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Janelia Fluor® 549 TFA (JF549 TFA) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor? 549, Azide (JF549, Azide) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor? products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
PA Janelia Fluor 549, SE (PA-JF549-NHS) is a bright photoactivatable fluorophore of JF549,SE (JF549,NHS). JF549,SE (JF549,NHS) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
DGN549-L is a DNA alkylator and can be utilized for antibody conjugation at lysine residues. DGN549-L can be used in the synthesis of antibody-drug conjugates (ADCs) .
Janelia Fluor® 549, SE (JF549, SE) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor® 549, Tetrazine (JF549, Tetrazine) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor® 549, Maleimide TFA (JF549, Maleimide TFA) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Macrocalin B is a diterpenoid, which can be isolated from Isodon xerophilus. Macrocalin B inhibits the proliferation of cancer cells K562, HL-60, A549, MKN, CA and HCT with IC50 of 2.81-171 μM. Macrocalin B inhibits the telomerase in K562 with an IC50 in nanomolar level .
LysoSR-549 is a multifunctional dye. Dyes are important tools in biological experiments. They can help researchers observe and analyze cell structures, track biomolecules, evaluate cell functions, distinguish cell types, detect biomolecules, study tissue pathology and monitor microorganisms. Their applications range from basic scientific research to clinical A wide range of diagnostics. Dyes are also widely used in traditional fields such as textile dyeing, as well as in emerging fields such as functional textile processing, food pigments and dye-sensitized solar cells.
Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC50 of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases .
hsa-miR-549a-5p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
hsa-miR-549a-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
hsa-miR-549a-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
hsa-miR-549a-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
hsa-miR-549a-5p agomirs are chemically-modified double-strand miRNA mimics with modified mature miRNA strand: 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 3' end cholesterol group, and full-length nucleotide 2'-methoxy modification. They are designed to mimic endogenous miRNAs and recommended for miRNA functional studies. Compared with miRNA mimics, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
hsa-miR-549a-3p agomirs are chemically-modified double-strand miRNA mimics with modified mature miRNA strand: 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 3' end cholesterol group, and full-length nucleotide 2'-methoxy modification. They are designed to mimic endogenous miRNAs and recommended for miRNA functional studies. Compared with miRNA mimics, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
hsa-miR-549a-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
hsa-miR-549a-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
Cepharadione B (compound 22) is a natural compound isolated from the leaves of Piper sanctum. Cepharadione B is a tyrosinase inhibitor with an IC50 value of 170 μM, and inhibits cell growth in A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cells .
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL .
Norcepharadione B is an alkaloid that can be isolated from Houttuynia cordata. Norcepharadione B exhibits moderate cytotoxicity against A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cell line with ED50s of 40, 26.4, 40, 14.2 and 38.2 μg/mL, respectively .
Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB) .
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
Chlorovaltrate K is a chlorinated valepotriate with anticancer effects. Chlorovaltrate K shows moderate cytotoxicity against A549, PC-3M, HCT-8 and Bel 7402 cell lines with IC50 values of 2.32-8.26 μM .
WES-1 (Compound 8g) is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). WES-1 has broad spectrum anti-proliferative activity against the cancer cells, such as leukemia (K-562 and MOLT-4), non-small cell lung cancer (NCI–H460), colon cancer (HCT 116 and HCT-15) and melanoma (LOX IMVI) cell lines .
Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation .
Topoisomerase II/EGFR-IN-1 is topoisomerase II/EGFR dual inhibitor. Topoisomerase II/EGFR-IN-1 has superior cytotoxic activity to MCF-7, A549 and HCT-116 cell lines, displays strong apoptotic activity and can be used for the research of cancer .
HDAC1/CDK7-IN-1 (compound 8e) is a dual CDK7 and HDAC1 inhibitor with IC50s of 893 nM and 248 nM, respectively. HDAC1/CDK7-IN-1 inhibits the growth cells of MDA-MB-231, MCF-7, A549, and HCT-116 cancer cells. HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis in HCT-116 cells, as well as hindered the migration of HCT-116 cells .
