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC₅₀ of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC₅₀ of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .

HY-W778562

10-Deacetyl-13-oxobaccatin III	Others	Cancer
10-Deacetyl-13-oxobaccatin III is an taxane that can be isolated from Taxus sumatrana. 10-Deacetyl-13-oxobaccatin III (30 μg/mL) shows cytotoxicity against A498, NCI-H226, A549, PC-3 cells, with inhibition a rate of 29.7%, 49.2%, 43.9%, 65.3% .

HY-158400

TEAD ligand 1	Ligands for Target Protein for PROTAC YAP	Cancer
TEAD ligand 1 is the ligand for target protein TEAD. TEAD ligand 1 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .

HY-179440

EA-C15	YAP	Cancer
EA-C15 is a potent and selective TEAD inhibitor with an IC₅₀ of 0.34 μM. EA-C15 covalently binds to the TEAD palmitoylation site, blocks palmitoylation and transcriptional activity, and inhibits YAP-dependent cancer cell proliferation and YAP-TEAD target gene (CTGF and CYR61) transcription. EA-C15 can be used for cancer research .

HY-168505

MSC-5046	YAP	Cancer
MSC-5046 is a selective TEAD1 inhibitor .

HY-158343

Thalidomide-NH-PEG2-C2-CH2	E3 Ligase Ligand-Linker Conjugates	Cancer
Thalidomide-NH-PEG2-C2-CH2 is a conjugate of E3 ligase ligand and linker. Thalidomide-NH-PEG2-C2-CH2 is utilized for synthesis of PROTAC TEAD degrader-1 (HY-158342) .

HY-157083

mCMY020	YAP	Cancer
mCMY020 is a covalent inhibitor of TEAD. mCMY020 effectively reduces YAP (Yes-associated protein)-driven transcription and selectively slows the proliferation of Hippo-deficient cancer cells. mCMY020 can be used in cancer research .

HY-180514

TEAD-IN-24	YAP	Cancer
TEAD-IN-24 (Example 65) is a TEAD inhibitor. TEAD-IN-24 exhibits anti-cancer activity against non-small cell lung cancer .

HY-181590

PROTAC TEAD1/IAP degrader-3	PROTACs SNIPERs YAP IAP	Cancer
PROTAC TEAD1/IAP degrader-3 is a TEAD1/IAP PROTAC degrader. PROTAC TEAD1/IAP degrader-3 recruits the cIAP1 and XIAP E3 ligases to form a ternary complex, drives proteasomal degradation of TEAD1, and triggers autoubiquitination and proteasomal degradation of cIAP1. PROTAC TEAD1/IAP degrader-3 inhibits cell proliferation. PROTAC TEAD1/IAP degrader-3 regulates Hippo pathway activity by downregulating CTGF gene expression in a TEAD-dependent manner. PROTAC TEAD1/IAP degrader-3 is applicable to the research of mesothelioma .

HY-185230

HC278	PROTACs YAP	Cancer
HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma .

HY-181537

PROTAC TEAD1/IAP degrader-2	PROTACs SNIPERs YAP IAP	Cancer
PROTAC TEAD1/IAP degrader-2 is an IAP-harnessing TEAD1 PROTAC degrader, with a DC₅₀ of 170 nM against TEAD1 in NCI-H2052 cells. PROTAC TEAD1/IAP degrader-2 exhibits moderate antiproliferative activity in Hippo pathway-dependent mesothelioma cells. PROTAC TEAD1/IAP degrader-2 inhibits the expression of CTGF, but with a weaker effect than the TEAD inhibitor VT-107 (HY-134957). PROTAC TEAD1/IAP degrader-2 can be used in mesothelioma-related research .

HY-181594

PROTAC TEAD/IAP degrader-1	PROTACs SNIPERs YAP	Cancer
PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma .

HY-P992430

OI-3	Transmembrane Glycoprotein Radionuclide-Drug Conjugates (RDCs)	Inflammation/Immunology Cancer
OI-3 is a monoclonal antibody targeting CD146 (MCAM). OI-3 specifically binds to CD146 on the surface of human mesothelioma cells and undergoes endocytosis; both chimeric (chOI-3) and murine (mOI-3) variants possess this activity. When conjugated with ²¹²Pb to form ²¹²Pb-TCMC-OI-3, OI-3 acts as a cytotoxic agent that delivers α-emitting radionuclides to induce targeted cytotoxicity. OI-3 can be used in research related to malignant peritoneal mesothelioma .

