Niraparib(MK4827) free base
CAS 1038915-60-4
Niraparib (MK-4827) is a highly potent PARP1 and PARP2 inhibitor with IC50s of 3.8 and 2.1 nM, respectively.
Cancer Research
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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CP-868596 (Crenolanib)
CAS 670220-88-9
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 2.1 nM/3.2 nM, 0.74 nM, respectively.
Panobinostat(LBH589)
CAS 404950-80-7
Panobinostat is a non-selective histone deacetylase (HDAC) inhibitor.
BMS-911543
CAS 1271022-90-2
BMS-911543 is a selective JAK2 inhibitor, with IC50s of 1.1 nM, less selective at JAK1, JAK3 and TYK2 (IC50, 75, 360, 66 nM, respectively).
AZD-7762
CAS 860352-01-8
AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC50 of 5 nM for Chk1.
SGX-523
CAS 1022150-57-7
SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.
Glasdegib(PF-04449913)
CAS 1095173-27-5
Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM.
PCI-32765 (Ibrutinib)
CAS 936563-96-1
Ibrutinib (PCI-32765) is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
Nintedanib (BIBF 1120)
CAS 656247-17-5
BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
BKM120 (NVP-BKM120, Buparlisib)
CAS 944396-07-0
NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
AZD-9291(Osimertinib)
CAS 1421373-65-0
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.
LGK-974
CAS 1243244-14-5
LGK974 is a potent and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM.
Motesanib Diphosphate (AMG-706)
CAS 857876-30-3
Motesanib Diphosphate is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is approximately 10-fold more selective for VEGFR than PDGFR and Ret.
Momelotinib (CYT387,CYT-387)
CAS 1056634-68-4
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
Foretinib(XL880)
CAS 849217-64-7
Foretinib is a multi-target tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.
JNJ 38877605
CAS 943540-75-8
JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.
CX6258
CAS 1202916-90-2
CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.
pac-1
CAS 315183-21-2
PAC-1 is an activator of procaspase-3 induces apoptosis in cancer cells with EC50 of 2.08 μM.
Apatinib Mesylate
CAS 1218779-75-9
Apatinib is a highly selective VEGFR2 inhibitor with an IC50 of 1 nM. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively.
GLPG0187
CAS 1320346-97-1
GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM.
Cediranib
CAS 288383-20-0
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
E7080 (Lenvatinib)
CAS 417716-92-8
Lenvatinib is an oral, multi-targeted tyrosine kinase inhibitor with IC50s of 4 and 5.2 nM for VEGFR2(KDR) and VEGFR3(Flt-4), respectively. Lenvatinib is less potent against VEGFR1/Flt-1 and shows approximately 10-fold selectivity for VEGFR2/3 over FGFR1,…
Defactinib (VS-6063, PF-04554878)
CAS 1073154-85-4
Defactinib is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities.
EPZ011989
CAS 1598383-40-4
EPZ011989 is a potent, selective orally bioavailable EZH2 inhibitor with Ki < 3 nM for EZH2 wt and EZH2 Y646; 15-fold selectivity over EZH1 and >3000-fold selectivity over other HMTase.IC50 value: < 3 nM ( Ki for wt EZH2, EZH2 Y646)Target: EZH2 inhibitorIn…
Ruxolitinib (INCB018424)
CAS 941678-49-5
Ruxolitinib is a potent and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3.
Prexasertib (LY2606368)
CAS 1234015-52-1
Prexasertib (LY2606368) is a potent, selective and ATP-competitive checkpoint kinase 1 (Chk1) inhibitor, with an IC50 and a Ki of <1 nM and 0.9 nM, respectively.
GDC0941(Pictilisib)
CAS 957054-30-7
GDC-0941 (Pictilisib) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
Delanzomib(CEP-18770)
CAS 847499-27-8
Delanzomib(CEP-18770) is a novel orally-active inhibitor of the chymotrypsin-like activity of the proteasome that down-modulates the nuclear factor-kappaB (NF-kappaB) activity.
ELR-510444
CAS 1233948-35-0
ELR510444 is a novel microtubule disruptor; inhibits MDA-MB-231 cell proliferation with IC50 of 30.9 nM; not a substrate for the P-glycoprotein drug transporter and retains activity in βIII-tubulin-overexpressing cell lines.ELR510444 is not a substrate for…
HA-15
CAS 1609402-14-3
HA15 is a molecule that targets specifically BiP/GRP78/HSPA5target: BiP, GRP78, HSPA5 [1]In vitro: HA15 induces ER stress leading to cancer cell death. kills cancer cells by targeting BiP to increase ER stress, leading to melanoma cell death by concomitant…
Vismodegib (GDC-0449)
CAS 879085-55-9
Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. It also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
TG101209
CAS 936091-14-4
TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
Molibresib(I-BET-762）
CAS 1260907-17-2
GSK 525762A is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.
Pirfenidone(AMR69)
CAS 53179-13-8
Pirfenidone is a drug used for the treatment of idiopathic pulmonary fibrosis. It inhibits FGFR, EGFR, PDGFR, TGF-β, thereby slowing tumor cell proliferation.
PF-299804 (Dacomitinib,PF-00299804)
CAS 1110813-31-4
Dacomitinib is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively.
Tucidinostat(Chidamide)
CAS 743420-02-2
Chidamide is a synthetic benzamide-type HDAC inhibitor, inhibits HDAC1, HDAC2, HDAC3 and HDAC10 with IC50s of 95, 160, 67 and 78 nM, respectively.
GZD824
CAS 1257628-77-5
GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. IC50 Value: 0.34/0.68 nM(Bce-Abl wt/T315I) [1]Target: Bcr-Abl in vitro: GZD824 potently suppressed proliferation of…
Duvelisib (IPI-145, INK1197)
CAS 1201438-56-3
Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
Pelitinib (EKB-569; WAY-EKB 569)
CAS 257933-82-7
Pelitinib (EKB-569;WAY-EKB 569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively.
PLX-4720
CAS 918505-84-7
PLX-4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM in a cell-free assay, equally potent to c-Raf-1(Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf.
BMS-986205(Linrodostat)
CAS 1923833-60-6
BMS-986205 is a selective indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor.
Idelalisib (CAL-101,GS-1101)
CAS 870281-82-6
Idelalisib (CAL-101) is a highly selective and potent p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
Glabridin
CAS 59870-68-7
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic,…
Meisoindigo
CAS 97207-47-1
Meisoindigo(Natura-α; N-Methylisoindigotin; Dian III), a derivative of Indigo naturalis, might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML).IC50 value:Target: apoptosis inducerin vitro: Meisoindigo inhibited the growth of…
Quizartinib (AC220)
CAS 950769-58-1
Quizartinib (AC220) is a potent Flt3 tyrosine kinase inhibitor with a Kd of 1.6±0.7 nM.
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