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WZ4003WZ4003
wz4003, a highly selective nuak kinase inhibitor, is with ic50 of 20 nm and 100 nm for nuak1 and nuak2, respectively. it is no significant inhibition on 139 other kinases.
���•r(sh��)�g:2025-06-07
TanespimycinTanespimycin,CP 127374,NSC 330507
tanespimycin (17-aag) is an inhibitor of hsp90 that selectively inhibits bt474 tumor cell hsp90 (ic50: 5 nm).
���•r(sh��)�g:2025-06-07
DovitinibDovitinib,TKI258,CHIR-258
dovitinib (tki258, chir258) is a multitargeted rtk inhibitor, mostly for class iii (flt3/c-kit, ic50: 1/2 nm), also effective to class iv (fgfr1/3) and class v (vegfr1-4) rtks (ic50: 8-13 nm), less potent to egfr, insr, epha2, c-met, igf-1r, tie2, and her
���•r(sh��)�g:2025-06-07
TariquidarTariquidar,XR9576,
tariquidar(kd=5.1 nm) is a specific and effective non-competitive inhibitor of p-glycoprotein. it can reverse drug resistance in mdr cell lines.
���•r(sh��)�g:2025-06-07
GSK690693GSK690693
gsk690693 is a pan-akt inhibitor targeting akt1/2/3 with ic50 of 2 nm/13 nm/9 nm, also sensitive to the agc kinase family: pka, prkx and pkc isozymes. phase 1.
���•r(sh��)�g:2025-06-07
OnalespibOnalespib,AT13387,Onalespib (AT13387)
onalespib is a synthetic, orally bioavailable, small-molecule inhibitor of heat shock protein 90 (hsp90) with potential antineoplastic activity. onalespib selectively binds to hsp90, thereby inhibiting its chaperone function and promoting the degradation
���•r(sh��)�g:2025-06-07
WortmanninWortmannin,KY-12420,SL-2052
wortmannin is the first described pi3k inhibitor with ic50 of 3 nm, with little selectivity within the pi3k family. also blocks autophagosome formation and potently inhibits dna-pk/atm with ic50 of 16 nm and 150 nm.
���•r(sh��)�g:2025-06-07
GSK461364GSK461364,GSK461364A,
gsk461364(ki=2.2 nm) inhibits purified plk1 .the specificity of gsk461364 for plk1 is more than 1000-fold over plk2/3.
���•r(sh��)�g:2025-06-07
TW-37TW-37,TW37,TW 37
tw-37 is an nonpeptide inhibitor to recombinant bcl-2, bcl-xl and mcl-1 (ki: 0.29/1.11/0.26 ��m).
���•r(sh��)�g:2025-06-07
EnzastaurinEnzastaurin,LY317615,
enzastaurin (ly317615) is an effective pkc�� selective inhibitor (ic50: 6 nm), 6- to 20-fold selectivity against pkc��/��/��.
���•r(sh��)�g:2025-06-07
Givinostat hydrochloride monohydrateGivinostat hydrochloride monohydrate,ITF-2357 hydrochloride mono
givinostat hydrochloride monohydrate is an hdac inhibitor.
���•r(sh��)�g:2025-06-07
SotrastaurinSotrastaurin,AEB071,
sotrastaurin is a potent pan-pkc inhibitor (kis: 0.95/0.64/2.1/3.2/1.8/0.22 nm for pkc��/��i/��/��/��/��).
���•r(sh��)�g:2025-06-07
DoramapimodDoramapimod,BIRB 796,
doramapimod is a highly potent inhibitor of p38 mapk (kd: 0.1 nm), but weakly inhibits c-raf, fyn, lck, erk-1, syk, ikk2, and zap-70.
���•r(sh��)�g:2025-06-07
NU7441NU7441,KU-57788,
nu7441 (ku-57788) is a highly effective and specific dna-pk inhibitor (ic50: 14 nm).
���•r(sh��)�g:2025-06-07
Obatoclax MesylateObatoclax Mesylate,GX15-070,Obatoclax
obatoclax is a bcl-2 antagonist (ki: 0.22 ��m) and can induce apoptosis with up-regulation of bim, induced cytochrome c release, and activation of caspase-3.
���•r(sh��)�g:2025-06-07
RO4929097RO4929097,RG-4733,
ro4929097, a �� secretase inhibitor (ic50: 4 nm), inhibits cellular processing of a��40 and notch (ec50: 14/5 nm).
