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In vivo efficacy

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Targets Recommended:
Cat. No. Nombre del producto Target Áreas de investigación Chemical Structure
  • HY-30272
    Monobenzone
    1 Publications Verification

    		 Hapten Cancer
    Monobenzone is a potent skin depigmenting agent. Monobenzone induces depigmentation and exhibits good potential for vitiligo research. Monobenzone is a potent inhibitor of RNR (Ribonucleotide reductase) enzyme activity by targeting RRM2 (a regulatory small subunit M2 of RNR) protein, and thus has significant anti-leukemia efficacy in vitro and in vivo. Monobenzone inhibits acute myeloid leukemia (AML) cells proliferation and DNA synthesis, induces cell cycle arrest, and Apoptosis .
    Monobenzone
  • HY-14262
    Vilazodone
    5+ Cited Publications

    EMD 68843; SB659746A

    		 5-HT Receptor Serotonin Transporter Neurological Disease
    Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
    Vilazodone
  • HY-139782
    SKLB325
    2 Publications Verification

    		 Histone Demethylase Apoptosis Cancer
    SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (KD) value of 0.755 μM, and the IC50 value of 0.7797 μM. SKLB325 exhibits antitumor effects on ovarian cancer in vivo and in vitro. SKLB325 induces apoptosis . SKLB325 exhibits remarkable antitumor efficacy in renal cell carcinoma (RCC) .
    SKLB325
  • HY-138364
    YUM70
    3 Publications Verification

    		 HSP Apoptosis Cancer
    YUM70 is a potent and selective inhibitor of glucose-regulated protein 78 (GRP78), with an IC50 of 1.5 μM for inhibiting GRP78 ATPase activity of the full-length protein. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. YUM70 also has in vivo efficacy in a pancreatic cancer xenograft model .
    YUM70
  • HY-137464A
    OATD-01
    1 Publications Verification

    		 Glycosidase Inflammation/Immunology
    OATD-01 is a highly potent, first-in-class, orally active and selective chitinase inhibitor with low nanomolar activity toward CHIT1 (hCHIT1,IC50=23 nM). OATD-01 shows excellect PK profile in multiple species and is selectivity against a panel of other off-targets. OATD-01 exhibits significant antifibrotic efficacy in vivo and can be used for pulmonary fibrosis (IPF) research .
    OATD-01
  • HY-108584
    Flindokalner

    BMS-204352

    		 Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo .
    Flindokalner
  • HY-151561
    WM382

    		Parasite Infection
    WM382 is an orally active and potent dual plasmepsin IX/X (PMIX/X) inhibitor with IC50 values of 1.4 nM and 0.03 nM, respectively. WM382 has robust in vivo efficacy at multiple stages of the malaria parasite life cycle and an excellent resistance profile .
    WM382
  • HY-108974
    Drotaverine hydrochloride

    		Phosphodiesterase (PDE) Calcium Channel Neurological Disease
    Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
    Drotaverine hydrochloride
  • HY-132822
    Ivospemin

    SBP-101

    		 Drug Derivative Cancer
    Ivospemin (SBP-101) is an antineoplastic spermine analog. Ivospemin has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin is promising for research of cancers .
    Ivospemin
  • HY-132893
    AZ14145845

    		TAM Receptor Cancer
    AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
    AZ14145845
  • HY-146185
    CCT373566

    		Molecular Glues Bcl-2 Family Cancer
    CCT373566 is a potent and orally active molecular glue degrader of transcriptional repressor BCL6, with an IC50 of 2.2 nM. CCT373566 shows strong antiproliferative efficacy in vitro and reduction in tumor growth in vivo .
    CCT373566
  • HY-P4072A
    (D)-PPA 1 TFA

    		PD-1/PD-L1 Cancer
    (D)-PPA 1 TFA is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 TFA serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 TFA binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy .
    (D)-PPA 1 TFA
  • HY-112081
    BAY-707

    		DNA/RNA Synthesis Cancer
    BAY-707, a chemical probe, is a substrate-competitive, highly potent and selective inhibitor of MTH1(NUDT1) with an IC50 of 2.3 nM. BAY-707 has a good pharmacokinetic (PK) profile to other MTH1 compounds and is well-tolerated in mice, but shows a clear lack of in vitro or in vivo anticancer efficacy .
    BAY-707
  • HY-14826
    Tilivapram

