Search Result

Results for "

antiproliferative efficacy

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (11) Aurora Kinase (1) Bcl-2 Family (1) CDK (3) Cholinesterase (ChE) (1) ClpP (1) DNA Methyltransferase (1) DNA/RNA Synthesis (2) Drug-Linker Conjugates for ADC (1) EGFR (1) Endogenous Metabolite (1) Epigenetic Reader Domain (1) Estrogen Receptor/ERR (1) FGFR (1) HDAC (2) Histone Acetyltransferase (1) HSP (2) HuR (1) MDM-2/p53 (1) Microtubule/Tubulin (6) MMP (2) MNK (1) Molecular Glues (1) mTOR (1) NF-κB (3) P-glycoprotein (2) PARP (2) Pim (1) PPAR (2) Progesterone Receptor (1) PROTACs (2) Ras (1) Reactive Oxygen Species (1) Somatostatin Receptor (2) SWI/SNF Complex (1) VEGFR (1)
By Research Areas:	Cancer (38) Endocrinology (2) Infection (1) Inflammation/Immunology (2) Neurological Disease (1)

By Targets:

Apoptosis (11)

Aurora Kinase (1)

Bcl-2 Family (1)

CDK (3)

Cholinesterase (ChE) (1)

ClpP (1)

DNA Methyltransferase (1)

DNA/RNA Synthesis (2)

Drug-Linker Conjugates for ADC (1)

EGFR (1)

Endogenous Metabolite (1)

Epigenetic Reader Domain (1)

Estrogen Receptor/ERR (1)

FGFR (1)

HDAC (2)

Histone Acetyltransferase (1)

HSP (2)

HuR (1)

MDM-2/p53 (1)

Microtubule/Tubulin (6)

MMP (2)

MNK (1)

Molecular Glues (1)

mTOR (1)

NF-κB (3)

P-glycoprotein (2)

PARP (2)

Pim (1)

PPAR (2)

Progesterone Receptor (1)

PROTACs (2)

Ras (1)

Reactive Oxygen Species (1)

Somatostatin Receptor (2)

SWI/SNF Complex (1)

VEGFR (1)

By Research Areas:

Cancer (38)

Endocrinology (2)

Infection (1)

Inflammation/Immunology (2)

Neurological Disease (1)

Inhibitors & Agonists

Peptides

Natural
Products

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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 .

HY-157516

CDK2-IN-22	CDK	Cancer
CDK2-IN-22 (compound 7I) is a potent CDK2 inhibitor with an IC₅₀ of 64.42 nM. CDK2-IN-22 presents a broad antiproliferative efficacy toward diverse cancer cells MV4-11, HT-29, MCF-7, and HeLa with IC₅₀ values of 0.83 μM, 2.12 μM, 3.12 μM, and 8.61 μM, respectively .

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-P10902

Lorutengitide	DNA/RNA Synthesis	Cancer
Lorutengitide is a transcriptional regulatory peptide, and exhibits antiproliferative efficacy .

HY-163766

Antiproliferative agent-51	Estrogen Receptor/ERR	Cancer
Antiproliferative agent-51 (Compound 18h) exhibits inhibitory efficacy against estrogen receptor α (ERα) mediated transcription, with an IC₅₀ of 1.6 nM. Antiproliferative agent-51 inhibits the proliferation of cancer cell ZR-75, with an IC₅₀ of 0.031 μM. Antiproliferative agent-51 exhibits antitumor efficacy in mouse models .

HY-123891

NS-062	EGFR	Cancer
NS-062 is an orally active, irreversible targeted covalent inhibitor for EGFR, and exhibits antiproliferative efficacy in drug-resistant double mutated H1975 cell with an IC₅₀ of 0.19 μM. NS-062 exhibits antitumor efficacy in mouse H1975 xenograft model .

HY-168102

Antiproliferative agent-59	Microtubule/Tubulin Apoptosis	Cancer
Antiproliferative agent-59 (Compound 14u) is an inhibitor for tubulin polymerization. Antiproliferative agent-59 exhibits antiproliferative activities against cancer cells Huh7, SGC-7901, and MCF-7 with IC₅₀ of 0.03, 0.18, and 0.13μM. Antiproliferative agent-59 arrests the cell cycle at G2/M phase and induces apoptosis in Huh7 cell. Antiproliferative agent-59 exhibits antitumor efficacy against liver cancer in Huh7 xenograft mouse models, without significant toxicity .

