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CK1-IN-1 is a casein kinase 1(CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively [1].
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 [1].
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[1].
(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 [1].
CK1tide is a substrate for casein kinase 1 (CK1) and can be used to assess CK1's in vitro catalytic activity by detecting whether CK1 can phosphorylate it [1].
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 [1].
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 [1].
JW67 inhibits the canonical Wnt signaling with an IC50 of 1.17μM [1]. 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 [1].
TA-01 is a potent CK1 and p38 MAPK inhibitor, with IC50s of 6.4 nM, 6.8 nM, 6.7 nM for CK1ε, CK1δ and p38 MAPK, respectively. TA-01 acts as a cardiogenic inhibitor.
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 [1] .
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 [1] .
MRT00033659 is a potent broad-spectrum kinase inhibitor of CK1 (IC50=0.9 µM for CK1δ) and CHK1 (IC50=0.23 µM). MRT00033659, a pyrazolo-pyridine analogue, induces p53 pathway activation and E2F-1 destabilisation [1].
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 [1].
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 [1] .
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 [1] .
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 [1] .
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 [1] .
PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
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 [1]. PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
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 [1].
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[1].
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.
TMX-4116 is a casein kinase 1α (CK1α) degrader. TMX-4116 shows the degradation preference for CK1α with DC50s less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4116 can be used for the research of multiple myeloma [1].
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.
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 [1] .
SJ3149 is a selective and potent molecular glue degrader of CK1α protein with broad antiproliferative activity. SJ3149 can be used in cancer research [1] .
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 [1].
DEG-77, a IKZF2 and CK1α targeted molecular glue, possesses suitable pharmacokinetic properties, solubility, and selectivity for in vivo studies (t1/2=8h)[1].
CKR-49-17 is an activator of CK1γ2. CKR-49-17 decreases C99 and β-amyloid levels. CKR-49-17 can be used in the research of Alzheimer's disease (AD)[1].
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 [1].
Casein kinase 1δ-IN-1 (compound 822) is an inhibitor of casein kinase 1 delta(CK1δ), exhibits inhibition of greater than 5%. Casein kinase 1δ-IN-1 can be used for neurodegenerative disorders such as Alzheimer's disease research [1].
FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease [1] .
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 [1].
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[1] .
(R)-CR8 (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 [1] . (R)-CR8 acts as a molecular glue degrader that depletes cyclin K .
(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 [1] . (R)-CR8 trihydrochloride acts as a molecular glue degrader that depletes cyclin K .
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 [1] .
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 [1] .
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 [1] .
c-Myc inhibitor 7 is a c-Myc inhibitor and a multiple target protein degrader. c-Myc inhibitor 7 effective degrades c-MYC, CK1α, GSPT1 and IKZF1/2/3 proteins in a variety of tumor cells. c-Myc inhibitor 7 can be used for c-Myc high expression related disease research, such as cancer, cardiovascular and cerebrovascular diseases, and viral infection [1].
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 [1] .
MGD-28 is a potent, orally active, Cereblon (CRBN)-dependent IKAROS protein degrader that degrades IKZF1 (DC50=3.8 nM), IKZF2 (DC50=56.3 nM), and IKZF3(DC50=7.1 nM) in a dose-dependent manner. In addition, MGD-4 also degrades CK1α (DC50=7.8 nM). MGD-28 has antiproliferative activity and can be used in multiple myeloma research [1].
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) [1] .
CK1tide is a substrate for casein kinase 1 (CK1) and can be used to assess CK1's in vitro catalytic activity by detecting whether CK1 can phosphorylate it [1].
CCK1-specific peptide substrate is a biological active peptide. (This peptide sequence is based on rabbit muscle glycogen synthase with Ser7 phosphorylated. It is a peptide substrate for Casein Kinase I (CK1). CK1 phosphorylates Ser10. Ser7 is phosphorylated by PKA in vivo.)
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) [1] .
CSNK1E protein is a casein kinase that preferentially phosphorylates acidic proteins such as casein. CSNK1E Protein, Human (His) is the recombinant human-derived CSNK1E protein, expressed by E. coli , with N-6*His labeled tag. The total length of CSNK1E Protein, Human (His) is 416 a.a., with molecular weight of ~51.3 kDa.
MIP-4/CCL18 Protein, Human (His) is a CC chemokine ligand that binds to PITPNM3, GPR30 and CCR8 receptors and also acts as a neutral CCR3 antagonist mediating inflammation, autoimmunity and carcinogenesis. MIP-4/CCL18 Protein, Human (His) is a recombinant human MIP-4/CCL18 (A21-A89) protein expressed by E. coli with a his tag at N end.
The CK1γ3 protein is a serine/threonine protein kinase in the casein kinase family that prefers acidic proteins, including casein. It has broad substrate specificity and can phosphorylate a variety of proteins, affecting diverse cellular processes. CK1γ3 Protein, Human (Sf9) is the recombinant human-derived CK1γ3 protein, expressed by Sf9 insect cells , with tag free. The total length of CK1γ3 Protein, Human (Sf9) is 446 a.a., .
