|
T9072 |
Tuxobertinib
|
BDTX-189 |
EGFR
,
HER
,
BTK
,
RIP kinase
|
|
Tuxobertinib (BDTX-189) is a potent and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations(KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively). BDTX-189 exhibits anticancer activ... |
|
TQ0092 |
Naquotinib
|
ASP8273 |
EGFR
|
|
Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR. |
|
T31014 |
Corrector C4
|
Corr 4a,Corrector C-4,Corr4a,Corrector C 4,Corr-4a |
Others
|
|
Corrector C4, a corrector commonly used to study cystic fibrosis mutants, works by alleviating the interaction between CFTR transmembrane domain mutants and protein homeostasis. |
|
T72062 |
BI-2865
|
|
Ras
|
|
BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cel... |
|
T11761 |
Tarlox-TKI
|
Kinase inhibitor-1 |
EGFR
|
|
Tarlox-TKI (Kinase inhibitor-1) is a pan-ErbB inhibitor, the active ingredient of Tarloxotinib, with antitumor activity.Tarlox-TKI inhibits NRG1 and suppresses HER2 mutants. |
|
T24943 |
VPC-14228
|
VPC 14228,VPC14228 |
Androgen Receptor
|
|
VPC-14228 is a specific AR-DBD inhibitor that acts by inhibiting both Y594A and Q592A mutants. |
|
T22592 |
ATPγS tetralithium salt
|
ATP-gamma-S tetralithium salt |
PERK
|
|
ATPγS tetralithium salt is a substrate for nucleotide hydrolysis and RNA unraveling activity of the eukaryotic translation initiation factor eIF4A, associated with p97 mutants and prions. |
|
T2104 |
AGI-5198
|
IDH-C35 |
Dehydrogenase
,
Isocitrate Dehydrogenase (IDH)
|
|
AGI-5198 (IDH-C35) is a highly effective and specific inhibitor of IDH1 R132H/R132C mutants (IC50: 0.07/0.16 μM). |
|
T6824 |
EAI045
|
|
EGFR
|
|
EAI045, an allosteric inhibitor, targets towards drug-resistant EGFR mutants but avoids the wild-type receptor. |
|
T2147 |
Nilotinib monohydrochloride monohydrate
|
Nilotinib (monohydrochloride monohydrate),AMN107 (monohydrochloride monohydrate) |
Bcr-Abl
,
Autophagy
|
|
Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against many BCR-ABL muta... |
|
T16516 |
PG01
|
Phenylglycine-01 |
CFTR
|
|
|
|
T7861 |
Flumatinib mesylate
|
HHGV678 mesylate |
Bcr-Abl
,
PDGFR
,
c-Kit
|
|
Flumatinib mesylate (HHGV678 mesylate) is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants. |
|
T2287 |
PIK-75 hydrochloride
|
PIK-75 HCl,PIK-75 |
Apoptosis
,
DNA-PK
,
PI3K
|
|
PIK-75 hydrochloride (PIK-75 HCl) is a p110α inhibitor with IC50 of 5.8 nM (200-fold more potently than p110β), isoform-specific mutants at Ser773, and also potently inhibits DNA-PK with IC50 of 2 nM in cell-free assays. |
|
T2620 |
G-749
|
G749 |
Apoptosis
,
FLT
,
c-RET
,
TAM Receptor
,
Aurora Kinase
|
|
G-749, a new-type FLT3 inhibitor, exhibits effective and sustained inhibition of the FLT3 wild type and mutants. |
|
T2329 |
Dolutegravir sodium
|
GSK1349572,GSK-1349572A |
HIV Protease
|
|
Dolutegravir sodium (GSK-1349572A) salt(DTG; GSK1349572) is an HIV integrase inhibitor(IC50: 2.7 nM), modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
|
T6198 |
Dolutegravir
|
S/GSK1349572,GSK1349572 |
HIV Protease
|
|
Dolutegravir (GSK1349572) (IC50=2.7 nM), a two-metal-binding HIV integrase inhibitor, exhibits medium activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
|
TQ0277 |
Pralsetinib
|
Blu667 |
c-RET
|
|
Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion). |
|
T11438 |
GNE-1858
|
|
Others
,
MAPK
|
|
|
|
T22324 |
Ensartinib hydrochloride
|
Ensartinib dihydrochloride,X-396 dihydrochloride |
Others
,
Trk receptor
,
c-Met/HGFR
,
ALK
|
|
Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both... |
|
T75129 |
Luxdegalutamide
|
ARV-766 |
Androgen Receptor
,
PROTACs
|
|
Luxdegalutamide (ARV-766) is an orally available and effective protein degrader of protein hydrolysis-targeted chimeras (PROTAC).Luxdegalutamide degrades the wild-type androgen receptor AR, as well as AR LBD mutants incl... |
|
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. |
|
T4428 |
CCT241736
|
|
FLT
,
Aurora Kinase
|
|
CCT241736 is an orally bioavailable dual FLT3/Aurora kinase inhibitor that also inhibits clinically relevant FLT3-resistant mutants including FLT3-ITD and FLT3, CCT241736, an advanced analog of CCT137690, is a preclinica... |
|
T8758 |
Poziotinib hydrochloride
|
HM 781-36B hydrochloride,NOV120101 hydrochloride |
EGFR
|
|
Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. It is an orally bioavaila... |
|
T63321 |
20S Proteasome activator 1
|
|
Proteasome
|
|
20S Proteasome activator 1 is a 20S proteasome activator with IC50 of 0.3 μM for trypsin-like sites, 0.7 μM for chymotrypsin-like sites and 1.8 μM for caspase sites. 20S Proteasome activator 1 prevents the accumulation o... |
|
T41068 |
P53R3
|
|
p53
|
|
P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53 R273H. This compound exhibits p53-dependent antiproliferativ... |
|
T9533 |
BC-LI-0186
|
4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide |
Others
|
|
BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protei... |
|
T1283 |
Clinafloxacin
|
PD 127391,CI-960,AM-1091 |
Antibacterial
,
Antibiotic
|
|
Clinafloxacin (CI-960)(PD-127391) is a fluoroquinolone antibiotic. |
|
T26388 |
4-CPI
|
4 CPI |
|
|
4-CPI inhibits non-active site mutants of cytochrome P450 2B4. |
|
T40150 |
Trk-IN-6
|
|
|
|
Trk-IN-6 shows excellent in vitro potency on a panel of TRK mutants ( IC 50 = 0.2-0.7 nM). |
|
T70565 |
Saussureamine C
|
|
|
|
Saussureamine C is an inhibitor of H274Y and N294S mutants. |
|
T28988 |
TNK-6123
|
TNK6123 |
|
|
TNK-6123 is an emivirine analog. TNK-6123 has improved activity against drug-resistant HIV mutants. |
|
T24944 |
VPC-14449
|
VPC14449,VPC 14449 |
|
|
VPC-14449 is a specific inhibitor of AR-DBD that acts by inhibiting both Y594A and Q592A mutants. |
|
TQ0277L |
Pralsetinib HCl (2097132-94-8 free base)
|
Pralsetinib HCl,Pralsetinib hydrochloride,BLU-667,BLU667,BLU 667 |
|
|
Pralsetinib is a selective and next-generation RET inhibitor (IC50: 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T, and CCDC6-RET fusion). BLU-667 is an effective and selective inhibitor of RET mutations, fusions... |
|
T31218 |
DBHDA
|
|
|
|
DBHDA is a reagent to convert a Cys into a Dha moiety by reacting with a C-terminal Cys residue and thus allowing the use of recombinant Ubl G76C mutants to prepare probes. |
|
T38943 |
L-Azidonorleucine hydrochloride
|
|
|
|
L-Azidonorleucine hydrochloride, an unnatural amino acid, serves as a surrogate for Methionine. It is utilized for labeling mammalian cell proteins and identifying a broad range of methionyl-tRNA synthetase (MetRS) mutan... |
