JAK/STAT
| Catalog No. |
Product Name |
Information |
Added |
|
S8538
|
PF-06651600
|
PF-06651600 is a potent and irreversible JAK3-selective inhibitor with an IC50 of 33.1 nM but without activity (IC50 > 10 000 nM) against JAK1, JAK2, and TYK2.
|
Mar 28 2018
|
|
S8605
|
C188-9
|
C188-9 is a potent inhibitor of STAT3 that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors.
|
Jan 10 2018
|
|
S8541
|
FM-381
|
FM-381 is a JAK3 specific reversible covalent inhibitor with IC50 of 127 pM for JAK3 and demonstrates 400-, 2,700- and 3,600-fold selectivity over JAK1, JAK2, and TYK2, respectively.
|
Dec 27 2017
|
|
A5042
|
STAT5a Rabbit Recombinant mAb
|
|
Oct 10 2017
|
|
A5044
|
STAT2 Rabbit Recombinant mAb
|
|
Oct 10 2017
|
|
A5045
|
STAT4 Rabbit Recombinant mAb
|
|
Oct 10 2017
|
|
A5003
|
STAT5b Rabbit Recombinant mAb
|
|
Oct 09 2017
|
|
A5020
|
STAT5A/B Rabbit Recombinant mAb
|
|
Oct 09 2017
|
|
A5024
|
JAK2 Rabbit Recombinant mAb
|
|
Oct 09 2017
|
|
S8561
|
HJC0152
|
HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.
|
Sep 19 2017
|
Cell Cycle
| Catalog No. |
Product Name |
Information |
Added |
|
S8699
|
SNS-314
|
SNS-314 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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
|
Apr 18 2018 |
|
S8652
|
Skp2 inhibitor C1 (SKPin C1)
|
Skp2 inhibitor C1 (SKPin C1) is a specific and selective small-molecule inhibitor of Skp2-mediated p27 degradation by reducing p27 binding through key compound-receptor contacts.
|
Apr 18 2018 |
|
A5268
|
p57 Kip2 Rabbit Recombinant mAb
|
|
Dec 21 2017 |
|
A5276
|
Chk2 Rabbit Recombinant mAb
|
|
Dec 21 2017 |
|
A5305
|
SOS1 Rabbit Recombinant mAb
|
|
Dec 21 2017 |
|
S2284
|
Colchicine
|
Colchicine is a microtubule polymerization inhibitor with an IC50 of 3 nM.
|
Dec 04 2017 |
|
S8469
|
CCG-203971
|
CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.
|
Nov 22 2017 |
|
S8632
|
Chk2 Inhibitor II (BML-277)
|
Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases.
|
Nov 02 2017 |
|
A5035
|
Cyclin D1 Rabbit Recombinant mAb
|
|
Oct 10 2017 |
|
A5004
|
Chk1 Rabbit Recombinant mAb
|
|
Oct 09 2017 |
TGF-beta/smad
| Catalog No. |
Product Name |
Information |
Added |
|
S7959
|
SIS3 HCl
|
SIS3, a novel specific inhibitor of Smad3, inhibits TGF-β and activin signaling by suppressing Smad3 phosphorylation without affecting the MAPK/p38, ERK, or PI3-kinase signaling pathways.
|
Oct 20 2016
|
|
S7663
|
Ruboxistaurin (LY333531 HCl)
|
LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.
|
Oct 10 2016
|
|
S7627
|
LDN-214117
|
LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
|
Apr 30 2015
|
|
S7624
|
SD-208
|
SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
|
Feb 02 2015
|
|
S7658
|
Kartogenin
|
Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
|
Nov 27 2014
|
|
S7530
|
Vactosertib (TEW-7197)
|
Vactosertib (TEW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
|
Nov 27 2014
|
|
S7119
|
Go6976
|
Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
|
Sep 15 2014
|
|
S1421
|
Staurosporine
|
Staurosporine is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
|
Aug 13 2014
|
|
S7146
|
DMH1
|
DMH1 is a selective BMP receptor inhibitor with IC50 of 107.9 nM for ALK2, exhibiting no inhibition on AMPK, ALK5, KDR (VEGFR-2) or PDGFR.
|
May 20 2014
|
|
S7147
|
LDN-212854
|
LDN-212854 is a potent and selective BMP receptor inhibitor with IC50 of 1.3 nM for ALK2, about 2-, 66-, 1641-, and 7135-fold selectivity over ALK1, ALK3, ALK4, and ALK5, respectively.
