Search Result
Results for "
HT-29
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-121458
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Apoptosis
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Cancer
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Nemorosone is the main component of the floral resin of Clusia rosea. Nemorosone has an antiproliferative effect on cancer cells. Nemorosone induces apoptosis in HT-29 and LoVo cells .
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- HY-122675
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Choline Kinase
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Cancer
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ACG416B (compound 18) is a potent inhibitor of ChoK (choline kinase) with an IC50 of 0.4 μM. ACG416B renders higher ChoK inhibitory and antiproliferative activities against the HT-29 human colon cancer cell .
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- HY-160811
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VEGFR
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Cancer
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hVEGF-IN-3 (compound 9) is a potent hVEGF inhibitor. hVEGF-IN-3 inhibits HT-29, MCF-7, and HEK-293 cells proliferation with IC50s of 61, 142, and 114 μM .
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- HY-13620
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LU 79553
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Topoisomerase
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Cancer
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Elinafide is an anticancer agent with a naphthalimide structure that targets DNA. Elinafide interferes with cell metabolism by inserting a planar ring into the DNA double helix and interacting with enzymes through its side chain.LU-79553 is a DNA-binding topoisomerase II inhibitor. The IC50 value of Elinafide for HT-29 cells is 0.014 μM .
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- HY-161361
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Mixed Lineage Kinase
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Cancer
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MLKL-IN-7 (compound 9) is a MLKL inhibitor, and shows anti-necroptosis activity in HT-29 cells with the IC50 of 148.4 nM .
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- HY-146274
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c-Met/HGFR
Apoptosis
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Cancer
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c-Met-IN-10 (compound 26a) is a highly potent c-Met kinase inhibitor with an IC50 value of 16 nM. c-Met-IN-10 has inhibitory activity against cancer cells A549, H460 and HT-29 with IC50s of 0.56 ~ 1.59 μM. c-Met-IN-10 suppresses the colony formation on HT-29 cells, induces HT-29 and A549 cells apoptosis, and inhibits A549 cells motility. c-Met-IN-10 can be used for researching anticancer .
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- HY-N8025
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Others
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Cancer
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Nephthenol is a terpenoid that can be isolated from Nephthea brassica. Nephthenol exhibits cytotoxicity in cells A549, HT-29, KB and P-388 with IC50s of 2.72, 3.01, 1.84, and 0.42 µg/mL, respectively .
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- HY-W727999
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Apoptosis
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Cancer
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Koenimbine is an anticancer agent that can be obtained from the leaves and fruits of Murraya koenigii. Koenimbine can induce apoptosis and necrosis in HT-29 and SW48 cells. Koenimbine can be used in the research of cancer .
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- HY-N3123
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Dihydrooxochelerythrine
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Others
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Cancer
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Oxychelerythrine is an alkaloid that can be isolated from Zanthoxylum integrifoliolum. Oxychelerythrine exhibits cytotoxicity against P-388 and HT-29 cell lines with ED50s of 3.25 and 5.48 μg/mL, respectively .
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- HY-157085
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HSP
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Cancer
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BX-2819 is a Hsp90 inhibitor with an IC50 value of 41 nM. BX-2819 inhibits the proliferation of cancer cells. BX-2819 can significantly inhibit the growth of NCI-N87 and HT-29 tumors in nude mice .
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- HY-N1631
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1-Hydroxyrutaecarpine
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Drug Derivative
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Others
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1-Hydroxyrutaecarpine (compound 1a) is a hydroxy-derivative of rutaecarpine. 1-Hydroxyrutaecarpine shows cytotoxicities with ED50s of 3.72, 7.44 µg/mL for P-388 and HT-29 cells, respectively. 1-Hydroxyrutaecarpine shows antiplatelet activity .
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- HY-161614
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Microtubule/Tubulin
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Cancer
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Tubulin inhibitor 44 (Compound 26r) is an inhibitor for tubullin. Tubulin inhibitor 44 exhibits cytotoxicity in cancer cells NCI-H460, BxPC-3 and HT-29, with IC50s of 0.96, 0.66 and 0.61 nM, respectively .
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- HY-107664A
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Neurotensin Receptor
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Neurological Disease
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SR 142948 dihydrochloride is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-149952
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ATM/ATR
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Cancer
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ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers .
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- HY-N10132
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nAChR
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Infection
Neurological Disease
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Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
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- HY-12855
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Autophagy
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Cancer
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Lys01, a dimeric form of Chloroquine (HY-17589A), is an autophagy inhibitor. Lys01 inhibits cell viability of 1205Lu, c8161, LN229, HT-29 cells with IC50s of 3.6, 3.8, 7.9, 6.0 μM. Lys01 can be used for anticancer research .
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- HY-147725
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 4 (compound 2) is a potent microtubule inhibitor. Microtubule inhibitor 4 shows cytotoxicity with IC50s of 4.0, 3.2, 2.1 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 4 shows the inhibition of tubulin polymerization .
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- HY-147727
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Microtubule/Tubulin
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Cancer
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Microtubule inhibitor 6 (compound 17o) is a potent microtubule inhibitor. Microtubule inhibitor 6 shows cytotoxicity with IC50s of 14.0, 6.6, 7.0 nM for NCI-H460, BxPC-3, HT-29 cells, respectively. Microtubule inhibitor 6 efficiently inhibits microtubule polymerization .
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- HY-N1655
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Others
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Cancer
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2,3-Dihydroamentoflavone 7,4'-dimethyl ether is a biflavonoid, which can be isolated from the aerial parts of Selaginella delicatula. 2,3-Dihydroamentoflavone 7,4'-dimethyl ether exhibits cytotoxicities against P-388 and HT-29 cell lines, with ED50 (median effective dose) values of 3.50 and 5.25 µg/mL, respectively .
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- HY-173074
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Microtubule/Tubulin
MDM-2/p53
Apoptosis
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Cancer
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Microtubulin-IN-1 (Compound 8g) is the inhibitor for microtubulin that targets colchicine-binding site, disrupts the microtubulin integrity, and induces the upregulation of p53. Microtubulin-IN-1 exhibits antiproliferative activity in a variety of cancer cell lines (IC50 for NCI-H460, BxPC-3 and HT-29 is 2.4, 1.6 and 2.07 nM, respectively), arrests the cell cycle at G2/M phase, and induces apoptosis in NCI-H460 .
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- HY-P3116
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Bacterial
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Cancer
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Thiocoraline is a depsipeptide that can be isolated by marine Micromonospora. Thiocoraline has antitumor activity with IC50s of 0.002, 0.002, 0.01 and 0.002 μg/mL in P388, A549, HT-29 and MEL-28 cells, respectively. Thiocoraline also a strong antimicrobial activity against Gram-positive microorganisms .
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- HY-161282
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Carbonic Anhydrase
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Neurological Disease
Cancer
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hCAII-IN-10 (compound 11d) is hCA II inhibitor with the IC50s of 14 nM and 29.2 μM for hCA II and hCA I, respectively. hCAII-IN-10 inhibits cell growth against HT-29 cells with the IC50 of 74 μM. hCAII-IN-10 shows strongly lowered intraocular pressure in the glaucomatous rabbit eye model .
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- HY-163806
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HDAC
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Neurological Disease
Cancer
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NT376 is a high potency and selectivity inhibitor of class-IIa Histone deacetylases (HDAC) with an IC50 value of 32 nM, similar to NT160 (HY-149285) (IC50= 46 nM) in HT-29 cells. NT376 is proming for research of various cancers and in the diseases of the central nervous system (CNS) such as Alzheimer’s and Huntington’s diseases .
