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Results for "

in vivo efficacy

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (2) Akt (1) Amyloid-β (1) Androgen Receptor (1) Antibiotic (3) Apoptosis (10) Autophagy (1) Bacterial (11) Bcl-2 Family (2) Bcr-Abl (1) Btk (1) c-Fms (1) c-Kit (1) c-Met/HGFR (2) Calcium Channel (2) Cannabinoid Receptor (1) Caspase (1) CDK (2) DNA/RNA Synthesis (2) Drug-Linker Conjugates for ADC (1) EGFR (3) ERK (2) FGFR (1) GABA Receptor (2) Glucosidase (1) GLUT (2) HBV (1) HDAC (5) Histone Demethylase (1) Histone Methyltransferase (1) HSP (1) Isotope-Labeled Compounds (2) Itk (1) JAK (2) JNK (1) Lipoxygenase (1) LPL Receptor (1) MAP4K (1) MDM-2/p53 (1) Melanocortin Receptor (1) MNK (1) mTOR (1) NADPH Oxidase (1) Necroptosis (1) NF-κB (1) PAK (1) Parasite (1) PARP (1) PD-1/PD-L1 (2) PDGFR (1) Phosphodiesterase (PDE) (2) PI3K (1) PI4K (1) Pim (1) Potassium Channel (1) PPAR (1) PROTACs (3) Raf (1) Ras (1) RET (1) Serotonin Transporter (2) SHP2 (1) TAM Receptor (1) Topoisomerase (3) Trk Receptor (1) URAT1 (1) α-synuclein (1)
By Research Areas:	Cancer (44) Cardiovascular Disease (1) Endocrinology (1) Infection (13) Inflammation/Immunology (8) Metabolic Disease (4) Neurological Disease (8)
Click Chemistry:	Alkynes (1)

Inhibitors & Agonists

Screening Libraries

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Inhibitory Antibodies

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Isotope-Labeled Compounds

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Targets Recommended: AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

HY-155250

Antibacterial agent 154	Bacterial	Infection
Antibacterial agent 154 (compound 7) is a derivative of Fluoroqinolones and is an orally effective antibacterial agent. Antibacterial agent 154 inhibits Gram-positive and Gram-negative bacteria. Antibacterial agent 154 demonstrated in vivo efficacy in a mouse model of staphylococcal sepsis .

HY-155146

Anticancer agent 146	Necroptosis	Cancer
Anticancer agent 146 (compound 1.19) is a necroptosis inducer. Anticancer agent 146 has anti-tumor efficacy in the mouse MDA-MB-231 xenograft model .

HY-132893

AZ14145845

TAM Receptor Cancer

AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
HY-157302

c-Met-IN-21

c-Met/HGFR Cancer

c-Met-IN-21 (compound 54) is a c-met inhibitor with an IC₅₀ value of 0.45? nM, and shows anti-tumor efficacy in vivo .

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

c-Met-IN-21	c-Met/HGFR	Cancer
c-Met-IN-21 (compound 54) is a c-met inhibitor with an IC₅₀ value of 0.45? nM, and shows anti-tumor efficacy in vivo .

HY-P2108

Lysobactin	Antibiotic Bacterial	Infection
Lysobactin, produced by several genera of Gram-negative gliding bacteria found in soil, is a potent antibiotic with in vivo efficacy against Staphylococcus aureus and Streptococcus pneumoniae .

HY-141896

RET-IN-7

RET Cancer

RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.
HY-124674

CCT365623

Lipoxygenase Cancer

CCT365623 is a potent and orally active LOX inhibitor with an IC₅₀ of 0.9 μM. CCT365623 has potent anti-metastatic efficacy in vivo .

RET-IN-7	RET	Cancer
RET-IN-7 demonstrates potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice.

CCT365623	Lipoxygenase	Cancer
CCT365623 is a potent and orally active LOX inhibitor with an IC₅₀ of 0.9 μM. CCT365623 has potent anti-metastatic efficacy in vivo .

HY-112240

Antibacterial agent 104	Antibiotic Bacterial	Infection
Antibacterial agent 104 (Compound 7) is a potent antibacterial agent. Antibacterial agent 104 displays excellent antibacterial activity in vitro and good efficacy in vivo against MRSA .

HY-12246

XEN445 1 Publications Verification	Others	Cardiovascular Disease
XEN445 is a potent and selective EL inhibitor(IC50=0.237 uM), that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.

HY-118269

OSI-296	c-Met/HGFR	Cancer
OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated .

HY-107561

A-943931 hydrochloride	Others	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 .

HY-146185

CCT373566	Bcl-2 Family	Cancer
CCT373566 is a potent and orally active 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 .

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 .

HY-121827

LH21	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 .

HY-W112166A

4,4'-Dicyanostilbene	Bacterial	Infection
4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC₅₀ of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA) .

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 .

HY-149430

YIAD-0205	Amyloid-β	Neurological Disease
YIAD-0205 is an orally available Aβ(1?42) aggregation inhibitor. YIAD-0205 demonstrated in vivo efficacy in an AD transgenic mouse model with five familial AD mutations (5XFAD) .

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 .

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 .

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 .

HY-152033

URAT1 inhibitor 4	URAT1 GLUT	Metabolic Disease
URAT1 inhibitor 4, a Lesinurad derivative, is a potent and orally active URAT1 inhibitor with an IC₅₀ of 7.56 μM. URAT1 inhibitor 4 has higher in vivo urate-lowering efficacy than Lesinurad (HY-15258) .