3-epi-Isocucurbitacin B (Compound 5) is a cucurbitane triterpene derived from Trichosanthes kirilowii. 3-epi-Isocucurbitacin B shows significant cytotoxicity to human tumor cells A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15 .
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
SB-1295 is an orally active CDK9/T1 inhibitor (IC50=0.17 μM). SB-1295 shows antiproliferative activity in HCT 116 and MIA PaCa-2 cells. SB-1295 also induces MIA PaCa-2 cell death by inducing intracellular ROS production, reducing mitochondrial membrane potential and inducing apoptosis. SB-1295 has the potential to study cancer .
4-Formylcolchicine is a potent anticancer agent. 4-Formylcolchicine shows cytotoxicity activity with IC50 values of 1.007, 0.128, 0.054 μM for A549, HT-29, HCT116 cells, respectively .
IDO/Tubulin-IN-2 (HT2) is a potent TDO and tubulin inhibitor. IDO/Tubulin-IN-2 also shows potent activity against U87, HepG2, A549, HCT-116, and LO2 cancer cell lines, with IC50 values of 0.43, 0.036, 0.041, 0.095 and 1.04 μM, respectively. IDO/Tubulin-IN-2 remarkably promotes the antitumor activity .
Gambogic acid B is an active compound. Gambogic acid B can be isolated from the resin of Garcinia hanburyi.. Gambogic acid B has cytotoxicity against A549, HCT116 and MDA MB 231 cells with IC50 values of 1.60 μM, 6.88 μM and 0.87 μM, respectively .
EGFR-IN-123 (compound D06) is a potent EGFR inhibitor. EGFR-IN-123 inhibits PC-9G, A549, A431 and HCT116 cells with IC50s of 0.74, 1.36, 1.20 and 2.53 μM, respectively .
NW16 is an orally active inhibitor for STAT3 with Kd of 11.0 μM. NW16 arrests the cell cycle at S phase, induces apoptosis in HCT116, and inhibits the proliferation of cancer cell HCT116, A549, and B16 with IC50s of 0.28, 1.22, and 9.86 μM, respectively. NW16 induces the production of ROS, inhibits the PI3K/AKT signaling pathway, and thus exhibits antitumor efficacy in mouse model .
Anticancer agent 139 (Compound 6h) has potent anticancer activity. Anticancer agent 139 displayed a π–cationic interaction with the residue Lys352 of Tublin. Anticancer agent 139 has good anticancer activity against SNB-19, OVCAR-8, and NCI-H40 with PGIs of 86.61, 85.26, and 75.99, respectively. Anticancer agent 139 also has moderate anticancer activity against HOP-62, SNB-75, ACHN, NCI/ADR-RES, 786-O, A549/ATCC, HCT-116, and MDA-MB-231 with PGIs of 67.55, 65.46, 59.09, 59.02, 57.88, 56.88, 56.53, 56.4, and 51.88 respectively .
Tubulin polymerization-IN-64 (Compound 8a) is an inhibitor for tubulin polymerization by occupying the colchicine binding site of tubulin, with IC50 of 6.9 μM. Tubulin polymerization-IN-64 inhibits proliferations of cancer cells A549, HeLa, HCT116 and HT-29, with IC50s of 2.42, 10.33, 6.28, 5.33 μM, respectively. Tubulin polymerization-IN-64 arrests cell cycle at G2/M phase, induces apoptosis in A549 .
MAT2A-IN-23 (compound 39) is a MAT2A inhibitor, with an IC50 of 4 nM. MAT2A-IN-23 inhibits SAM in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 3 and 2 nM, respectively. MAT2A-IN-23 inhibits SDMA in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 2 and >3000 nM, respectively. MAT2A-IN-23 inhibits HCT-116 (MTAP −/−) cell proliferation with with an IC50 of 47 nM .
8-epi-Helenalin is a semitterpene lactone with anti-tumor activity that can be isolated from Inula britannicaL. var. chinensis (Rupr.) Reg. and the ED50 values of 8-epi-Helenalin for HL-60, A549, MCF7, HCT-15, SK-OV-3 and Malme-3M are 12.2 μM, 53.8 μM, 9.1 μM, 8.7 μM, 18.7 μM and 8.3 μM, respectively. 8-epi-Helenalin can be used for anti-tumor studies .