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- HY-139062
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C6 Ceramide (d18:1/6:0) Urea; Cer(d18:1/6:0) Urea; D-erythro-Urea-C6-Ceramide
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Apoptosis
Ceramidase
Autophagy
β-catenin
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Cancer
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C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
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- HY-170834
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Microtubule/Tubulin
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Cancer
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Antiproliferative agent-66 (Compound B3) is an antiproliferative agent that induces apoptosis and cell cycle arrest with IC50 values in the range of 2.03-3.6 µM against SH-SY5Y neuroblastoma, HT-29 colorectal adenocarcinoma, and fibroblast cells. Antiproliferative agent-66 is also a tubulin polymerization inhibitor with an IC50 of 0.79 µM .
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- HY-101524
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TC13172
2 Publications Verification
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Mixed Lineage Kinase
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Cancer
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TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells .
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- HY-151542
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Mixed Lineage Kinase
Necroptosis
RIP kinase
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Neurological Disease
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MLKL-IN-4 (compound 56) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-4 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 82 nM . MLKL-IN-4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-151541
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Mixed Lineage Kinase
Necroptosis
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Neurological Disease
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MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC50 of 31 nM . MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-157740
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HDAC
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Cancer
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XSJ-10 is a HDAC inhibitor containing a RAS/RAF protein interfering unit, with IC50s of 0.05 and 0.04 μM in PANC-1 cells and HT-29 cells. XSJ-10 can effectively induce the apoptosis of cancer cells and suppress the tumor by strongly inhibiting the RAS-RAF-MEK-ERK signaling pathway and the acetylation level of HDAC3 .
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- HY-164350
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Ras
ERK
p38 MAPK
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Cancer
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KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .
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- HY-163390
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RIP kinase
Necroptosis
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Inflammation/Immunology
Cancer
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RIP1 kinase inhibitor 9 (compound SY-1) is a selective RIP kinase inhibitor. RIP1 kinase inhibitor 9 effectively suppresses the central inflammatory response induced by epilepsy. RIP1 kinase inhibitor 9 inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis in HT-29 cells with an EC50 of 7.04 nM .
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- HY-157516
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CDK
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Cancer
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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 .
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- HY-169409
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VEGFR
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Cancer
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VEGFR-2-IN-59 (Compound 3h) is an inhibitor for VEGFR2 with an IC50 of 3.73 µM. VEGFR-2-IN-59 exhibits cytotoxicity in cancer cell A549, HT-29, A375, MCF7 and NHDF with IC50 of 20.91, 19.70, 9.63, 17.43 and 20.71 μM. VEGFR-2-IN-59 inhibits formation of tubular structure and exhibits anti-angiogenic property .
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- HY-169652
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Reactive Oxygen Species
AMPK
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Cancer
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NPC26 is a small molecule mitochondrial disruptor with anti-tumor activity. NPC-26 shows significant anti-proliferative and cytotoxic effects on CRC cell lines (HCT-116, DLD-1, and HT-29). NPC26 can damage mitochondrial function, leading to the opening of the mitochondrial permeability transition pore (mPTP) and the production of reactive oxygen species, ultimately inducing cell death. NPC-26 can kill CRC cells by activating the AMP-activated protein kinase (AMPK) signaling pathway .
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- HY-123707
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Microtubule/Tubulin
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Cancer
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KPU-300 (compound 6b) is a tubulin inhibitor. KPU-300 has potent cytotoxicity with an IC50 value of 7.0 nM against HT-29 cells .
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- HY-W928623
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ATTSC
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Bacterial
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Infection
Cancer
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2-Acetylthiophene thiosemicarbazone is an antibacterial agent. 2-Acetylthiophene thiosemicarbazone exhibits anticancer activity, with an IC50 value of 8.6 μM against HT-29 cells .
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- HY-156375
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Pyruvate Kinase
PDK-1
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Cancer
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PKM2 activator 6 (Compound Z10) is a PKM2 activator and PDK1 inhibitor (KD: 121 and 19.6 μM respectively). PKM2 activator 6 induces colorectal cell apoptosis, and inhibits cell proliferation and migration . PKM2 activator 6 inhibits glycolysis. PKM2 activator 6 inhibits proliferation of DLD-1, HCT-8, HT-29, MCF-10A cells (IC50: 10.04, 2.16, 3.57, 66.39 μM) .
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- HY-126779
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Fungal
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Cancer
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Stictic acid is a secondary metabolite that can be isolated from the lichen Lobaria pulmonaria (L.) Hoffm. Stictic acid inhibits growth of human colon adenocarcinoma HT-29 cells (IC50: 29.29 μg/mL) .
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- HY-169735
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Aurora Kinase
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Cancer
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Aurora A inhibitor 4 (compound C9) is a potent inhibitor of Aurora A, with the GI50 of 4.26 and 7.08 μM in DU 145 cells and HT-29 cells, respectively .
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- HY-139248
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Drug Derivative
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Cancer
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Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively) .
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- HY-139206
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- HY-P10761
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Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
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Cancer
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DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130?nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-N12430
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Others
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Cancer
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Marsdenoside A (compound 7) is a Marsdenoside isolated from Alocasia genus. Marsdenoside A has a weak growth inhibitory effect on two tumor cell lines, MGC-803 and HT-29, with IC50 >50 μg/mL.
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- HY-N8225
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(-)-Manassantin B
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Others
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Others
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Manassantin B (compound 6) is a kind of lignan. Manassantin B can be isolated from the ethyl acetate extract of the roots of Saururus chinensis. Manassantin B has cytotoxicities against HT-29 with an IC50 value of 12 μM .
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- HY-107664
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Neurotensin Receptor
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Neurological Disease
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SR 142948 is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders .
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- HY-149511
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c-Met/HGFR
Apoptosis
PDGFR
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Cancer
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MET/PDGFRA-IN-2 (compound 8h) is a MET and PDGFRA protein inhibitor. MET/PDGFRA-IN-2 induces cell apoptosis. MET/PDGFRA-IN-2 inhibits proliferation of MET-positive cells (IC50s: 9.7, 6.1, 12.0, 11.5, 8.6, 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
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- HY-173166
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PPAR
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Cancer
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PPARγ agonist 17 (Compound C1) is a PPARγ agonist. PPARγ agonist 17 enhances PPARγ activity and blocks the cell cycle in G2/M phase, inhibits cell migration and induces apoptosis in HT-29 cells. PPARγ agonist 17 has a broad spectrum anti-proliferative activity in cancer cells with relatively low toxicity in normal cells which cannot cross the blood-brain barrier .
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- HY-N3057
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Others
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Cancer
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Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
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- HY-12855A
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Lys05
3 Publications Verification
Lys01 trihydrochloride
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Autophagy
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Cancer
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Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
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- HY-157963
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- HY-147348
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Biochemical Assay Reagents
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Cancer
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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 .
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- HY-13734
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IV-2
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Apoptosis
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Cancer
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PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively.
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- HY-N12437
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Others
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Cancer
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Marsdenoside B (compound 8) is a Marsdenoside isolated from Alocasia genus. Marsdenoside B inhibits the growth of tumor cell lines MGC-803 and HT-29 with IC50s of 25.6 μg/mL and 32.4 μg/mL, respectively.
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- HY-149510
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c-Met/HGFR
Apoptosis
PDGFR
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Cancer
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MET/PDGFRA-IN-1 (compound 8c) is a MET and PDGFRA protein inhibitor (IC50: 36 μM for MET). MET/PDGFRA-IN-1 inhibits MET phosphorylation and induces cell apoptosis. MET/PDGFRA-IN-1 inhibits proliferation of MET-positive cells (IC50s: 15.3, 19.0, 22.0, 25.6, 21.0, 31.5 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, K562 cells respectively) .
