|
T5465 |
PF-5274857
|
PF-5274857 freebase |
Smo
|
|
PF-5274857 (PF-5274857 free base) is an effective and selective hedgehog signaling pathway inhibitor (IC50: 5.8 nM and a Ki: 4.6 nM). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor t... |
|
T12134 |
MYCMI-6
|
NSC354961 |
Apoptosis
,
c-Myc
|
|
MYCMI-6 (NSC-354961) is a potent and selective inhibitor of endogenous MYC:MAX protein interactions，reduces proliferation and induces massive apoptosis in tumor tissue from a MYC-driven xenograft tumor model without seve... |
|
T2100 |
CX-5461
|
|
DNA/RNA Synthesis
|
|
CX-5461, a selective inhibitor of rRNA synthesis, suppresses Pol I-driven transcription of rRNA. |
|
T12753 |
RORγt Inverse agonist 6
|
|
ROR
|
|
|
|
T7738 |
H3B-6527
|
|
FGFR
|
|
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma, with antineoplastic activity. |
|
T69980 |
XMU-MP-2
|
|
BTK
,
Protease
|
|
XMU-MP-2 is a potent and selective protease inhibitor with anticancer activity that inhibits the growth of oncogenic BRK-driven tumors in a mouse xenograft model. |
|
T22062 |
CCG-100602
|
|
Rho
,
Ras
|
|
CCG-100602 inhibits RhoA/C-mediated, SRF-driven luciferase expression in PC-3 prostate cancer cells (IC50 :9.8 μM). |
|
T9240 |
Sulfopin
|
Acetamide, 2-chloro-N-(2,2-dimethylpropyl)-N-(tetrahydro-1,1-dioxido-3-thienyl)- |
Others
|
|
Sulfopin is a highly selective covalent inhibitor of Pin1 with an apparent Ki of 17nM. Sulfopin blocks Myc-driven tumors in vivo. |
|
T4980 |
Betrixaban maleate
|
|
Factor Xa
|
|
Betrixaban maleate is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa. |
|
T9141 |
ERK-IN-3
|
ASN007 free base |
ERK
|
|
ERK-IN-3 (ASN007 free base) is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations. |
|
T12777 |
RTC-5
|
TRC-382 |
EGFR
|
|
RTC-5 (TRC-382) is a phenothiazine compound that has been specifically enhanced for its potent anti-cancer properties. It exhibits considerable effectiveness against an EGFR-driven cancer xenograft model. The mechanism ... |
|
T34656 |
SKLB 1028
|
Ruserontinib |
EGFR
,
FLT
,
Bcr-Abl
|
|
SKLB 1028 (Ruserontinib) is a new type of oral multikinase inhibitor of EGFR, FLT3, and Abl. SKLB 1028 shows excellent activity in FLT3-driven AML models and considerable potency in CML models containing Abl mutants. |
|
T72984 |
(Rac)-SHIN2
|
|
Others
|
|
(Rac)-SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor that enhances NOTCH1-driven in vivo survival of primary T-ALL in mice and can be used to study T-cell acute lymphoblastic leukemia (T-ALL). |
|
T76758 |
Rilotumumab
|
AMG 102 |
c-Met/HGFR
|
|
Rilotumumab (AMG 102) is a monoclonal antibody targeting hepatocyte growth factor that inhibits HGF/ MET-driven signaling. Rilotumumab has antitumor effects and can be used to study castration-resistant prostate cancer (... |
|
T27499 |
GSK-A1
|
|
HCV Protease
,
PI4K
|
|
GSK-A1 is a specific inhibitor of PI4KA, also inhibited calcium-driven PRL secretion without affecting calcium signaling and Prl expression. GSK-A1 has anti-hepatitis C virus (HCV) potential. |
|
T13058 |
T025
|
|
CDK
|
|
T025 is a pan CLK inhibitor with Kds of 4.8, 0.096, 6.5, 0.61, and 0.074 nM for CLK1-4, respectively. T025 displays anti-proliferative activities with IC50s of 30-300 nM in hematological and solid cancer cell lines. T025... |
|
T67934 |
MRT-2359
|
|
Others
|
|
MRT-2359 is a potent and orally available GSPT1 reducer with antitumour activity.MRT-2359 inhibits the growth of drug-resistant non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC) cells.MRT-2359 exhibits... |
|
T9656 |
AP-1/NF-κB activation inhibitor 1
|
|
NF-κB
,
DNA/RNA Synthesis
|
|
