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off-target cytotoxicity

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By Targets:	17β-HSD (2) Acetyl-CoA synthetase (1) ADC Payload (1) Apoptosis (1) ClpP (1) Dengue Virus (1) DNA/RNA Synthesis (1) Drug-Linker Conjugates for ADC (1) Endogenous Metabolite (1) Itk (1) Microtubule/Tubulin (1) Parasite (1) Transmembrane Glycoprotein (1)
By Research Areas:	Cancer (6) Infection (2) Inflammation/Immunology (1) Neurological Disease (1)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P99650

Grisnilimab WT1	Transmembrane Glycoprotein	Cancer
Grisnilimab (WT1) is an IgG2a monoclonal antibody targeting CD7. Grisnilimab only binds to lymphoid tissues and T lymphocytes, with no off-target binding to normal tissues. Grisnilimab can be used to synthesize the immunotoxin WT1-SMPT-dgRTA, which exerts cytotoxic effects on T-lymphoblastic leukemia cells. Grisnilimab is applicable to relevant research on leukemia .

HY-172199

THX6	ClpP	Cancer
THX6 is an hClpP activator with an EC₅₀ of 1.18 μM. THX6 improves off-target profile with no affinity for hD2R and only weak affinity for hD3R (K_i = 51.1 µM) in HEK293 cells. THX6 shows good cytotoxicity in ONC201-resistant cells with an IC₅₀ of 0.13 μM. THX6 changes the levels of fatty acids (PUFAs, MUFAs, and SFAs) in DIPG cells. THX6 decreases the level of proteins involved in oxidative phosphorylation, biogenesis, and mitophagy proteins, thereby resulting in a global collapse of mitochondrial integrity and function. THX6 can be used for diffuse intrinsic pontine glioma research .

HY-145951

Amidate-VC-PAB-MMAF	Drug-Linker Conjugates for ADC	Cancer
Amidate-VC-PAB-MMAF consists a cleavable ADC linker (Amidate-VC-PAB) and a potent tubulin polymerization inhibitor (MMAF). Amidate-VC-PAB-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs). Amidate-VC-PAB-MMAF reduces off-target cytotoxicity of ADCs .

HY-155534

17β-HSD10-IN-1	17β-HSD	Others
17β-HSD10-IN-1 (compound 9) is an orally active inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with blood-brain permeability. 17β-HSD10-IN-1 doesn't result additional effects for mitochondrial off-targets and cytotoxic or neurotoxic effects .

HY-16984

GNE-4997	Itk	Inflammation/Immunology
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a K_i of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity .

HY-164107

Auristatin S	ADC Payload Microtubule/Tubulin	Cancer
Auristatin S is an Auristatin payload with potent antitumor activity. Auristatin S attenuates bystander activity with improved off-target toxicity. Auristatin S has excellent tolerability in Karpas/KarpasBVR cell models. Auristatin S can be used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types .

HY-174212

MXC-017	Apoptosis	Cancer
MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.

HY-114939

Phelorphan	DNA/RNA Synthesis	Others
Phelorphan is a purine MTH1 inhibitor identified through chemical array screening. Although it targets cellular MTH1, its cytotoxicity to cancer cells is weaker than that of other reported inhibitors. The cytotoxicity of MTH1 inhibitors may be attributed to off-target effects, and MTH1 is not essential for cancer cell survival.

HY-175368

DENV-IN-13	Dengue Virus	Infection
DENV-IN-13 (Compound 30) is a DENV2 protease inhibitor with an EC₅₀ of 9.8  μM for DENV2 protease in HeLa cells. DENV-IN-13 has potent antiviral activity with negligible cytotoxicity and no inhibition of the off-targets thrombin and trypsin. DENV-IN-13 can be used for flaviviral infections research .

HY-155535

17β-HSD10-IN-2	17β-HSD	Neurological Disease
17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor，targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10)，a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer .

HY-111094

NPD7155	Endogenous Metabolite	Cancer
NPD7155 is a purine-based competitive inhibitor of MTH1, designed to target cancer cells while exhibiting off-target effects that contribute to its cytotoxicity.

HY-182685

MMV693183	Acetyl-CoA synthetase Parasite	Infection
MMV693183 is an orally active inhibitor of Plasmodium falciparum acetyl-CoA synthetase (AcAS), with an IC₅₀ of 300 nM against Plasmodium falciparum. MMV693183 exhibits potent inhibitory activity against clinical isolates of malaria parasites, including Artemisinin (HY-B0094)-resistant strains. MMV693183 is metabolized in vivo into the active antimetabolite CoA-MMV693183, which exerts effects of killing asexual blood-stage parasites and blocking transmission to Anopheles mosquitoes by binding to and inhibiting the function of acetyl-CoA synthetase, thereby reducing the levels of acetyl-CoA and 4'-phosphopantetheine. In humanized mouse models, MMV693183 shows favorable in vivo efficacy, drug-like properties, and no significant cytotoxicity or off-target activity against human cells. MMV693183 is widely used in malaria-related research as a parasiticide and metabolic disruptor .

Cat. No.	Product Name	Target	Research Area	Image

HY-P99650

Grisnilimab WT1	Transmembrane Glycoprotein	Cancer
Grisnilimab (WT1) is an IgG2a monoclonal antibody targeting CD7. Grisnilimab only binds to lymphoid tissues and T lymphocytes, with no off-target binding to normal tissues. Grisnilimab can be used to synthesize the immunotoxin WT1-SMPT-dgRTA, which exerts cytotoxic effects on T-lymphoblastic leukemia cells. Grisnilimab is applicable to relevant research on leukemia .

17β-HSD10-IN-1	Monophenols Classification of Application Fields Other Diseases Phenols Endogenous metabolite Disease Research Fields Source Classification	17β-HSD
17β-HSD10-IN-1 (compound 9) is an orally active inhibitor of 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10) with blood-brain permeability. 17β-HSD10-IN-1 doesn't result additional effects for mitochondrial off-targets and cytotoxic or neurotoxic effects .

17β-HSD10-IN-2	Monophenols Neurological Disease Classification of Application Fields Ketones, Aldehydes, Acids Phenols Endogenous metabolite Disease Research Fields Source Classification	17β-HSD
17β-HSD10-IN-2 (compound 11) is a benzothiazolylurea-based inhibitor，targeting to 17β-hydroxysteroid dehydrogenase type 10 (17β-HSD10)，a multifunctional mitochondrial enzyme. 17β-HSD10-IN-2 don't lead to mitochondrial off-targets and cytotoxic or neurotoxic effects. 17β-HSD10 inhibitors can be used for research in Alzheimer's disease (AD) and hormone-dependent cancer .

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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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off-target cytotoxicity

Inhibitors & Agonists

Inhibitory Antibodies

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