    AVE8112

    		 Phosphodiesterase (PDE) Neurological Disease
    Tilivapram (AVE8112) is an orally active PDE4 inhibitor with procognitive effects. Tilivapram exhibits in vivo efficacy and improves processing speed and psychomotor speed. Oral administration of tilivapram may induce dose-related adverse reactions such as nausea and dizziness, but transdermal delivery enables slow, controlled elevation of plasma concentrations, thereby significantly reducing gastrointestinal discomfort and dizziness. Tilivapram is applicable to research related to neuropsychiatric disorders .
    Tilivapram
  • HY-149428
    AD4
    1 Publications Verification

    		 PROTACs Cancer
    AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
    AD4
  • HY-156331
    VU6004909

    		mGluR Neurological Disease
    VU6004909 is a blood-brain barrier penetrated mGlu1 positive allosteric modulator (PAM), with the EC50s of 25.7 nM and 31 nM for human mGlu1 and rat mGlu1, respectively. VU6004909 reduces dorsolateral striatal dopamine (DA) release in vivo and displays antipsychotic efficacy .
    VU6004909
  • HY-163084
    HJ445A

    		Myosin Cancer
    HJ445A is a potent MYOF inhibitor and binds to the MYOF-C2D domain with a KD of 0.17 μM. HJ445A potently repressed the proliferation of gastric cancer cells with IC50 values of 0.16 and 0.14 μM in MGC803 and MKN45, respectively. HJ445A demonstrates superior antitumor efficacy in vivo and can be used for cancer research .
    HJ445A
  • HY-143444
    JAK-IN-20

    		JAK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo .
    JAK-IN-20
  • HY-160649
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan

    		Drug-Linker Conjugates for ADC Topoisomerase Cancer
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan (HY-13631) with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo .
    MC-Gly-Gly-Phe-Gly-GABA-Exatecan
  • HY-108493
    CS-2100

    		LPL Receptor Inflammation/Immunology
    CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR .
    CS-2100
  • HY-150023
    BI-1622

    		EGFR Itk PI4K Btk CDK Raf JAK Cancer
    BI-1622 is an orally active, potent and highly selective HER2 (ERBB2) inhibitor, with an IC50 of 7 nM. BI-1622 shows greater than 25-fold selectivity over EGFR. BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models with engineered H2170 and PC9 cells and had a favorable agent metabolism and pharmacokinetics profile .
    BI-1622
  • HY-179024
    NP3-742

    		NOD-like Receptor (NLR) Interleukin Related Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    NP3-742 is an orally active NLRP3 inhibitor that binds to the NLRP3 NACHT domain. NP3-742 inhibits IL-1β release with IC50s of 6 nM and 47 nM in both the cellular and whole blood assays, respectively. NP3-742 is highly selective against a panel of more than 50 enzymes, receptors and sodium and calcium channels. NP3-742 can be used for the study of gout, cardiovascular disease or osteoarthritis .
    NP3-742
  • HY-W1117786
    Nampt-IN-10

    		ADC Payload NAMPT Cancer
    Nampt-IN-10 (Compound 4) is an efficient inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). Nampt-IN-10 exhibits nanomolar-level inhibitory activity against cell lines such as MDA-MB453, NCI-N87, and NCI-H526. Nampt-IN-10 can be used as an ADC payload, and the ADC constructed with it as the core demonstrates significant anti-tumor activity .
    Nampt-IN-10
  • HY-179392
    Sunitinib-platinum(IV) prodrug-1

    		Apoptosis DNA Alkylator/Crosslinker VEGFR PDGFR Cancer
    Sunitinib-platinum(IV) prodrug-1 (Complex A) is a Pt(IV) prodrug based on Cisplatin (HY-17394), and this design aims to enable Pt(IV) to be reduced to active Pt(II) under intracellular reducing conditions, while simultaneously releasing a derivative of Sunitinib (HY-10255A) with tyrosine kinase inhibitor (TKI) activity. Sunitinib-platinum(IV) prodrug-1 exhibits excellent cytotoxicity against renal cell carcinoma (RCC), causing DNA crosslinking and apoptosis. Sunitinib-platinum(IV) prodrug-1 inhibits the VEGFR/PDGFR signaling pathway, suppressing tumor growth and angiogenesis. Sunitinib-platinum(IV) prodrug-1 can be used for research on renal cell carcinoma .
    Sunitinib-platinum(IV) prodrug-1
  • HY-107561
    A-943931 hydrochloride

