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MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation [2] .
MK2-IN-1 hydrochloride (compound 1) is a potent and selecitve MAPKAPK2(MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 hydrochloride impaires the phosphorylation level of serine residues in the Tfcp2l1 protein [2].
MK2-IN-1 (compound 1) is a potent and selecitve MAPKAPK2(MK2) inhibitor with an IC50 of 0.11 uM for MK2 and an EC50 of 0.35 uM for pHSP27. MK2-IN-1 impaires the phosphorylation level of serine residues in the Tfcp2l1 protein [2].
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2(MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo .
MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2(MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2 .
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation [2] .
MK2-IN-6 (Compound 11) is a potent and selective irreversible MK2 inhibitor with an IC50 value of 2.3 nM. MK2-IN-6 inhibits MK2 kinase activity, achieving prolonged MK2 signaling suppression and reducing pathological inflammatory cytokines in macrophages. MK2-IN-6 inhibits the M2-like protumor phenotype of macrophages both in vitro and in vivo, which is proming for research of colorectal cancer .
Peraquinsin is a MK2 activator. Peraquinsin can be used for the research of vascular disorder or endothelial barrier disorder. Peraquinsin also is an antihypertensive agent .
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease .
Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2(MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases .
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
(R)-Zunsemetinib is the isomer of Zunsemetinib (HY-139553), and can be used as an experimental control. Zunsemetinib (CDD-450) is an orally active and selective p38α mitogen-activated protein kinase-activated protein kinase 2(MK2) pathway inhibitor. Zunsemetinib can be used for the research of immuno-inflammatory diseases .
LLC355 is a discoidin domain receptor 1 (DDR1) ATTEC degrader. LLC355 efficiently degrades DDR1 protein with a DC50 value of 150.8 nM in non-small cell lung cancer NCI-H23 cells. LLC355 induces DDR1 degradation via lysosome-mediated autophagy. LLC355 potently inhibits cancer cell tumorigenicity, migration, and invasion .
Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2(MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
LLC1 is an amiloride (HY-B0285) derivative with cytotoxicity against breast cancer cells, particularly those resistant to treatment. The IC50 values of LLC1 for MCF7, MCF7 MX-100, MCF7 TS, MCF7 TR-1, and MCF7 TR-5 are 13, 12, 25, 26, and 19 mM, respectively. LLC1 shows potential for research in the field of cancer therapy .
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2(NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002); Pink: NSD2 inhibitor (HY-161575)) .
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2(MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect .
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
(R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis .
Isogambogic acid is an antibiotic and anti-cancer agent which efficiently elicit cell death in LLC and SK-LU-1 within a low micromolar range with IC50s of 2.26 μM and 2.02 μM. Isogambogic acid can be used for cancer research .
Lucialdehydes A is a lanostante-type triterpene aldehydes, isolated from the fruiting bodies of Ganoderma lucidum. Lucialdehydes A shows cytotoxic effects on tumor cells, including Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines .
Thalidomide-Pip-N-boc is a conjugate of E3 ligase ligand and linker. Thalidomide-Pip-N-boc is utilized for synthesis of PROTAC Degrader LLC0424 (HY-161574) .
Lucialdehyde B is a tetracyclic triterpene isolated from the substrates of Ganoderma lucidum with antiviral and cytotoxic activities. Lucialdehyde B has cytotoxic effects against Lewis lung cancer (LLC), T-47D, Sarcoma 180 and Meth-A tumor cell lines .
7-Ketositosterol is a phytosterol isolated from the fruits of the mulberry tree (Morus alba L.). 7-Ketositosterol can significantly inhibit Cisplatin (HY-17394)-induced apoptosis in LLC-PK1 cells and has the potential to improve Cisplatin-induced nephrotoxicity .
RORγt agonist 4 (compound 14) is a potent and selective agonist of RORγt. RORγt agonist 4 significantly enhances metabolic stability. RORγt agonist 4 improves the situation of tumor models of mouse B16F10 melanoma and LLC lung adenocarcinoma .
IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile .
TBK1-IN-1 is a potent and selective TANK binding kinase 1 (TBK1) inhibitor with an IC50 value of 22.4 nM. TBK1-IN-1 inhibits TBK1 downstream target genes cxcl10 and ifnβ expression. TBK1-IN-1 has anticancer activity .
Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity [2] .
Oxythiamine (Hydroxythiamin), an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine inhibits cancer cell apoptosis and inhibits cell proliferation [2] .
Loxoprofen sodium is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium can reduce atherosclerosis and shows antitumor activity [2] .
Loxoprofen sodium dihydrate is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium dihydrate is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium dihydrate can reduce atherosclerosis and shows antitumor activity [2] .
Oxythiamine (Hydroxythiamine) chloride hydrochloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine chloride hydrochloride is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride hydrochloride inhibits cancer cell apoptosis and inhibits cell proliferation [2] .
Oxythiamine (Hydroxythiamine) chloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride inhibits cancer cell apoptosis and inhibits cell proliferation [2] .
Loxoprofen (Standard) is the analytical standard of Loxoprofen. This product is intended for research and analytical applications. Loxoprofen is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen can reduce atherosclerosis and shows antitumor activity [2] .
Loxoprofen (sodium) (Standard) is the analytical standard of Loxoprofen (sodium). This product is intended for research and analytical applications. Loxoprofen sodium is a non-steroidal, orally active anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively. Loxoprofen sodium can reduce atherosclerosis and shows antitumor activity [2] .
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression [2].
PLD-IN-1 (Compound 3r) is an orally active inhibitor for phospholipase D with an IC50 of 1.97 μM. PLD-IN-1 reduces the expression of CD24, CD47 and PD-L1, enhances the calreticulin expression, and thus modulates the immune evasion mechanism in lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the cell viability of lung cancer cell A549, HCC44, H460 and HCC15 with IC50 of 18.44, 22.31, 24.85 and 21.45 μM, respectively. PLD-IN-1 can induce apoptosis and inhibits migration in cell A549. PLD-IN-1 enhances the level of pro-inflammatory M1 macrophages and decreases the level of anti-inflammatory M2 macrophages, exhibits antitumor efficacy in mouse model .
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer agents. α-Carotene is isolated from yellow-orange and dark-green vegetables [2].
α-Carotene (Standard) is the analytical standard of α-Carotene. This product is intended for research and analytical applications. α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer agents. α-Carotene is isolated from yellow-orange and dark-green vegetables [2].
Fibrinogen (Bovine) is a selective proteolytic molecule that can be activated by thrombin to assemble fibrin clots. Fibrinogen can regulate the activation of NF-KB in endothelial cells and upregulate the expression of inflammatory chemokines MCP-1 and MCP-1. Fibrinogen plays a key role in blood clotting, thrombosis, atherosclerosis and the pathological development of venous grafts, and can be used in the study of blood clotting and vascular diseases [2] .
Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research [2] .
Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research [2] .
Peimisine (Standard) is the analytical standard of Peimisine. This product is intended for research and analytical applications. Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research [2] .
Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes [2] .
Fibrinogen (Bovine) is a selective proteolytic molecule that can be activated by thrombin to assemble fibrin clots. Fibrinogen can regulate the activation of NF-KB in endothelial cells and upregulate the expression of inflammatory chemokines MCP-1 and MCP-1. Fibrinogen plays a key role in blood clotting, thrombosis, atherosclerosis and the pathological development of venous grafts, and can be used in the study of blood clotting and vascular diseases [2] .
MK2-IN-5 (Hsp25 kinase inhibitor) acetate is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 acetate targets the protein interaction domain in the MAPK pathway. MK2-IN-5 acetate inhibits HSP25 and HSP27 phosphorylation [2] .
MMI-0100 is a cell-permeant peptide inhibitor of mitogen activated protein kinase activated protein kinase II (MK2). MMI-0100 reduces intimal hyperplasia ex vivo and in vivo. MMI-0100 suppresses IL-6 expression without effect on IL-8 expression. MMI-0100 suppresses fibrotic processes such as vein graft disease .
MK2-IN-5 is a Mk2 pseudosubstrate (Ki= 8 μM). MK2-IN-5 targets the protein interaction domain in the MAPK pathway. MK2-IN-5 inhibits HSP25 and HSP27 phosphorylation [2] .