AP-1/NF-κB activation inhibitor 1 is a potent inhibitor of AP-1 and NF-κB mediated transcriptional activation ( IC 50 =1 μM), does not blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation in... |
|
T15183 |
Dynarrestin
|
|
Hedgehog/Smoothened
|
|
Dynarrestin is an inhibitor of cytoplasmic dyneins 1 and 2. Dynarrestin suppresses hedgehog (Hh)-dependent proliferation of neuronal precursors and tumor cells. It inhibits dynein 1-driven microtubule gliding in vitro pl... |
|
T60077 |
SCP1-IN-1
|
|
Others
|
|
SCP1-IN-1 (compound SH T-62) is a potent and selective covalent inhibitor against SCP1. SCP1-IN-1 promotes REST degradation and reduces transcriptional activity. In some glioblastoma cells, the high level of REST protein... |
|
T77499 |
MSU-42011
|
|
NOS
,
Retinoid Receptor
,
NO Synthase
,
PERK
,
Lipid
|
|
MSU-42011 is an orally active retinoid X receptor-like (RXR) agonist.MSU-42011 potently inhibits the expression of iNOS, low SREBP-induced and activated RXR, and p-ERK at the protein level.MSU-42011 has demonstrated anti... |
|
T4341 |
Betrixaban
|
PRT054021 |
Factor Xa
|
|
Betrixaban (PRT054021) is a non-vitamin K oral anticoagulant whose action is driven by the competitive and reversible inhibition of the factor Xa [1]. It was selected among all lead compounds due to its low hERG channel ... |
|
T62061 |
COX-2-IN-6
|
|
COX
,
Prostaglandin Receptor
|
|
COX-2-IN-6 is a potent, selective, and orally available cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 0.84 μM and a Ki of 69 nM.COX-2-IN-6 inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.COX-2-IN-6 is u... |
|
T64529 |
MDL-800
|
MDL 800,MDL800 |
Sirtuin
|
|
MDL-800 is a SIRT6 modulator with antitumor activity for the study of hepatocellular carcinoma and non-small cell lung cancer. |
|
T3678 |
Entrectinib
|
RXDX-101,NMS-E628 |
Trk receptor
,
ROS
,
ALK
,
Autophagy
,
ROS Kinase
|
|
Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectini... |
|
T13063 |
T6167923
|
|
MyD88
|
|
T6167923 is a potent, selective inhibitor of MyD88-dependent signaling pathways. It achieves this by directly binding to the Toll/IL1 receptor (TIR) domain of MyD88, preventing MyD88 homodimer formation. Subsequently, T6... |
|
T22021 |
ACHP
|
IKK-2 Inhibitor VIII |
IκB/IKK
|
|
ACHP (IKK-2 Inhibitor VIII) is a novel selective and potent IKK inhibitor with inhibitory effects on IKK-α and IKK-β. ACHP has anti-HIV-1 activity and inhibits HIV-1 long terminal repeat (LTR)-driven gene expression thro... |
|
T36816 |
S-trityl-L-Cysteine
|
STLC |
Kinesin
|
|
S-trityl-L-Cysteine is a non-natural amino acid and an inhibitor of Eg5, also known as KSP and Kif11, a mitotic kinesin necessary for mitotic spindle formation. S-trityl-L-Cysteine inhibits the ATPase activity of Eg5 in ... |
|
T39491 |
HS-131
|
|
|
|
HS-131, a near-infrared dye-conjugated Hsp90 inhibitor, effectively identifies oncogene-driven breast cancers across various molecular subtypes. |
|
T26836 |
BLL5 Maleate
|
|
|
|
BLL5 Maleate is a first-in-class selective PRMT5 inhibitor, it blocks EBV-driven B lymphocyte transformation and survival while leaving normal B cells unaffected. |
|
T70130 |
NPA101.3
|
|
|
|
NPA101.3 is a a Second-Generation RET/VEGFR2 Inhibitor. It is a potential clinical candidate for RET-driven cancers. |
|
T10719 |
CCT365623 hydrochloride
|
|
Lipoxygenase
|
|
CCT365623 hydrochloride is an orally active inhibitor of lysyl oxidase (LOX) (IC50: 0.89 μM). It suppresses EGFR (pY1068) and AKT phosphorylation driven by EGF. |
|
T24513 |
MYRA-A
|
NSC-339585,NSC 339585,NSC339585 |
|
|
MYRA-A is an inducer of apoptosis in a Myc-dependent manner that acts by inhibiting Myc-driven transformation and disrupting MYC-Max interaction. |
|
T10060L |
DT-061
|
|