HY-146465

Anticancer agent 60	Microtubule/Tubulin	Cancer
Anticancer agent 60 (compound 3h) has antiproliferative activity against human HepG2 cells (IC₅₀ = 4.13 μM) and presents antitumor efficacy in a human HepG2 xenograft mouse model .

HY-114803

Kokusaginine	Cholinesterase (ChE) Apoptosis Microtubule/Tubulin	Neurological Disease Cancer
Kokusaginine is a furoquinoline alkaloids, which exhibits inhibitory efficacy for acetylcholinesterase (AChE) with an IC₅₀ of 28.2 μM. Kokusaginine exhibits anti-proliferative and apoptotic inducing effects in MCF-7/ADR cells .

HY-16775

Vilaprisan BAY 1002670	Progesterone Receptor	Cancer
Vilaprisan is a selective progesterone receptor modulator (SPRM), which targets progesterone receptors. Vilaprisan can inhibit cell proliferation and stimulate apoptosis. Vilaprisan has oral efficacy and anti-proliferative activity against uterine leiomyoma (UF ).

HY-163760

ZM-32	HuR MMP	Cancer
ZM-32 is an inhibitor for human antigen R (HuR), that downregulates the expression of VEGF-A and MMP9, and thus inhibits breast cancer tumor angiogenesis. ZM-32 exhibits broad-spectrum anti-proliferative effects in a variety of cancer cell lines, and exhibits antitumor efficacy against MDA-MB-231 in mouse models .

HY-170812

BET/Aurora kinase-IN-1	Aurora Kinase	Cancer
BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .

HY-155350

Tubulin polymerization-IN-53	Microtubule/Tubulin	Others
Tubulin polymerization-IN-53 (compound 4b) is an inhibitor of β-tubulin polymerization. Tubulin polymerization-IN-53 can arrest the cell cycle at the G2/M stage. Tubulin polymerization-IN-53 has *antiproliferative* efficacy against the MDA-MB-231 cell line with an IC₅₀ value of 3.24 μM .

HY-149717

Antitumor agent-122	Others	Cancer
Antitumor agent-122 (Compound 5j) is an antitumor agent with good efficacy, limited toxicity and low resistance. Antitumor agent-122 has antiproliferative activity for MGC-803 cell, HepG2 cell, SKOV3 cell and T24 cell with IC₅₀ values of 5.23 μM, 3.60 μM, 1.43 μM, 3.03 μM, respectively .

HY-144720

BRG1-IN-1	SWI/SNF Complex	Cancer
BRG1-IN-1 (Compound 11d) is a potent inhibitor of SMARCA4/BRG1. BRG1-IN-1 shows better efficacy than PFI-3 in sensitizing GBM cells to the antiproliferative and cell death inducing effects of Temozolomide in vitro. BRG1-IN-1 enhances the inhibitor effect of Temozolomide on the growth of subcutaneous GBM tumors .

HY-15990

CH5164840	HSP	Cancer
CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (K_d = 0.52 nM) and strong anti-proliferative activity against human cancer cell lines (HCT116 IC₅₀ = 0.15 μM, NCI-N87 IC₅₀ = 0.066 μM). CH5164840 (16) is orally active (t_1/2 = 2.64 h) with potent antitumor efficacy .

HY-N2453

Convallatoxin	PPAR NF-κB P-glycoprotein	Inflammation/Immunology Cancer
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .

HY-16381A

Pasireotide acetate 5+ Cited Publications SOM230 acetate	Somatostatin Receptor	Endocrinology Cancer
Pasireotide (SOM230) acetate, a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide acetate can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide acetate also exhibits antisecretory, antiproliferative, and proapoptotic activity .

HY-155313

β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE	Drug-Linker Conjugates for ADC	Cancer
β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE (compound 20) is auristatins-glucuronide conjugate. Antitumor agent-122 shows in vitro antiproliferative activities against β-glucuronidase pretreated and untreated cancer cells with an IC₅₀ value of 5.7 nM - 9.7 nM. Antitumor agent-122 shows potent antitumor efficacy in HCT-116 xenograft mouse model without inducing side effects .

HY-16381

Pasireotide 5+ Cited Publications SOM230	Somatostatin Receptor	Endocrinology Cancer
Pasireotide (SOM230), a long-acting cyclohexapeptide somatostatin analogue, can improve agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pK_i=8.2/9.0/9.1/<7.0/9.9, respectively). Pasireotide can suppress GH, IGF-I and ACTH secretion, indicating potential efficacy in acromegaly and Cushing's disease. Pasireotide also exhibits antisecretory, antiproliferative, and proapoptotic activity .