The CK1d protein is an important serine/threonine protein kinase that complexly controls cellular processes such as Wnt signaling, DNA repair, and circadian rhythms. Its versatility is evident in phosphorylating a variety of proteins, including connexin-43/GJA1, MAP1A, p53/TP53, and YAP1. CK1d Protein, Human (Sf9, GST) is the recombinant human-derived CK1d protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of CK1d Protein, Human (Sf9, GST) is 414 a.a., .
The CK1γ3 protein is a serine/threonine protein kinase in the casein kinase family that prefers acidic proteins, including casein. It has broad substrate specificity and can phosphorylate a variety of proteins, affecting diverse cellular processes. CK1γ3 Protein, Human (Sf9, GST) is the recombinant human-derived CK1γ3 protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of CK1γ3 Protein, Human (Sf9, GST) is 446 a.a., .
Casein kinase I α is a member of casein kinases that exhibits a preference for phosphorylation of acidic proteins such as casein. It phosphorylates many substrates, including CTNNB1 at "Ser-45" involved in Wnt signaling. Casein Kinase I alpha Protein, Human (sf9, GST) is the recombinant human-derived Casein Kinase I alpha protein, expressed by Sf9 insect cells , with N-GST labeled tag. The total length of Casein Kinase I alpha Protein, Human (sf9, GST) is 337 a.a., with molecular weight of ~62 kDa.
Casein kinase I α is a member of casein kinases that exhibits a preference for phosphorylation of acidic proteins such as casein. It phosphorylates many substrates, including CTNNB1 at "Ser-45" involved in Wnt signaling. CSNK1A1 Protein, Human (sf9, His, Strep) is the recombinant human-derived CSNK1A1, expressed by Sf9 insect cells , with Strep, His labeled tag. The total length of CSNK1A1 Protein, Human (sf9, His, Strep) is 336 a.a.,
CSNK1A1L Protein, Human (sf9, His, GST) is the recombinant human-derived CSNK1A1L, expressed by Sf9 insect cells , with His, GST labeled tag. The total length of CSNK1A1L Protein, Human (sf9, His, GST) is 336 a.a.,
CSNK1E, a member of the casein kinase family, is characterized by its preferential phosphorylation of acidic proteins, particularly caseins. The protein plays a pivotal role in Wnt signaling, as evidenced by its phosphorylation of DVL1 and DVL2, contributing to the intricate regulation of this pathway. Beyond its involvement in Wnt signaling, CSNK1E serves as a central component of the circadian clock, influencing the circadian period length by orchestrating the speed and rhythmicity of PER1 and PER2 phosphorylation. Acting in equilibrium with PP1, it governs the nuclear transport and degradation of PER1 and PER2, thereby intricately regulating the circadian rhythm. Additionally, CSNK1E demonstrates its regulatory influence by inhibiting cytokine-induced granulocytic differentiation, further emphasizing its multifaceted roles in cellular processes. CSNK1E Protein, Human (P. pastoris, His) is the recombinant human-derived CSNK1E protein, expressed by P. pastoris , with N-6*His labeled tag. The total length of CSNK1E Protein, Human (P. pastoris, His) is 416 a.a., with molecular weight of 49.3 kDa.
Casein kinase I gamma-2 is a serine/threonine protein kinase that targets acidic proteins and phosphorylates a variety of substrates, such as COL4A3BP/CERT, MTA1 and SMAD3, especially destabilizing SMAD3 and inhibiting TGF- beta reaction. Hyperphosphorylation of COL4A3BP/CERT disrupts ER-to-Golgi transport and affects the synthesis of ceramide and sphingomyelin. CSNK1G2 Protein, Human (sf9, GST) is the recombinant human-derived CSNK1G2, expressed by Sf9 insect cells , with GST labeled tag. The total length of CSNK1G2 Protein, Human (sf9, GST) is 414 a.a.,
Casein kinase I gamma-2 Protein, Human (His) is an approximately 55.0 kDa human casein kinase I isoform gamma-2 protein with a His-flag expressed in E. coli. Human Casein kinase I isoform gamma-2 may exhibit overexpression during tumorigenesis and belongs to the CKI family.
Casein kinase I gamma-2 is a serine/threonine protein kinase that targets acidic proteins and phosphorylates a variety of substrates, such as COL4A3BP/CERT, MTA1 and SMAD3, especially destabilizing SMAD3 and inhibiting TGF- beta reaction. Hyperphosphorylation of COL4A3BP/CERT disrupts ER-to-Golgi transport and affects the synthesis of ceramide and sphingomyelin. Casein Kinase I gamma-2 Protein, Human (sf9, His) is the recombinant human-derived Casein Kinase I gamma-2 protein, expressed by Sf9 insect cells , with N-His labeled tag. The total length of Casein Kinase I gamma-2 Protein, Human (sf9, His) is 398 a.a., with molecular weight of ~48 kDa.
CSNK1A1; Casein kinase I isoform alpha; CKI-alpha; CK1
WB, IP
Human, Rat
Casein Kinase 1 alpha Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 39 kDa, targeting to Casein Kinase 1 alpha. It can be used for WB,IP assays with tag free, in the background of Human, Rat.
Cytokeratin 1 Antibody (YA2665) is a biotin-conjugated non-conjugated IgG antibody, targeting Cytokeratin 1, with a predicted molecular weight of 66 kDa (observed band size: 66 kDa). Cytokeratin 1 Antibody (YA2665) can be used for WB experiment in human, mouse, rat background.
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