���•r(sh��)�g:2025-06-07
DMXAADMXAA,ASA-404,Vadimezan
vadimezan is a fused tricyclic analogue of flavone acetic acid with potential antineoplastic activity. vadimezan induces the cytokines tumor necrosis alpha (tnf-alpha), serotonin and nitric oxide, resulting in hemorrhagic necrosis and a decrease in angiog
���•r(sh��)�g:2025-06-07
Fosbretabulin DisodiumFosbretabulin Disodium,CA 4P,Combretastatin A4 disodium phosphate
fosbretabulin (combretastatin a4 phosphate (ca4p)) disodium, a water-soluble prodrug of combretastatin a4 (ca4), is a microtubule-targeting agent that binds ��-tubulin (kd: 0.4 ��m). fosbretabulin disodium inhibits the polymerization of tubulin (ic50: 2.4 ��
���•r(sh��)�g:2025-06-07
TipifarnibTipifarnib,R115777,IND 58359
tipifarnib is a nonpeptidomimetic quinolinone with potential antineoplastic activity. tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. by inhibiting
���•r(sh��)�g:2025-06-07
Trichostatin ATrichostatin A,TSA,
trichostatin a is a natural derivative of dienohydroxamic acid isolated from species of the bacterial genus streptomyces. trichostatin a (tsa) reversibly and specifically inhibits histone deacetylases, resulting in hyperacetylation of core histones which
���•r(sh��)�g:2025-06-07
CP-466722CP-466722,CP466722,CP 466722
cp-466722, an effective and reversible atm inhibitor, does not inhibit atr and pi3k or pikk family members in cells.
���•r(sh��)�g:2025-06-07
AMG-208AMG-208,AMG208,AMG 208
amg 208 is a highly selective c-met inhibitor with ic50 of 9 nm. phase 1.
���•r(sh��)�g:2025-06-07
AZ191AZ191
az191��ic50 of 17 nm�� is an effective and specific dyrk1b inhibitor. the specificity of az191 for dyrk1b is about 5- and 110-fold greater over dyrk1a and dyrk2, respectively.
���•r(sh��)�g:2025-06-07
YYA-021YYA-021,YYA021,YYA 021
yya-021 inhibits hiv entry, with high anti-hiv activity and low cytotoxicity.
���•r(sh��)�g:2025-06-07
IdasanutlinIdasanutlin,RG7388,Ro 5503781
idasanutlin (rg-7388) is an effective and specific p53-mdm2 inhibitor (ic50: 6 nm).
���•r(sh��)�g:2025-06-07
TalazoparibTalazoparib,LT-673,BMN-673
talazoparib is a new-type parp inhibitor (ic50: 0.58 nm), it similarly binds to parp1/2 (kis: 1.2/0.85 nm).
���•r(sh��)�g:2025-06-07
PF-04691502PF-04691502,PF04691502,PF 04691502
pf-04691502 is a potent and selective inhibitor of pi3k and mtor kinases with antitumor activity.
���•r(sh��)�g:2025-06-07
H 89 2HClH 89 2HCl,H-89 dihydrochloride,Protein kinase inhibitor H-89 dihydrochloride
h 89 is a potent inhibitor of protein kinase a (pka; ic50: 0.14 ��m, ki: 48 nm).
���•r(sh��)�g:2025-06-07
AvagacestatAvagacestat,BMS-708163,
avagacestat (bms-708163) is a potent, selective, orally bioavailable ��-secretase inhibitor of a��40 and a��42 with ic50 of 0.3 nm and 0.27 nm, demonstrating a 193-fold selectivity against notch. phase 2.
���•r(sh��)�g:2025-06-07
XL888XL888
xl888 is an atp-competitive inhibitor of hsp90 ( ic50: 24 nm). heat shock protein 90 (hsp90) is a chaperone that maintains the functionality of client proteins involved in cell proliferation, cell cycling, and apoptosis. through this action, specific clie
���•r(sh��)�g:2025-06-07
NMS-P937NMS-P937,NMS-1286937,
nms-p937 (nms1286937), an oral, specific polo-like kinase 1 (plk1) inhibitor, is with ic50 of 2 nm. the specificity of nms-p937 forplk1 is 5000-fold higher over plk2/plk3.
���•r(sh��)�g:2025-06-07
CobicistatCobicistat,GS-9350,Tybost
cobicistat is a carbamate and thiazole derivative that functions as a cytochrome p450 cyp3a inhibitor to enhance the concentration of anti-hiv agents, with which it is used in combination, for the treatment of hiv infections.
���•r(sh��)�g:2025-06-07
BAPTA-AMBAPTA-AM,BAPTA/AM,
bapta-am is a selective, permeable free calcium chelator.