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
Tubulin polymerization-IN-62 (Compound 14b) is an inhibitor for microtubule polymerization (IC50 is 7.5 μM) and a degrader for α- and β-tubulin. Tubulin polymerization-IN-62 inhibits proliferation of cancer cells MCF-7, A549 and HCT-116, with IC50 of 32, 60 and 29 nM, respectively. Tubulin polymerization-IN-62 arrests the cell cycle at G2/M phase, inhibits the migration of MCF-7. Tubulin polymerization-IN-62 exhibits antitumor efficacy with a tumor growth inhibition rate (TGI) of 74.27% in 4T1 homograft mouse model .
PROTAC KSP-IN-1 (Compound 21) is a PROTAC Degrader for kinesin spindle protein (KSP), that degrades KSP in HCT-116 with DC50 of 114.8 nM. PROTAC KSP-IN-1 inhibits the proliferation of HCT-116 with IC50 of 10 nM, arrests the cell cycle of HCT-116 at G2/M phase, and induces apoptosis in HCT-116. PROTAC KSP-IN-1 exhibits antitumor efficacy in mouse model . (Blue: Ligand for E3 Ligase Cereblon (HY-103596); Blank: Linker (HY-168726); Pink: Target Protein Ligand (HY-168727))
1 α-hydroxytorilin (compound 3) is a sesquiterpenoid. 1 α-hydroxytorilin can be isolated from Torilis japonica. 1α-hydroxytorilin has cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells with ED50 values of 20.52, 18.24, 17.48, 42.54 μg/mL, respectively .
ASR-490 reduces the viability of HCT116 and SW620 cells by downregulating Notch1 signaling. ASR-490 overcomes Notch1 overexpression and inhibits the growth of HCT/Notch1 transfectants. ASR-490 inhibits the tumor growth in control (pCMV/HCT116) and Notch1/HCT116 in xenotransplanted mice .
Scr-IN-1 (Compound 4e) is a Tyrosine kinase inhibitor. Scr-IN-1 inhibits HCT-116 cells and MIA-PaCa-2 cells with IC50s of 0.16 μM and 1.16 μM, respectively. Scr-IN-1 displays selectivity profile on HCT-116 cells and MIA-PaCa-2 cells with SI > 625 and SI > 86, respectively. Scr-IN-1 induces Apoptosis in HCT-116 colon cancer cell and does not cause any change in the rate of necrotic cells. Scr-IN-1 is a novel SRC kinase inhibitor candidate for HCT-116 cells. Scr-IN-1 is potential for cancer research .
Hsp90-IN-39 (Compound 16t) is a HSP90 inhibitor with notable selectivity for the HSP90α isoform. Hsp90-IN-39 demonstrates significant antiproliferative activity in various cancer cell lines, including MCF-7, HCT116, SKBr3, K562, and A549. Hsp90-IN-39 holds potential for cancer research .
FL77-24, a FL118 analog and apoptosis inducer, possesses antitumor activity, with IC50 values of 99.4 nM, 118 nM, <6.4 nM, 28.5 nM and <6.4 nM in HCT116, HepG2, MCF-7, A549 and HeLa cells, respectively. FL77-24 mainly causes cell cycle arrest in S and G2/M phases .
Glucozaluzanin C is a lignan isolated from the MeOH extract of the roots of Ainsliaea acerifolia (Compositae). Glucozaluzanin C has ED50 value of 2.45 μg/mL, 1.37μg/mL, 0.40 μg/mL, 1.41 μg/mL, 1.43 μg/mL for A549 cells, SK-OV-3 cells, SK-MEL-2 cells, XF498 cells, HCT15 cells, respectively .
HCT-116-IN-1, a γ-lactam-fused pyridone derivative, has anticancer activity and displayed high cytotoxicity against HCT116 cells with an IC50 of 5.59 μM .