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- HY-163692
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Microtubule/Tubulin
Apoptosis
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Cancer
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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 .
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- HY-160170
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Necroptosis
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Cancer
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Necrosis inhibitor 3 (compound B3) is a poteng inhibitor of necrosis, with the IC50 value of 0.29 nM in HT29 cells .
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- HY-N12820
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Others
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Cancer
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3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C can be isolated from Alocasia cucullata (Lour.) G. Don. 3-O-6-Deoxy-3-O-methyl-β-D-allopyranosyl-(1→4)-β-D-oleandropyranosyl-tenacigenin C has moderate tumor cells inhibitory activity against MGC-803 and HT-29 cells with IC50 values of 45.6 and 28.4 μg/mL, respectively .
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- HY-N8934
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Others
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Cancer
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6β-Hydroxytomentosin, a sesquiterpenoid, can be found in flowers of Inula japonica. 6β-Hydroxytomentosin exhibits weak cytotoxicities against A549, SK-OV-3, HepG-2 and HT-29 cell lines .
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- HY-159795
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PF-07799933; ARRY-440
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Raf
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Cancer
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Claturafenib ( PF-07799933) is an inhibitor of pan-mutant BRAF. Claturafenib inhibits pERK in HT29 cells with an IC50 value of 1.6 nM .
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- HY-156775
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Others
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Cancer
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Antitumor agent-119 (compound 13K) is a 2-benzoxazolyl hydrazone derivative with anticancer activities. Antitumor agent-119 inhibits the cell growth of Butkitt, CCRF-CEM, HeLa, and HT-29 with IC50 values of 30 nM, 140 nM, 100 nM, and 40 nM, respectively .
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- HY-14444
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NPI-2358
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Microtubule/Tubulin
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Cancer
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Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells . Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cells .
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- HY-161852
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PI3K
Apoptosis
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Cancer
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PI3K-IN-55 (Compound 6a) is a potent inhibitor for PI3K. PI3K-IN-55 affects PI3K/Akt/p53 signaling pathway, inhibits the proliferation of cancer cells A549, Hela, HepG2, MCF-7 and HT-29, with IC50s of 1.03-6.78 μM. PI3K-IN-55 induces apoptosis in cell MCF-7 .
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- HY-N6002
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Apoptosis
Autophagy
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Cancer
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3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 µM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer .
|
-
- HY-169074
-
|
|
E3 Ligase Ligand-Linker Conjugates
|
Cancer
|
|
Thalidomide-N-methylpiperazine is an E3 Ligase Ligand-Linker Conjugate. Thalidomide-N-methylpiperazine can be used to synthesize PROTAC MLKL Degrader-2 (HY-169072) to exhibit antinecroptotic activity on human cell lines and effectively degrade MLKL in the HT-29 xenograft mouse model .
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-
- HY-161628
-
|
|
Topoisomerase
|
Cancer
|
|
Tapcin is a dual inhibitor for topoisomerase I and topoisomerase II, with IC50 of 203 and 71 nM. Tapcin inhibits proliferations of cancer cells A-375, HeLa, Huh7.5, U2-OS, A549, Caco-2 and HT29, with IC50s of 441, 1.04, 40.5, 0.002, 0.006, 0.287 and 0.842 nM, respectively. Tapcin exhibits antitumor activity in HT29 xenograft model .
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-
- HY-N3057R
-
|
|
Others
|
Cancer
|
|
Pinostrobin chalcone (Standard) is the analytical standard of Pinostrobin chalcone. This product is intended for research and analytical applications. Pinostrobin chalcone is found to be potent natural cytotoxic compounds against MDA-MB-231 and HT-29 colon cancer cell lines(IC50 = 20.42±2.23 and 22.51±0.42 μg/mL) .
|
-
- HY-121199
-
|
|
Apoptosis
|
Cancer
|
|
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 .
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-
- HY-B1714A
-
|
|
Others
|
Cancer
|
|
NSC 601980 is an anti-tumor compound. In yeast screening experiments, NSC 601980 inhibits cell proliferation in COLO205 and HT29 cell lines with LogGI50 of -6.6 and -6.9, respectively.
|
-
- HY-156098
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-19 (Compound 21j) is a c-Met inhibitor (IC50: 1.99 nM). c-Met-IN-19 shows cytotoxicity against A549, HT-29, SGC-7901, MDA-MB-231 cells with IC50s of 0.25, 0.36, 0.98, 0.76 μM .
|
-
- HY-155240
-
|
|
Tyrosinase
|
Cancer
|
|
Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
|
-
- HY-75564
-
|
|
Endogenous Metabolite
|
Cancer
|
|
Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM .
|
-
- HY-155152
-
|
|
P-glycoprotein
BCRP
|
Cancer
|
|
P-gp/BCRP-IN-2 (compound 15) is an oxadiazole derivative and a dual inhibitor of the ABC transporter P-glycoprotein (IC50: 1.6 nM) and BCRP (IC50: 600 nM). P-gp/BCRP-IN-2 also enhances the anti-proliferative effects of Doxorubicin (HY-15142A) in drug-resistant human adenocarcinoma colon cancer cell lines HT29/DX and MDCK-MDR1 cells .
|
-
- HY-169938
-
|
|
HDAC
Histone Demethylase
Apoptosis
|
Cancer
|
|
LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
|
-
- HY-N1261
-
|
|
Others
|
Cancer
|
|
Scutebarbatine B shows significant cytotoxic activities against three human cancer lines, namely, HONE-1 nasopharyngeal, KB oral epidermoid carcinoma, and HT29 colorectal carcinoma cells, with IC50 values in the range 3.5-8.1 mM [1]<
|
-
- HY-B1714
-
|
|
Drug Derivative
|
Cancer
|
|
NSC 601980 analog is an analogue of NSC601980. In yeast screening experiments, NSC 601980 exhibited antitumor activity, effectively inhibiting cell proliferation in both COLO 205 and HT29 cell lines, with Log GI 50 values of -6.6 and -6.9, respectively.
|
-
- HY-169239
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-20 (compound ±34) is a reversible monoacylglycerol lipase (MAGL) inhibitor. MAGL-IN-20 exhibits appreciable antiproliferative activities against several cancer cells, including H460, HT29, CT-26, Huh7 and HCCLM-3. .
|
-
- HY-P1435
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-120528A
-
-
- HY-115949
-
|
|
HSP
|
Cancer
|
|
Antitumor agent-47 (Compound 3e) is a silibinin derivative with an antitumor activity. Antitumor agent-47 shows cytotoxic activity against NCI-H1299 and HT29 cells with IC50 values of 8.07 µM and 6.27 µM, respectively .
|
-
- HY-120528
-
-
- HY-N8387
-
|
|
Ras
|
Cancer
|
|
Neogrifolin is an inhibitor of KRAS. Neogrifolin suppress KRAS expression in human colon cancer cells. Neogrifolin has anti-cell viability activity against HeLa, SW480 and HT29 cells wih IC50s of 24.3, 34.6, and 30.1 μM, respectively .
|
-
- HY-146778
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 25 is a potent tubulin inhibitor with an IC50 value of 0.98 μM. Tubulin inhibitor 25 exhibits remarkable activity against cancer cell line HT29. Tubulin inhibitor 25 displays the potent inhibition on cell migration and tube formation that contributes to the anti-angiogenesis .
|
-
- HY-P1435A
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds TFA is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds TFA can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-N8462
-
|
Scutebatin C
|
Others
|
Cancer
|
|
6-O-Nicotinoylscutebarbatine G is an alkaloid that can be isolated from Scutellaria barbata.6-O-Nicotinoylscutebarbatine has cytotoxic activities against HONE-1, KB and HT29 cells with IC50s of 3.1, 2.1 and 5.7 μM, respectively .
