Search Result
Results for "
CK1 inhibitor
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114858
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Casein Kinase
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Cancer
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Epiblastin A is an ATP competitive casein kinase 1 (CK1) inhibitor with IC50s of 8.9, 0.5, and 4.7 µM for CK1α, CK1δ, and CK1 ɛ, respectively. Epiblastin A induces reprogramming of epiblast stem cells into embryonic stem cells by inhibition of CK1 .
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- HY-111820
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Casein Kinase
p38 MAPK
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Cardiovascular Disease
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CK1-IN-1 (Compound 1c) is a casein kinase 1 (CK1) inhibitor with IC50 values of 15 nM and 16 nM for CK1δ and CK1ε, respectively. CK1-IN-1 inhibits p38α MAPK with an IC50 of 73 nM. CK1-IN-1 can be used to study cardiomyogenesis .
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- HY-158975
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Casein Kinase
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Cancer
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VRK1/CK1-IN-1 (compound 36) is a dual inhibitor of vaccinia-related kinase 1 (VRK1) and casein kinase 1 (CK1), with the Ki of 37.9 nM for VRK1 and IC50s of 17 nM and 15 nM for δ and ε isoforms of CK1, respectively .
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- HY-153866
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Casein Kinase
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Cancer
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CK1-IN-2 (compound Nr.4) is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively .
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- HY-128433
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- HY-10324
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Casein Kinase I inhibitor
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Casein Kinase
Autophagy
Apoptosis
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Cancer
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D4476 is a potent, selective and cell-permeable inhibitor of casein kinase 1(CK1) with an IC50 value of 0.3 μM in vitro.
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- HY-103383
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CDK
Casein Kinase
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Neurological Disease
Cancer
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(R)-DRF053 dihydrochloride is a potent casein kinases 1 (CK1), CDK1/cyclin B and CDK5/p25 inhibitor with IC50s of 14 nM, 220 nM and 80 nM, respectively. (R)-DRF053 dihydrochloride prevents the CK1-dependent production of amyloid-beta in a cell model .
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- HY-12470
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Casein Kinase
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Others
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PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
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- HY-153866A
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Casein Kinase
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Cancer
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CK1-IN-2 (compound Nr.4) hydrochloride is a potent CK1 inhibitor with an IC50 values of 123, 19.8, 26.8, 74.3 nM for CK1a, CK1d, CK1e, p38a, respectively .
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- HY-162756
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Casein Kinase
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Neurological Disease
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CK1-IN-4 (Compound 59) is an inhibitor for casein kinase CK1δ with IC50 of 2.74 μM. CK1-IN-4 exhibits neuroprotective effect in Ethacrynic acid (HY-B1640)-treated SH-SY5Y cells .
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- HY-100114
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- HY-12774
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IC261
4 Publications Verification
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Casein Kinase
Apoptosis
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Cancer
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IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
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- HY-110052
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TBCA
1 Publications Verification
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Casein Kinase
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Cancer
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TBCA is a highly selective CK2 (casein kinase II) inhibitor with an IC50 of 110 nM and a Ki of 77 nM. TBCA shows selectivity for CK2 over CK1, DYRK1A and a panel of 27 other kinases .
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- HY-12470A
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Casein Kinase
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Cancer
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PF-4800567 hydrochloride is a potent and selective inhibitor of?casein kinase?1? (CK1?), with an?IC50?of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 hydrochloride is useful in probing unique roles between these two kinases in multiple signaling pathways .
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- HY-117857
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- HY-108442
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JW67
1 Publications Verification
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Wnt
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Cancer
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JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM . JW67 affects the multiprotein complex consisting of β-catenin/GSK-3β/AXIN/APC/CK1 that rapidly reduces active β-catenin with a subsequent downregulation of Wnt target genes. JW67 also inhibits colorectal cancer cell growth .
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- HY-15424
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NSC 113939; 5-ITu
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Adenosine Kinase
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Cancer
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5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
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- HY-15424R
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Adenosine Kinase
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Cancer
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5-Iodotubercidin (Standard) is the analytical standard of 5-Iodotubercidin. This product is intended for research and analytical applications. 5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
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- HY-W011109
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Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
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Cancer
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CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases .
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- HY-133028
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Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
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Cancer
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CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases .
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- HY-171301
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- HY-171292
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Casein Kinase
p38 MAPK
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Others
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CK1δ-IN-9 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1δ with IC50 of 1.4 nM. CK1δ-IN-9 inhibits p38α and p38β with IC50 of 0.25 μM and 0.78 μM. CK1δ-IN-9 exhibits pharmacokinetic characteristics with a good oral bioavailability (70%) and a moderate clearance .
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- HY-W842364
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Casein Kinase
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Neurological Disease
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CK1δ-IN-3 (compound 376) is a casein kinase 1δ (CK1δ) inhibitor. CK1δ-IN-3 can be utilized in neurodegenerative disorders research .