β-Catenin modulator-7 (Compound 5) is a modulator for β-catenin. β-Catenin modulator-7 inhibits the expression of β-catenin in HCT-116 cytoplasm and nucleus, suppresses the phosphorylation of GSK 3β. β-Catenin modulator-7 promotes NO release in HCT-116, and inhibits the proliferation of cancer cell HCT-116 with IC50 of 0.6-0.9 μM. β-Catenin modulator-7 can be used in reasearch about colon cancer .
MC4033 shows IC50s of 39.4 μM, 52.1 μM, 41 μM and 30.1 μM in HCT116, H1299, A549 and U937, respectively .
MC4033 (25, 50, 100, and 200 μM, 72 h) reduces the level of H4K16Ac in HT29 cells, suggesting its ability to inhibit KAT8 in cells .
RJ-34, an aristolactam analogue, exhibits potent antitumor activities against a broad array of cancer cell lines with GI50 values in the subnanomolar range (GI50 <0.1 nM for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells) .
MAPK-IN-3 (Compound 4a) is an anti-proliferative agent that shows particularly strong inhibitory effects on KYSE 30, HCT 116, and HGC 27, with IC50 values of 0.57 μM, 3.27 μM, and 2.28 μM, respectively. MAPK-IN-3 blocks the cell cycle via a p53-dependent mechanism and induces cell apoptosis through a p53-independent mechanism. MAPK-IN-3 downregulates the expression of cell cycle-related proteins like Cyclin D1 and cyclin B1, upregulates pro-apoptotic proteins such as cleaved PARP, cleaved caspase-7, and cleaved caspase-9, and reduces the expression of anti-apoptotic proteins like Bcl-2. Additionally, MAPK-IN-3 increases the intracellular level of ROS in KYSE 30 cells and upregulates the expression of members of the MAPK signaling pathway associated with ROS, such as p-ERK, p-p38 and p-JNK .
EGFR/HER2/DHFR-IN-2 (Compound 4b) is an inhibitor of EGFR, HER2, and DHFR (IC50: 0.248, 0.156, 0.138 μM respectively). EGFR/HER2/DHFR-IN-2 has anticancer activities against a panel of cancer cells (IC50: 9.14, 7.33, 14.18, 24.87, 20.07, 6.16 μM for Hep G2, HeLa, HEp-2, HCT 116, PC-3, MCF7 cells). EGFR/HER2/DHFR-IN-2 reduce breast cancer tumor growth .
Frangulin B (Compd 11g), a potent anticancer agent, is a potential pan RecQ helicase inhibitor . Frangulin B (Compd 11g) induces apoptosis in both HCT-116 and MDA-MB-231 cell lines, but also causes an G2/M phase cell cycle arrest in HCT-116 cells .
Emeguisin A is a depsidone with an antibacterial activity. Emeguisin A inhibits the human colon carcinoma (HCT-116) cell viability with rate of 87.06% .
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
IGF2BP1-IN-1 (Compound A11) is a IGF2BP1 inhibitor and inhibits downstream signaling. IGF2BP1-IN-1 binds to IGF2BP1 protein with a KD value of 2.88 nM. IGF2BP1-IN-1 inhibits cancer cells proliferation (IC50: 9 nM for A549 cell, 34 nM for HCT116). IGF2BP1-IN-1 induces cancer cell apoptosis. GF2BP1-IN-1 inhibits tumor growth in A549 xenograft mouse model .
Angiogenesis inhibitor 3 (compound 8) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 3 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.00 and 0.71 μM. Angiogenesis inhibitor 3 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 3 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 3 inhibits the angiogenesis in zebrafish embryos .
Angiogenesis inhibitor 2 (compound 72) is a potent angiogenesis inhibitor. Angiogenesis inhibitor 2 inhibits the proliferation of HUVEC and HCT-15 cells, with IC50 values of 1.93 and 0.21 μM. Angiogenesis inhibitor 2 induces the apoptosis of HUVEC and HCT-15 cells. Angiogenesis inhibitor 2 shows anticancer activity, and suppresses the invasion of cancer cells. Angiogenesis inhibitor 2 inhibits the angiogenesis in zebrafish embryos .