|
-
- HY-130602
-
|
|
PROTACs
MEK
|
Cancer
|
|
MS432 is a first-in-class and highly selective PD0325901-based von Hippel-Lindau-recruiting PROTAC degrader for MEK1 and MEK2. MS432 displays good plasma exposure in mice, exhibiting DC50 values of 31 nM and 17 nM for MEK1, MEK2 in HT29 cells respectively .
|
-
- HY-100753
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-1 (compound 7d) is an excellent, selective and orally active STAT3 inhibitor, with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. STAT3-IN-1 (compound 7d) induces tumor cells apoptosis .
|
-
- HY-146505
-
|
|
Microtubule/Tubulin
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-6 (compound 5f) is a potent tubulin polymerization inhibitor, with an IC50 of 1.09 μM. Tubulin polymerization-IN-6 inhibits cell migration and tube formation and contributes to the anti-angiogenesis. Tubulin polymerization-IN-6 can greatly inhibit tumor growth on HT29 xenograft Balb/c nude mice .
|
-
- HY-164467
-
|
|
Wnt
|
Cancer
|
|
CCT070535 blocks TCF-dependent transcription at the TCF level, with GI50 values of 17.6 μM, 11.1 μM, 11.8 μM and 13.4 μM in HT29 (APC mutant), HCT116 (oncogenic β-catenin), SW480 (APC mutant) and SNU475 (Axin mutant) cells, respectively .
|
-
- HY-118899
-
|
|
Endogenous Metabolite
|
Cancer
|
|
XR5944 is an anti-tumor compound with DNA-targeting activity. As a topoisomerase inhibitor, XR5944 can effectively inhibit the activities of topoisomerase I and II. XR5944 shows excellent anti-tumor activity against human and mouse tumor cells in vitro and in vivo. XR5944 exhibits significant potency in multiple cell lines, with IC50 values of 0.04-0.4 nM. XR5944 is not affected by atypical drug resistance in cells and remains significantly active even in cells overexpressing P-glycoprotein or multidrug resistance-related proteins. XR5944 showed anti-tumor efficacy in human tumor models of H69 small cell lung cancer and HT29 colon cancer, inducing tumor regression in most animals in the HT29 model. XR5944 can be used to study biological processes related to colon and lung cancer .
|
-
- HY-161900
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 22 (QR-5) is an apoptosis inducer with IC50 values of 63.1 and 46.5 μM for colon cancer cell lines SW480 and HT29, respectively. Apoptosis inducer 22 induces apoptosis by inhibiting the Wnt/β-catenin axis in colon cancer cells. Apoptosis inducer 22 can be used in anti-colon cancer research.
|
-
- HY-156792
-
|
|
Ser/Thr Kinase
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
|
-
- HY-115950
-
|
|
Drug Derivative
|
Cancer
|
|
Antitumor agent-48 (Compound 4a) is a 2,3-dehydrosilybin derivative with an antitumor activity. Antitumor agent-48 shows cytotoxic activity against MCF-7, NCI-H1299, HepG2 and HT29 cells with IC50 values of 8.06 µM, 13.1 µM, 16.51 µM and 12.44 µM, respectively .
|
-
- HY-149302
-
|
|
Apoptosis
Autophagy
Histone Acetyltransferase
|
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 .
|
-
- HY-170966
-
|
|
HDAC
|
Cancer
|
|
HDAC1-IN-9 (13c) is a HDAC1 inhibitor. HDAC1-IN-9 inhibits HDAC1 enzyme with an IC50 of 1.07 µM. HDAC1-IN-9 exhibits the highest anti-proliferative effect against HT-29 (human colon adenocarcinoma), with anIC50 of 1.78 μM. HDAC1-IN-9 induces substantial Apoptosis in HCT-116 (human colon cancer) cells. HDAC1-IN-9 possesses antiangiogenic property. HDAC1-IN-9 reduces the expression levels of VEGFR-2 and phosphorylated VEGFR-2 (pVEGFR-2) by approximately 80 % .
|
-
- HY-147825
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF V600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively .
|
-
- HY-103387
-
|
|
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC50 of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC50 of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects .
|
-
- HY-124007
-
|
ISAHA
|
HDAC
|
Cancer
|
|
4-Iodo-SAHA (1k) is an orally active class I and class II histone deacetylase (HDAC) inhibitor with EC50s of 1.1, 0.95, 0.12, 0.24, 0.85 and 1.3 μM for Skbr3, HT29, U937, JA16 and HL60 cell lines, respectively. 4-Iodo-SAHA (1k) can be used for the research of cancer .
|
-
- HY-162721
-
|
|
Others
|
Cancer
|
|
Anticancer agent 242 (7) possesses anticancer activity in A2780 (IC50 = 0.24 μM, ovarian adenocarcinoma), A2780cis (IC50 = 0.45 μM, resistant derivative of A2780), CCD18Co (IC50 = 0.59 μM, non-malignant human fibroblasts), A549 (IC50 = 0.32 μM, lung carcinoma), HT29 (IC50 = 0.26 μM, colorectal adenocarcinoma), and MCF7 (IC50 = 0.55 μM, breast adenocarcinoma) .
|
-
- HY-155203
-
|
|
Apoptosis
Reactive Oxygen Species
Ferroptosis
|
Cancer
|
|
Anticancer agent 154 (Compound 8h) increases the levels of reactive oxygen species and leads to mitochondrial damage. Anticancer agent 154 induces cell apoptosis and DNA damage. Anticancer agent 154 also induces ferroptosis by reducing the GSH level and GPX4 expression and increasing the lipid peroxidation level. Anticancer agent 154 inhibits cancer cell (HT29, H1975, A549, and MCF-7) proliferation with IC50s of 1.0-1.9 μM .
|
-
- HY-155780
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 52 (compound 7j) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-N7175
-
|
9,11-Dehydroergosterol peroxide; 9(11)-DHEP
|
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
|
-
- HY-146366
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
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 .
|
-
- HY-155781
-
|
|
COX
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 53 (compound 7c) is an orally active selective COX-2 inhibitor. Anti-inflammatory agent 52 has anti-HT29 transfer activity, which leads to periodic arrest in S phase and G2/M phase. Anti-inflammatory agent 52 has safety, moderate ability to suppress inflammation. Anti-inflammatory agent 52 has a rare property of suppressing the development of tumor in mouse model, showing anti-cancer activity .
|
-
- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
|
-
- HY-149523
-
|
|
Apoptosis
NO Synthase
Caspase
|
Inflammation/Immunology
Cancer
|
|
Anticancer agent 157 (compound 15) is a NO inhibitor (IC50=0.62 μg/mL) with anti-inflammatory and anticancer activities. Anticancer agent 157 can bind to iNOS (inducible NO synthase) and caspase 8, causing nuclear fragmentation and chromatin condensation, inducing apoptosis. Anticancer agent 157 inhibits HT29 colon cancer cells (IC50=2.45 μg/mL), Hep-G2 liver cancer cells (IC50=3.25 μg/mL), and B16-F10 murine melanoma cells (IC50=3.84 μg/mL) .
|
-
- HY-125387
-
|
|
Src
|
Inflammation/Immunology
|
|
TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
|
-
- HY-170932
-
|
|
EGFR
COX
Apoptosis
|
Cancer
|
|
EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor. EGFR/COX-2-IN-1 inhibits EGFR WT, EGFR T790M, COX-1 and COX-2 with IC50s of 0.12, 0.076, 20.1 and 1.52 μM respectively. EGFR/COX-2-IN-1 inhibits and with IC50s of , respectively. EGFR/COX-2-IN-1 inhibits MCF-7, HT-29 and A-549 with IC50s of 1.20, 5.14 and 14.81 μM, respectively. EGFR/COX-2-IN-1 displays Apoptosis induction by up-regulating Bax and down-regulating Bcl-2 protein levels. EGFR/COX-2-IN-1 results in a significant increase in the percentage of cells at the G2/M in MFC-7 cells. EGFR/COX-2-IN-1 exhibits broad-spectrum antitumor effects .