    		Histamine Receptor Inflammation/Immunology
    A-943931 (Compound 10) is a histamine H4 receptor antagonists. A-943931 has improved pharmacotropic and in vivo efficacy in models of pain and inflammation. A-943931 can be used in vivo anti-inflammatory and anti-nociception research .
    A-943931 hydrochloride
  • HY-163149
    AB-452

    		HBV Infection
    AB-452, a Dihydroquinolizinone (DHQ) analogue, is a potent and orally active HBV RNA destabilizer. AB-452 inhibits PAPD5/7 proteins in vitro with good in vivo efficacy in a chronic HBV mouse model .
    AB-452
  • HY-146397
    TD-802

    		PROTACs Androgen Receptor Cancer
    TD-802 (Compound 33c) is an androgen receptor (AR) PROTAC degrader with good microsomal stability. TD-802 has good antitumor efficacy in vivo and can be used for metastatic castration-resistant prostate cancer research .
    TD-802
  • HY-130628
    PAK4-IN-1

    		PAK Cancer
    PAK4-IN-1 (Compound 19) is a potent, selective, orally active PAK4 inhibitor with robust anti-tumor efficacy in vivo. PAK4-IN-1 is stable under both acidic and neutral conditions .
    PAK4-IN-1
  • HY-P4072
    (D)-PPA 1

    		PD-1/PD-L1 Cancer
    (D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy .
    (D)-PPA 1
  • HY-P3350
    LS-BF1

    		Bacterial Infection
    LS-BF1 is a stable and low toxic cationic antimicrobial peptide. LS-BF1 displays broad spectrum of antibacterial activity, including the challenging ESKAPE pathogens, by cell membrane disruptive mechanism. LS-BF1 shows good in vivo efficacy for elimination of bacteria in a mouse infection model[1].
    LS-BF1
  • HY-177740
    BTX306

    		Molecular Glues Apoptosis Caspase Cancer
    BTX306 is a cereblon-targeting molecular glue degrader. BTX306 reduces myeloma cell viability and induces apoptosis. BTX306 overcomes myeloma cell resistance to Lenalidomide (HY-A0003) or Bortezomib (HY-10227). BTX306 is active against primary myeloma cells, and shows efficacy in vivo. BTX306 can be used for myeloma research .
    BTX306
  • HY-178504
    Lug-15

    		Bacterial Infection
    Lug-15 is a rapid bactericidal agent. Lug-15 exhibits strong antibacterial activity against both Gram-positive and Gram-negative bacteria, including drug-resistant strains. Lug-15 rapidly kills bacteria primarily through membrane disruption and had a very low propensity to induce bacterial resistance. Lug-15 demonstrates low hemolytic toxicity and significant therapeutic potential in various infection models. Lug-15 can be used for research on combating infections caused by multi-drug resistant bacteria .
    Lug-15
  • HY-178762S
    RIPK1-IN-35

    		RIP kinase Necroptosis Inflammation/Immunology
    RIPK1-IN-35 is a selective and orally active RIPK1 inhibitor with an IC50 of 5.33 nM. RIPK1-IN-35 has a potent protective effect against necroptosis in both human and murine cells. RIPK1-IN-35 shows good therapeutic effects in both TNF-α-induced systemic inflammatory response syndrome and DSS (HY-116282C)-induced inflammatory bowel disease models. RIPK1-IN-35 can be used to the study of inflammatory diseases related to necroptosis .
    RIPK1-IN-35
  • HY-115814
    AM-1430

    		PI3K Inflammation/Immunology
    AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases .
    AM-1430
  • HY-156511
    ETC-168

    		MNK Cancer
    ETC-168 is a selective and oral active MNK inhibitor with the IC50 values of 23 and 43 nM against MNK1 and MNK2, respectively. ETC-168 shows antiproliferative efficacy in vivo and in vitro .
    ETC-168
  • HY-121827
    LH21
    1 Publications Verification

    		 Cannabinoid Receptor Metabolic Disease
    LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats. , and displays efficacy as a feeding inhibitor .
    LH21
  • HY-162144
    BDM91288