Phosphatase
|
|
DT-061 is an orally bioavailable protein phosphatase 2A (PP2A) activator. It could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis. |
|
T70214 |
BMS-986202
|
|
|
|
BMS-986202 is a novel Tyk2 inhibitor, binding to Tyk2 JH2, showing efficacies for IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus. |
|
T28221 |
NVP-QAV-680
|
NVP-QAV680,QAV690 free acid,NVP,QAV-690 free acid,NVPQAV680,QAV 690 free acid |
|
|
NVP-QAV-680 is a potent and selective antagonist of CRTh2 receptor. NVP-QAV-680 has nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. |
|
T70026 |
DC-034
|
|
|
|
DC-034 is a potent downregulator of MYC transcription in cancer cells by a G4-dependent mechanism, thereby selectively inhibiting MYC significantly greater than other G4-driven genes. |
|
T10407 |
Gartisertib
|
ATR inhibitor 2 |
ATM/ATR
|
|
ATR inhibitor 2 is an orally active, ATP-competitive, and selective ATR inhibitor (Ki <150 pM) with antitumor activity. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylati... |
|
T72430 |
L-Kynurenine sulfate
|
|
|
|
L-Kynurenine sulfate, an aryl hydrocarbon receptor (AHR) agonist, activates AHR-driven polarization of naive T cells towards the anti-inflammatory Treg phenotype. |
|
T39453 |
ERK-IN-3 benzenesulfonate
|
|
|
|
ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK . ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC 50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancer... |
|
T62877 |
RET-IN-7
|
|
|
|
RET-IN-7 exhibits strong inhibitory effects against RET kinase in vitro and shows significant efficacy in treating RET-driven tumor xenografts in mice through multiple-day dosing. |
|
T76215 |
KRpep-2d
|
|
|
|
KRpep-2d, a potent inhibitor of K-Ras, effectively suppresses the proliferation of cancer cells driven by K-Ras. This compound is suitable for use in cancer research [1]. |
|
T36246 |
SJF 8240
|
|
|
|
c-MET degrader. Comprises MET inhibitor foretinib (GSK 1363089; Cat. No. 6056) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Degrades c-MET within 6 hours in vitro. Inhibits agonist-driven AKT phosph... |
|
T80643 |
BEBT-109
|
|
EGFR
|
|
BEBT-109 is a potent selective inhibitor of pan-mutant EGFR with enhanced pharmacokinetic properties, suitable for research on various mutant-EGFR-driven non-small cell lung cancer (NSCLC) [1]. |
|
T79672 |
DUB-IN-7
|
|
|
|
DUB-IN-7 (compound 43), a deubiquitinating enzyme (DUB) inhibitor, has utility in researching diseases driven by aberrant JAK2 activity, including leukemia [1]. |
|
T36245 |
SJF 1528
|
|
|
|
Potent EGFR Degrader (DC50 values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. Comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by ... |
|
T76215L |
KRpep-2d TFA
|
|
|
|
KRpep-2d (TFA) is a potent inhibitor of K-Ras, effectively hindering the proliferation of K-Ras-driven cancer cells, thereby serving as a valuable asset for cancer research [1]. |
|
T10210 |
A-9758
|
|
ROR
|
|
A-9758 is a RORγ ligand and a selective RORγt inverse agonist (IC50: 5 nM) and exhibits robust potency against IL-17A release. It is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 s... |
|
T76078 |
Neurogranin (48-76), mouse
|
|
|
|
Neurogranin (48-76), mouse, is a peptide comprising residues 48-76 of Neurogranin, a post-synaptically exclusive calmodulin-binding protein that mediates NMDAR-driven synaptic plasticity by regulating the calcium-calmodu... |
|
T76913 |
Avdoralimab
|
|
|
|
Avdoralimab (IPH 5401), a fully human IgGκ monoclonal antibody, specifically inhibits the complement C5a receptor 1 (C5aR1) by preventing its interaction with C5a. This compound is utilized in research concerning complem... |
