PI3K/Akt/mTOR
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S6571
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BQR695
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Aug 28 2019
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S6574
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KDU691
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Aug 28 2019
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S6504
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BX517
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Jul 31 2019
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S6516
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GNE-477
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Jul 24 2019
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S8693
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Selective PI3Kδ Inhibitor 1 (compound 7n)
|
Selective PI3Kδ Inhibitor 1 (compound 7n) is an inhibitor of PI3Kδ with an IC50 of 0.9 nM and >1000-fold selectivity against other class I PI3K isoforms [PI3K α/γ/β=3670/1460/21300 nM].
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Jun 24 2019
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S6414
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Apilimod
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Apilimod is a cell permeable small molecule that specifically inhibits PIKfyve with an IC50 of 14 nM in an in vitro kinase assay. It is also an inhibitor of IL-12/23 and shows no activity toward other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K isoforms.
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Apr 30 2019
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S5818
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acalisib (GS-9820)
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acalisib (GS-9820) is a highly selective and potent p110δ inhibitor (IC50 = 14 nM) with 114- to 400-fold selectivity over the other class I PI3K enzymes and no activity against Class II and III PI3K family members or other PI3K-related proteins including mTOR and DNA-PK.
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Feb 20 2019
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S8803
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MK-3903
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MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.
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Feb 14 2019
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S8654
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ex229 (compound 991)
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EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.
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Jan 09 2019
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S8752
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leniolisib(CDZ 173)
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Leniolisib(CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.
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Jan 09 2019
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JAK/STAT
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S8162
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Upadacitinib (ABT-494)
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Aug 21 2019
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S6524
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NSC 42834
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Jul 31 2019
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S6521
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WHI-P258
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Jul 24 2019
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S8684
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Selective JAK3 inhibitor 1
|
Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.
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Jun 11 2019
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S8804
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PF-06700841
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PF-06700841 is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.
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May 08 2019
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S8765
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PF-04965842
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PF-04965842 is a potent JAK1 inhibitor with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM for JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2, respectively.
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Mar 06 2019
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S5917
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Solcitinib
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Solcitinib is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.
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Jan 23 2019
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S5903
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JANEX-1
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JANEX-1 is a small molecule inhibitor of JAK3 that selectively inhibits JAK3 at an IC50 of 78 µM without altering the activity of JAK1 or JAK2, or any other protein tyrosine kinases (IC50 ≥ 350 µM).
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Jan 16 2019
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S5902
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1,2,3,4,5,6-Hexabromocyclohexane
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1,2,3,4,5,6-Hexabromocyclohexane is a potent inhibitor of JAK2 tyrosine kinase autophosphorylation with IC50 value to be estimated in low micromolar range.
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Jan 16 2019
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S5904
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WHI-P97
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WHI-P97 is a potent inhibitor of JAK-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays.
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Jan 09 2019
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DNA Damage
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S6506
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Compound 401
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Jul 31 2019
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S6359
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Purine
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Purine is a heterocyclic aromatic organic compound which plays crucial roles in DNA and RNA. It is also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A.
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May 16 2019
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S6077
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Cytidine 5′-triphosphate (disodium salt)
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Cytidine 5'-triphosphate is a pyrimidine nucleoside triphosphate that is involved in a variety of biochemical reactions. It is used in the synthesis of RNA by RNA polymerases.
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Apr 03 2019
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S5840
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Palifosfamide
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Palifosfamide is a novel DNA alkylator and the active metabolite of ifosfamide with potential antineoplastic activity.
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Feb 20 2019
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S9451
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Uridine 5'-monophosphate
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Uridine 5'-monophosphate is a nucleotide that is used as a monomer in RNA.
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Dec 12 2018
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S8556
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AZ31
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AZ31 is a selective and novel ATM inhibitor with an IC50 of <0.0012 μM. It shows excellent selectivity over closely related enzymes (>500 fold selective over DNA-PK and PI3Kα and >1000 fold selective over mTOR, PI3Kβ and PI3Kγ).
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Dec 06 2018
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S5627
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Amsacrine hydrochloride
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Amsacrine hydrochloride is the hydrochloride salt form of amsacrine, which is an inhibitor of topoisomerase II with antineoplastic activity.
