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Results for "

antiproliferative efficacy

" in MedChemExpress (MCE) Product Catalog:

20

Inhibitors & Agonists

2

Peptides

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    CCT373566
  • 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-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-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-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-144720
    BRG1-IN-1

    		Others Cancer
    BRG1-IN-1 (Compound 11d) is a potent inhibitor of 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-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-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-16381
    Pasireotide

    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-16381A
    Pasireotide acetate
    1 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-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-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-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-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-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-100555
    CH5138303

    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-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-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

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