Lucialdehydes A is a lanostante-type triterpene aldehydes, isolated from the fruiting bodies of Ganoderma lucidum. Lucialdehydes A shows cytotoxic effects on tumor cells, including Lewis lung carcinoma (LLC), T-47D, Sarcoma 180, and Meth-A tumor cell lines .
Oxythiamine (Hydroxythiamin), an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine inhibits cancer cell apoptosis and inhibits cell proliferation [2] .
Oxythiamine (Hydroxythiamine) chloride hydrochloride, an analogue of anti-metabolite, can suppress the non-oxidative synthesis of ribose and induce cell apoptosis. Oxythiamine chloride hydrochloride is a thiamine antagonist and inhibits transketolase (TK). Oxythiamine chloride hydrochloride inhibits cancer cell apoptosis and inhibits cell proliferation [2] .
Isogambogic acid is an antibiotic and anti-cancer agent which efficiently elicit cell death in LLC and SK-LU-1 within a low micromolar range with IC50s of 2.26 μM and 2.02 μM. Isogambogic acid can be used for cancer research .
Lucialdehyde B is a tetracyclic triterpene isolated from the substrates of Ganoderma lucidum with antiviral and cytotoxic activities. Lucialdehyde B has cytotoxic effects against Lewis lung cancer (LLC), T-47D, Sarcoma 180 and Meth-A tumor cell lines .
7-Ketositosterol is a phytosterol isolated from the fruits of the mulberry tree (Morus alba L.). 7-Ketositosterol can significantly inhibit Cisplatin (HY-17394)-induced apoptosis in LLC-PK1 cells and has the potential to improve Cisplatin-induced nephrotoxicity .
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer agents. α-Carotene is isolated from yellow-orange and dark-green vegetables [2].
α-Carotene (Standard) is the analytical standard of α-Carotene. This product is intended for research and analytical applications. α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer agents. α-Carotene is isolated from yellow-orange and dark-green vegetables [2].
Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research [2] .
Peimisine (Ebeiensine) hydrochloride is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine hydrochloride shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research [2] .
Peimisine (Standard) is the analytical standard of Peimisine. This product is intended for research and analytical applications. Peimisine (Ebeiensine) is a muscarinic M receptor antagonist and angiotensin converting enzyme (ACE) inhibitor. Peimisine shows anti-tumor, anti-inflammatory, antihypertensive activities. Peimisine can induce apoptosis and be used in cough and asthma research [2] .
Phytosphingosine is a phospholipid with anti-inflammatory, antibacterial, and anti-cancer activities, which can induce apoptosis. Phytosphingosine is an immune regulator and can be used in the study of inflammatory skin diseases. Phytosphingosine is also an activator of GPR120 with an IC50 value of 33.4 μM and can be used in the study of type II diabetes [2] .
The MAPKAPK2 protein is a stress-activated kinase involved in multiple cellular processes, including cytokine production, endocytosis, cytoskeletal reorganization, cell migration, cell cycle control, chromatin remodeling, DNA damage response, and transcriptional regulation. MAPKAPK2 Protein, Human is the recombinant human-derived MAPKAPK2 protein, expressed by E. coli , with tag free. and ΔH217-P237, S216G, , , mutation. The total length of MAPKAPK2 Protein, Human is 318 a.a., .
The MAPKAPK2 protein is a stress-activated kinase involved in multiple cellular processes, including cytokine production, endocytosis, cytoskeletal reorganization, cell migration, cell cycle control, chromatin remodeling, DNA damage response, and transcriptional regulation. MAPKAPK2 Protein, Human (His) is the recombinant human-derived MAPKAPK2 protein, expressed by E. coli , with N-6*His labeled tag and ΔH217-P237, S216G, , , mutation. The total length of MAPKAPK2 Protein, Human (His) is 318 a.a., .
The MAPKAPK2 protein is a stress-activated kinase involved in multiple cellular processes, including cytokine production, endocytosis, cytoskeletal reorganization, cell migration, cell cycle control, chromatin remodeling, DNA damage response, and transcriptional regulation. MAPKAPK2 Protein, Human (323a.a) is the recombinant human-derived MAPKAPK2, expressed by E. coli , with tag Free labeled tag. ,
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