|
T9810 |
TNIK-IN-5
|
|
Wnt/beta-catenin
|
|
TNIK-IN-5 is an potent TNIK inhibitor (IC50= 0.05 μM). TNIK-IN-5 potently inhibits Wnt signaling in intact cells. TNIK-IN-5 exhibits excellent in vitro anti-colorectal cancer activity. |
|
T6255 |
Bromosporine
|
|
Epigenetic Reader Domain
,
CDK
|
|
Bromosporine is a broad spectrum inhibitor for bromodomains for BRD2/4/9 and CECR2 (IC50: 0.41/0.29/0.122/0.017 μM), respectively. |
|
T36970 |
STD1T
|
|
DUB
|
|
STD1T is a selective and potent inhibitor of the deubiquitinase USP2a with potential anticancer activity that reduces cell cycle protein D1 protein levels in HCT116 colon and MCF-7 breast cancer cells. |
|
T21854 |
Proteasome inhibitor IX
|
PS-IX,AM114 |
Proteasome
|
|
Proteasome inhibitor IX (PS-IX) is an inhibitor of chymotrypsin-like activity of the 20S proteasome (IC50 ~1 μM). Proteasome inhibitor IX shows potent anticancer activity. Proteasome inhibitor IX exhibits HCT116 p53+/+ c... |
|
T24131 |
HDAC3-IN-T247
|
HDAC3 inhibitor T247,HDAC3 inhibitor-T247,HDAC3 IN T247,T247 |
Histone Demethylase
,
Antiviral
|
|
HDAC3-IN-T247 (HDAC3 inhibitor T247) is a selective and potent histone deacetylase 3 (HDAC3) inhibitor with anticancer and antiviral activities.HDAC3-IN-T247 induces NF-κB acetylation in human colon cancer HCT116 cells i... |
|
T78156 |
MC4033
|
|
Apoptosis
|
|
MC4033 exhibits inhibitory concentration 50 (IC50) values of 39.4 µM in HCT116, 52.1 µM in H1299, 41 µM in A549, and 30.1 µM in U937 [1]. Additionally, treatment with MC4033 at concentrations of 25, 50, 100, and 200 µM f... |
|
T13436 |
(E)-[6]-Dehydroparadol
|
(6)-Dehydroparadol |
Nrf2
|
|
(E)-[6]-Dehydroparadol ((6)-Dehydroparadol), an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator. |
|
T5699 |
SSE15206
|
|
Apoptosis
,
Microtubule Associated
|
|
SSE15206 is a microtubule polymerization inhibitor that overcomes multidrug resistance. Causes aberrant mitosis resulting in G2/M arrest due to incomplete spindle formation in cancer cells. |
|
T9575 |
MRTX9768
|
|
Histone Methyltransferase
|
|
MRTX-9768 is a synthetic lethal-based inhibitor designed to bind the PRMT5-MTA complex and selectively target MTAP/CDKN2A-deleted tumors. |
|
T22632 |
TASIN-1
|
1-[(4-methoxyphenyl)sulfonyl]-4'-methyl-4,1'-bipiperidine |
APC
|
|
TASIN-1 is a small molecule inhibitor of mutant adenomatous polyposis coli (APC). |
|
T9557 |
TNIK-IN-2
|
|
Wnt/beta-catenin
|
|
TNIK-IN-2 is an inhibitor Traf2- and Nck-interacting protein kinase (TNIK, IC50 = 1.33 μM)) which is a downstream signal protein of the Wnt/β-catenin pathway. |
|
T64391 |
Antiproliferative agent-15
|
|
Others
|
|
Antiproliferative agent-15 is a reagent with anticancer activity. Antiproliferative agent-15 showed antiproliferative activity against human colon cancer (HCT116 and HCT15) and brain cancer (LN-229 and GBM-10). |
|
T11421 |
Glutaminase-IN-1
|
CB839 derivative |
transporter
|
|
|
|
T78157 |
PARP-1-IN-3
|
|
Apoptosis
,
PARP
|
|
PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-inflammatory activity, induces apoptosis, and arrests the cell... |
|
T83079 |
Anticancer agent 172
|
|
|
|
Anticancer agent 172 (8d) exhibits potent activity against cancer, achieving an IC50 value of 6.96 μM in HCT116 cells [1]. |
|
T83080 |
Anticancer agent 171
|
|
|
|
Compound 6a (Anticancer Agent 171), an oxime analogue, demonstrates anticancer activity by inhibiting HCT116 cells with an IC50 of 3.43 μM and may be utilized for cancer research [1]. |
|
T72544 |
4-Formylcolchicine
|
|
|
|
4-Formylcolchicine, a potent anticancer agent, demonstrates cytotoxicity with IC 50 values of 1.007 µM for A549 cells, 0.128 µM for HT-29 cells, and 0.054 µM for HCT116 cells. |
|
T83090 |
Anticancer agent 131