|
May 20 2014
|
GPCR & G Protein
| Catalog No. |
Product Name |
Information |
Added |
|
S4932
|
Proxyphylline
|
Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets).
|
Apr 18 2018
|
|
S3988
|
Theophylline-7-acetic acid
|
Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.
|
Apr 12 2018
|
|
A5270
|
GRK2 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
S3734
|
Albiglutide
|
Albiglutide is a glucagon-like peptide-1 agonist (GLP-1 agonist).
|
Dec 19 2017
|
|
S8575
|
A2AR antagonist 1
|
A2AR antagonist 1 is a potent A2AR (Adenosine A2A Receptor) antagonist with Ki values of 4 nM and 264 nM for A2AR and A1R, respectively.
|
Nov 15 2017
|
|
S8637
|
Ipragliflozin (ASP1941)
|
Ipragliflozin (ASP1941) is a highly selective sodium-glucose cotransporter 2 (SGLT2) inhibitor with an IC50 value of 7.4 nM for hSGLT2 and a 254-fold selectivity versus SGLT1.
|
Oct 24 2017
|
|
S2879
|
AMD3465 hexahydrobromide
|
AMD3465 is a monomacrocyclic CXCR4 antagonist.
|
Sep 06 2017
|
|
S8558
|
Tofogliflozin(CSG 452)
|
Tofogliflozin is a novel sodium-glucose co-transporter 2(SGLT2) inhibitor with IC50 values of 2.9 nM and 8444 nM for hSGLT2 and Hsglt1, respectively.
|
Aug 29 2017
|
|
S8517
|
Lixisenatide
|
Lixisenatide is a once-daily short-acting glucagon-like peptide-1 (GLP-1) receptor agonist (GLP-1RA) with an IC50 of 1.4 nM for the human GLP-1 receptor in receptor binding studies.
|
Jul 11 2017
|
|
S8415
|
PACAP 1-38
|
PACAP 1-38 is a highly potent PACAP receptor agonist (Kd = 100 pM). It stimulates adenylate cyclase and phagocytosis.
|
Mar 31 2017
|
PTK
| Catalog No. |
Product Name |
Information |
Added |
|
S8675
|
H3B-6527
|
H3B-6527 is a highly selective covalent FGFR4 inhibitor with an IC50 value of <1.2 nM and at least 250-fold selectivity over FGFR1-3 (IC50 values of 320, 1,290 and 1,060 nM respectively).
|
Feb 28 2018
|
|
S7674
|
Savolitinib(AZD6094, HMPL-504)
|
Savolitinib (volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase.
|
Feb 28 2018
|
|
S3759
|
Norcantharidin
|
Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.
|
Feb 07 2018
|
|
S8553
|
Avapritinib (BLU-285)
|
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous KIT mutation, D816V in KIT Exon 17 (IC50 = 0.5 nM).
|
Oct 24 2017
|
|
S7754
|
Gilteritinib (ASP2215)
|
Gilteritinib(ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
|
Oct 17 2017
|
|
A5006
|
Met (c-Met) Rabbit Recombinant mAb
|
|
Oct 09 2017
|
|
S8511
|
Belizatinib (TSR-011)
|
"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C).
"
|
Sep 19 2017
|
|
S8407
|
PF-06273340
|
PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
|
Aug 29 2017
|
|
S8583
|
TPX-0005
|
TPX-0005 is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
|
Aug 01 2017
|
|
S8573
|
Sitravatinib (MGCD516)
|
Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.
|
Jul 26 2017
|
Epigenetics
| Catalog No. |
Product Name |
Information |
Added |
|
S8607
|
JQ-EZ-05 (JQEZ5)
|
JQ-EZ-05 is a specific and reversible EZH1/2 inhibitor.
|
Apr 12 2018
|
|
S7230
|
UNC0642
|
UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
|
Apr 03 2018
|
|
S8479
|
LLY-283
|
LLY-283 is the potent and selective SAM-competitive chemical probe for PRMT5. It inhibits PRMT5 enzyme activity with IC50 of 20 nM for methylation of an H4R3 derived peptide substrate, and shows greater than 100-fold selectivity over other histone methyltransferases and non-epigenetic targets.