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- HY-169713
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Casein Kinase
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Neurological Disease
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CK1δ-IN-5 (Compound 24) is a Casein kinase 1δ (CK1δ) inhibitor. CK1δ-IN-5 can be used in the research of neurodegenerative diseases .
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- HY-169556
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- HY-169719
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- HY-171298
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- HY-W840382
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- HY-100536
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Wnt
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Cancer
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IWP-3 is an potent inhibitor of Wnt production with an IC50 of 40 nM. IWP-3 inhibits Porcupine (Porcn) function thereby blocking palmitoylation of Wnt proteins. IWP-3 inhibits CK1γ3 and CK1ε only moderately and does not inhibit CK1α .
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- HY-18285
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Wnt
Casein Kinase
ERK
CDK
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Cancer
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Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively .
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- HY-173494
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GSK-3
Casein Kinase
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Cancer
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GSK-3β/CK-1δ-IN-1 (8d) is a dual and blood-brain barrier penetrated GSK-3β / CK-1δ inhibitor, with IC50 values of 0.77 μM for GSK-3β and 0.57 μM for CK-1δ, respectively. GSK-3β/CK-1δ-IN-1 (8d) can be used in the research for neuroblastoma .
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- HY-15490
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Casein Kinase
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Cancer
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PF-670462 dihydrochloride is a potent and selective inhibitor of casein kinase (CK1ε and CK1δ), with IC50s of 7.7 nM and 14 nM, respectively.
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- HY-100011
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SR-3029
2 Publications Verification
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Casein Kinase
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Cancer
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SR-3029 is a potent and ATP competitive CK1δ and CK1ε inhibitor, with IC50s of 44 nM and 260 nM, respectively, and Kis of 97 nM for both kinases.
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- HY-171277
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Casein Kinase
p38 MAPK
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Cancer
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Casein kinase 1δ-IN-27 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1α, CK1δ, CK1ε, and p38α with IC50s of 22, 16.5, 9.41 and 14.8 nM, respectively. Casein kinase 1δ-IN-27 inhibits the DUX4 expression with an IC50 of 10 nM .
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- HY-145939
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BRD5846
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Casein Kinase
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Cancer
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BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
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- HY-149292
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Casein Kinase
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Cancer
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SR-4133 is a potent and highly CK1ε selective inhibitor with an IC50 of 58 nM. SR-4133 binds to the ATP-binding site of CK1ε. SR-4133 displays nanomolar growth inhibition of bladder cancer cells, and inhibits the phosphorylation of 4E-BP1 .
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- HY-12443
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Casein Kinase
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Neurological Disease
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PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
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- HY-171290
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Casein Kinase
p38 MAPK
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Inflammation/Immunology
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Casein kinase 1δ-IN-31 (Compound 16) is the inhibitor for casein kinase (CK) that inhibits CK1α, CK1δ, and p38α with IC50s of 196, 17, and 18 nM, respectively. Casein kinase 1δ-IN-31 inhibits Double Homeobox 4 (DUX4) with IC50 of 1200 nM .
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- HY-155958
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-9 (compound 737) is a potent casein kinase 1δ (CK1δ/CK15) inhibitor. Casein kinase 1δ-IN-9 can be used for the research of neurodegenerative disorders such as Alzheimer's disease .
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- HY-153904
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-5 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 47 nM. Casein kinase 1δ-IN-5 shows neuroprotective and anti-inflammatory properties both in vitro. Casein kinase 1δ-IN-5 has the potential for neurodegenerative diseases research.
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- HY-162336
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- HY-10456
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p38 MAPK
Casein Kinase
Wnt
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Inflammation/Immunology
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TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
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- HY-153905
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-6 is a potent and selective protein kinase CK-1δ inhibitor with an IC50 of 23 nM. Casein kinase 1δ-IN-6 shows neuroprotective and anti-inflammatory properties both in vitro and in vivo. Casein kinase 1δ-IN-6 is a promising drug candidate and can be used for neurodegenerative diseases research.
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- HY-156040
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Casein Kinase
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Cancer
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Casein kinase 1δ-IN-10 is a casein kinase 1δ (CK1δ) inhibitor (WO2012080729A2; compound 685) .
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- HY-121944
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Casein Kinase
Wnt
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Others
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Ricinine exhibits hepatoprotection in CCl4-induced liver damage. Ricinine is also a CK1α inhibitor, and may activate Wnt pathway .
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- HY-148455
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- HY-171279
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p38 MAPK
Casein Kinase
Apoptosis
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Inflammation/Immunology
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Casein kinase 1δ-IN-29 (Compound 18) is the inhibitor for p38α and casein kinase 1 that inhibits p38α, CK1δ and CK1ε with IC50 of 0.041 µM, 0.005 µM and 0.447 µM, respectively. Casein kinase 1δ-IN-29 arrests cell cycle at subG1 phase, induces apoptosis in cell AC1-M88 .
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- HY-108907
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Casein Kinase
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Cancer
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SR-1277 is a potent, selective and ATP competitive CK1δ/ε inhibitor, with IC50s of 49 nM and 260 nM, respectively. SR-1277 also inhibits FLT3, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9/cyclin K, with IC50s of 305 nM, 1340 nM, 311 nM and 109 nM, respectively. SR-1277 can be used for the research of cancer .