|
-
- HY-161863
-
|
|
Microtubule/Tubulin
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-67 (Compound 5h) is an inhibitor for tubulin polymerization on colchicine binding site with an IC50 of 2.92 μM. Tubulin polymerization-IN-67 inhibits the proliferation of cancer cells HT29, A549, U2OS, MG-63 and HeLa with IC50s of 0.12-4.13 μM. Tubulin polymerization-IN-67 arrests the cell cycle at G2/M phase, induces apoptosis in cell U2OS, inhibits the cell migration of A549. Tubulin polymerization-IN-67 reduces the mitochondrial membrane potential (MMP) and increase intracellular ROS, inhibits the angiogenesis in HUVECs. Tubulin polymerization-IN-67 exhibits antitumor efficacy in mice
|
-
- HY-162927
-
|
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
p53-MDM2-IN-6 (Compound 10a), a LSM-83177 hydrazone analog, is a potent p53-MDM2 inhibitor with an IC50 value of 11.08 µg/mL. p53-MDM2-IN-6 arrests the cell cycle in the S phase and induces early and late Apoptosis with antiproliferative activity against HT29 cell lines with an IC50 value of 10.44 µg/mL. p53-MDM2-IN-6 inhibits p53-MDM2 interaction with increment in p-53 level and decrease the expression of GST enzymes. p53-MDM2-IN-6 is promising for research of colorectal cancer .
|
-
- HY-147655
-
|
|
Ser/Thr Kinase
|
Cancer
|
|
CQ211 is a potent and selective RIOK2 inhibitor with a Kd of 6.1 nM. CQ211 exhibits potent proliferation inhibition activity against multiple cancer cell lines .
|
-
- HY-147799
-
|
|
Carbonic Anhydrase
|
Cancer
|
|
hCA XII/II/IX-IN-1 (Compound 3) is a potent human carbonic anhydrase (hCA) inhibitor with IC50 values of 2.6, 0.004, 0.005 and 0.001 μM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA XII/II/IX-IN-1 shows anticancer activity .
|
-
- HY-N9650
-
|
Mammea A/AD cyclo D
|
Drug Derivative
|
Cancer
|
|
Mesuagin (Mammea A/AD cyclo D) shows anticancer activity and can be isolated from the Mammea americana L. seeds .
|
-
- HY-148052
-
|
|
RIP kinase
|
Cancer
|
|
RIPK3-IN-2 is a RIP3 inhibitor. RIPK3-IN-2 can be used in diseases caused by or associate with activated necrotic pathways research .
|
-
- HY-N15227
-
|
|
Others
|
Cancer
|
|
(+)-N-Methylhernovine is an aporphine alkaloid that can be isolated from Hernandia nymphaeifolia. (+)-N-Methylhernovine exhibits slight cytotoxicity in cancer cells .
|
-
- HY-146014
-
-
- HY-125097
-
|
|
Bacterial
|
Cancer
|
|
5'-Hydroxy-staurosporine is an indolocarbazole alkaloid that can be isolated from marine Micromonospora sp. (strain L-31-CLCO-002). 5'-Hydroxy-staurosporine can be used in tumor related research .
|
-
- HY-125850
-
-
- HY-131446
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
|
-
- HY-N0278
-
|
Pulsatilla camphor; Anemonine; trans-Anemonin
|
PKC
NO Synthase
|
Inflammation/Immunology
|
|
Anemonin (Pulsatilla camphor), a selective iNOS inhibitor, is also a PKC-θ inhibitor. Anemonin can significantly inhibit the translation or protein stability of PKC-θ protein. Anemonin also ameliorates dextran sodium sulfate-induced acute ulcerative colitis (UC) in mice. Anemonin can be used in the research of inflammation-related diseases .
|
-
- HY-N15413
-
|
|
Parasite
|
|
|
Thalidasine (compound 3) is a bisbenzyltetrahydroisoquinoline alkaloid. Thalidasine is a anticancer agent against human colon adenocarcinoma cells. Thalidasine exhibits antileishmanial activity and can be used for Leishmania infection research research .
|
-
- HY-144277
-
-
- HY-D2363
-
|
|
FAP
Radionuclide-Drug Conjugates (RDCs)
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
DOTA.SA.FAPi TFA inhibits fibroblast activation protein (FAP) with an IC50 of 0.9 nM. DOTA.SA.FAPi TFA targets protease PREP with an IC50 of 5.4 μM. DOTA.SA.FAPi TFA can be used a PET tracer, when labeled with 68Ga, and used for research about cancer . DOTA.SA.FAPi (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-100429
-
CAN508
1 Publications Verification
|
CDK
|
Cancer
|
|
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity .
|
-
- HY-153400
-
|
|
ATM/ATR
|
Cancer
|
|
ATR-IN-22 (Compound 34) is an orally active ATR inhibitor. ATR-IN-22 inhibits MIAPaCa-2 proliferation (IC50 <1 μM). ATR-IN-22 shows anti-tumor activity in colon cancer .
|
-
- HY-N0777
-
|
|
Others
PERK
ERK
Akt
PI3K
Lipase
|
Metabolic Disease
|
|
Isorhamnetin-3-O-glucoside is an orally active natural compound. Isorhamnetin 3-O-glucoside increases P-ERK, ERK, P-Akt (Ser473), P-PI3K, and PDX-1. Isorhamnetin 3-O-glucoside downregulates C/EBPα and inhibits lipase. Isorhamnetin 3-O-glucoside reduces lipids and inhibits obesity .
|
-
- HY-161383
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-9 (compound 11) is an orally active CHK1 inhibitor with an IC50 value of 0.55 nM. CHK1-IN-9 can enhance the effect of DNA-damaging drugs on tumor cells. CHK1-IN-9 has synergistic anticancer effects with Gemcitabine (HY-17026) .
|
-
- HY-136464
-
|
|
β-catenin
|
Cancer
|
|
β-catenin-IN-2 is a potent β-catenin inhibitor, compound H1B1, extracted from patent US20150374662A1. β-catenin-IN-2 can be used for the study of colorectal cancer .
|
-
- HY-146367
-
|
|
VEGFR
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent .
|
-
- HY-152238
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-12 is a potent, orally active and selective PI3K/mTOR inhibitor with IC50 values of 0.06 nM and 3.12 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-12 has antitumor activity. PI3K/mTOR Inhibitor-12 has lower liver toxicity .
|
-
- HY-130978
-
|
|
DNA Alkylator/Crosslinker
ADC Cytotoxin
|
Cancer
|
|
Duocarmycin DM, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity .
|
-
- HY-128915
-
|
|
DNA Alkylator/Crosslinker
ADC Cytotoxin
|
Cancer
|
|
Duocarmycin DM free base, a DNA minor-groove alkylator, is an antibody agent conjugates (ADCs) toxin. Duocarmycin DM free base is based on its characteristic curved indole structure and a spirocyclopropylcyclohexadienone electrophile to act anticancer activity .
|
-
- HY-117295A
-
|
|
Arrestin
|
Inflammation/Immunology
Cancer
|
|
7-Fluorotryptamine hydrochloride is a potent agonist of GPRC5A. 7-Fluorotryptamine hydrochloride induces GPRC5A-mediated β-arrestin recruitment. 7-Fluorotryptamine hydrochloride can be used for research of immune and cancer signaling .
