p38 MAPK

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1076	SB203580	<1 mg/mL	43 mg/mL	'<1 mg/mL
S1574	Doramapimod (BIRB 796)	<1 mg/mL	100 mg/mL	100 mg/mL
S1077	SB202190 (FHPI)	<1 mg/mL	66 mg/mL	12 mg/mL
S1494	Ralimetinib (LY2228820) dimesylate	100 mg/mL	4 mg/mL	'3 mg/mL
S5967	Berberine chloride hydrate	39 mg/mL	78 mg/mL	'<1 mg/mL
S6920	SEA0400	<1 mg/mL	74 mg/mL	'74 mg/mL
S6005	VX-702	<1 mg/mL	81 mg/mL	'<1 mg/mL
S2726	PH-797804	<1 mg/mL	96 mg/mL	7 mg/mL
S1458	Neflamapimod (VX-745)	<1 mg/mL	15 mg/mL	'<1 mg/mL
S2928	TAK-715	<1 mg/mL	80 mg/mL	16 mg/mL
S3940	3'-Hydroxypterostilbene	<1 mg/mL	54 mg/mL	54 mg/mL
S8125	Pamapimod	<1 mg/mL	81 mg/mL	28 mg/mL
S6502	SD 0006	<1 mg/mL	80 mg/mL	2 mg/mL
S7741	SB239063	<1 mg/mL	60 mg/mL	7 mg/mL
S7214	Skepinone-L	<1 mg/mL	85 mg/mL	'85 mg/mL
S0752	AUDA	<1 mg/mL	78 mg/mL	6 mg/mL
S0542	R1487	<1 mg/mL	<1 mg/mL	''''<1 mg/mL
S4884	Trans-Zeatin	<1 mg/mL	43 mg/mL	2 mg/mL
S9315	Praeruptorin A	-1 mg/mL	77 mg/mL	-1 mg/mL
S9075	Mulberroside A	-1 mg/mL	100 mg/mL	-1 mg/mL
S8124	BMS-582949	<1 mg/mL	81 mg/mL	'<1 mg/mL
S7799	Pexmetinib (ARRY-614)	<1 mg/mL	100 mg/mL	100 mg/mL
S6807	TA-02	<1 mg/mL	67 mg/mL	3 mg/mL
S8706	UM-164	<1 mg/mL	100 mg/mL	<1 mg/mL
S5183	PD 169316	<1 mg/mL	14 mg/mL	'<1 mg/mL
S1950	Metformin HCl	33 mg/mL	<1 mg/mL	'<1 mg/mL
S5958	Metformin	26 mg/mL	26 mg/mL	'''26 mg/mL
S2266	Asiatic Acid	<1 mg/mL	97 mg/mL	<1 mg/mL
S2271	Berberine chloride (NSC 646666)	<1 mg/mL	40 mg/mL	<1 mg/mL
S7686	ML141	<1 mg/mL	81 mg/mL	<1 mg/mL
S6347	5'-N-Ethylcarboxamidoadenosine (NECA)	<1 mg/mL	62 mg/mL	'''<1 mg/mL
S9514	Rotundic acid	-1 mg/mL	98 mg/mL	-1 mg/mL

亜型選択性的な製品

p38 MAPK製品

All (32) p38 MAPK阻害剤(25) p38 MAPK活性剤(5) p38 MAPK作動薬(1) p38 MAPKモジュレータ(1)