EGFR kinase inhibitor 7 (compound 18i) is an EGFR inhibitor (IC50=42.3 nM) with anticancer activity. EGFR kinase inhibitor 7 has significant in vitro cytotoxicity and apoptosis induction ability. EGFR kinase inhibitor 7 has antiproliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively .
HCT116 is a peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 of 54 nM. HCT116 can inhibit the N-terminal methylation level of NTMT1/2 substrates in HCT116 cells, and is used for the study of NTMT1/2 probes.
Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
Nonactin is a macrotetrolide antibiotic and mitochondrial uncoupler with antibacterial, insecticidal, and acaricidal activities. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4+, and it can also inhibit the surface expression of endogenous HSP60. In addition, Nonactin can induce apoptosis in β-catenin mutant tumor cells and has anti-tumor activity .
Eupenifeldin is pentacyclic bistropolone isolated from cultures of Eupenicillium brefeldianum ATCC 74184. Eupenifeldin is cytotoxic against the HCT-116 cell line. Eupenifeldin has the potential for the research of leukemia .
Germanicol is a selective antineoplastic agent against human colon cancer cell lines HCT-116 and HT29 . Germanicol induces apoptosis via chromatin condensation and DNA damage .
AUH Human Pre-designed siRNA Set A contains three designed siRNAs for AUH gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight .
4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan is a lignans that can be isolated from the Viburnum foetidum. 4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan has cytotoxicity against A549, SK-OV-3, SKMEL-2 and HCT15 cell line with IC50s of 67.14, 67.38, 64.11 and 76.31 μg/mL, respectively .
GTSE1-IN-1 (compound Y18) is an orally active GTSE1 inhibitor with anticancer activity. GTSE1-IN-1 significantly inhibits cancer cell proliferation by inhibiting the transcription and expression of GTSE1, causing DNA damage and persistently inducing cell cycle arrest and cell senescence. In addition, GTSE1-IN-1 significantly inhibits the adhesion, migration and invasion of colorectal cancer HCT116 cells and non-small cell lung cancer A549 cells in vitro .
Rostratin A is a cytotoxic disulfide found in the marine-derived fungus Exserohilum rostratum. Rostratin A shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with an IC50 of 8.5 μg/mL .
Goniothalenol is a styryl lactone that can be isolated from Goniothalamus griffithii. Goniothalenol exhibits cytatoxic activity against A2780, HCT-8, KB and MCF-7 cell lines .
Pradimicin Q is an antibiotic. The cytotoxicity (IC50) to human colon HCT-116 cells and murine melanoma B16-F10 cells are 75 and 100 μg/mL, respectively .
Anticancer agent 160 (Compound 6) is a natural product derived from Parthenium hysterophorus. Anticancer agent 160 is cytotoxic to HCT-116 cells, IC50=5.0 μM .
Antitumor agent-93 (compound 7D) is an anticancer agent that can effectively inhibit the growth of several tumor cell lines, such as MDA-MB-231 and HCT-116 cell lines .
Makaluvamine A is a member of Makaluvamines. Makaluvamines can be isolated from Fijian sponges of the genus Zyzzya, and possess inhibitory activity toward topoisomerase II along with cytotoxic activity against HCT-116 human colon cancer cells .
Hsp90-IN-38 (compound 20m) is a HSP90 (heat shock protein) inhibitor. Hsp90-IN-38 exhibits strong HSP90 binding affinity with a Kd of 87 nM. Hsp90-IN-38 inhibits ATPase with an IC50 of 0.13 μM. Hsp90-IN-38 inhibits HCT116, MCF-7, SKBr3, K562 and A549 cells with IC50s of 0.187, 0.072, 0.105, 0.403 and 031 μM, respectively .
CDK9-IN-35 (compound 10j) is an inhibitor of CDK9/Cyclin T1 with an IC50 value of 10.2 nM and against the HCT-116 cell line with an IC50 value of 20 nM .
Anticancer agent 16 exhibits good cytotoxic activity against HCT-116, NCI-H460, and SKOV3 cell lines with IC50 8.55 μΜ, 5.41 μΜ, and 6.4 μΜ, respectively.