|
Mar 28 2018
|
|
S8627
|
OSS_128167
|
OSS_128167 is a specific SIRT6 inhibitor with IC50 values of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
|
Feb 28 2018
|
|
S8495
|
WT161
|
WT161 is a potent, selective, and bioavailable HDAC6 inhibitor with IC50 values of 0.4 nM, 8.35 nM and 15.4 nM for HDAC6, HDAC1 and HDAC2, respectively; shown to have >100-fold selectivity over other HDACs.
|
Feb 28 2018
|
|
S8071
|
UNC0638
|
UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.
|
Feb 08 2018
|
|
S3944
|
Valproic acid
|
Valproic acid is a fatty acid with anticonvulsant properties used in the treatment of epilepsy. It is also a histone deacetylase inhibitor and is under investigation for treatment of HIV and various cancers.
|
Jan 25 2018
|
|
S8664
|
GSK3326595 (EPZ015938)
|
GSK3326595 (EPZ015938) is an orally active, potent and selective inhibitor of protein arginine methyltransferase 5 (PRMT5) and potently inhibits tumor growth in vitro and in vivo in animal models.
|
Jan 03 2018
|
|
A5240
|
ASH2L Rabbit Recombinant mAb
|
WBELISA
|
Dec 21 2017
|
|
A5247
|
PRMT5 Rabbit Recombinant mAb
|
WBELISA
|
Dec 21 2017
|
NF-κB
| Catalog No. |
Product Name |
Information |
Added |
|
S3633
|
Pyrrolidinedithiocarbamate ammonium
|
Ammonium pyrrolidine dithiocarbamate (PDTC) is a potent nuclear factor-κB (NF-κB) inhibitor that inhibits IκB phosphorylation, blocks NF-κB translocation to the nucleus and reduces the expression of downstream cytokines.
|
Nov 15 2017
|
|
S8261
|
GSK583
|
GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM.
|
Feb 09 2017
|
|
S4712
|
Diethylmaleate
|
Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB.
|
Oct 26 2016
|
|
S7948
|
MRT67307 HCl
|
MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively.
|
Apr 25 2016
|
|
S7691
|
PS-1145
|
PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
|
Mar 09 2016
|
|
S7851
|
AZD3264
|
AZD3264 is a novel IKK2 inhibitor.
|
Nov 27 2015
|
|
S7672
|
Omaveloxolone (RTA-408)
|
Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
|
Sep 14 2015
|
|
S7697
|
LY2409881
|
LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases.
|
Apr 20 2015
|
|
S7441
|
WS3
|
WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
|
Dec 04 2014
|
|
S7442
|
WS6
|
WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
|
Nov 12 2014
|
Metabolism
| Catalog No. |
Product Name |
Information |
Added |
|
S4837
|
Ibudilast
|
Ibudilast is a relatively non-selective phosphodiesterase inhibitor with anti-inflammatory and neuroprotective activities.
|
Apr 18 2018
|
|
S4856
|
Iproniazid
|
Iproniazid is a non-selective, irreversible monoamine oxidase (MAO) inhibitor (MAOI) that is used as an antidepressive agent.
|
Apr 18 2018
|
|
S5014
|
Crisaborole (AN2728)
|
Crisaborole is a small-molecule, boron-based, selective PDE4 inhibitor and has broad-spectrum anti-inflammatory activity.
|
Apr 18 2018
|
|
S4930
|
Cetilistat
|
Cetilistat is a novel highly lipophilic benzoxazinone that inhibits gastrointestinal and pancreatic lipases. It shows a good safety and tolerability profile in vivo
|
Apr 12 2018
|
|
S8557
|
IDO inhibitor 1
|
IDO inhibitor 1 is a potent inhibitor of IDO (indoleamine-(2,3)-dioxygenase) with IC50 of 3 nM.
|
Mar 21 2018
|
|
S3945
|
L-Cycloserine
|
L-Cycloserine is a potent inhibitor of the sphingolipid pathway via inhibiting 3-ketodihydrosphingosine synthetase. It also inhibits HIV-1 cytopathic effects, replication, and infectivity.
|
Feb 07 2018
|
|
S5146
|
3-Methylpyrazole
|
3-Methylpyrazole (3-MP) is a weak or non-inhibitor of alcohol dehydrogenase.
|
Jan 16 2018
|
|
S8608
|
Adenosine Dialdehyde (ADOX)
|
Adenosine Dialdehyde (ADOX) is an adenosine analog and S-adenosylmethionine-dependent methyltransferase inhibitor with an IC50 of 40 nM.