HY-N2453R

Convallatoxin (Standard)	PPAR NF-κB P-glycoprotein	Inflammation/Immunology Cancer
Convallatoxin (Standard) is the analytical standard of Convallatoxin. This product is intended for research and analytical applications. Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties .

HY-101144

RSM-932A TCD-717	Others	Cancer
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC₅₀s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .

HY-158113

CBPD-409	Histone Acetyltransferase PROTACs	Cancer
CBPD-409 is an orally active PROTAC degrader for CBP/p300, with DC₅₀ of 0.2–0.4 nM. CBPD-409 exhibits antiproliferative effects in AR+ prostate cancer cell lines VCaP, LNCaP and 22Rv1, with IC₅₀s of 1.2–2.0 nM. CBPD-409 exhibits antitumor efficacy (Red: CBP inhibitor GNE049 (HY-108435); Blue: CRBN/cullin 4A Thalidomide (HY-14658); Black: Linker) .

HY-163083

JN122	MDM-2/p53 Apoptosis	Cancer
JN122, a spiroindoline-containing molecule, is a MDM2 inhibitor. JN122 Inhibits MDM2/p53 protein–protein interaction and exerts robust in vivo antitumor efficacy. JN122 has antiproliferative activity in HCT-116 cells and HEK-293 cells with IC₅₀ values of 39.6 nM and 4.28μM, respectively. JN122 can promote activation of p53 and its target genes, inhibited cell cycle progression, and induced cell apoptosis .

HY-155529

FD1024	Pim	Cancer
FD1024 is PIM inhibitor (IC₅₀s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice .

HY-172088

Tubulin/MMP-IN-3	Microtubule/Tubulin MMP NF-κB Apoptosis	Cancer
Tubulin/MMP-IN-3 (Compound 15j) is the dual inhibitor for tubulin polymerization and MMP, and inhibits MMP-2 and MMP-9 with IC₅₀ of 21.13 μM and 19.24 μM. Tubulin/MMP-IN-3 inhibits NF-κB signaling pathway, causes mitochondrial dysfunction and the apoptosis through a mitochondrial-dependent pathway. Tubulin/MMP-IN-3 exhibits antiproliferative activity in a variety of cancer cells, arrests the cell cycle at G2/M phase, and exhibits antitumor efficacy in mouse models .

HY-173048

CLPP-2068	ClpP Apoptosis Reactive Oxygen Species	Cancer
CLPP-2068 is the orally active activator for human caseinolytic protease P (HsClpP) with an EC₅₀ of 50.4 nM. CLPP-2068 exhibits anti-proliferative efficacy in OCI-LY10 cancer cell with an IC₅₀ of 5.2 nM. CLPP-2068 decreases mitochondrial membrane potential, increases mitochondrial ROS levels, and induces mitochondrial dysfunction. CLPP-2068 arrests the cell cycle at G1 phase, and induces apoptosis in cell OCI-LY10. CLPP-2068 exhibits antitumor activity in mouse xenograft models .

HY-168716

SOS1-IN-17	Ras	Cancer
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC₅₀ of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC₅₀ of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC₅₀ of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .

HY-146276

CDK/HDAC-IN-2	HDAC CDK Apoptosis	Cancer
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC₅₀ of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .

HY-170405

YB-3–17	PROTACs mTOR	Cancer
YB-3-17 is a bifunctional molecule, that inhibits mTOR (IC₅₀=0.22 nM) or degrades G1 to S phase transition 1 gene (GSPT1, DC₅₀=5 nM) in a PROTAC mechanism. YB-3-17 exhibits antiproliferative activity in multi glioblastoma cell lines with IC₅₀ of nanomolare levels. YB-3-17 exhibits antitumor efficacy in mouse models . (Pink: ligand for target protein (HY-170407); Black: linker (HY-A0102); Blue: ligand for E3 ligase Cereblon (HY-14658))

HY-155965

VEGFR/PARP-IN-1	VEGFR PARP Apoptosis	Cancer
VEGFR/PARP-IN-1 (Compound 14b) is a VEGFR/PARP dual inhibitor (IC₅₀s: 191 nM and 60.9 nM respectively). VEGFR/PARP-IN-1 inhibits DNA damage repair, induces cell apoptosis, and arrests cell in the G2/M phase. VEGFR/PARP-IN-1 has good antiproliferative efficacy against BRCA wild-type breast cancer cells (IC₅₀: 4.1 and 3.5 μM for MDA-MB-231 and MCF-7 cells). VEGFR/PARP-IN-1 is an antitumor and anti-metastasis agent .