|
-
- HY-137487
-
|
|
PROTACs
Raf
|
Cancer
|
|
PROTAC BRAF-V600E degrader-1 is a potent PROTAC BRAF-V600E degrader with Kd value of 2.4 nM and 2 nM for BRAF and BRAF-V600E, respectively. PROTAC BRAF-V600E degrader-1 degrades BRAF-V600E via the ubiquitin-proteasome system (UPS). PROTAC BRAF-V600E degrader-1 can inhibit melanoma cell growth .
|
-
- HY-161459
-
|
|
Apoptosis
Hedgehog
Gli
|
Cancer
|
|
GLI1-IN-1 (CBC-1) is a GLI-1 inhibitor with excellent water solubility and anticancer activity. GLI1-IN-1 can induce apoptosis and suppress the growth of colorectal cancer by inhibiting the Hedgehog(HH) (IC50=1.3 μM) pathway .
|
-
- HY-147812
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
POLA1 inhibitor 1 (Compound 12) is an orally active POLA1 inhibitor. POLA1 inhibitor 1 shows antitumor activity against several tumor histotypes and Adarotene-resistant cell line .
|
-
- HY-163797
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
|
-
- HY-146743
-
|
|
Apoptosis
|
Cancer
|
|
Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors .
|
-
- HY-138962
-
|
K-Carrageenan Karra Type
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
κ-Carrageenan is a natural polymer which predominantly available in red seaweeds. κ-Carrageenan is an effective agent carrier to deliver curcumin in cancer cells and to induce apoptosis. κ-carrageenan serves as a potential inflammatory agent that magnifies existing intestinal inflammation .
|
-
- HY-170366
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
VEGFR-2-IN-58 (Compound 7b) inhibits VEGFR-2 with an IC50 of 42.5 nM. VEGFR-2-IN-58 displays selective cytotoxicity against cancer cells. VEGFR-2-IN-58 shows cellular growth arrest at the G2/M phase in cancer cells. VEGFR-2-IN-58 induces cancer cells Apoptosis, increasing BAX expression and reducing Bcl2 expression. VEGFR-2-IN-58 inhibits wound closure in cancer cells .
|
-
- HY-N6621
-
|
|
Topoisomerase
|
Cancer
|
|
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities .
|
-
- HY-113099R
-
-
- HY-113099
-
|
Indole-3-lactic acid
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Indolelactic acid (Indole-3-lactic acid) is a tryptophan (Trp) catabolite in Azotobacter vinelandii cultures. Indolelactic acid has anti-inflammation and potential anti-viral activity .
|
-
- HY-146210
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-50 (Compound 9h) is a potent EGFR inhibitor against L858R resistance mutation (TEL-EGFR-L858R-BaF3: GI50=8 nM, TEL-EGFR-T790M-L858R-BaF3: GI50=6.03 μM). EGFR-IN-50 shows anti-proliferative activity to cancer cells .
|
-
- HY-170958
-
|
|
Src
Apoptosis
|
Cancer
|
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 .
|
-
- HY-B1787
-
|
|
mTOR
Drug Metabolite
|
Cancer
|
|
Sulindac sulfone is an mTORC1 pathway inhibitor and a metabolite of Sulindac. Sulindac sulfone inhibits colon cancer cell growth and induces cell cycle arrest. Sulindac sulfone is used in cancer research .
|
-
- HY-108352
-
|
VCE 004
|
Topoisomerase
|
Cancer
|
|
HU 331 (HU 331) is a highly specific Topoisomerase II inhibitor with anticancer activity. HU 331 has shown promising inhibitory effects on human cancer cell lines in vitro and human tumor xenografts in nude mice in vivo .
|
-
- HY-159483
-
|
|
Topoisomerase
Autophagy
Glutathione Peroxidase
|
Cancer
|
|
SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH .
|
-
- HY-157387
-
|
|
c-Met/HGFR
Apoptosis
|
Cancer
|
|
c-Met-IN-22 (compound 51am) is an orally active inhibitor against c-Met with an IC50 value of 2.54 nM. c-Met-IN-22 has antiproliferative and antitumor activities. c-Met-IN-22 induces cell apoptosis .
|
-
- HY-N2518R
-
-
- HY-N2518
-
-
- HY-131421
-
|
8-Piperidino-cyclic AMP
|
PKA
|
Cancer
|
|
8-PIP-cAMP is a selective cAMP-dependent protein kinase activator and can be used for study of cancer .
|
-
- HY-N3376
-
|
Spermatheridine; VLT045
|
Apoptosis
|
Cancer
|
|
Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant?Mitrephora sirikitiae?and has anti-cancer activities . Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9 .
|
-
- HY-151613A
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS15 TFA is a potent and selective AKT PROTAC degrader. MS15 TFA inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively .
|
-
- HY-N10558
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
PM050489 is an effective polyketone inhibitor of Microtubule/Tubulin that can be isolated from Madagascan sponge Lithoplocamia lithistoides. PM050489 inhibits mitosis with an IC50 value of 26.4 nM. PM050489 has antitumor activity and can be used in cancer research .
|
-
- HY-143317
-
|
|
Epigenetic Reader Domain
|
Cancer
|
|
XY153 (compound 8l) is a BD2-selective BET inhibitor and selectively binds to BRD4 BD2. XY153 binds to BRD4 BD2, BRD3 BD2 and BRD2 BD2 with IC50s of 0.79, 5.31 and 5.09 nM, respectively. XY153 shows potent antiproliferative activity against multiple tumor cell lines. XY153 can be used for the research of acute myeloid leukemia (AML) and cancer .
|
-
- HY-N9481
-
-
- HY-P1791
-
|
Lactoferricin B; Lfcin B
|
Bacterial
Fungal
Apoptosis
|
Infection
Cancer
|
|
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities .
|
-
- HY-151613
-
|
|
PROTACs
Akt
|
Cancer
|
|
MS15 is a potent and selective AKT PROTAC degrader. MS15 inhibits the AKT1, -2, and -3 activities, with IC50 values of 798 nM, 90 nM, and 544 nM, respectively .
|
-
- HY-173164
-
|
|
EGFR
Raf
Apoptosis
|
Cancer
|
|
EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAF V600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity .
|
-
- HY-P1791B
-
|
Lactoferricin B acetate; Lfcin B acetate
|
Bacterial
Fungal
Apoptosis
|
Infection
Cancer
|
|
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities .
|
-
- HY-149393
-
|
|
Mixed Lineage Kinase
RIP kinase
|
Cancer
|
|
RIPK3-IN-3 (compound 20) is a selective inhibitor of RIP kinase RIPK3 (IC50=10 nM). RIPK3 mediates the phosphorylation of Mixed Lineage Kinase (MLKL) and causes necroptosis, while RIPK3-IN-3 inhibits p-MLKL oligomerization and thereby inhibits necroptosis. RIPK3-IN-3 also downregulates CXCL5 secretion and inhibits AsPC-1 cell migration and invasion .
|
-
- HY-N0596R
-
|
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
|
-
- HY-N0596
-
|
20(R)-Panaxadiol
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
|
-
- HY-120027
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Kribb3 is an inhibitor for microtubule. KRIBB3 inhibits the proliferation of cancer cells with GI50 of 0.2-2.5 μM, arrests cell cycle at G2/M phase, and induces apoptosis in HCT-116. Kribb3 exhibits antitumor activity in mouse models .
