| DC74363 |
Fulzerasib |
Fulzerasib is a potent selective inhibitor of KRAS gene mutation. |
|
| DC74364 |
G12Si-5 |
G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM. |
|
| DC74365 |
RMC-4998
Featured
|
RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM. |
|
| DC74366 |
RSC-1255 |
RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity. |
|
| DC74367 |
SCH53239 |
SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein. |
|
| DC74368 |
SIJ1772 |
SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively. |
|
| DC74369 |
SIJ1795 |
SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively. |
|
| DC74370 |
Z640 |
Z640 is a novel non-selective atypical PKC (aPKC) agonist, increases PKCζ and PKCι kinase activity with EC50 of 1.09 and 3.47 µM in vitro kinase activity assays, respectively. |
|
| DC74371 |
CDD-1115 |
CDD-1115 (CDD1115) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.8 nM and Kiapp of 6.2 nM. |
|
| DC74372 |
CDD-1281
Featured
|
CDD-1281 (CDD1281) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 1.2 nM and Kiapp value of 8 nM. |
|
| DC74373 |
CDD-1653 |
CDD-1653 (CDD1653) is a potent, selective inhibitor of BMP type 2 receptor BMPR2 with IC50 of 2.8 nM, >360-fold over ALK1, and is inactive versus all other type 1 and type 2 TGFβ family kinases. |
|
| DC74374 |
Ki26894 |
Ki26894 (Ki 26894) is a small molecule TGF-beta type I receptor (TbetaR-I) kinase inhibitor, inhibits TGF-β-induced transcriptional activation in MDA-231-D-TβFluc/Rluc cells with IC50 of 0.49 uM. |
|
| DC74375 |
SRI-31277 |
SRI-31277 is a tripeptide inhibitor of thrombospondin 1 activation of TGF-β, specifically inhibits TGF-β activation mediated through TSP-1 with pIC50 of 8.28 nM. |
|
| DC74376 |
Ensartinib dihydrochloride |
Ensartinib (X-396) dihydrochloride is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM. |
|
| DC74377 |
Ficonalkib |
Ficonalkib is a potent, selective anaplastic lymphoma kinase (ALK) inhibitor for treating an ALK-mediated disease. |
|
| DC74378 |
ACP-5862 |
ACP-5862 is a major metabolite of acalabrutinib and potent and selective covalent BTK inhibitor with IC50 of 5 nM. |
|
| DC74379 |
DZD8586 |
DZD8586 is an oral, non-covalent, BBB penetrant LYN and BTK dual inhibitor, overcomes resistance mutations to the approved covalent and non-covalent BTK inhibitors. |
|
| DC74380 |
BLU-808 |
BLU-808 is a potent and selective wt c-KIT inhibitor, potently inhibits c-KIT–dependent phosphorylation and proliferation with IC50 values in the sub-nanomolar and nanomolar range, respectively. |
|
| DC74381 |
Dalmelitinib |
Dalmelitinib is a potent, selective c-Met tyrosine kinase inhibitor with IC50 of 0.7 nM, inhibits cell growth of gastric cells SNU5 with IC50 of 2.0 nM, binds to the ATP-binding region of c-MET kinase. |
|
| DC74382 |
Tepotinib
Featured
|
Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated varia |
|
| DC74383 |
WM-S1-030
Featured
|
WM-S1-030 is a highly potent, specific inhibitor of recepteur d'origine nantais (RON kinase, MST1R) with IC50 of 0.39 nM in in vitro enzyme activity. |
|
| DC74384 |
KI-301690 |
KI-301690 (KI 301690) is a novel potent, specific DDR1 inhibitor, synergized with gemcitabine to suppress the growth of pancreatic cancer cells. |
|
| DC74385 |
FC162 |
FC162 is a potent inhibitor of DYRK1A with IC50 of 11, 18, and 68 nM, against DYRK1A, CLK1, and GSK3, respectively. |
|
| DC74386 |
Leucettinib-21 |
Leucettinib-21 is a potent, selective DYRKs and CLKs kinases with IC50 of 2.4, 6.7, 12, 33, and 5 nM for DYRK1A, DYRK1B, CLK1, CLK2, and CLK4, respectively. |
|
| DC74387 |
Y020-3945 |
Y020-3945 is a selective dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor with IC50 of 0.53 uM. |
|
| DC74388 |
YK-2-69 |
YK-2-69 is a potent, hilghly selective inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase 2 (DYRK2) with IC50 value of 9 nM, shows weak inhibition against DYRK1B (IC50=542 nM) and no activity against DYRK1A/3/4 (IC50>1,000 nM). |
|
| DC74389 |
ARRY-380 analog |
An analog of ARRY-380, a potent and selective HER2 inhibitor with IC50 of 8 nM. |
|
| DC74390 |
AZD-9291 dimesylate |
A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively. |
|
| DC74391 |
BI-1622 |
BI-1622 (BI 1622) is a potent, selective, covalent and orally active HER2 inhibitor with IC50 of 7 nM, potently inhibits HER2 exon 20 mutants while sparing WT EGFR. |
|
| DC74392 |
BI-4732 |
BI-4732 is a potent, highly BBB penetrant, fourth-generation EGFR inhibitor against EGFR activating mutations, including C797S. |
|
