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Epigenetics | 表观遗传学



产品 151 到 200 共 312个

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Catalog No. Product Name Application Product Information
A10004 SALE

MLN8237 (Alisertib)

Aurora A Kinase 抑制剂
MLN8237 (Alisertib) 是一种选择性Aurora A抑制剂,无细胞试验中IC50为1.2 nM,作用于Aurora A比作用于Aurora B选择性强200倍以上。Phase 3。
A10448 SALE

Hesperadin

Aurora B Kinase 抑制剂
Hesperadin is a human Aurora B inhibitor with an IC50 of 40 nM for the prevention of the phosphorylation of substrate. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
A10109 SALE

AZD1152-HQPA (Barasertib)

Aurora Kinase B 抑制剂
AZD 1152-HQPA is a highly potent and selective inhibitor of Aurora B, with Ki values to be 0.36 (Aurora B) and 1369 nM (Aurora A) respectively and has a high specificity versus a panel of 50 other kinases.
A10981 SALE

VX-680 (MK-0457, Tozasertib)

Aurora Kinase 抑制剂
VX-680 is a potent and selective small-molecule inhibitor of the Aurora kinases.
A10715 SALE

Danusertib (PHA-739358)

Aurora 抑制剂
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
A10601 SALE

MLN8054

Aurora A 抑制剂
MLN8054 is an inhibitor of Aurora A kinase, induces senescence in human tumor cells both in vitro and in vivo.
A10494

JNJ-7706621

CDK/Aurora A/B 抑制剂
JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
A10352 SALE

ENMD-2076

Aurora A / FLT3 抑制剂
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
A10508 SALE

KW-2449

FLT3/FGFR/Bcr-Abl/Aurora 抑制剂
KW-2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase.
A11066

AMG 900

Aurora Kinase 抑制剂
AMG 900 is a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines.
A11067 SALE

TAK-901

Aurora Kinase A/B 抑制剂
TAK-901 is a novel inhibitor of Aurora A/B with IC50 of 21 nM/15 nM. It is not a potent inhibitor of cellular JAK2, c-Src or Abl. Phase 1.
A11081

CCT137690

Aurora Kinase 抑制剂
CCT137690 is a highly selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 15 nM, 25 nM and 19 nM. It has little effect on hERG ion-channel.
A10100

Aurora A Inhibitor I

Aurora A 抑制剂

Aurora A Inhibitor I is a potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 3.4 nM (Aurora A) and unusually high selectivity 1000 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.

A10184

CCT129202

Aurora 抑制剂

CCT129202 is a representative of a structurally novel series of imidazopyridine small-molecule inhibitors of Aurora kinase activity. It shows high selectivity for the Aurora kinases over a panel of other kinases tested and inhibits proliferation in multiple cultured human tumor cell lines.

A11168 SALE

GSK1070916

Aurora Kinase B/C 抑制剂

GSK1070916 is a potent Aurora B/C kinase inhibitor (with IC50 of 3.5 nM/6.5 nM) with broad antitumor activity in tissue culture cells and human tumor xenograft models.

A11171

PF-03814735

Aurora A/B Kinase 抑制剂
PF-03814735 is a novel, potent and reversible inhibitor of Aurora A/B with IC50of 0.8 nM/5 nM, is less potent to Flt3, FAK, TrkA, and minimally active to Met and FGFR1. Phase 1.
A10714 SALE

PHA-680632

Aurora 抑制剂
PHA-680632 is potent inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 27 nM, 135 nM and 120 nM, respectively. It has 10- to 200-fold higher IC50 for FGFR1, FLT3, LCK, PLK1, STLK2, and VEGFR2/3.
A11410 SALE

MK-5108 (VX-689)

Aurora A Kinase 抑制剂
MK-5108, also known as VX-689, is a competitive inhibitor of the ATP-binding site of aurora A kinase.
A10851

SNS-314

Aurora 抑制剂
SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.
A11009 SALE

ZM-447439

Aurora Kinase 抑制剂
ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
A10248 SALE

CYC116 (CYC-116)

Aurora Kinase 抑制剂
Aurora kinase/VEGFR 2 inhibitor CYC116 inhibits Aurora kinases A and B and vascular endothelial growth factor receptor 2 (VEGFR2), resulting in disruption of the cell cycle, rapid cell death, and the inhibition of angiogenesis.
A13250 SALE

Reversine

human A3 adenosine receptor 拮抗剂 /Aurora 抑制剂
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
A13396 SALE