|
|
|
|
HCT-116-IN-1, a γ-lactam-fused pyridone derivative, exhibits anticancer properties, demonstrating significant cytotoxicity towards HCT116 cells, with an IC50 value of 5.59 μM [1]. |
|
T71815 |
TX-1918
|
|
|
|
TX-1918 is a cell-permeable tyrphostin derivative that inhibits eukaryotic elongation factor-2 kinase (eEF-2K). TX-1918 disrupts the proliferation of HepG2 and HCT116 tumor cells. |
|
T35607 |
10'-Desmethoxystreptonigrin
|
|
|
|
10'-Desmethoxystreptonigrin is an antibiotic originally isolated from Streptomyces and a derivative of the antibiotic streptonigrin. It is active against a variety of bacteria, including S. aureus, S. faecalis, E. coli, ... |
|
T63509 |
Top/HDAC-IN-1
|
|
|
|
Top/HDAC-IN-1 is a dual topoisomerase (Top)/HDAC inhibitor that acts on HDAC1 (IC50: 18 nM), HDAC2 (IC50: 230 nM), HDAC3 (IC50: 790 nM), HDAC6 (IC50: 87 nM) and HDAC8 (IC50: 5250 nM). Top/HDAC-IN-1 exhibited potent antit... |
|
T38381 |
CAY17c
|
|
|
|
CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and cla... |
|
T13643 |
Demethoxydeacetoxypseudolaric acid B analog
|
|
Others
|
|
Demethoxydeacetoxypseudolaric acid B analog has potent activities against HMEC-1, HL-60, A-549, MB-MDA-468, BEL-7402, HCT116, and Hela cells with IC50s ranging from 0.136 to 1.162 μM. and is semi-synthesized by efficient... |
|
T83011 |
Antitumor agent-105
|
|
|
|
Antitumor Agent-105 (Compound 37) exhibits antitumor activity, demonstrating inhibition of A549, H1299, H460, HCT116, and MDA-MB-231 cells with respective IC50 values of 6.7, 8.3, 4.3, 4.4, and 6.7 μM [1]. |
|
T36627 |
Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)
|
|
|
|
Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used a... |
|
T62943 |
ZLWT-37
|
|
|
|
ZLWT-37 is a potent, orally active inhibitor of CDKs, acting on CDK9 (IC50: 0.002 μM) and CDK2 (IC50: 0.054 μM). ZLWT-37 is capable of blocking the cell cycle of HCT116 cells in G2/M phase and apoptosis. |
|
T37584 |
Tryptoquivaline D
|
|
|
|
Tryptoquivaline D is a fungal metabolite that has been found inNeosartorya siamensisand has anticancer activity.1,2It induces nuclear chromatin condensation, a marker of apoptosis, in HCT116 colon and HepG2 liver cancer ... |
|
T36464 |
Caylin-1
|
|
|
|
Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-1 is a nutlin-3 analog which contains chlorine substituents at the 3 and 4 posit... |
|
T36465 |
Caylin-2
|
|
|
|
Nutlin-3 is an activator of p53 that functions by inhibiting the interaction of p53 with MDM2, a negative regulator of p53 activity. Caylin-2 is a nutlin-3 analog in which trifluoromethyl groups have been substituted for... |
|
T37010 |
D-threo Sphinganine (d18:0)
|
D-threo Sphinganine (d18:0) |
|
|
D-threo Sphinganine (d18:0) is a synthetic bioactive sphingolipid and stereoisomer of sphinganine (d18:0) and L-erythro sphinganine (d18:0) . It induces autophagy in HCT116 cells when used at a concentration of 12 μM. D-... |
|
T39200 |
β-catenin-IN-37
|
|
|
|
β-Catenin-IN-37 is a selective inhibitor of the protein-protein interaction between β-Catenin and T-cell factor (Tcf), known as β-catenin/Tcf PPI. It effectively inhibits canonical Wnt signaling and impedes the growth of... |
|
T61996 |
Antiproliferative agent-6
|
|
|
|
Antiproliferative agent-6 (compound 8a) is a potent antitumor compound. Antiproliferative agent-6 shows antiproliferative activity. Antiproliferative agent-6 inhibits cancer cell lines HCT116, MCF-7, H460 and non-tumor a... |
|
T62934 |
ZLHQ-5f
|
|
|
|
ZLHQ-5f is a dual inhibitor of CDK2 and Topo I, acting on CDK2/CycA2 (IC50: 0.145 μM). ZLHQ-5f has a good safety profile by blocking the cell cycle of HCT116 cells in S phase and inducing apoptosis. |
|
T63383 |
