colony formation

12R-LOX-IN-2 is an inhibitor of 12R-lipoxygenase (12R-LOX).12R-LOX-IN-2 inhibits imiquimod (IMQ)-induced hyperproliferation of psoriatic keratinocytes and inhibits colony formation.12R-LOX-IN-2 also decreases the protein level of Ki67 and the mRNA expression of IL-17A in IMQ-induced cells. 12R-LOX-IN-2 may be useful in the study of psoriasis and other skin-associated inflammatory diseases.

UNC1062 is a highly selective tyrosine kinase inhibitor that specifically targets MERTK. This compound effectively suppresses MERTK-mediated downstream signaling, induces apoptosis in cell cultures, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. Notably, UNC1062 demonstrates potent inhibition of MERTK kinase activity, with an IC50 of 1.1 nM and a Morrison Ki of 0.33 nM. It also displays specificity within the TAM family, exhibiting IC50 values of 60 nM for TYRO3 and 85 nM for AXL [1].

CDC25B-IN-1 is an inhibitor of CDC25B with a Ki of 8.5 μM. CDC25B-IN-1 increases the G2/M phase by inhibiting cell proliferation and colony formation.

ZDLD20 is an orally active and selective CDK4 inhibitor, a β-carboline analog with anti-HCT116 and anticancer activity that inhibits colony formation, inhibits invasion and migration, induces apoptosis, and prevents the G1 phase of the cell cycle.

Antiproliferative agent-26 (compound 4g) exhibits a broad spectrum of activity against leukemia, CNS cancers, melanoma, renal, and breast cancers at a concentration of 10 μM. It hinders colony formation and induces cell cycle arrest in the G1 phase at 5 μM, while arresting the cell cycle at the S phase at 25 μM [1].

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)

PI3K-IN-47 (Compound 27) is a potent bivalent inhibitor targeting the phosphoinositide 3-kinases (PI3K) family, exhibiting inhibitory concentration (IC50) values of 0.44 nM for PI3Kα, and 7.18 nM, 13.92 nM, 22.83 nM for PI3Kβ, PI3Kγ, and PI3Kδ respectively. It is effective in inducing G1 phase cell cycle arrest, and exhibits anti-neoplastic properties by restraining colony formation and cell migration. Additionally, PI3K-IN-47 has demonstrated the ability to suppress tumor growth in HGC-27 xenograft mouse models [1].

Antiproliferative Agent-27 (Compound 11) is a notable antiproliferative agent that markedly diminishes tumor cell colony formation and induces apoptosis, demonstrating potential for utilization in cancer research [1].

MPS1/TTK inhibitor is an inhibitor of monopolar spindle 1 (MPS1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors. It inhibits MPS1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating MPS1 checkpoint inhibition, when used at a concentration of 100 nM. MPS1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).

QD-394 is an inducer of reactive oxygen species (ROS) production.1It induces lipid peroxidation, increases in intracellular accumulation of reactive oxygen species (ROS), and decreases in the reduced glutathione (GSH) to oxidized GSH (GSSG) ratio in MIA PaCa-2 pancreatic cancer cells when used at concentrations ranging from 0.5 to 10 μM. QD-394 is cytotoxic to MIA PaCa-2, PANC-1, and BxPC-3 cancer cells (IC50s = 0.64, 0.34, and 0.9 μM, respectively). QD-394 acts synergistically with napabucasin to reduce colony formation in MIA PaCa-2 cells. 1.Hu, S., Sechi, M., Singh, P.K., et al.A novel redox modulator induces a GPX4-mediated cell death that is dependent on iron and reactive oxygen speciesJ. Med. Chem.63(17)9838-9855(2020)

Y08060 is an effective and selective BET Inhibitor for the Treatment of Prostate Cancer. Y08060 effectively suppresses cell growth, colony formation, and expression of androgen receptor (AR), AR regulated genes, and MYC in prostate cancer cell lines. Y08060 has IC50 values of 3.23 and 4.41 μM in inhibition of cell viability in the C4 2B and LNCaP cell lines, respectively.