    		Bacterial Infection
    BDM91288 is an orally active AcrB efflux pump inhibitor of pyridinium piperazine. BDM91288 can enhance the in vivo efficacy of levofloxacin (HY-B0330) in the treatment of Klebsiella pneumoniae pulmonary infection in mouse models .
    BDM91288
  • HY-19277
    CP-114271

    		Adrenergic Receptor Metabolic Disease
    CP-114271 is a potent selective β3-adrenergic receptor agonist. CP-114271 possesses an in vivo efficacy in rodent models. CP-114271 can be used for obesity research .
    CP-114271
  • HY-176753
    Lipid 20b

    		Liposome Inflammation/Immunology
    Lipid 20b is a thiophene ionizable cationic lipid. Lipid 20 b can be used to generate lipid nanoparticles (LNPs) for the delivery of mRNA in vivo. Lipid 20b can be studied in research for enhancing mRNA vaccine delivery and transfection efficacy .
    Lipid 20b
  • HY-132822A
    Ivospemin hydrochloride

    SBP-101 hydrochloride

    		 Drug Derivative Cancer
    Ivospemin (SBP-101) hydrochloride is an antineoplastic spermine analog. Ivospemin hydrochloride has shown efficacy in slowing pancreatic and ovarian tumor progression in vitro and in vivo. Ivospemin hydrochloride shows modest induction of polyamine catabolism, but stronger repression of ornithine decarboxylase activity. Ivospemin hydrochloride is promising for research of cancers .
    Ivospemin hydrochloride
  • HY-146697
    IHMT-TRK-284

    		Trk Receptor c-Fms PDGFR Bcr-Abl c-Kit Apoptosis Cancer
    IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
    IHMT-TRK-284
  • HY-133015
    Mcl-1 inhibitor 3

    		Bcl-2 Family Cancer
    Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity .
    .
    Mcl-1 inhibitor 3
  • HY-174424
    NPH16

    		PD-1/PD-L1 Apoptosis Cancer
    NPH16 is an orally active PD-1/PD-L1 inhibitor with an IC50 of 24.4 nM. NPH16 can promote HepG2 cell apoptosis. NPH16 shows excellent in vivo antitumor efficacy and favorable pharmacokinetic properties. NPH16 can be used for the study of liver cancer .
    NPH16
  • HY-164387
    Sutetinib

    		EGFR PDGFR VEGFR Cancer
    Sutetinib is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
    Sutetinib
  • HY-14262S1
    Vilazodone-d8 hydrochloride

    EMD 68843-d8; SB659746A-d8

    		 5-HT Receptor Serotonin Transporter Isotope-Labeled Compounds Neurological Disease
    Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders .
    Vilazodone-d8 hydrochloride
  • HY-N12044
    Asparanin A

    		Apoptosis Cancer
    Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth .
    Asparanin A
  • HY-146811
    HSGN-94

    		Bacterial Inflammation/Immunology
    HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistant Enterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model .
    HSGN-94
  • HY-164387A
    Sutetinib maleate

    		EGFR VEGFR PDGFR Cancer
    Sutetinib maleate is the maleate form of Sutetinib (HY-164387). Sutetinib maleate is an orally active inhibitor for tyrosine kinase, that is associated with tumor growth and angiogenesis, such as VEGFR (Ki= 0.009 µM for VEGFR-1/2/3), PDGFR (Ki= 0.008 µM for PDGFR-α/β) and proto-oncogene cKIT. Sutetinib maleate inhibits the proliferation, migration, and tubular structure formation of endothelial cells and fibroblasts, and exhibits board-spectrum antitumor efficacy in vitro and in vivo .
    Sutetinib maleate
  • HY-169937
    (R)-SR-C-107

    		Epigenetic Reader Domain Cancer
    (R)-SR-C-107 is an orally available inhibitor of ENL (YEAST domain-containing protein) designed to target acute myeloid leukemia (AML). (R)-SR-C-107 targets ENL with IC50 and KD of 40 nM and 144 nM, respectively. (R)-SR-C-107 demonstrates in vivo efficacy in a xenograft mouse model of AML, with a tumor regression rate of 45% at a dose of 200 mg/kg (PO; QD) .
    (R)-SR-C-107
  • HY-135495
    AM-0466

    		Sodium Channel Histamine Receptor Inflammation/Immunology
    AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing .
    AM-0466

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