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Dec 06 2018
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S9321
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Topotecan
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Topotecan is an antineoplastic agent used to treat ovarian cancer that works by inhibiting DNA topoisomerases.
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Nov 16 2018
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S9360
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4-Hydroxyquinazoline
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4-Hydroxyquinazoline is a PARP inhibitor with a high potency for PARP-1 and no effects on enzymes other than PARP.
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Nov 16 2018
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S8729
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AZ32
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AZ32 is a specific inhibitor of the ATM kinase that possesses good BBB penetration in mouse with an IC50 value of <0.0062 μM for ATM enzyme. It shows adequate selectivity over ATR and also has high cell permeability.
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Oct 18 2018
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TGF-beta/Smad
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S8868
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NG25
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Oct 10 2019
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S8772
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LY 3200882
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LY 3200882 is a potent, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). It potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells and in vivo in subcutaneous tumors in a dose dependent fashion.
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Jan 09 2019
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S1292
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Chelerythrine Chloride
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Chelerythrine is a potent, selective antagonist of PKC with IC50 of 0.66 mM.
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Oct 26 2018
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S7959
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SIS3 HCl
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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.
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Oct 20 2016
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S7663
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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.
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Oct 10 2016
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S7627
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LDN-214117
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LDN-214117 is a potent and selective BMP type I receptor kinase ALK2 inhibitor with IC50 of 24 nM.
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Apr 30 2015
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S7624
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SD-208
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SD-208 is a selective TGF-βRI (ALK5) inhibitor with IC50 of 48 nM, >100-fold selectivity over TGF-βRII.
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Feb 02 2015
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S7658
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Kartogenin
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Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes.
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Nov 27 2014
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S7530
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Vactosertib (TEW-7197)
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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.
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Nov 27 2014
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S1421
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Staurosporine
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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.
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Aug 13 2014
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GPCR & G Protein
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S6565
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JK184
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Aug 28 2019
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S6512
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Defensamide (MHP)
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Jul 31 2019
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S6418
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PF 429242
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PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).
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Apr 30 2019
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S5819
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MRE-269(ACT-333679)
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MRE-269(ACT-333679) is a prostaglandin I2 (IP) receptor agonist with a binding affinity for the human IP receptor that is 130-fold greater than that for other human prostanoid receptor.
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Jan 29 2019
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S9327
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Carboprost
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Carboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties.
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Dec 07 2018
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S5753
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Setipiprant(ACT-129968, KYTH-105)
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Setipiprant(ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1.
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Nov 01 2018
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S5358
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Regadenoson
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Regadenoson is a selective A2A adenosine receptor agonist with coronary vasodilating activity.
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Aug 10 2018
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S5413
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Ertugliflozin
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Ertugliflozin is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.
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Aug 10 2018
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S3003
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Prostaglandin E2 (PGE2)
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Prostaglandin E2 palys important effects in labour (softens cervix and causes uterine contraction) and also stimulates osteoblasts to release factors that stimulate bone resorption by osteoclasts.
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Aug 09 2018
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S8694
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CID16020046 (CID 16020046)
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CID16020046 is a selective GPR55 antagonist, inhibiting GPR55 constitutive activity with IC50 of 0.15 μM in yeast. It demonstrates weak activity against a broad spectrum of other GPCRs, ion channels, kinases, and nuclear receptor.
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Aug 09 2018
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Epigenetics
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S8297
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ARV-825
|
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Aug 08 2019
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S6497
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SMI-16a
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Jul 31 2019
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S8743
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SKLB-23bb
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SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.
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Jul 09 2019
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S8438
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T-3775440 HCl
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T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.
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Jul 09 2019
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S8769
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Tinostamustine(EDO-S101)
|
Tinostamustine(EDO-S101) is a first-in-class alkylating deacetylase inhibitor with IC50 values of 9 nM, 9 nM, 25 nM and 107 nM for HDAC1, HDAC2, HDAC3 and HDAC8 (Class 1 HDACs) respectively and 6 nM, 72 nM for HDAC6 and HDAC10 (Class II HDACs).
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Jun 26 2019
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S8846
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compound 3i (666-15)
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Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
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Jun 26 2019
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S8739
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PLX51107
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PLX51107 is as a novel BET inhibitor with modest preference for bromodomain-1 (BD1) versus bromodomain-2 (BD2) within each BET protein (Kd = 1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively. Among non-BET proteins, PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range).