MK-8745

Aurora Kinase A 抑制剂
MK-8745 is a novel Aurora-A specific inhibitor. It induces apoptotic cell death in a p53-dependent manner when tested in vitro in cell lines of multiple lineages.
A14382

SAR156497

Aurora Kinase 抑制剂
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition.
A15011

AZD1152

Aurora B 抑制剂
AZD1152 is a pro-drug that rapidly undergoes phosphatase-mediated cleavage in serum to release barasertib-hQPA, a selective Aurora B kinase inhibitor that has shown preliminary activity in clinical studies of patients with acute myeloid leukemia (AML).
A15762

BI-847325

MEK/Aurora 抑制剂
BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.
A13069 SALE

XL-228

IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂
XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
A13567

TC-A-2317 HCl

Aurora kinase A 抑制剂
TC-A-2317 hydrochloride is a potent Aurora kinase A inhibitor (Ki = 1.2 nM compared to 101 nM for inhibition of Aurora kinase B). Selective over 60 other kinases (IC50 values > 1000 nM). Exhibits good cell permeability and antitumor activity.
A14059

SCH-1473759

Aurora A/B 抑制剂
SCH-1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively.
A15970

HOI-07

Aurora B 抑制剂
HOI-07 is a potently Aurora B kinase inhibitor.
A10862 SALE

SRT1720 HCl

SIRT1 Activator
SRT1720 is an inhibitor developed intended as a small-molecule activator of the sirtuin subtype SIRT1.
A10377 SALE

EX 527 (Selisistat)

SIRT1 抑制剂
EX 527 is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor with IC50 of 38 nM in a cell-free assay.
A12904

AK-7

SIRT2 抑制剂
AK-7 is a cell- and brain-permeable inhibitor of SIRT2 (IC50 = 15.5 μM).
A12527

Inauhzin

SIRT1 抑制剂
Inauhzin is a potent SIRT inhibitor, which effectively reactivates p53 by inhibiting SIRT1 activity, promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress.
A14188

SRT2104 (GSK2245840)

SIRT1 activator
SRT2104 (GSK2245840) is a selective SIRT1 activator involved in the regulation of energy homeostasis. Phase 2.
A14225 SALE

AGK2

SIRT2 抑制剂
AGK2 is a potent, and selective SIRT2 inhibitor with IC50 of 3.5 μM.
A14370

AK-1

SIRT2 抑制剂
AK-1 inhibits SIRT2 selectively over SIRT1 and SIRT3.
A15247

SRT 1720

SIRT1 Activator
SRT 1720 is a selective activator of human SIRT1 (EC1.5 = 0.16 μM) versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5 = 37 uM??SIRT3: EC1.5 > 300 uM).
A15902 SALE

SirReal2

Selective SIRT2 抑制剂
SirReal2 is a potent and selective Sirt2 inhibitor with IC50 of 140 nM.
A12226 SALE

Sirtinol

sirtuin 抑制剂
Sirtinol is a cell-permeable, specific inhibitor of sirtuin NAD-dependant histone deacetylases. It is a specific SIRT1 and SIRT2 inhibitor with IC50 of 131 μM and 38 μM in cell-free assays, respectively.
A10388 SALE

Fisetin (Fustel)

-
Fisetin is a flavonol, a structurally distinct chemical substance that belongs to the flavonoid group of polyphenols. It can be found in many plants, where it serves as a colouring agent. Possible anti-aging, anti-inflammatory, anti-cancer, and anti-viral properties of fisetin are under active scientific investigation.
A11783 SALE

GSK 1210151A (I-BET151)

BET Bromodomain 抑制剂
GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.
A12545 SALE

PFI-1

BET 抑制剂
PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.
A11440 SALE

GSK 525762A (I-BET-762)

BET 抑制剂
GSK-525762A is a small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family
A13068

CPI-203

BET bromodomain 抑制剂
CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).
A13163 SALE

Bromosporine

bromodomain 抑制剂
Bromosporine is a broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.
A13717

UNC 669

L3MBTL 抑制剂
UNC669 is a small-molecule antagonist of methyl-lysine (KMe) reader protein with selectivity for L3MBTL1 and L3MBTL3 (IC50 of 4.2μM and 3.1μM respectively)
A12729 SALE

(+)-JQ1

BET 抑制剂
(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.
A13227

SGC-CBP30

CBP/p300 bromodomain 抑制剂
SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
A13890 SALE

OTX015

BET 抑制剂
OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).

产品 151 到 200 共 312个

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