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
Janelia Fluor® 549 TFA (JF549 TFA) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor? 549, Azide (JF549, Azide) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor? products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
PA Janelia Fluor 549, SE (PA-JF549-NHS) is a bright photoactivatable fluorophore of JF549,SE (JF549,NHS). JF549,SE (JF549,NHS) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor® 549, SE (JF549, SE) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor® 549, Tetrazine (JF549, Tetrazine) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Janelia Fluor® 549, Maleimide TFA (JF549, Maleimide TFA) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
LysoSR-549 is a multifunctional dye. Dyes are important tools in biological experiments. They can help researchers observe and analyze cell structures, track biomolecules, evaluate cell functions, distinguish cell types, detect biomolecules, study tissue pathology and monitor microorganisms. Their applications range from basic scientific research to clinical A wide range of diagnostics. Dyes are also widely used in traditional fields such as textile dyeing, as well as in emerging fields such as functional textile processing, food pigments and dye-sensitized solar cells.
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
Braftide is an allosteric inhibitor for BRAF kinase by targeting the dimer interface of BRAF kinase and inhibiting the formation of BRAF dimers. Braftide inhibits wild-type BRAF and oncogenic BRAF G469A with IC50 of 364 nM and 172 nM, respectively. Braftide inhibits MAPK signaling pathway, inhibits proliferation of KRAS mutant tumor cells (EC50 is 7.1 and 6.6 μM, for HCT116 and HCT-15), in combination of TAT sequence .
HCT116 is a peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 of 54 nM. HCT116 can inhibit the N-terminal methylation level of NTMT1/2 substrates in HCT116 cells, and is used for the study of NTMT1/2 probes.
Verrucarin J (Muconomycin B) is a metabolite of the Myrothecium fungus family. Verrucarin J generates reactive oxygen species (ROS) and induces apoptosis of cancer cell lines, such as A549, HCT 116 and SW-620 cells. Verrucarin J shows activities against Candida albicans and Mucor miehei. Verrucarin J inhibits arenavirus Junin (JUNV) yield with an IC50 of 1.2 ng/mL .
Macrocalin B is a diterpenoid, which can be isolated from Isodon xerophilus. Macrocalin B inhibits the proliferation of cancer cells K562, HL-60, A549, MKN, CA and HCT with IC50 of 2.81-171 μM. Macrocalin B inhibits the telomerase in K562 with an IC50 in nanomolar level .
Cepharadione B (compound 22) is a natural compound isolated from the leaves of Piper sanctum. Cepharadione B is a tyrosinase inhibitor with an IC50 value of 170 μM, and inhibits cell growth in A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cells .
Norcepharadione B is an alkaloid that can be isolated from Houttuynia cordata. Norcepharadione B exhibits moderate cytotoxicity against A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15 cell line with ED50s of 40, 26.4, 40, 14.2 and 38.2 μg/mL, respectively .
Broussonol E is a diprenylated flavonol. Broussonol E can be isolated from the leaves of Broussonetia kazinoki. Unlike some dinonylated flavonol derivatives, Broussonol E has no cytotoxicity to human tumor cell lines (A549, HCT-8, KB) .
Kopsoffinol, a bisindole alkaloid, shows in vitro growth inhibitory activity against human PC-3, HCT-116, MCF-7, and A549 cells and moderate effects in reversing multidrug-resistance in vincristine-resistant human KB cells .
Chlorovaltrate K is a chlorinated valepotriate with anticancer effects. Chlorovaltrate K shows moderate cytotoxicity against A549, PC-3M, HCT-8 and Bel 7402 cell lines with IC50 values of 2.32-8.26 μM .
3-epi-Isocucurbitacin B (Compound 5) is a cucurbitane triterpene derived from Trichosanthes kirilowii. 3-epi-Isocucurbitacin B shows significant cytotoxicity to human tumor cells A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT15 .
Gambogic acid B is an active compound. Gambogic acid B can be isolated from the resin of Garcinia hanburyi.. Gambogic acid B has cytotoxicity against A549, HCT116 and MDA MB 231 cells with IC50 values of 1.60 μM, 6.88 μM and 0.87 μM, respectively .