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Apr 24 2019
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S8296
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dBET1
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dBET1 is a CRBN-based BET degrader with an IC50 of 20 nM, showing highly selectivity. Out of 7,429 proteins, only the expression of the oncoproteins MYC and PIM1, as well as BRD2, BRD3 and BRD4 are significantly downregulated by dBET1 treatment.
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Apr 11 2019
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S8753
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INCB054329（INCB-054329; INCB-54329）
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INCB054329(INCB-054329; INCB-54329) is a structurally distinct bromodomain and extraterminal domain (BET) inhibitor with IC50 values of 44 nM, 5 nM, 9 nM, 1 nM, 28 nM, 3 nM, 119 nM and 63 nM for BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, BRD4-BD2, BRDT-BD1 and BRDT-BD2, respectively.
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Apr 03 2019
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S8762
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dBET6
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dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.
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Mar 27 2019
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NF-κB
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S8642
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GSK'963
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GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
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Jul 03 2018
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S3633
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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.
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Nov 15 2017
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S8261
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GSK583
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GSK583 is a highly potent and selective inhibitor of RIP2 kinase with an IC50 of 5 nM.
|
Feb 09 2017
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S4712
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Diethylmaleate
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Diethylmaleate is the diethyl ester of maleic acid and a glutathione-depleting compound that inhibits NF-kB.
|
Oct 26 2016
|
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S7948
|
MRT67307 HCl
|
MRT67307 is a potent and dual IKKϵ and TBK1 inhibitor with IC50 of 160 and 19 nM, respectively.
|
Apr 25 2016
|
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S7691
|
PS-1145
|
PS-1145 is a specific IKK inhibitor with IC50 of 88 nM.
|
Mar 09 2016
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S7851
|
AZD3264
|
AZD3264 is a novel IKK2 inhibitor.
|
Nov 27 2015
|
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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
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S7441
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WS3
|
WS3 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
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Dec 04 2014
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S7442
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WS6
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WS6 is a β cell proliferation inducer via modulation of Erb3 binding protein-1 (EBP1) and the IκB kinase pathway.
|
Nov 12 2014
|
Proteases
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
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S6417
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GK921
|
GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition.
|
Apr 30 2019
|
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S8778
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UPGL00004
|
UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.
|
Mar 14 2019
|
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S4956
|
Benzamidine HCl
|
Benzamidine is an inhibitor of serine proteases with Ki values of 35, 350, and 220 µM for trypsin, plasmin, and thrombin, respectively.
|
Jan 16 2019
|
|
S4997
|
4-Butylresorcinol
|
4-Butylresorcinol is a potent inhibitor of tyrosinase and is used in cosmetics as a depigmenting agent.
|
Nov 28 2018
|
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S5720
|
Glecaprevir
|
Glecaprevir is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a.
|
Oct 18 2018
|
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S5652
|
Elbasvir
|
Elbasvir is an NS5A inhibitor, preventing hepatitis C viral RNA replication and virion assembly. Median EC50 values range from 0.2 to 3600 pmol/L, based on genotype.
|
Sep 11 2018
|
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S5365
|
Alogliptin
|
Alogliptin is a potent, selective inhibitor of the serine protease dipeptidyl peptidase IV (DPP-4)with IC50 values of 2.63 nM and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9.
|
Aug 15 2018
|
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S5543
|
1, 10-Phenanthroline monohydrate
|
1,10-Phenanthroline is a classic chelating bidentate ligand for transition metal ions that has played an important role in the development of coordination chemistry. It is an inhibitor of metallopeptidases.
|
Jul 27 2018
|
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S5250
|
Darunavir
|
Darunavir is a nonpeptidic HIV protease inhibitor, used to treat HIV infection.
|
Jul 04 2018
|
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S5402
|
Dasabuvir(ABT-333)
|
Dasabuvir(ABT-333) is a non-nucleoside inhibitor of NS5B viral RNA-dependent RNA polymerase that inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates with IC50 values between 2.2 and 10.7 nM. It is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases.
