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tdi

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By Targets:	Adenylate Cyclase (2) Amyloid-β (1) Apoptosis (1) Biochemical Assay Reagents (1) Cyclic GMP-AMP Synthase (1) Cytochrome P450 (1) DNA Methyltransferase (1) Epigenetic Reader Domain (1) Histone Methyltransferase (2) Large Tumor Suppressor (LATS) (1) MAP4K (1) Parasite (1) PARP (1) SARS-CoV (2) STING (1) TNF Receptor (1) YAP (1)
By Research Areas:	Cancer (5) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (2)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-150042

TDI-011536 3 Publications Verification	Large Tumor Suppressor (LATS) YAP	Cardiovascular Disease Others
TDI-011536 is a potent Lats kinase inhibitor, interrupts Hippo-Yap signaling and initiates the proliferation of lesioned heartmuscle cells. TDI-011536 can be used in studies of organ conservation and regeneration .

HY-151798

TDI-11861	Adenylate Cyclase	Others
TDI-11861 is an orally active soluble sAC inhibitor optimized and designed based on TDI-10229 (HY-132298), with an IC₅₀ of 3.3 nM and a K_D of 1.4 nM. TDI-11861 has advantages such as high affinity, slow dissociation, and good pharmacokinetics. TDI-11861 can be used for research on male contraception and related sAC pharmacology .

HY-132298

TDI-10229	Adenylate Cyclase	Others
TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC₅₀ of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound .

HY-162350

TDI-11055	Epigenetic Reader Domain Apoptosis	Cancer
TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC₅₀ values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia .

HY-164288

TDI-6570 tdi-006570	Cyclic GMP-AMP Synthase STING	Neurological Disease Inflammation/Immunology
TDI-6570 (TDI-006570) is a blood-brain barrier-permeable, orally active cGAS inhibitor with an IC₅₀ of 1.64 μM. TDI-6570 exhibits high gastrointestinal absorption and a long brain half-life in mice, and shows no toxicity to primary neurons. By inhibiting the cGAS-STING-IFN signaling pathway, TDI-6570 reduces STING levels and the activation of TBK1, blocks double-stranded DNA-induced cGAS activation and downstream interferon-stimulated gene expression, thereby reducing tau protein spread and improving synaptic loss. TDI-6570 reverses memory deficits, increases the amplitude of long-term potentiation, enhances the MEF2C transcriptional network, restores PSD-95 and vGAT punctate structures, and significantly improves cognitive resilience. TDI-6570 can be applied to the research of Alzheimer's disease, Parkinson's disease, systemic lupus erythematosus, as well as various central nervous system and autoimmune diseases .

HY-144330

TDI-6118	Histone Methyltransferase	Cancer
TDI-6118 (Compound 5) is a potent brain-penetrant inhibitor of EZH2. EZH2-IN-12 has the potential for the research of central nervous system malignancies .

HY-170524

TDI-015051	SARS-CoV DNA Methyltransferase Cytochrome P450	Infection
TDI-015051 is a highly selective, orally active antiviral agent that targets the coronavirus NSP14 guanine-N7 methyltransferase. TDI-015051 binds to substrates in a non-competitive manner and forms a stable ternary complex, precisely blocking the capping and methylation processes of viral mRNA. TDI-015051 potently inhibits a variety of coronaviruses (including SARS-CoV-2 and MERS). By impairing viral replication and translation and inducing a moderate type I interferon-mediated immune response, it significantly reduces pulmonary viral load and exhibits a synergistic effect with Nirmatrelvir (HY-138687). In addition, TDI-015051 does not inhibit non-coronavirus methyltransferases, and the drug-resistant mutations it induces impair viral fitness, demonstrating excellent antiviral properties and safety. TDI-015051 can be used for research on COVID-19 and the replication mechanism of coronaviruses .The IC₅₀ values of TDI-015051 against SARS-CoV-2, α-hCoV-NL63, α-hCoV-229E, β-hCoV-MERS are 0.15 nM, 1.7 nM, 2.6 nM and 3.6 nM, respectively, and the K_a value against SARS-CoV-2 is 0.061 nM .

HY-121815

TDI-2760	Amyloid-β	Neurological Disease
TDI-2760 is an Aβ aggregation inhibitor with an IC₅₀ of 1.67 μM. TDI-2760 can inhibit the Aβ-fibrinogen interaction and Aβ aggregation, and also modulate the contact system activation induced by Aβ42. TDI-2760 can be used in research related to vascular abnormalities and Aβ aggregation in Alzheimer's disease .

HY-161079

TDI-8304	Parasite	Infection
TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent Plasmodium falciparum (Pf20S) inhibitor. TDI-8304 shows highly selective for Pf20S over human proteasomes .

HY-173349

TDI-012804	PARP	Cancer
TDI-012804 is a TNKS2 inhibitor that selectively inhibits intracellular endogenous TNKS2 protein. TDI-012804 increases the expression of AXIN1 protein in cells that are heterozygous (Tnks1HET) and completely knocks out (Tnks1KO) for TNKS1. TDI-012804 inhibits the proliferation of ApcQ1405X/Tnks1KO organoids (EC₅₀ of 59.1 nM) and is selectively toxic to Tnks1KO AKP-G12D and AKP-G13D organoids .

HY-182448

TDI-11904	Histone Methyltransferase	Cancer
TDI-11904 is a peripherally active EZH2 inhibitor with an EZH2 IC₅₀ of 0.9 nM. TDI-11904 inhibits EZH2 methyltransferase activity, reduces the trimethylation level of H3K27me3, and decreases intracellular H3K27me3 content. TDI-11904 inhibits the proliferation of lymphoma cells. TDI-11904 can be used for the research of lymphoma .

HY-178025

TDI-014925	SARS-CoV	Infection
TDI-014925 (Compound 58) is a SARS-CoV-2 methyltransferase nonstructural protein 14 (NSP14) inhibitor with an IC₅₀ of 0.2 nM. TDI-014925 has an antiviral activity with significant microsomal stability and no CYP inhibitory activity. TDI-014925 can be used for COVID-19 research .

HY-180472

*2,4-TDI* dimer**	Biochemical Assay Reagents	Others
2,4-TDI dimer is a dimer formed by the polymerization of two molecules of toluene-2,4-diisocyanate (2,4-TDI). 2,4-TDI dimer is mainly used for the preparation of long-lasting inner layer materials for solid rocket engines .

HY-123965

PF-06745013	MAP4K TNF Receptor	Metabolic Disease Cancer
PF-06745013 (Compound 37) is a MAP4K4 inhibitor without time-dependent inhibition (TDI) risk of CYP3A4 (IC₅₀ of 0.4  nM for MAP4K4). PF-06745013 has no accumulation CNS-impaired and non-ATP competitive activities in mouse models. PF-06745013 can be used for inflammatory diseases like diabetes and cancers research .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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tdi

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