8-epi-Helenalin is a semitterpene lactone with anti-tumor activity that can be isolated from Inula britannicaL. var. chinensis (Rupr.) Reg. and the ED50 values of 8-epi-Helenalin for HL-60, A549, MCF7, HCT-15, SK-OV-3 and Malme-3M are 12.2 μM, 53.8 μM, 9.1 μM, 8.7 μM, 18.7 μM and 8.3 μM, respectively. 8-epi-Helenalin can be used for anti-tumor studies .
1 α-hydroxytorilin (compound 3) is a sesquiterpenoid. 1 α-hydroxytorilin can be isolated from Torilis japonica. 1α-hydroxytorilin has cytotoxicity against human A549, SK-OV-3, SK-MEL-2, and HCT15 tumor cells with ED50 values of 20.52, 18.24, 17.48, 42.54 μg/mL, respectively .
Glucozaluzanin C is a lignan isolated from the MeOH extract of the roots of Ainsliaea acerifolia (Compositae). Glucozaluzanin C has ED50 value of 2.45 μg/mL, 1.37μg/mL, 0.40 μg/mL, 1.41 μg/mL, 1.43 μg/mL for A549 cells, SK-OV-3 cells, SK-MEL-2 cells, XF498 cells, HCT15 cells, respectively .
Emeguisin A is a depsidone with an antibacterial activity. Emeguisin A inhibits the human colon carcinoma (HCT-116) cell viability with rate of 87.06% .
Angelylalkannin is a naphthoquinone compound isolated from the root of Alkanna tinctoria. Angelylalkannin showed significant inhibitory effects in the antiproliferative effect test on human colon cancer cells HCT-116 and SW-480. The median inhibitory concentration (IC50) of Angelylalkannin was 4.76 mM for HCT-116 cells and 7.03 mM for SW-480 cells. Like alkannin, Angelylalkannin can arrest the cell cycle in the G1 phase and induce apoptosis at a concentration of 1-10 mM.
Nonactin is a macrotetrolide antibiotic and mitochondrial uncoupler with antibacterial, insecticidal, and acaricidal activities. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4+, and it can also inhibit the surface expression of endogenous HSP60. In addition, Nonactin can induce apoptosis in β-catenin mutant tumor cells and has anti-tumor activity .
Eupenifeldin is pentacyclic bistropolone isolated from cultures of Eupenicillium brefeldianum ATCC 74184. Eupenifeldin is cytotoxic against the HCT-116 cell line. Eupenifeldin has the potential for the research of leukemia .
Germanicol is a selective antineoplastic agent against human colon cancer cell lines HCT-116 and HT29 . Germanicol induces apoptosis via chromatin condensation and DNA damage .
4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan is a lignans that can be isolated from the Viburnum foetidum. 4,4'-Dihydroxy-3,3',9-trimethoxy-9,9'-epoxylignan has cytotoxicity against A549, SK-OV-3, SKMEL-2 and HCT15 cell line with IC50s of 67.14, 67.38, 64.11 and 76.31 μg/mL, respectively .
Rostratin A is a cytotoxic disulfide found in the marine-derived fungus Exserohilum rostratum. Rostratin A shows in vitro cytotoxicity against human colon carcinoma (HCT-116) with an IC50 of 8.5 μg/mL .
Goniothalenol is a styryl lactone that can be isolated from Goniothalamus griffithii. Goniothalenol exhibits cytatoxic activity against A2780, HCT-8, KB and MCF-7 cell lines .
Pradimicin Q is an antibiotic. The cytotoxicity (IC50) to human colon HCT-116 cells and murine melanoma B16-F10 cells are 75 and 100 μg/mL, respectively .
Benzoin (DL-Benzoin), a natural balsamic resin, is a PI3Kα inhibitor with anticancer effects. Benzoin inihits the growth of colon cancer cell line (HCT-116). Benzoin can be used as a food additive .
The EIF5 protein is a key member of the 43S pre-initiation complex (43S PIC) and actively participates in mRNA cap-proximal binding, scanning 5'-untranslated regions and locating start codons. EIF5 Protein, Human (His-SUMO) is the recombinant human-derived EIF5 protein, expressed by E. coli , with N-SUMO, N-6*His labeled tag. The total length of EIF5 Protein, Human (His-SUMO) is 431 a.a., with molecular weight of 65.2 kDa.