|
Jan 10 2018
|
|
S8657
|
PF-06840003
|
PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor. Although it has moderate hIDO1 enzyme inhibition (IC50 0.41 μM), it is a highly efficient compound (LE 0.53, LipE 5.1), driven by its tight packing within the enzyme, as well as the high density of hydrogen bonds it forms with hIDO-1 despite its small size.
|
Jan 03 2018
|
|
A5229
|
LRP1 Rabbit Recombinant mAb
|
WBELISA
|
Dec 21 2017
|
Proteases
| Catalog No. |
Product Name |
Information |
Added |
|
S4935
|
Asunaprevir
|
Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
|
Apr 12 2018
|
|
S5015
|
Simeprevir
|
Simeprevir is a competitive, reversible, macrocyclic, noncovalent hepatitis C virus (HCV) NS3/4A protease inhibitor that acts directly against the hepatitis C virus. It has a medium inhibitory concentration (IC50) <13 nM for all HCV NS3/4A enzymes(genotypes 1a, 1b, 2, 4, 5, and 6), but has an IC50 value of 37 nM for genotype 3.
|
Apr 12 2018
|
|
A5284
|
Cathepsin L/V/K/H Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5287
|
Cathepsin B Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
S3733
|
Boceprevir
|
Boceprevir is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1.
|
Dec 05 2017
|
|
S3724
|
Velpatasvir
|
Velpatasvir is a second-generation NS5A inhibitor that inhibits hepatitis C viral replication through acting on the crucial "membranous web" that facilitates RNA replication.
|
Nov 29 2017
|
|
S3728
|
Grazoprevir
|
Grazoprevir anhydrous is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively.
|
Nov 23 2017
|
|
S3692
|
N-Ethylmaleimide (NEM)
|
N-Ethylmaleimide (NEM) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group.
|
Nov 15 2017
|
|
S8565
|
Omarigliptin (MK-3102)
|
Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
|
Jul 11 2017
|
|
S8457
|
UK-371804 HCl
|
UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
|
Mar 02 2017
|
Microbiology
| Catalog No. |
Product Name |
Information |
Added |
|
S4848
|
Dalbavancin
|
Dalbavancin is a lipoglycopeptide antibiotic that has bactericidal activity against Gram-positive bacteria including various staphylococci.
|
Apr 18 2018
|
|
S5012
|
Octenidine Dihydrochloride
|
Octenidine, a cationic surfactant, is active against gram-positive and gram-negative bacteria.
|
Apr 18 2018
|
|
S3999
|
α-santonin
|
α-santonin, a naturally occurring sesquiterpene lactone, is a potent antiparasitic agent.
|
Apr 12 2018
|
|
S4812
|
Ceftizoxime
|
Ceftizoxime is a semisynthetic cephalosporin antibiotic which can be administered intravenously or by suppository. It is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic gram-positive and gram-negative organisms.
|
Apr 12 2018
|
|
S4854
|
Bedaquiline fumarate
|
Bedaquiline fumarate, an oral diarylquinoline, is a bactericidal antimycobacterial drug. It is a proton-translocating ATP synthetase inhibitor.
|
Apr 12 2018
|
|
S5159
|
Doxycycline
|
Doxycycline is an antibiotic that is used in the treatment of a number of types of infections caused by bacteria and protozoa.
|
Apr 03 2018
|
|
S5164
|
Chlorotetracycline
|
Chlortetracycline is a tetracycline antibiotic and commonly used to treat conjunctivitis in cats.
|
Apr 03 2018
|
|
S4813
|
Cefuroxime axetil
|
Cefuroxime axetil, a prodrug of the cephalosporin cefuroxime, is a second generation oral cephalosporin antibiotic with in vitro antibacterial activity against several gram-positive and gram-negative organisms.
|
Apr 03 2018
|
|
S4844
|
Cefcapene Pivoxil Hydrochloride
|
Cefcapene Pivoxil is the pivalate ester prodrug form of cefcapene, a semi-synthetic third-generation cephalosporin with antibacterial activity.
|
Apr 03 2018
|
|
S5009
|
Brivudine
|
Brivudine is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. It is incorporated into the viral DNA and blocks the action of DNA polymerases, thus inhibiting viral replication.