HY-100555

CH5138303	HSP	Infection Cancer
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with K_d of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC₅₀ values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .

HY-161688

HDAC-IN-73	Apoptosis HDAC	Cancer
HDAC-IN-73 (compound P-503) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-73 shows IC₅₀s values of 0.17, 0.49 µM for HDAC1 and HDAC6, respectively. Notably, HDAC-IN-73's inhibitory potency against HDAC6 is heightened, exhibiting a 9-fold greater efficacy than PsA (HY-N2150) (IC₅₀=3.9 μM). HDAC-IN-73 shows potent antiproliferative activity, induces apoptosis, and causes cell cycle arrest at G2 / M phase. HDAC-IN-73 has the potential to be used for the research of cancer such as colon cancer .

HY-121081

BAY-958	CDK	Cancer
BAY-958 is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated in vitro, particularly within the CDK family. It shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. In pharmacokinetic studies, BAY-958 exhibited good metabolic stability but had low aqueous solubility and moderate permeability, leading to challenges in bioavailability. Despite these limitations, BAY-958 hydrochloride effectively inhibited tumor growth in mouse xenograft models without significant toxicity, indicating promising efficacy in vivo. However, its suboptimal physicochemical properties prompted further development efforts to identify compounds with improved overall characteristics for potential clinical use .

HY-172217

DNMT1-IN-5	DNA Methyltransferase Apoptosis	Cancer
DNMT1-IN-5 (Compound 55) is the inhibitor for DNMT that inhibits DNMT1 and DNMT3A with IC₅₀ of 2.42 μM and 14.4 μM. DNMT1-IN-5 exhibits antiproliferative activity in a variety of cancer cell lines (IC₅₀s for TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226 and HCT116 are 0.19-2.37 μM), arrests the cell cycle at G2/M phase, and induces apoptosis in TMD-8 and DOHH2 cells. DNMT1-IN-5 exhibits antitumor efficacy in TMD-8 xenograft mouse models .

HY-169170

PARP1/BRD4-IN-3	Apoptosis DNA/RNA Synthesis Epigenetic Reader Domain PARP	Cancer
PARP1/BRD4-IN-3 (compound HF4) is a potent BRD4 and PARP1 inhibitor with IC₅₀ values of 1210, 2019 nM for BRD4, PARP1, respectively. PARP1/BRD4-IN-3 shows antiproliferative activities. PARP1/BRD4-IN-3 induces apoptosis and cell cycle arrest at G0/G1 phase. PARP1/BRD4-IN-3 causes DNA damage and reduces the protein expression of Rad51. PARP1/BRD4-IN-3 shows antitumor efficacy .

HY-145836

FGFR4-IN-8	FGFR	Cancer
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 ^V550L, FGFR4 ^V550M and FGFR4 ^C552S with IC₅₀s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC₅₀ value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .

HY-170924

Tubulin polymerization-IN-76	Microtubule/Tubulin Apoptosis	Cancer
Tubulin polymerization-IN-76 (compound 20b) is a potent and orally active Tubulin polymerization inhibitor. Tubulin polymerization-IN-76 inhibits Tubulin polymerization with an IC₅₀ of 2.505 μM by acting on the colchicine binding site, thereby disrupting intracellular Microtubule networks and interfering with cell mitosis. Tubulin polymerization-IN-76 demonstrates exceptional efficacy against MGC-803 and HGC-27 cells with IC₅₀s of 1.61 and 1.82 nM, respectively. Tubulin polymerization-IN-76 effectively inhibits the colony formation and cell migration activities, and induces G2/M phase cycle arrest and Apoptosis in MGC-803 and HGC-27 cells.Tubulin polymerization-IN-76 shows a broad-spectrum antiproliferative activity .

HY-119618

R1498	Endogenous Metabolite	Cancer
R1498 is a multi-target kinase inhibitor with anti-angiogenic and anti-proliferative activities. R1498 mainly targets targets such as Aurora kinase and VEGFR2, which are associated with tumor development. R1498 showed moderate in vitro growth inhibition in a variety of tumor cells, with IC50 values in the micromolar range. R1498 showed anti-tumor efficacy superior to sorafenib in a variety of gastric cancer and hepatocellular carcinoma xenograft models, with tumor growth inhibition rates exceeding 80%, and tumor shrinkage was observed in some models. R1498 showed a 10-30% tumor shrinkage rate in three xenograft models derived from human primary gastric cancer tumors, further demonstrating its inhibitory potential. R1498 effectively inhibited Aurora A activity in vivo and reduced tumor vascularization .

Cat. No.	Product Name	Target	Research Area