MAT2A-IN-23 (compound 39) is a MAT2A inhibitor, with an IC50 of 4 nM. MAT2A-IN-23 inhibits SAM in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 3 and 2 nM, respectively. MAT2A-IN-23 inhibits SDMA in the HCT-116 (MTAP −/−) and in the HCT-116 WT cell line with IC50s of 2 and >3000 nM, respectively. MAT2A-IN-23 inhibits HCT-116 (MTAP −/−) cell proliferation with with an IC50 of 47 nM .
Antitumor agent-183 (compound 3f) has antitumor activity with metabolic stability. Antitumor agent-183 inhibits cancer cell growth, with IC50s less than 5 nM for A549, HCT116, and HS578T cells. The albumin-bound nanoparticle formulation of Antitumor agent-183 has prolonged retention in the tumor tissues .
Janelia Fluor? 549, Azide (JF549, Azide) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor? products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute. It contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing alkyne groups. It can also undergo ring strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing DBCO or BCN groups.
Janelia Fluor® 549, Tetrazine (JF549, Tetrazine) is a fluorescent dye with the absorption maximum (λab (max)) of 549 nm and emission maximum (λem (max)) of 571 nm . Janelia Fluor® products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
hDHODH-IN-15 (Compound H19) is an inhibitor for human dihydroguanylate dehydrogenase (hDHODH) with an IC50 of 0.21 µM. hDHODH-IN-15 exhibits cytotoxicity in cancer cells NCI-H226, HCT-116, and MDA-MB-231, with IC50 of 0.95-2.81 µM. hDHODH-IN-15 induces ferroptosis in HCT-116, and exhibits antitumor efficacy .
DC-Chol hydrochloride is a cationic lipid. DC-Chol hydrochloride could inhibit Aβ40 fibril formation under appropriate experimental conditions. DC-Chol hydrochloride strongly inhibits amyloidogenesis of oxidized hCT in a dose-dependent manner. DC-Chol hydrochloride induces the production of Th1 (IL-2 and IFN-γ) and Th2 (IL-5) cytokines. DC-Chol hydrochloride can enhance the body's immune response to antigens. DC-Chol hydrochloride is used as a gene delivery vector. DC-Chol hydrochloride can be used in research in areas such as hepatitis B vaccines to improve vaccine immunity .
hsa-miR-549a-5p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
hsa-miR-549a-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
hsa-miR-549a-5p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
hsa-miR-549a-3p inhibitors are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA inhibitors have full-length nucleotide 2'-methoxy modification. The miRNA inhibitors strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning.
hsa-miR-549a-5p agomirs are chemically-modified double-strand miRNA mimics with modified mature miRNA strand: 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 3' end cholesterol group, and full-length nucleotide 2'-methoxy modification. They are designed to mimic endogenous miRNAs and recommended for miRNA functional studies. Compared with miRNA mimics, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
hsa-miR-549a-3p agomirs are chemically-modified double-strand miRNA mimics with modified mature miRNA strand: 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 3' end cholesterol group, and full-length nucleotide 2'-methoxy modification. They are designed to mimic endogenous miRNAs and recommended for miRNA functional studies. Compared with miRNA mimics, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
hsa-miR-549a-3p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
hsa-miR-549a-5p antagomirs are chemically-modified oligonucleotides that hybridize with mature miRNAs. The miRNA antagomirs have 2 phosphorothioates at the 5' end, 4 phosphorothioates at the 3' end, 1 cholesterol group at the 3' end, and full-length nucleotide 2'-methoxy modification. The miRNA antagomirs strongly compete with mature miRNAs to prevent the complementary pairing of miRNAs and their target genes, thereby inhibiting miRNAs from functioning. Stability of miRNA antagomirs appears to be significantly higher than miRNA inhibitors, they exhibits enhanced cellular uptake, stability and regulatory activity in vivo.
AUH Human Pre-designed siRNA Set A contains three designed siRNAs for AUH gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
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