Tetramethylcurcumin is a novel curcumin analog, is an effective inhibitors of STAT3 phosphorylation, DNA binding activity, and transactivation in vitro.it also inhibits colony formation in soft agar, cell invasion, and exhibit synergy with the anti-cancer drug doxorubicin against breast cancer cells.

ORY-1001 is a KDM1A inhibitor (IC50 <20nM) with high selectivity against related FAD dependent aminoxidases (MAO-A/B, IL4I1, KDM1B >100uM, SMOX 7uM). Treatment of THP-1 (MLL-AF9) cells with ORY-1001, results in a time/dose dependent me2H3K4 accumulation a

Antitumor agent-58 is an antitumour agent that effectively inhibits colony formation and cell migration in MGC-803 cells and induces mitochondrial dysfunction in MGC-803 cells. Antitumor agent-58 exhibited potent inhibitory activity against tumour growth in xenograft models carrying MGC-803 cells.

PI3Kα-IN-13 (Compound 18a), a PI3Kα inhibitor with an IC50 of 2.5 nM, effectively induces apoptosis and hampers the proliferation of various cancer cell lines, exhibiting IC50 values of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), and 9.85 μM (SW620). This compound also impedes tumor cell colony formation, migration, and invasion [1].

KV1.3-IN-1 (Compound trans-18), a selective KV1.3 channel inhibitor with IC50 values of 230 nM in Ltk cells and 26.12 nM in PHA-activated T-lymphocytes, disrupts intracellular Ca2+ signaling and impedes T-cell activation and proliferation, as well as colony formation [1].

CAP 3 is a cholic acid-peptide conjugate (CAP) with antibacterial activity. It is active against the Gram-negative bacteria E. coli, K. pneumoniae, and A. baumanii (MIC99s = 8, 16, and 16 μM, respectively). CAP 3 increases the fluidity of model Gram-negative bacterial membranes and binds to LPS in vitro. It reduces the biomass and number of colony-forming units in E. coli biofilms in a concentration-dependent manner. CAP 3 inhibits E. coli biofilm formation on catheters implanted in mice infected with E. coli at the incision site when applied as a coating on the catheters. CAP 3 (40 mg/kg) also reduces bacterial load in E. coli-infected wounds in mice. It is cytotoxic to A459 cells (IC50 = 56.4 μM) and has hemolytic activity against human red blood cells with a 50% lysis (HC50) value of 48 μM.

Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties. This compound halts the cell cycle at the G0/G1 phase, augments nitric oxide (NO) production, and demonstrates anti-tumor efficacy [1].

FY-21 is a selective LSD1 inhibitor (IC50= 340 nM) that inhibits proliferation and colony formation of leukemia cells, decreases mRNA levels of the transcription factors HOXA9 and MEIS1, and can be used in the study of leukemia.

GSD-11 inhibits the Akt/mTOR signaling pathway. GSD-11 inhibits the PANC-1 cells migration and colony formation. GSD-11 is a potent and selective anti-austerity agent that has the potential for the pancreatic cancer research [1].

S49076 HCl (S-49076 Hydrochloride) is an effective inhibitor of MET, AXL/MER, and FGFR1/2/3. S49076 HCl potently blocked cellular phosphorylation of MET, AXL, and FGFRs and inhibited downstream signaling in vitro and in vivo. In cell models, S49076 HCl inhibited the proliferation of MET- and FGFR2-dependent gastric cancer cells blocked MET-driven migration of lung carcinoma cells, and inhibited colony formation of hepatocarcinoma cells expressing FGFR1/2 and AXL. In tumor xenograft models, a good pharmacokinetic/pharmacodynamic relationship for MET and FGFR2 inhibition following oral administration of S49076 HCl was established and correlated well with impact on tumor growth.

