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Results for "

antiproliferative efficacy

" in MedChemExpress (MCE) Product Catalog:

47

Inhibitors & Agonists

3

Peptides

3

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 .
    CCT373566
  • 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 .
    CDK2-IN-22
  • 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 ).
    Vilaprisan
  • 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-P10902
    Lorutengitide

    		DNA/RNA Synthesis Cancer
    Lorutengitide is a transcriptional regulatory peptide, and exhibits antiproliferative efficacy .
    Lorutengitide
  • 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 .
    Antiproliferative agent-51
  • 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 .
    NS-062
  • 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 .
    Antiproliferative agent-59
  • 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 .
    Anticancer agent 60
  • 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 .
    Kokusaginine
  • 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 .
    ZM-32
  • 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 .
    BET/Aurora kinase-IN-1
  • 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 .
    Tubulin polymerization-IN-53
  • 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 .
    Antitumor agent-122
  • HY-15990
    CH5164840

    		HSP Cancer
    CH5164840 (16) shows high binding affinity for N-terminal Hsp90a (Kd = 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 (t1/2 = 2.64 h) with potent antitumor efficacy .
    CH5164840
  • 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 .
    Convallatoxin
  • 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 .
    BRG1-IN-1
  • HY-16381A
    Pasireotide acetate
    2 Publications Verification

    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, pKi=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 .
    Pasireotide acetate
  • 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 .
    β-Glucuronide-NB-bis[N(Me)-methyl ester]-MMAE
  • 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, pKi=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 .
    Pasireotide
  • HY-N2453R
    Convallatoxin (Standard)

    		Reference Standards 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 .
    Convallatoxin (Standard)
  • 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 .
    RSM-932A
  • 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) .
    CBPD-409
  • 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 .
    JN122
  • 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 .
    Tubulin/MMP-IN-3
  • 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 .
    FD1024
  • HY-173048
    CLPP-2068

    		ClpP Apoptosis Reactive Oxygen Species (ROS) 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 .
    CLPP-2068
  • HY-168716
    SOS1-IN-17

    		SOS1 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 .
    SOS1-IN-17
  • 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 .
    CDK/HDAC-IN-2
  • 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))
    YB-3–17
  • 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 .
    VEGFR/PARP-IN-1
  • 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 Kd 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 .
    CH5138303
  • HY-174458
    MD-4251

    		PROTACs MDM-2/p53 IKZF Family Casein Kinase Cancer
    MD-4251 is an orally active MDM2 PROTAC degrader. MD-4251 potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and actives p53. MD-4251 shows strong antiproliferative activity against acute leukemia cells (wild-type p53) with minimal efficacy in mutant type. MD-4251 induces complete tumor regression in RS4;11 xenograft mice model . Pink: MDM2 ligand (HY-130684); Blue: CRBN ligase ligand (HY-W883326); Black: linker
    MD-4251
  • HY-174382
    ROR1-IN-3

    		Akt mTOR NF-κB ROR Apoptosis Cancer
    ROR1-IN-3 (Compound 24d) is a potent and highly selective ROR1 kinase inhibitor (IC50 = 17.6 nM). ROR1-IN-3 demonstrates robust antitumor activity and inhibitory effect against ROR1 both in vitro and in vivo. ROR1-IN-3 has robust antiproliferative efficacy in vitro and in vivo. ROR1-IN-3 induces apoptosis in cancer cell lines. ROR1-IN-3 inhibits ROR1 downstream AKT/mTOR and NF-κB signaling pathway. ROR1-IN-3 can be studied in antitumor research .
    ROR1-IN-3
  • 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 .
    HDAC-IN-73
  • HY-175502
    MGD-22

    		Molecular Glues IKZF Family Apoptosis Cancer
    MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL) .
    MGD-22
  • 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 .
    BAY-958
  • HY-175497
    ROR1-IN-4

    		ROR Apoptosis Bcl-2 Family PARP Cancer
    ROR1-IN-4 is a selective ROR1 inhibitor with a Kd of 52 nM. ROR1-IN-4 shows potent anti-proliferative activity against TNBC cell line MDA-MB-231 (IC50 = 75 nM). ROR1-IN-4 reduces colony formation, induces apoptosis and inhibits the phosphorylation of ROR1 (Tyr786) in MDA-MB-231 cells. ROR1-IN-4 demonstrates superior anti-tumor efficacy in nude mice bearing MDA-MB-231 subcutaneous xenografts. ROR1-IN-4 can be used for the study of triple-negative breast cancer (TNBC) .
    ROR1-IN-4
  • 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 .
    DNMT1-IN-5
  • 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 .
    PARP1/BRD4-IN-3
  • HY-175320
    PROTAC c-Met degrader-5