HY-163073

Anti-MRSA agent 9	Bacterial	Infection
Anti-MRSA agent 9 (compound 39) shows antibacterial effects against clinically isolated methicillin-resistant Staphylococcus aureus (MRSA) with MIC values of 1 μg/ml. Anti-MRSA agent 9 also shows anti-MRSA efficacy in vivo .

HY-108974

Drotaverine hydrochloride	Phosphodiesterase (PDE) Calcium Channel
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.

HY-143444

JAK-IN-20	JAK	Inflammation/Immunology
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 .

HY-149759

SHP2-IN-23	SHP2 ERK	Cancer
SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC₅₀=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC₅₀=5 nM .

HY-162171

Antibacterial agent 179	Bacterial	Infection
Antibacterial agent 179 (Compound 23) is a potent antibacterial agent, which effectively kills both Gram-negative and Gram-positive bacteria. Antibacterial agent 179 shows potent in vivo antibacterial efficacy in murine corneal infection models caused by Staphylococcus aureus or Pseudomonas aeruginosa .

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 .

HY-149429

PPARδ agonist 9	PPAR	Metabolic Disease
PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC₅₀: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) .

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 .

HY-14262

Vilazodone 3 Publications Verification 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 .

HY-145688

HDAC-IN-33	HDAC	Cancer
HDAC-IN-33 is a potent HDAC inhibitor with IC₅₀s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity .

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 .

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 .

HY-158081

CRN04894	Melanocortin Receptor	Endocrinology
CRN04894 (compound 17h) is an orally active MC2R antagonist that demonstrates in vivo efficacy in rat model of adrenocorticotropic hormone (ACTH)-stimulated corticosterone secretion[1]. CRN04894 binds to human or rat MC2R with K_B values of 0.34 nM and 0.23 nM, respsectively .

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 (K_i= 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 . .

HY-112081

BAY-707	DNA/RNA Synthesis	Cancer
BAY-707 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 .

HY-115581

Thymidine 3',5'-disphosphate Deoxythymidine 3′,5′-diphosphate; pdTp	Apoptosis	Cancer
Thymidine 3',5'-disphosphate (Deoxythymidine 3′,5′-diphosphate; pdTp) is a selective small molecule inhibitor of staphylococcal nuclease and tudor domain containing 1 (SND1, the miRNA regulatory complex RISC subunit) and inhibits SND1 activity. Thymidine 3',5'-disphosphate exhibits anti-tumor efficacy in vivo .

HY-145687

HDAC-IN-32	HDAC	Cancer
HDAC-IN-32 is a potent HDAC inhibitor with IC₅₀s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity .

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].

HY-118032

Bozepinib	Apoptosis Autophagy JNK ERK	Cancer
Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice .

HY-138364

YUM70 1 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 .

HY-108974S

Drotaverine-d10 hydrochloride	Isotope-Labeled Compounds Phosphodiesterase (PDE) Calcium Channel
Drotaverine-d₁₀ (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. 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[1][2].

HY-139782

SKLB325	Histone Demethylase Apoptosis	Cancer
SKLB325 is a Jumonji domain-containing 6 (JMJD6) inhibitor with a binding affinity (K_D) 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) .

HY-149065

D-685	α-synuclein	Neurological Disease
D-685, a prodrug of D-520, exhibits higher in vivo anti-Parkinsonian efficacy in a reserpinized Parkinson's disease (PD) animal model than the parent D-520. D-685 reduces accumulation of human α-synuclein (α-syn) protein. D-685 exhibits facile brain penetration .

HY-19925

AIC-292
AIC-292 is a potent and selective inhibitor of HIV-1 nonnucleoside reverse transcriptase. AIC-292 inhibits wild-type HIV-1 laboratory strains at low nanomolar concentrations. AIC-292 displays potent antiviral in vivo efficacy in a mouse xenograft model. AIC-292 has the potential for the research of HIV-1 infection .

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 .

HY-W112166

(E/Z)-4,4'-Dicyanostilbene	Others	Infection
(E/Z)-4,4'-Dicyanostilbene is the isomer of 4,4'-Dicyanostilbene (HY-W112166A), and can be used as an experimental control. 4,4'-Dicyanostilbene (compound 43) is a potent antimalarial agent against the Dd2 strain, with an EC₅₀ of 27 nM. 4,4'-Dicyanostilbene exhibits in vivo efficacy against methicillin-resistant Staphylococcus aureus (MRSA) .

HY-163084

HJ445A	Others	Cancer
HJ445A is a potent MYOF inhibitor and binds to the MYOF-C2D domain with a K_D 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 .

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 .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N12044

Asparanin A	Structural Classification Polysaccharides Liliaceae Source classification Plants Saccharides Asparagus officinalis L.	Apoptosis
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 .

HY-122292

Celastramycin A	Structural Classification Animals Antibiotics Source classification	Antibiotic Bacterial
Celastramycin A is an antibiotic isolated from Streptomyces MaB-QuH-8, which exhibits antimicrobial activity against series of gram-negative bacteria and mycobacteria, with MICs between 0.05-3.1 μg/ml . Celastramycin A exhibits immunosuppressing efficacy in ex vivo Drosophila through immune deficiency pathway (IC₅₀ of 0.008 μg/ml), inhibits the immunoresponse in human innate immunity through TNF-α signaling, inhibits IL-8 production in HUEVCs with IC₅₀ of 0.06 μg/ml .

Cat. No.	Product Name	Chemical Structure

HY-108974S

Drotaverine-d10 hydrochloride

Drotaverine-d₁₀ (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. 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[1][2].