|
Apr 03 2018
|
Apoptosis
| Catalog No. |
Product Name |
Information |
Added |
|
S8606
|
HDM201
|
HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs.
|
Apr 18 2018
|
|
S8650
|
BTSA1
|
BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.
|
Feb 28 2018
|
|
S8483
|
CBL0137 (CBL-0137)
|
CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).
|
Jan 16 2018
|
|
A5259
|
APAF1 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5262
|
Phospho-PAK1/2/3(S144/S141/S139) Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5264
|
Phospho-RSK1 (S380) Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5272
|
p73 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5273
|
STK3 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5293
|
Bid Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
S8580
|
COTI-2
|
COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.
|
Dec 19 2017
|
Angiogenesis
| Catalog No. |
Product Name |
Information |
Added |
|
A2006
|
Bevacizumab
|
Bevacizumab is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD.
|
Nov 16 2017
|
|
A2007
|
Trastuzumab
|
Trastuzumab is a humanized, recombinant monoclonal antibody that binds to the extracellular domain of HER2, MW:145.53 KD.
|
Nov 16 2017
|
|
A2008
|
Pertuzumab
|
Pertuzumab, a humanized monoclonal antibody and the first in the class of agents called the HER2 dimerization inhibitors, impairs the ability of HER2 to bind to other members of the HER family, MW: 148 KD.
|
Nov 16 2017
|
|
S8230
|
Ensartinib (X-396)
|
Ensartinib (X-396) is a novel, potent and specific ALK TKI with the IC50 less than 4 nM in Ambit assays.
|
Oct 09 2017
|
|
S8578
|
PRN1371
|
PRN1371 is an irreversible covalent FGFR1-4 kinase inhibitor, with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, 2, 3, 4 and CSF1R, respectively.
|
Sep 26 2017
|
|
S8441
|
LW 6
|
LW6 is a hypoxia-inducible factor 1(HIF) inhibitor which potently inhibits HIF-1α accumulation by degrading HIF-1α without affecting the HIF-1a mRNA levels during hypoxia. It inhibits hypoxia-induced HIF-1α transcription activity with IC50 of 2.64 μM in cell-based HRE-reporter gene assays.
|
Sep 19 2017
|
|
S8442
|
TAK-659
|
TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
|
Aug 08 2017
|
|
A2000
|
Cetuximab
|
Cetuximab, a novel molecular-targeted agent,is an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EGFR to block ligand stimulation. MW : 145.781 KD.
|
Jun 02 2017
|
|
S8229
|
Brigatinib (AP26113)
|
Brigatinib (AP26113) is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits ROS1, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
|
May 10 2017
|
|
S8523
|
GSK2256098
|
GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM.
|
Apr 27 2017
|
Stem Cell & Wnt
| Catalog No. |
Product Name |
Information |
Added |
|
S8661
|
CA3
|
CA3 has potent inhibitory effects on YAP1/Tead transcriptional activity and primarily targets YAP1 high and therapy-resistant esophageal adenocarcinoma cells endowed with CSC properties.
|
Mar 15 2018
|
|
S7160
|
Glasdegib (PF-04449913)
|
Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
|
Mar 07 2018
|
|
S8647
|
iCRT3
|
iCRT3 is an antagonist of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays.
|
Jan 10 2018
|
|
A5254
|
YAP1 Rabbit Recombinant mAb
|
WBELISA
|
Dec 21 2017
|
|
A5298
|
ADAM10 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
S8597
|
LYN-1604
|
LYN-1604 is a potential ULK1 agonist with IC50 of 1.66 μM against MDA-MB-231 cells and it binds to wild-type ULK1 with a binding affinity in the nanomole range (Kd=291.4 nM). The ULK1 (Y89A) mutant protein caused a sharp decrease in binding affinity with lower response and Kd than wild-type ULK1, ULK1 (K50A) and ULK1 (L53A) mutants.
|
Dec 05 2017
|
|
S8644
|
GNF-6231
|
GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.
|
Dec 05 2017
|
|
A5038
|
Beta Catenin Rabbit Recombinant mAb
|
|
Oct 10 2017
|
|
A5007
|
GSK3 beta Rabbit Recombinant mAb
|
|
Oct 09 2017
|
|
S8554
|
Super-TDU
|
Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.