Tubulin/HDAC-IN-3 (compound 12a) serves as a potent dual inhibitor of tubulin polymerization and HDAC1/8, exhibiting IC50 values of 5.4 μM for tubulin polymerization, and 0.155 and 0.177 μM for HDAC1 and HDAC8, respectively. Its mechanism of action includes obstructing the cell cycle, triggering apoptosis, and suppressing colony formation [1].

GGTI-2166 is a geranylgeranyl transferase I inhibitor. GGTI-2166 inhibit the pOC formation induced by RANKL or TNF-alpha in cultures of both mouse marrow-derived macrophage-colony-stimulating factor (M-CSF) dependent monocytes (MD cells) and the mouse monocyte cell line RAW 264.7 (RAW cells). GGTI-2166 inhibited TRAP activity induced by RANKL or TNF-alpha in both cell cultures and prevented the incorporation of [3H]all-trans geranylgeraniol into prenylated proteins in RAW cells.

QA-68 (QA-68-ZU81), a potent bromodomain-containing protein 9 (BRD9) degrader, effectively inhibits cell cycle progression and cell colony formation. Demonstrating antiproliferative activity, this compound is particularly effective against acute myeloid leukemia (AML) cell lines [1].

AEW541, also known as NVP-AEW541, is a novel, potent IGF-IR kinase inhibitor. NVP-AEW541 is capable of distinguishing between the IGF-IR (IC50 = 0.086 microM) and the closely related InsR (IC50 = 2.3 microM) in cells. NVP- AEW541 abrogates IGF-I-mediated survival and colony formation in soft agar at concentrations that are consistent with inhibition of IGF-IR autophosphorylation. Note: AEW541 has a Cis-configuration on the cyclobutane ring. Its CAS# is 475489-16-8. Many vendors and Sc-finder scholar made mistake - AEW541 was mistakenly listed as CAS#475488-34-7, the trans-isomer of AEW541. The correct structure of AEW541 can be confirmed from Joel Slade, et al (from Novartis), Org. Process Res. Dev. 2007, 11, 5, 825–835.

HPI 1 is a hedgehog (Hh) signaling inhibitor. Inhibits Sonic hedgehog (Shh)-, SAG- and Gli-induced Hh pathway activation in Shh-LIGHT2 cells (IC50 values are 1.5, 1.5, 4, and 6 μM for Shh-, SAG-, Gli2- and Gli1-induced activation).

(-)-Agelastatin A inhibits osteopontin-mediated adhesion, invasion, and colony formation.

SR31527 (SR31527 chloride) is a potent KIFC1 inhibitor with an IC50 of 6.6 µM against KIFC1. SR31527 chloride has a moderate inhibitory effect on cell viability and colony formation.

RKI1313 (RKI-1313) was a selective inhibitor for ROCK-dependent signaling, cytoskeletal changes, anchorage-independent colony formation, migration, and invasion.

CUR5g is an autophagy inhibitor that inhibits migration and colony formation in A549 cells and acts through a UVRAG-dependent mechanism by blocking the recruitment of STX17 to autophagosomes.CUR5g is often used in combination with cisplatin for the study of cancer.

Mtb-IN-3 (compound 10c), a selective and potent Mycobacterium tuberculosis (Mtb) inhibitor, exhibits strong antimycobacterial activity in vitro without inducing cytotoxic effects and inhibits colony formation in the spleen in murine tuberculosis models [1].

HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony formation, arresting the cell cycle at the G2 phase, and inducing apoptosis [1].

CP-07 is a selective and effective PROTAC CDK9 degrader (DC50: 43 nM), demonstrating inhibition of 22RV1 cell proliferation (IC50: 62 nM) and colony formation by attenuating levels of Mcl-1 and c-Myc. Additionally, CP-07 has been shown to impede the growth of 22RV1 xenograft tumors and is applicable in prostate cancer research [1].