|
-
- HY-N0743
-
|
|
α-synuclein
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Senkyunolide A is a phthalide, anti-tumor cell proliferation agent with anticancer activity. Senkyunolide A protects neurons from corticosterone (HY-B1618)-induced apoptosis by decreasing protein phosphatase PP2A and α-synuclein phosphorylation and protein level. Senkyunolide A also inhibits osteoarthritis through the NLRP3 signaling pathway and suppresses the expression of CD137, a diagnostic biomarker for atherosclerosis .
|
-
- HY-150026
-
|
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
|
-
- HY-150027
-
|
|
VEGFR
PDGFR
|
Cancer
|
|
Multi-kinase-IN-3 (compound 2) is a potent angiokinase inhibitor. Multi-kinase-IN-3 shows inhibition activity against VEGFR-2 and PDGFRβ, with IC50 values of 58.3 and 55 nM, respectively .
|
-
- HY-143241
-
|
|
HDAC
MDM-2/p53
Apoptosis
|
Cancer
|
|
HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC50 values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC50 of 1.41 μM .
|
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
-
- HY-172146
-
|
|
CDK
|
Cancer
|
|
CDK4/6-IN-24 (Compound A) is the inhibitor for CDK4/6. CDK4/6-IN-24 exhibits board-spectrum antitumor activity that inhibits multi cancer cells with IC50 of submicromolar levels .
|
-
- HY-15883
-
|
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
GNE-900 is a an ATP-competitive, selective, and orally active ChK1 inhibitor with IC50s of 0.0011, 1.5 µM for ChKl, ChK2, respectively. GNE-900 abrogates the G2-M checkpoint, enhances DNA damage, and induces Apoptosis. gemcitabine (HY-17026) and GNE-900 administration shows anti-tumor activity .
|
-
- HY-163402
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
EGFR-IN-108 chloride (Compound Ru3S) is an EGFR inhibitor with an IC50 value of 5.8 nM for hEGFR. EGFR-IN-108 chloride induces apoptosis and has anti-proliferative activity against cancer cells. EGFR-IN-108 chloride also has anti-angiogenic effects .
|
-
- HY-16594
-
|
|
Proteasome
Apoptosis
ROS Kinase
|
Infection
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
- HY-146209
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity .
|
-
- HY-N2071
-
-
- HY-146884
-
|
|
c-Met/HGFR
VEGFR
|
Cancer
|
|
MET kinase-IN-3 (compound 8) is an orally active and potent MET inhibitor, with an IC50 of 9.8 nM. MET kinase-IN-3 shows good and broad-spectrum antiproliferative activity against cancer cell lines .
|
-
- HY-B0714
-
|
Dexketoprofen tromethamine salt
|
COX
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Dexketoprofen trometamol (Dexketoprofen tromethamine salt) is an orally active non-selective COX inhibitor. Dexketoprofen trometamol has a pain-relieving effect, anti-inflammatory effect and anti-cancer effect .
|
-
- HY-134050
-
|
Apt-1
|
RIP kinase
Autophagy
Apoptosis
Beclin1
Necroptosis
|
Inflammation/Immunology
|
|
Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin .
|
-
- HY-122650
-
|
|
Autophagy
|
Cancer
|
|
PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer .
|
-
- HY-W505771
-
-
- HY-168565
-
|
|
Apoptosis
Microtubule/Tubulin
Reactive Oxygen Species
|
Cancer
|
|
Tubulin polymerization-IN-70 (compound Q19) is a potent tubulin polymerization inhibitor. Tubulin polymerization-IN-70 shows antiproliferative activity. Tubulin polymerization-IN-70 target the colchicine binding site of tubulin and inhibited tubulin polymerization. Tubulin polymerization-IN-70 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin polymerization-IN-70 induces mitochondrial membrane potential decrease and increases the levels of reactive oxygen species (ROS). Tubulin polymerization-IN-70 shows antiangiogenic and anticancer activity .
|
-
- HY-159480
-
|
|
Src
ATM/ATR
Apoptosis
mTOR
AMPK
|
Cancer
|
|
AD1058 is an orally active, selective, and blood-brain barrier permeable inhibitor of ATR. AD1058 exhibits in vivo anticancer activity, inhibiting cell proliferation, disrupting the cell cycle, and inducing Apoptosis. AD1058 can be utilized in research on brain and central nervous system metastases stemming from advanced solid tumors .
|
-
- HY-18174A
-
|
LY2606368 dihydrochloride
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dihydrochloride inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity .
|
-
- HY-132302A
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-132302
-
|
|
Akt
PKA
PKC
ROCK
Ribosomal S6 Kinase (RSK)
SGK
|
Cancer
|
|
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice .
|
-
- HY-18174H
-
|
LY2606368 lactate
|
Checkpoint Kinase (Chk)
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
|
Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib (HY-18174). Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib lactate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity .
|
-
- HY-18174B
-
|
LY2606368 Mesylate Hydrate; LY2940930
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib Mesylate Hydrate (LY2606368 Mesylate Hydrate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib Mesylate Hydrate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib Mesylate Hydrate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib Mesylate Hydrate shows potent anti-tumor activity .
|
-
- HY-18174E
-
|
LY2606368 dimesylate
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib dimesylate (LY2606368 dimesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib dimesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib dimesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dimesylate shows potent anti-tumor activity .
|
-
- HY-18174
-
Prexasertib
Maximum Cited Publications
22 Publications Verification
LY2606368
|
Checkpoint Kinase (Chk)
Apoptosis
|
Cancer
|
|
Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity .
|
-
- HY-18174C
-
|
LY2606368 mesylate
|
Checkpoint Kinase (Chk)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Prexasertib mesylate (LY2606368 mesylate) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity .
|
-
- HY-A0012
-
|
UK-88525 hydrobromide
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-149052
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Inflammation/Immunology
|
|
SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a Kd of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC50=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects .
|
-
- HY-A0033
-
|
UK-88525
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (UK-88525) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-A0012R
-
|
UK-88525 (hydrobromide) (Standard)
|
mAChR
p38 MAPK
Akt
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Darifenacin (hydrobromide) (Standard) is the analytical standard of Darifenacin (hydrobromide). This product is intended for research and analytical applications. Darifenacin (hydrobromide) is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin (hydrobromide) binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin (hydrobromide) can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin (hydrobromide) inhibits tumor growth in colorectal cancer cells and has anti-tumor effects .
|
-
- HY-153863
-
|
|
PROTACs
MEK
Raf
|
Cancer
|
|
MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader. MS934 also degrades CRAF. MS934 can be used for the research of variety of human cancers, such as melanoma, nonsmall cell lung cancer (NSCLC), colorectal cancer, primary brain tumors, and hepatocellular carcinoma (Pink: Target protein ligand (HY-168288); Black: linker (HY-168289); Blue: E3 ligase ligand (HY-112078)) .
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-
- HY-14909
-
|
CDDO; RTA 401
|
Keap1-Nrf2
Necroptosis
|
Metabolic Disease
Cancer
|
|
Bardoxolone (RTA 401; CDDO) is a novel nuclear regulatory factor (NRf-2) activator. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis. Bardoxolone methyl enhances the antioxidant system, modulates inflammatory cytokines and inhibits apoptosis in rat kidney, demonstrating inhibition on APAP-induced acute kidney injury (AKI) and analgesic effect. Additionally, Bardoxolone methyl decreases Paclitaxel (PAC) (HY-B0015)-induced mitochondrial damage in neuronal cells. Bardoxolone methyl is promising for the research of chemotherapy-induced neuropathic pain and chronic kidney disease .