HY-186118

TEAD ligand 6	Ligands for Target Protein for PROTAC YAP	Neurological Disease Cancer
TEAD ligand 6 is a TEAD ligand. TEAD ligand 6 serves as a ligand for target protein for PROTAC (Ligands for Target Protein for PROTAC) and is used to develop and design PROTAC-based TEAD degraders, such as KG-FP-003 (HY-186117). TEAD ligand 6 applies to glioblastoma research .

HY-183728

LC-TEAD01	YAP	Cancer
LC-TEAD01 is a potent covalent transcription enhancer-associated domain (TEAD) inhibitor with an IC₅₀ of 116 nM and a K_i of 0.132 μM. LC-TEAD01 disrupts the TEAD-YAP interaction and inhibits TEAD-dependent transcriptional activity. LC-TEAD01 suppresses the proliferation of NF2-deficient cancer cells. LC-TEAD01 inhibits tumor growth in NF2-deficient xenograft models. LC-TEAD01 can be used in studies related to NF2-deficient malignant pleural mesothelioma .

HY-182672

VT101	YAP	Cancer
VT101 is a TEAD inhibitor with an IC₅₀ of 454 nM. VT101 is applicable for cancer research .

製品番号	製品名	Target	研究分野	Image

HY-P992430

OI-3	Transmembrane Glycoprotein Radionuclide-Drug Conjugates (RDCs)	Inflammation/Immunology Cancer
OI-3 is a monoclonal antibody targeting CD146 (MCAM). OI-3 specifically binds to CD146 on the surface of human mesothelioma cells and undergoes endocytosis; both chimeric (chOI-3) and murine (mOI-3) variants possess this activity. When conjugated with ²¹²Pb to form ²¹²Pb-TCMC-OI-3, OI-3 acts as a cytotoxic agent that delivers α-emitting radionuclides to induce targeted cytotoxicity. OI-3 can be used in research related to malignant peritoneal mesothelioma .

Kushenol A 4 Publications Verification Leachianone E	Flavonoids Classification of Application Fields Leguminosae Flavonones Phenols Polyphenols Sophora flavescens Aiton Plants Disease Research Fields Source Classification Cancer	Tyrosinase Glycosidase
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC₅₀ and K_ivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC₅₀: 45 μM; K_i: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .

Mulberrofuran G	Phenols Polyphenols Plants Moraceae Morus alba Linn. Source Classification	Tyrosinase NADPH Oxidase HBV SARS-CoV Reactive Oxygen Species (ROS) JAK STAT Apoptosis Caspase PARP
Mulberrofuran G is a NOX inhibitor (IC₅₀: 6.9 μM) and tyrosinase inhibitor. Mulberrofuran G exhibits anti-inflammatory, antioxidant, antiviral, antitumor, and neuroprotective effects. Mulberrofuran G can be used in the research of tumors, nervous system diseases, and other conditions .

19-Hydroxy-10-deacetylbaccatin III	Terpenoids Taxaceae Diterpenoids Plants Source Classification Taxus chinensis (Pilger) Rehd.	Others
19-Hydroxy-10-deacetylbaccatin III (compound 13) is a taxane with potential antitumor activity. 19-Hydroxy-10-deacetylbaccatin III has weak cytotoxicity against A498 and NCI-H226 cell lines. The study found that the inhibition rates of 30 μg/mL 19-Hydroxy-10-deacetylbaccatin III on A498, NCI-H226 and PC-3 were 16.6% and 32% respectively .

10-Deacetyl-13-oxobaccatin III	Terpenoids Taxaceae Diterpenoids Plants Taxus baccata L. Source Classification	Others
10-Deacetyl-13-oxobaccatin III is an taxane that can be isolated from Taxus sumatrana. 10-Deacetyl-13-oxobaccatin III (30 μg/mL) shows cytotoxicity against A498, NCI-H226, A549, PC-3 cells, with inhibition a rate of 29.7%, 49.2%, 43.9%, 65.3% .

製品番号	製品名		Classification

HY-159119

hDHODH-IN-15		Alkynes
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC₅₀ of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC₅₀ of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .

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