|
T61179 |
EMI48
|
|
|
|
EMI48, a derivative of EMI1, exhibits increased efficacy against mutant EGFR compared to EMI1. It specifically inhibits EGFR triple mutants [1]. |
|
T68368 |
HWY-5069 bromide
|
|
|
|
HWY-5069 bromide is an isoquinolinium derivative that inhibits the proliferation of wild-type and all mutants of Schizosaccharomyces pombe. |
|
T69045 |
ON012380
|
|
|
|
ON012380 is a non-ATP-competitive Bcr-Abl inhibitor, potently inhibiting imatinib-resistant Bcr-Abl mutants such as T315I. |
|
T28898 |
T145
|
T 145,T-145 |
|
|
T145 inhibits growth of Enterococcus faecalis, Staphylococcus aureus and Mycobacterium tuberculosis (Mtb) with sub μg/ml potencies that are potentially therapeutically valuable. T145 minimizes selection of spontaneous re... |
|
T35913 |
EMI56
|
|
|
|
EMI56, a derivative of EMI1, exhibits enhanced potency against mutant EGFR compared to EMI1. Additionally, EMI56 effectively inhibits EGFR triple mutants[1]. |
|
T15442 |
GSK864
|
|
Others
|
|
GSK864 is an inhibitor of isocitrate dehydrogenase 1 (IDH1) mutant. GSK864 inhibits IDH1 mutants R132C, R132H, and R132G (IC50: 8.8, 15.2, and 16.6 nM). |
|
T71006 |
BI-1388
|
|
|
|
BI-1388 is a highly potent inhibitor of HCV NS3 protease activity, inhibiting viral replication for various HCV genotypes and for resistant mutants D168V and R155K. |
|
T20163L |
Acetyltrialanine acetate
|
Acetyltrialanine acetate(19245-85-3 Free base) |
Others
|
|
Acetyltrialanine acetate is the nitrogen source of mutants of Salmonella typhimurium. |
|
T12175 |
Naquotinib mesylate
|
ASP8273 (mesylate) |
EGFR
|
|
Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR). |
|
T27201 |
DPC-082
|
DPC 082 |
|
|
DPC-082 is a reverse transcriptase inhibitor. DPC-082 exhibits low-nanomolar potency toward wild-type virus, L100I and K103N single-mutation variants, and multiplies amino acid-substituted HIV type 1 mutants. |
|
T70597 |
G-749 hydrochloride
|
|
|
|
G-749 hydrochloride is a novel FLT3 inhibitor that showed potent and sustained inhibition of the FLT3 wild type and mutants including FLT3-ITD, FLT3-D835Y, FLT3-ITD/N676D, and FLT3-ITD/F691L in cellular assays. |
|
T23975 |
Deacylcortivazol
|
UNII-3JO09QT49F,DAC,NSC 325316 |
|
|
Deacylcortivazol (DAC) is a potent glucocorticoid. When incubated with glucocorticoid-resistant mutants derived from the glucocorticoid-sensitive human leukemic cell line CEM-C7, DAC caused significant growth inhibition.... |
|
T32288 |
JH-IX-179
|
JH-IX179,JH-IX 179 |
|
|
JH-IX-179 is a novel type I ATP competitive and highly selective FLT3 inhibitor. JH-IX-179 is much more selective for FLT3 and FLT3 mutants than for Kronani. In addition, JH-IX-179 showed little human serum protein bindi... |
|
T70844 |
CM-118
|
|
|
|
CM-118 is a potent and selective dual inhibitor of c-Met and ALK which potently abrogates hepatocyte growth factor (HGF)-induced c-Met phosphorylation and cell migration, as well as phosphorylation of ALK, EML4-ALK, and ... |
|
T63927 |
KRAS G12C inhibitor 25
|
|
|
|
KRAS G12C inhibitor 25 is an inhibitor of KRAS G12C. KRAS G12C inhibitor 25 inhibits the SOS1-assisted GDP/GTP exchange activity of KRAS-G12C mutants with an IC50 value of 0.48 nM. |