Glutaminase C Inhibitor 11 is a potent inhibitor specifically targeting Glutaminase C (GAC), demonstrating significant inhibition of GAC enzyme activity with an EC50 value of 10.64 nM. It effectively diminishes the viability of A549 non-small cell lung cancer (NSCLC) cells, presenting an IC50 of 4.025 nM. Moreover, at concentrations of 0.1 and 1 µM, it substantially impedes colony formation and reduces intracellular glutamate levels in A549 cells. Demonstrating efficacy in vivo, Glutaminase C Inhibitor 11 at a dosage of 100 mg/kg markedly curtails tumor growth in an A549 mouse xenograft model.

c-Met-IN-10 is a potent c-Met kinase inhibitor (IC50: 16 nM). c-Met-IN-10 inhibits the activity of cancer cells A549, H460 and HT-29, and inhibits A549 cell movement by inhibiting HT-29 cell colony formation, which in turn induces apoptosis in HT-29 and A549 cells. c-Met-IN-10 can be used in anticancer studies. -Met-IN-10 is capable of being used in anticancer studies.

ZDLD13 is a β-carboline that exhibits potent anti-HCT116 activity inclusive of inhibition of invasion and migration, inhibition of colony formation, inducing of apoptosis as well as arresting of G1 phase in cell cycle. ZDLD13 is an orally active and selective inhibitor of CDK4/CycD3 (IC 50 = 0.38 μM) which exhibits significant inhibition of tumor growth in HCT116 tumor xenograft model [1].

Diphenyl disulfide (Phenyl disulfide) shows anticancer activity in breast cancer cell lines.Diphenyl disulfide induces and enhances apoptosis in breast cancer cells through Bax protein hydrolysis activation and concomitant autophagy.Diphenyl disulfide inhibits cell proliferation and viability and reduces colony formation in a dose-dependent manner. Diphenyl disulfide can be used to treat breast cancer.

YM458, a potent dual inhibitor of EZH2 and BRD4, exhibits IC50 values of 490 nM and 34 nM, respectively. This compound effectively hinders cell proliferation and colony formation, while also inducing cell cycle arrest and apoptosis in solid tumor cells, making it a viable candidate for anticancer research [1].

ATX inhibitor 13 (compound 10c) is an orally active ATX inhibitor (IC50: 3.4 nM). ATX inhibitor 13 is capable of blocking the cell cycle of RAW264.7 cells in the G2 phase, inhibiting cell proliferation and migration and inducing apoptosis. ATX inhibitor 13 exhibited an inhibitory effect on tumour colony formation.

IV-23, a potent inhibitor of cell growth both in vitro and in vivo, effectively reduces colony formation, arrests the cell cycle at the M phase, and induces apoptosis in esophageal squamous cell carcinoma through Noxa-mediated pathways. This compound emerges as a promising anticancer agent with significant potential.

KH-3 is a potent inhibitor (IC50: 0.35 μM) of the RNA-binding protein Hu antigen R (HuR) and exhibits anti-proliferative effects. KH-3 interferes with HuR-FOXQ1 Mrna interactions, inhibits breast cancer cell invasion, and delays lung colony formation.

ALK-IN-23 is a potent inhibitor of ALK, acting on ALKWT (IC50: 1.6 nM), ALKL1196M (IC50: 0.71 nM) and ALKG1202R (IC50: 1.3 nM). -IN-23 has inhibitory effects on cancer cell migration and colony formation in vitro. In the H2228 xenograft nude mouse model, ALK-IN-23 showed good anti-tumour effects with low toxicity.

WB-308 is an EGFR inhibitor that acts by decreasing NSCLC cell proliferation and colony formation and causing G2/M arrest and apoptosis.

PAR2 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth in the presence and absence of growth factors. PAR2 (1-6) inhibits LPS-induced pulmonary neutrophil influx and increases in matrix metalloproteinase-2 (MMP-2) activity in mice.