|
Jun 24 2018
|
MAPK
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
|
S6502
|
SD 0006
|
|
Aug 08 2019
|
|
S6538
|
B-Raf IN 1
|
|
Aug 08 2019
|
|
S8801
|
CC-90003
|
CC-90003 is an irreversible inhibitor of ERK1/2 with IC50s in the 10-20 nM range and shows good kinase selectivity in a 258-kinase biochemical assay.
|
Jan 09 2019
|
|
S8701
|
MK-8353 (SCH900353)
|
MK-8353 (SCH900353) is an orally bioavailable, selective, and potent ERK inhibitor that inhibits activated ERK1 and ERK2 in vitro, with IC50 values of 23.0 nM and 8.8 nM, respectively (IMAP kinase assay), and nonactivated ERK2, with an IC50 of 0.5 nM (MEK1-ERK2-coupled assay).
|
Dec 20 2018
|
|
S8708
|
AZD0364
|
AZD0364 is a pre-clinical ERK1/2 inhibitor with an IC50 of 0.6 nM for ERK2.
|
Dec 20 2018
|
|
S7965
|
PLX8394
|
PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
|
Nov 22 2018
|
|
S8745
|
LXH254
|
LXH254 is a type II ATP-competitive inhibitor that inhibits both B- and CRAF kinase activities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays.
|
Oct 10 2018
|
|
S5069
|
Dabrafenib Mesylate
|
Dabrafenib Mesylate is the mesylate salt form of dabrafenib, an orally bioavailable inhibitor of B-raf (BRAF) protein with IC50s of 0.8 nM, 3.2 nM and 5 nM for B-Raf (V600E), B-Raf (WT) and C-Raf, respectively.
|
Jul 12 2018
|
|
S8690
|
RAF709
|
RAF709 is a potent inhibitor of B/C RAF kinase with almost equivalent IC50 values of 0.4 nM for B-RAF and C-RAF, showing a high level of selectivity, demonstrating greater than 99% on-target binding to BRAF, BRAFV600E, and CRAF at 1 μM and very few off-targets with DDR1 (>99%), DDR2 (86%), FRK (92%), and PDGFRb (96%), the only kinases with binding >80% at 1 μM.
|
May 22 2018
|
|
S8534
|
LY3214996
|
LY3214996 is a selective and novel ERK1/2 inhibitor with IC50 of 5 nM for both enzymes in biochemical assays. It potently inhibits cellular phospho-RSK1 in BRAF and RAS mutant cancer cell lines.
|
Nov 02 2017
|
Stem Cells & Wnt
| 製品コード |
製品名称 |
製品説明 |
添加時期 |
|
S8704
|
iCRT14
|
iCRT14 is a β-catenin/Tcf inhibitor with a Ki value of 54 ± 5.2 μM in homogeneous fluorescence polarization (FP) assay.
|
Jul 09 2019
|
|
S5815
|
WAY-316606
|
WAY-316606, a specific antagonist of SFRP1, functions as an activator of canonical Wnt/β-catenin signalling in the human hair bulb.
|
Feb 20 2019
|
|
S8761
|
Adavivint (SM04690)
|
SM04690 is a potent and specific inhibitor of canonical Wnt signaling with an EC50 of 19.5 nM for inhibiting the TCF/LEF reporter. It is ∼150- to 500-fold more potent than the other known Wnt inhibitors across multiple cellular assays.
|
Jan 23 2019
|
|
S5439
|
5-Bromoindole
|
5-bromoindole is an important pharmaceutical chemical intermediate and a potential inhibitor of glycogen synthase kinase 3 (GSK-3).
|
Jul 12 2018
|
|
S8645
|
IWP-O1
|
IWP-O1 is a porcn inhibitor with an EC50 value of 80 pM in a cultured cell reporter assay of Wnt signaling and effectively suppresses the phosphorylation of Dvl2/3 in HeLa cells.
|
Jun 01 2018
|
|
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
|
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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
|
|
S8644
|
GNF-6231
|
GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.
|
Dec 05 2017
|
|
S8554
|
Super-TDU
|
Super-TDU is an inhibitory peptide targeting YAP-TEADs interaction.
|
Sep 19 2017
|
|
S8572
|
Amcasertib (BBI503)
|
Amcasertib (BBI503), a first-in-class cancer stemness kinase inhibitor, is claimed to inhibit Nanog and other CSC pathways by targeting kinases with potential anticancer activity.
|
Aug 01 2017
|
