|
T13176 |
TNO155
|
Batoprotafib |
Phosphatase
|
|
TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity. |
|
T9756 |
AZD-9574
|
|
PARP
|
|
AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies. |
|
T16781 |
Rogaratinib
|
BAY1163877 |
FGFR
|
|
Rogaratinib (BAY1163877) is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity. |
|
T62902 |
NDI-034858
|
TAK-279,NDI-03485 |
IL Receptor
,
Tyrosine Kinases
|
|
NDI-034858 (TAK-279) is a tyrosine kinase 2 (TYK2) inhibitor (Kd<200 pM) that targets the JH2 structural domain of Tyk2 for the treatment of autoimmune diseases caused by aberrant expression of IL12 and IL23. |
|
T79492 |
H-NTPDase8-IN-1
|
|
Phosphatase
|
|
h-NTPDase8-IN-1 is a specific aminosulfonylbenzamide inhibitor of h-NTPDases8 (IC 50 = 0.28 ± 0.07 μM). h-NTPDase8-IN-1 can be used to study diseases brought about by aberrant h -NTPDase expression. |
|
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. |
|
T15576 |
Indibulin
|
ZIO 301,D 24851 |
Apoptosis
,
Microtubule Associated
|
|
Indibulin (D 24851) is a synthetic small molecule with antimitotic and potential antineoplastic activities.Indibulin an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neu... |
|
TQ0236 |
Tirabrutinib
|
ONO-4059,GS-4059,Velexbru |
BTK
|
|
Tirabrutinib (GS-4059) (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (Btk) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to Btk and ... |
|
T71639 |
AUH-6-96
|
|
|
|
AUH-6-96 is an inhibitor of JAK/STAT signaling, inhibiting both constitutive and interleukin-6-induced STAT3 phosphorylation, selectively affecting cell viability only of cancer cells harboring aberrant JAK/STAT signalin... |
|
T24647 |
PKR-IN-C51
|
PKRINC51,PKR IN C51,PKR-inhibitor-C51,PKR inhibitor C51 |
|
|
PKR-IN-C51 is an inhibitor of protein kinase R. It acts by correcting the aberrant splicing of MBNL1-dependent pre-mRNAs in DM1 cells without affecting the splicing pattern in normal non-DM1 cells. |
|
T70318 |
AMG-337 monohydrate
|
|
|
|
AMG-337 monohydrate is a highly selective small molecule MET inhibitor. Aberrant hepatocyte growth factor (HGF)/MET signaling has been implicated in hepatocarcinogenesis, suggesting that MET may serve as an attractive th... |
|
T36718 |
Tie2 Inhibitor 7
|
|
|
|
Tie2 Inhibitor 7 blocks Tie2 kinase activity with a Ki value of 1.3 μM.. It has been shown to inhibit angiopoietin 1-induced Tie2 autophosphorylation and downstream signaling with an IC50 value of 0.3 μM. This compound c... |
|
T61435 |
(S)-Cdc7-IN-18
|
|
|
|
(S)-Cdc7-IN-18, a potent CDC7 inhibitor, effectively impedes the overactivation of MCM2, a crucial tumor cell marker, induced by huCdc7 overexpression. Consequently, it inhibits the aberrant proliferation of tumor cells.... |
|
T70941 |
CLR01 sodium
|
|
|
|
CLR01 is a molecular tweezer. CLR01 reduces aggregated, pathologic, and seeding-competent α-synuclein in experimental multiple system atrophy. CLR01 inhibits aberrant superoxide dismutase 1 (SOD1) self-assembly in vitro ... |
|
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]. |
|
T68267 |
RO5068760
|
|
|
|
RO5068760 , a substituted hydantoin, is a potent, highly selective, non-adenosine triphosphate (ATP)-competitive MEK1/2 inhibitors. RO5068760 shows significant efficacy in a broad spectrum of tumors with aberrant mitogen... |
|
T62680 |
(R)-MLT-985
|
|
|
|
(R)-MLT-985 (compound 11) is a potent inhibitor of MALT1 protease (IC50: 3 nM). (R)-MLT-985 has an IC50 value of 20 nM for MALT1-dependent IL-2 in Jurkat cells.(R)-MLT-985 inhibits growth and aberrant CARD11/BCL10/MALT1 ... |
|
T74644 |
DB0614
|
|
PROTACs
|
|
DB0614 (Example 21) is a bifunctional compound designed for the targeted degradation of kinases, effectively breaking down a wide array of kinases including AAK1, AURKA, BMP2K, CAMKK1, CDK16, CML, CDK6, EIF2AK2, FER, GAK... |
|
T60360 |
LSD1/2-IN-3
|
|
|
|
LSD1/2-IN-3 is a selective inhibitor of lysine-specific demethylase 1 ( LSD1 ) with a Ki value of 11 nM rather than 7 μM for LSD2. There is aberrant expression of LSD1 in tumor stem cells, LSD1/2-IN-1 inhibits LSD1 cell ... |
|
T68459 |
RO4927350
|
|
|
|
RO4927350 is a potent and highly selective non-ATP-competitive MEK1/2 inhibitor. RO4927350 selectively blocks the MAPK pathway signaling both in vitro and in vivo, which results in significant antitumor efficacy in a bro... |
|
T70527 |
DAT-230
|
|
|
|
DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -tr... |
|
T74642 |
DB1113
|
|
PROTACs
|
|
DB1113 (Example 24) is a bifunctional compound designed for the targeted degradation of various kinases. It effectively degrades a range of kinases, including ABL1, ABL2, BLK, CDK11B, CDK4, CSK, EPHA3, FER, GAK, LIMK1, M... |
|
T60359 |
Cis-4-Br-2,5-F2-PCPA
|
|
|
|
cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. There is aberrant expression of LSD1 in cancer stem cells, cis-4-Br-2,5-F2-PCPA inhibits LSD1 cell proliferation and b... |
|
T82971 |
ARI-1
|
|
|
|
ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor that binds to ROR1's extracellular Frizzled domain, effectively inhibiting aberrant ROR1 expression linked to non-small cell lung cancer (NSCLC)... |
|
T68480 |
4SC-207
|
|
|
|
4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell ... |