    		PROTACs c-Met/HGFR Apoptosis STAT Cancer
    PROTAC c-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader with DC50s of 0.42 and 0.32 nM in EBC-1 and Hs746T cells, respectively. PROTAC c-Met degrader-5 significantly induces cell apoptosis, G1 cell cycle arrest, and inhibits cell migration and invasion. PROTAC c-Met degrader-5 has potent antiproliferative and degradation efficacy against c-Met-addicted cancer cells and Tepotinib (HY-14721)-resistant cancer cells . Pink: c-Met ligand (HY-W425461); Blue: CRBN ligase ligand (HY-14658); Black: linker
    PROTAC c-Met degrader-5
  • 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 .
    FGFR4-IN-8
  • 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 .
    R1498
  • HY-170924
    Tubulin polymerization-IN-76

    		Microtubule/Tubulin Apoptosis Mitosis 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 .
    Tubulin polymerization-IN-76
  • HY-175542
    KB-15

    		STAT Apoptosis Reactive Oxygen Species (ROS) PARP Cancer
    KB-15 is a STAT3 inhibitor. KB-15 exhibits potent anti-proliferative activity against AGS gastric cancer cells (IC50 = 0.29 μM) and BGC-823 gastric cancer cells (IC50 = 0.65 μM). KB-15 exerts anti-tumor effects by inhibiting STAT3 phosphorylation, downregulating HO-1 expression, and promoting intracellular ROS accumulation. KB-15 induces G0/G1 phase cell cycle arrest and apoptosis, as well as suppresses colony formation and migration of gastric cancer cells. KB-15 demonstrates excellent anti-tumor efficacy in BGC-823 subcutaneous xenograft model. KB-15 can be used for the study of gastric cancer .
    KB-15
  • HY-162098
    PROTAC tubulin-Degrader-1

    		PROTACs Microtubule/Tubulin Apoptosis Cancer
    PROTAC tubulin-Degrader-1 is a α/β/β3-tubulin PROTAC degrader. PROTAC tubulin-Degrader-1 exhibits potent anti-proliferative activity against multiple human tumor cell lines. PROTAC tubulin-Degrader-1 induces G2/M phase arrest and apoptosis and inhibits colony formation in A549 and A549/Taxol cells. PROTAC tubulin-Degrader-1demonstrates potent anti-tumor efficacy in A549 and A549/Taxol (Taxol-resistant) xenograft model. PROTAC tubulin-Degrader-1 can be used for the study of non-small cell lung cancer (NSCLC). (Pink: Tubulin ligand (HY-N2146), Blue: CRBN Ligand (HY-10984), Black: Linker (HY-N6056)) .
    PROTAC tubulin-Degrader-1
  • HY-175610
    PROTAC FLT3/JAK2/BRD4 Degrader-1

    		PROTACs FLT3 JAK Epigenetic Reader Domain Cancer
    PROTAC FLT3/JAK2/BRD4 Degrader-1 is a PROTAC degrader that target FLT3, JAK2, and BRD4 with DC50 values of 5.23, 0.678, and 1.17 nM, respectively. PROTAC FLT3/JAK2/BRD4 Degrader-1 exhibits potent antiproliferative activity against MV4;11 cells (IC50 = 0.79 nM) and FLT3 mutant-transformed Ba/F3 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 induces apoptosis in MV4;11 cells. PROTAC FLT3/JAK2/BRD4 Degrader-1 demonstrates significant anti-tumor efficacy in the MV4;11 xenograft model established in NOD SCID mice. PROTAC FLT3/JAK2/BRD4 Degrader-1 can be used for the study of acute myeloid leukemia (AML). (Pink: FLT3/JAK2/BRD4 ligand (HY-175611), Blue: CRBN Ligand (HY-W087383), Black: Linker, E3 ligase ligand-linker conjugate (HY-W897939)) .
    PROTAC FLT3/JAK2/BRD4 Degrader-1

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