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-
- HY-17598
-
|
|
Oxidative Phosphorylation
Parasite
p38 MAPK
Raf
Apoptosis
|
Infection
Cancer
|
|
Rafoxanide is a poent, orally active halogenated salicylaniline agent with antiparasitic activity. Rafoxanide interferes with energy metabolism in trematodes by uncoupling oxidative phosphorylation. Rafoxanide is also found to be a potent inhibitor of the BRAF V600E mutant protein, which is important in colorectal cancer. Rafoxanide can be used for the control of infestation with Hemonchus species or Fasciola species in sheep and cattle as well as Oestrus ovis in sheep. Rafoxanide can also be used for cancer research .
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- HY-Y0966R
-
|
|
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine (Standard) is the analytical standard of Glycine. This product is intended for research and analytical applications. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
-
- HY-Y0966
-
|
|
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
-
- HY-13594
-
|
Ce6
|
Bcl-2 Family
Caspase
PARP
Apoptosis
Fluorescent Dye
|
Infection
Cancer
|
|
Chlorin e6 is a photosensitizer and has strong absorption peaks at wavelength of 402 and 662 nm, as well as exhibiting intense fluorescence at 668 nm. Chlorin e6 has antimicrobial efficacy and anticancer activity. Chlorin e6 induces cell apoptosis via caspase-3 activation and can be used for the research of cancer .
|
-
- HY-14543
-
-
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1435
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-D2363
-
|
|
FAP
Radionuclide-Drug Conjugates (RDCs)
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
DOTA.SA.FAPi TFA inhibits fibroblast activation protein (FAP) with an IC50 of 0.9 nM. DOTA.SA.FAPi TFA targets protease PREP with an IC50 of 5.4 μM. DOTA.SA.FAPi TFA can be used a PET tracer, when labeled with 68Ga, and used for research about cancer . DOTA.SA.FAPi (TFA) can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P1791B
-
|
Lactoferricin B acetate; Lfcin B acetate
|
Bacterial
Fungal
Apoptosis
|
Infection
Cancer
|
|
Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 acetate has antitumor activities .
|
-
- HY-P3116
-
|
|
Bacterial
|
Cancer
|
|
Thiocoraline is a depsipeptide that can be isolated by marine Micromonospora. Thiocoraline has antitumor activity with IC50s of 0.002, 0.002, 0.01 and 0.002 μg/mL in P388, A549, HT-29 and MEL-28 cells, respectively. Thiocoraline also a strong antimicrobial activity against Gram-positive microorganisms .
|
-
- HY-P10761
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Carbonic Anhydrase
|
Cancer
|
|
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130?nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
|
-
- HY-P1435A
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds TFA is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds TFA can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-144277
-
-
- HY-P1791
-
|
Lactoferricin B; Lfcin B
|
Bacterial
Fungal
Apoptosis
|
Infection
Cancer
|
|
Lactoferrin 17-41 (Lactoferricin B), a peptide corresponding to residues 17-41 of bovine lactoferrin, has antimicrobial activity against a wide range of microorganisms, including Gram-positive and Gramnegative bacteria, viruses, protozoa, and fungi. Lactoferrin 17-41 has antitumor activities .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99492
-
|
SB-408075; huC242-DM1
|
Antibody-Drug Conjugates (ADCs)
Microtubule/Tubulin
|
Cancer
|
|
Cantuzumab mertansine (SB-408075; huC242-DM1), an ADC, is an immunoconjugate of the potent maytansine derivative (DM1; HY-19792) and the humanized monoclonal antibody (huC242) directed to CanAg. Cantuzumab mertansine has cytotoxic toward colon cancer cells and has broad antitumor efficacy against a range of CanAg-positive human tumor xenografts .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-121458
-
-
-
- HY-126779
-
-
-
- HY-N8225
-
-
-
- HY-N3057
-
-
-
- HY-N8025
-
-
-
- HY-W727999
-
-
-
- HY-N3123
-
-
-
- HY-N10132
-
-
-
- HY-N1655
-
-
-
- HY-N12430
-
-
-
- HY-N12437
-
-
-
- HY-N12820
-
-
-
- HY-N8934
-
-
-
- HY-N6002
-
-
-
- HY-N3057R
-
-
-
- HY-121199
-
-
-
- HY-75564
-
-
-
- HY-N1261
-
-
-
- HY-N8387
-
-
-
- HY-N8462
-
-
-
- HY-N7175
-
|
9,11-Dehydroergosterol peroxide; 9(11)-DHEP
|
Structural Classification
Classification of Application Fields
Source classification
Solanum lyratum Thunberg
Solanaceae
Plants
Disease Research Fields
Steroids
Cancer
|
Apoptosis
Endogenous Metabolite
|
|
5,8-Epidioxyergosta-6,9(11),22-trien-3-ol (9,11-Dehydroergosterol peroxide), an important steroid from medicinal mushroom, exerts antitumor activity in several tumor types. 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol inhibits HT29 cell growth by inducing CDKN1A expression, thus causing cell cycle arrest and apoptosis .
|
-
-
- HY-N9650
-
-
-
- HY-N15227
-
-
-
- HY-125850
-
-
-
- HY-N0278
-
-
-
- HY-N15413
-
-
-
- HY-N0777
-
-
-
- HY-138962
-
-
-
- HY-N6621
-
-
-
- HY-113099R
-
-
-
- HY-113099
-
-
-
- HY-N2518R
-
-
-
- HY-N2518
-
-
-
- HY-N3376
-
-
-
- HY-N10558
-
-
-
- HY-N9481
-
-
-
- HY-N0596R
-
-
-
- HY-N0596
-
-
-
- HY-N0743
-
-
-
- HY-16594
-
|
|
Structural Classification
Microorganisms
Antibiotics
Source classification
Other Antibiotics
|
Proteasome
Apoptosis
ROS Kinase
|
|
Lactacystin is a potent, orally active, irreversible, cell-permeable, selective 20S proteasome inhibitor (IC50 = 4.8 μM). Lactacystin also inhibits the lysosomal enzyme cathepsin A. Lactacystin inhibits cell growth and induces apoptosisand cell cycle arrest, and has antiviral and antioxidative activity. Lactacystin induces neurite outgrowth and hypertension. Lactacystin has the potential for the research of cancer, Neurological Disease, hypertension and Malaria, and so on [1] [2] [3] [4] [5] [6] [7] [8] [9] [10] .
|
-
-
- HY-N2071
-
-
-
- HY-W505771
-
-
-
- HY-Y0966R
-
-
-
- HY-Y0966
-
-
| Cat. No. |
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Source |
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* This product has been "discontinued".
Optimized version of product available:
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| Cat. No. |
Product Name |
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Classification |
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- HY-125387
-
|
|
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Alkynes
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TOP1210 is a narrow-spectrum tyrosine kinase inhibitor with potent inhibitory activity against P38α, Src, and Syk kinases. TOP1210 effectively reduced proinflammatory cytokines released by peripheral blood monocytes, primary macrophages, HT29 cells, inflammatory cells in ulcerative colitis (UC) biopsies, and myofibroblasts isolated from inflamed colonic UC mucosa. TOP1210 showed significant anti-inflammatory effects in cell experiments and UC biopsies, superior to some selective kinase inhibitors. The multi-kinase inhibition of TOP1210 provides the possibility of obtaining a wider range of therapeutic effects, especially in the regulation of autoimmune responses .
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| Cat. No. |
Product Name |
|
Classification |
-
- HY-Y0966
-
|
|
|
Fillers
|
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Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
|
-
- HY-160066
-
|
|
|
Aptamers
|
|
SYL3C aptamer sodium is a DNA aptamer that targets the epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets multiple human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III is 38 nM and 67 nM, respectively. SYL3C aptamer sodium provides stability, high binding affinity, and selectivity for targeted cancer therapy, cancer cell imaging, and circulating tumor cell detection .
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