���•r(sh��)�g:2025-06-07
U73122U73122
u73122, an effective plc inhibitor, reduces agonist-induced ca2+ increases in platelets and pmn.
���•r(sh��)�g:2025-06-07
Rupatadine FumarateRupatadine Fumarate,Rupafin,Alergoliber
rupatadine fumarate (ur-12592 fumarate) is a potent dual paf/h1 antagonist with ki of 0.55/0.1 um.
���•r(sh��)�g:2025-06-07
Quetiapine FumarateQuetiapine Fumarate,ICI-204636,
quetiapine fumarate, an atypical antipsychotic, is used in the treatment of bipolar i mania, schizophrenia, bipolar ii depression, bipolar i depression.
���•r(sh��)�g:2025-06-07
WZ4002WZ4002
wz4002 is a mutant-selective egfr inhibitor for egfr(l858r) and egfr(t790m) with ic50 of 2 nm/8 nm.
���•r(sh��)�g:2025-06-07
TrelagliptinTrelagliptin,SYR-472,
trelagliptin is a highly specific and long-acting dpp-4 inhibitor.
���•r(sh��)�g:2025-06-07
OzagrelOzagrel,OKY-046,Domenan
ozagrel is a selective thromboxane a(2) (txa(2)) synthetase inhibitor with ic50 of 11 nm for rabbit platelet, used for the improvement of postoperative cerebrovascular contraction and accompanying cerebral ischaemia.
���•r(sh��)�g:2025-06-07
Lapatinib DitosylateLapatinib Ditosylate,GW-572016 ditosylate,Lapatinib (GW-572016) Ditosylate
lapatinib is an effective egfr and erbb2 inhibitor (ic50: 10.8/9.2 nm for egfr/erbb2).
���•r(sh��)�g:2025-06-07
Ambroxol hydrochlorideAmbroxol hydrochloride,Ambroxol HCl,Mucoangin
ambroxol hydrochloride is a metabolite of bromhexine that stimulates mucociliary action and clears the air passages in the respiratory tract. it is usually administered as the hydrochloride.
���•r(sh��)�g:2025-06-07
EntinostatEntinostat,SNDX-275,MS-275
entinostat (ms-275) is an inhibitor of hdacs that inhibits hdac1 and hdac3 (ic50s: 0.18/0.74 ��m).
���•r(sh��)�g:2025-06-07
Vilazodone HClVilazodone HCl,SB659746A,EMD 68843
vilazodone hcl��a partial agonist of 5-ht1a receptors and specific serotonin reuptake inhibitor (ssri), is utilized in treating of the major depressive disorder.
���•r(sh��)�g:2025-06-07
Tebipenem PivoxilTebipenem Pivoxil,ME1211,Orapenem
tebipenem pivoxil, an orally activity carbapenem antibiotic, is utilized in treating otolaryngologic and respiratory infections.
���•r(sh��)�g:2025-06-07
ImatinibImatinib,STI571,CGP057148B
matinib is an inhibitor of the receptor tyrosine kinases c-abl, bcr-abl, pdgfr, and c-kit (ic50: 600/100/100 nm).
���•r(sh��)�g:2025-06-07
DaclatasvirDaclatasvir,EBP 883,BMS-790052
daclatasvir (bms-790052) is a highly selective inhibitor of hcv ns5a with ec50 of 9-50 pm, for a broad range of hcv replicon genotypes and the jfh-1 genotype 2a infectious virus in cell culture. phase 3.
���•r(sh��)�g:2025-06-07
IrinotecanIrinotecan,CPT-11,(+)-Irinotecan
irinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. it is a derivative of camptothecin that inhibits the action of topoisomerase i. irinotecan prevents religation of the dna strand by binding to topoisome
���•r(sh��)�g:2025-06-07
Benidipine hydrochlorideBenidipine hydrochloride,KW-3049,Benidipine HCl
benidipine hcl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
���•r(sh��)�g:2025-06-07
Pemetrexed Disodium HydratePemetrexed Disodium Hydrate,Pemetrexed disodium hemipenta hydrate,Pemetre
pemetrexed disodium hydrate is a new-type antifolate and antimetabolite for ts, dhfr, and garft. the ki of pemetrexed disodium hydrate for ts, dhfr and garft is 1.3 nm, 7.2 nm and 65 nm, respectively.
���•r(sh��)�g:2025-06-07
Adenine hydrochlorideAdenine hydrochloride,Adenine HCl,6-Aminopurine hydrochloride
adenine hcl is a hydrochloride salt form of adenine which is a nucleobase with a variety of roles in biochemistry.
���•r(sh��)�g:2025-06-07

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