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- HY-120675
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SSTC3
2 Publications Verification
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Casein Kinase
Wnt
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Cancer
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SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors .
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- HY-171300
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- HY-148112
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-1 is an inhibitor of casein kinase 1δ (CK1δ). Casein kinase 1δ-IN-1 can be used for the research of neurodegenerative diseases such as tauopathies .
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- HY-123954
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Casein Kinase inhibitor A51
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Casein Kinase
CDK
Apoptosis
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Cancer
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BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
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- HY-169573
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-16 (compound 506) is a casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-16 can be utilized in neurodegenerative disorders research .
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- HY-169677
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-30 (Compound 581) is a Casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-30 can be used in the research of neurodegenerative diseases .
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- HY-169574
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-17 (compound 753) is a casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-17 can be utilized in neurodegenerative disorders research .
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- HY-169577
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Casein Kinase
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Neurological Disease
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Casein kinase 1δ-IN-18 (compound 660) is a casein kinase 1δ (CK1δ) inhibitor. Casein kinase 1δ-IN-18 can be utilized in neurodegenerative disorders research .
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- HY-171278
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Casein Kinase
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Metabolic Disease
Cancer
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Casein kinase 1δ-IN-28 (Compound 4) is the inhibitor for CK1ε with an IC50 of 0.0146 μM. Casein kinase 1δ-IN-28 exhibits a metabolite rate in human liver microsomes of 52% .
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- HY-123955
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Casein Kinase
CDK
Apoptosis
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Cancer
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Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
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- HY-174371
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Molecular Glues
Casein Kinase
MDM-2/p53
MALT1
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Cancer
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INNO-220 is an orally active, CRBN-dependent molecular glue degrader targeting CK1α. INNO-220 induces cell cycle arrest at G0/G1 phase and triggers apoptosis by degrading CK1α. INNO-220 disrupts the assembly and function of the CARD11/BCL10/MALT1 complex, thereby inhibiting NF-κB signaling in stimulated T cells and lymphoma cells that harbor an activating mutation in CARD11. INNO-220 provides a new direction for lymphoma research.
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- HY-13912
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IWP-2
Maximum Cited Publications
24 Publications Verification
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Wnt
Porcupine
Casein Kinase
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Cancer
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IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ .
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- HY-18340
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CR8, (R)-Isomer
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Molecular Glues
CDK
Apoptosis
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Neurological Disease
Cancer
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(R)-CR8, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 induces apoptosis and has neuroprotective effect . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
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- HY-18340A
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CR8, (R)-Isomer trihydrochloride
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Molecular Glues
CDK
Apoptosis
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Neurological Disease
Cancer
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(R)-CR8 (CR8) trihydrochloride, a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)-CR8 trihydrochloride inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)-CR8 trihydrochloride induces apoptosis and has neuroprotective effect . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
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- HY-12279
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TGR-1202; RP5264
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PI3K
Casein Kinase
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Cancer
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Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
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- HY-12279A
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TGR-1202 tosylate; RP5264 tosylate
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PI3K
Casein Kinase
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Cancer
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Umbralisib (TGR-1202) tosylate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach .
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- HY-12279C
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TGR-1202 hydrochloride; RP5264 hydrochloride
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PI3K
Casein Kinase
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Cancer
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Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
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- HY-12279B
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TGR-1202 sulfate; RP-5264 sulfate
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PI3K
Casein Kinase
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Cancer
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Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach .
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- HY-N6841
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Glucose-6-Phosphate Isomerase (GPI)
Casein Kinase
Virus Protease
Flavivirus
PI3K
Akt
mTOR
Apoptosis
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Infection
Cancer
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Rhodiolin, a flavonoid, is an orally active glucose 6-phosphate isomerase (GPI) inhibitor. Rhodiolin inhibits papillary thyroid cancer (PTC) by targeting glycolysis enzyme glucose 6-phosphate isomerase GPI and suppressing PI3K/AKT/mTOR phosphorylation and induce apoptosis. Rhodiolin as a NS2B-NS3 protease inhibitor can disrupt dengue viral replication. Rhodiolin is also a potential candidate for developing anticancer strategies inhibiting CK1ε kinase. Rhodiolin can be used for the study of anti-tumor and anti-viral .
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- HY-N3127
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Casein Kinase
PI3K
VEGFR
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Metabolic Disease
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Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ) .
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- HY-12279CR
-
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PI3K
Casein Kinase
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Cancer
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Umbralisib (hydrochloride) (Standard) is the analytical standard of Umbralisib (hydrochloride). This product is intended for research and analytical applications. Umbralisib (TGR-1202) hydrochloride is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach .
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- HY-12279R
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PI3K
Casein Kinase
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Cancer
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Umbralisib (Standard) is the analytical standard of Umbralisib. This product is intended for research and analytical applications. Umbralisib (TGR-1202) is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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