|
Sep 19 2017
|
Ubiquitin
| Catalog No. |
Product Name |
Information |
Added |
|
A5265
|
UBE2I Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5316
|
PIAS1/PIAS2/PIAS3 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5320
|
USP14 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
S7109
|
Pevonedistat (MLN4924)
|
MLN4924 is a small molecule inhibitor of Nedd8 activating enzyme (NAE) with IC50 of 4 nM.
|
Aug 31 2017
|
|
S8288
|
VLX1570
|
VLX1570 is a competitive inhibitor of proteasome DUB activity, with an IC50 of ~10 μM in vitro.
|
May 19 2017
|
|
S7892
|
Avadomide(CC-122)
|
Avadomide(CC-122), a new chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma(DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4CRBN.
|
Mar 31 2017
|
|
S4920
|
b-AP15
|
b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
|
Mar 30 2015
|
|
S7529
|
ML323
|
ML323 displays reversible, nanomolar inhibitory activity and excellent selectivity toward USP1/UAF1 with IC50 of 76 nM.
|
Jun 30 2014
|
|
S7142
|
NSC697923
|
NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
|
Apr 09 2014
|
|
S7285
|
NMS-873
|
NMS-873 is an allosteric and specific p97 inhibitor with IC50 of 30 nM that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM).
|
Jan 29 2014
|
Neuronal Signaling
| Catalog No. |
Product Name |
Information |
Added |
|
S4817
|
Atenolol
|
Atenolol is a selective β1 receptor antagonist with log Kd values of −6.66±0.05, −5.99±0.14, −4.11±0.07 for binding to the human β1-, β2- and β3-adrenoceptors.
|
Apr 12 2018
|
|
S4838
|
Acotiamide hydrochloride
|
Acotiamide Hydrochloride is the hydrochloride salt form of acotiamide, a prokinetic agent with gastrointestinal (GI) motility-enhancing activity. It is a new orally active selective acetylcholinesterase inhibitor.
|
Apr 12 2018
|
|
S8603
|
NGP 555
|
NGP 555 is a small-molecule modulator of γ-secretase and has been successful in achieving good oral absorption, brain penetration, CNS activity, and specificity for a lipid-based membrane target preclinically.
|
Apr 03 2018
|
|
S5131
|
Homotaurine
|
Homotaurine is a synthetic organic compound that has GABAergic activity by mimicking GABA. It is a GABAA partial agonist as well as a GABAB receptor partial agonist with low efficacy.
|
Mar 21 2018
|
|
S3643
|
Amitraz
|
Amitraz is a triazapentadiene, an α2 adrenergic agonist and a member of the amidine chemical family. It is a non-systemic acaricide and insecticide.
|
Dec 27 2017
|
|
S4760
|
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)
|
HP-β-cyclodextrin (HP-β-CD), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation.
|
Dec 27 2017
|
|
A5308
|
GDNF Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5315
|
EAAT2 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5317
|
Amyloid beta A4 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
|
A5319
|
NUR77 Rabbit Recombinant mAb
|
|
Dec 21 2017
|
Others
| Catalog No. |
Product Name |
Information |
Added |
|
S4836
|
Nilutamide
|
Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
|
Apr 18 2018
|
|
S4851
|
Tafluprost
|
HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs.
|
Apr 18 2018
|
|
S5006
|
Teprenone
|
Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis.
|
Apr 18 2018
|
|
S5013
|
Ioversol
|
Ioversol is an organoiodine compound used as a radiographic contrast agent.
|
Apr 18 2018
|
|
S4931
|
Propiverine hydrochloride
|
Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence.
|
Apr 18 2018
|
|
S4852
|
Gadopentetate Dimeglumine
|
Gadopentetate Dimeglumine, a complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid, is an extracellular intravenous contrast agent used in magnetic resonance imaging.
|
Apr 18 2018
|
|
S8692
|
Stenabolic (SR9009)
|
|
Apr 12 2018
|
|
S5007
|
Delamanid
|
Delamanid is a new anti-tuberculosis drug with an excellent intracellular bactericidal activity and a high accumulation rate.
|
Apr 12 2018
|
|
S4927
|
Cyclen
|
Cyclen is a macrocycle capable of selectively binding cations that used as a ligand in chemistry for instance with chemicals used in MRI contrast agents.
|
Apr 12 2018
|
|
S4928
|
Brivaracetam
|
Brivaracetam is a racetam derivative with anticonvulsant properties, usually used in the treatment of partial-onset seizures.
|
Apr 12 2018
|