SZ-015268
|
|
|
|
SZ-015268 is a CDK7 inhibitor (IC50: 23.56 nM) and inhibits the proliferation of HCC70 (IC50: 33 nM), OVCAR-3 (IC50: 80.56 nM), HCT116 (IC50: 12.53 nM) and HCC1806 (IC50: 61.55 nM) cells. 015268 exhibited a highly signif... |
|
T81740 |
Multi-kinase-IN-6
|
|
Trk receptor
|
|
Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that effectively impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX ca... |
|
T37644 |
Bengamide B
|
|
|
|
Potent inhibitor of NF-κB activation (IC50 = 85 nM); decreases IκBα phosphorylation. Attenuates LPS-induced nitric oxide production and expression of TNF-α, IL-6 and MCP. Suppresses proliferation of HeLa and HCT116 cell... |
|
T74453 |
JPS014
|
|
|
|
JPS014, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC), exhibiting potency as an HDAC1/2 degrader. This correlation is ... |
|
T74455 |
JPS035
|
|
|
|
JPS035, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC), specifically HDAC1/2. Its potent activity is associated with an... |
|
T77937 |
JPS014 TFA
|
|
HDAC
,
PROTACs
|
|
JPS014 TFA, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC), particularly HDAC1/2. This activity is associated with a hi... |
|
T74456 |
JPS036
|
|
|
|
JPS036, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), efficiently degrades class I histone deacetylase (HDAC), particularly HDAC1/2. Its activity results in a substantial inc... |
|
T74454 |
JPS016
|
|
|
|
JPS016, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC). It serves as a potent HDAC1/2 degrader, resulting in a signific... |
|
T77938 |
JPS016 TFA
|
|
HDAC
,
PROTACs
|
|
JPS016, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC), particularly HDAC1/2. This activity is associated with a substa... |
|
T35668 |
Neoaureothin
|
|
|
|
Neoaureothin is a bacterial metabolite that has been found in Streptomyces. It is an androgen receptor (AR) antagonist that inhibits binding of dihydrotestosterone (DHT) to ARs (IC50 = 13 μM) and inhibits DHT-induced exp... |
|
T62349 |
Tubulin polymerization-IN-8
|
|
|
|
Tubulin polymerization-IN-8 (compound IIc) is a potent inhibitor of tubulin polymerization that has been demonstrated to concentration-dependently induce cell cycle arrest at the G2/M phase in HCT116 tumor cells. It also... |
|
T62331 |
Autophagy-IN-1
|
|
|
|
Autophagy-IN-1 is a potent inhibitor of autophagy/mitophagy, blocking autophagosomal-lysosomal fusion in cancer cells while selectively increasing autophagic flux. Autophagy-IN-1 significantly inhibits tumour growth in t... |
|
T83949 |
DC 432
|
|
|
|
DC 432, a potent peptidomimetic inhibitor of N-terminal methyltransferase 1/2 (NTMT1/2) with an IC50 value of 54 nM, incorporates a BM30 peptide enhanced by five arginine residues. It effectively reduces the N-terminal m... |
|
T79724 |
IGF2BP1-IN-1
|
|
|
|
IGF2BP1-IN-1 (Compound A11), an inhibitor of IGF2BP1, impedes the associated downstream signaling and demonstrates a high affinity for the IGF2BP1 protein with a dissociation constant (K D) of 2.88 nM. The compound effec... |
|
T73515 |
MC2590
|
|
Apoptosis
,
HDAC
|
|
MC2590 is a potent and selective histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis. |
|
T83881 |
4-(3,4-Difluorobenzo)curcumin
|
CDF |
|
|
4-(3,4-Difluorobenzo)curcumin (CDF) is a semisynthetic coumarin noted for its antiparasitic and anticancer properties. It effectively reduces the population of Vero cells infected by T. gondii promastigotes and amastigot... |
|
T83958 |
CELT-327
|
|
|
|
CELT-327 is a potent, selective fluorescent hA2B/A3 adenosine receptor antagonist, exhibiting K_i values of 35.6 nM at A2B and 45.7 nM at A3 receptors. It efficiently labels HCT116 cells expressing A2B adenosine receptor... |