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1076	SB203580 SB203580 (RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.	Mol Cell, 2021, S1097-2765(21)00269-0 Nat Commun, 2021, 12(1):2923 Theranostics, 2021, 11(10):4770-4789	A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
S1574	Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.	Mol Immunol, 2021, 133:135-145 Int Immunopharmacol, 2021, 98:107848 Exp Ther Med, 2021, 21(5):440	Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.
S1077	SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.	Immunity, 2021, S1074-7613(21)00210-7 Cell Death Dis, 2021, 12(4):316 Mol Oncol, 2021, 10.1002/1878-0261.13046	C, Jurkat cells with SB202190 at 1, 5, and 10 μM were tested, and a decreased SRP72 expression was found when using at 10 μM (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 μM at 240 versus 0 and 120 versus 0 min (p<0.05).
S1494	Ralimetinib (LY2228820) dimesylate Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.	Nat Commun, 2021, 12(1):1717 Cell Death Dis, 2021, 12(4):316 Radiother Oncol, 2021, 156:136-144	Relationship of JNK, p38 MAPK, and PI3K activation in TNF-α-induced signaling. Western blot analysis of the effect of another p38 MAPK inhibitor, LY2228820, on TNF-α signaling. HUVECs were pretreated with LY2228820 (10 umol/L) or wortmannin (1 umol/L) for 1 h, followed by stimulation with TNF-α (5 ng/mL) for 15 min (n=2).
S5967^新	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201
S6920^新	SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S6005	VX-702 VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.	Cancers (Basel), 2021, 13(6)1205 Int J Mol Sci, 2021, 22(9)4960 Cell, 2020, 182(3):685-712.e19	Reduction of IL-10 expression due to p38 inhibition is observed also in CpG-stimulated B cells and using VX-702. B cells were pre-treated with 10 uM of VX-702 for 1 h and stimulated with LPS or CpG for 24 or 48 h. Bar graphs indicate mean (±SEM) IL-10 concentrations at 48 h from n = 4 (LPS) and n = 3 (CpG) experiments. Significant differences against the no inhibitor condition were calculated using a paired Student's t-test and indicated as follows: p < 0.05, **p < 0.001.
S2726	PH-797804 PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.	Aging (Albany NY), 2021, 13(5):6346-6358 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Effect of MEK inhibitor PH-797804 in A549 cells. A549 cells were incubated with increasing concentrations of PH-797804 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.
S1458	Neflamapimod (VX-745) Neflamapimod (VX-745) is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.	EMBO J, 2021, e106188 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	A) TRAP staining of BMMs cultured with M-CSF and RANKL for 7 d in the presence of SB203580 (50 nM) or VX-745 (50 nM). B) Bone slice assay indicated the effects of compounds on bone resorption.
S2928	TAK-715 TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.	Oncogene, 2021, 10.1038/s41388-020-01628-x Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
S3940	3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies.
S8125	Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.	J Leukoc Biol, 2020, 10.1002/JLB.3A0120-379RR J Pharmacol Exp Ther, 2020, 374(3):489-498 Nat Commun, 2019, 10(1):688
S6502	SD 0006 SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β).	Eur Rev Med Pharmacol Sci, 2020, 24(21):10966-10974
S7741	SB239063 SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.	EBioMedicine, 2021, 66:103290 Biomed Pharmacother, 2021, 134:111155 J Agric Food Chem, 2021, 10.1021/acs.jafc.1c00199	KLF4 protein half-life is elongated under p38 inhibition. MCF7 cells plated in six-well plate were treated with DMSO or p38 inhibitors (SB203580 and SB239063) for 6 h. Then CHX was added 0, 2, 4 or 6 h before harvest. KLF4 protein level was tested by immunoblotting
S7214	Skepinone-L Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM.	Am J Physiol Renal Physiol, 2020, 318(2):F322-F328 Mol Cancer Ther, 2019, 18(9):1506-1519 Cancer Res, 2018, 78(5):1275-1292	TLR4/MAPK pathway regulated macrophage polarization towards M1 phenotype. LPS/INF-γ induced macrophages were cultured in the absence or presence of siTLR4, SP600125(an inhibitor of JNK), SCH772984(an inhibitor of ERK) and Skepinone-L(an inhibitor of p38) respectively for 24h. Then, all the cells were harvested for western blot assay.
S0752	AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S0542	R1487 R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM.	Drug Test Anal, 2020, 10.1002/dta.2917
S4884	Trans-Zeatin Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently.
S9315	Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S9075	Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S8124	BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.	EMBO J, 2021, e107182 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
S7799	Pexmetinib (ARRY-614) Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.	Theranostics, 2021, 11(4):1626-1640 Sci Rep, 2021, 11(1):5752 J Pharmacol Exp Ther, 2019, 370(2):219-230
S6807	TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S8706	UM-164 UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
S5183	PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.	PLoS One, 2021, 16(5):e0252541
S1950	Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.	Immunity, 2021, S1074-7613(21)00210-7 Mol Cell, 2021, S1097-2765(21)00232-X Autophagy, 2021, 1-22	Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
S5958^新	Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.	J Cell Mol Med, 2021, 10.1111/jcmm.16742 Oncotarget, 2021, 12(7):674-685
S2266	Asiatic Acid Asiatic acid (Dammarolic acid, Asiantic acid) is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.	J Mater Chem B, 2019, 7(40):6125-6138 Molecules, 2019, 24(12) J Med Virol, 2019, 91(8):1440-1447
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210 Biology (Basel), 2021, 10(3)250
S7686	ML141 ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.	Cell Rep, 2021, 36(1):109254 FASEB J, 2021, 35(5):e21598 Sci Rep, 2021, 11(1):8168	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
S6347^新	5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.
S9514	Rotundic acid Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.

製品コード	製品説明	文献中Selleckの製品使用例	お客様のフィードバック
S1076	SB203580 SB203580 (RWJ 64809, PB 203580) is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM. SB203580 induces mitophagy and autophagy.	Mol Cell, 2021, S1097-2765(21)00269-0 Nat Commun, 2021, 12(1):2923 Theranostics, 2021, 11(10):4770-4789	A, effects of p38 inhibitor SB203580 (1, 5, and 10 μM) on SRP72 protein expression was evaluated by WB using antibodies against human SRP72,SRP54, and GAPDH. A decreased intensity of SRP72 bands was noted when using the inhibitor at 5 μM concentration at 240 min (lane 6) and 10 μM at 120 and 240 min (lanes 8 and 9). B, results were analyzed and RUA illustrated, finding significant results at 5 μM, 240 versus 0 min, and 10 μM, 240 versus 0 and 120 versus 0 min, respectively, (p<0.05).
S1574	Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.	Mol Immunol, 2021, 133:135-145 Int Immunopharmacol, 2021, 98:107848 Exp Ther Med, 2021, 21(5):440	Effect of blockade of p38 or MEK on MK2 activation following TLR stimulation in moDC. MoDC were pre-treated with p38 inhibitors SB203580 10 mM (S), BIRB0796 (B) 0.1 or 1.0 mM or MEK inhibitor UO126 10 mM (U) for 1hr followed by poly I:C/R848 stimulation for 30 min then Western blotted for p-MK2 with β-actin loading control.
S1077	SB202190 (FHPI) SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo. SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. SB202190 significantly suppresses Erastin‐dependent ferroptosis.	Immunity, 2021, S1074-7613(21)00210-7 Cell Death Dis, 2021, 12(4):316 Mol Oncol, 2021, 10.1002/1878-0261.13046	C, Jurkat cells with SB202190 at 1, 5, and 10 μM were tested, and a decreased SRP72 expression was found when using at 10 μM (lanes 8 and 9). D, results were analyzed and RUA illustrated, finding significant results at 10 μM at 240 versus 0 and 120 versus 0 min (p<0.05).
S1494	Ralimetinib (LY2228820) dimesylate Ralimetinib (LY2228820) dimesylate is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.	Nat Commun, 2021, 12(1):1717 Cell Death Dis, 2021, 12(4):316 Radiother Oncol, 2021, 156:136-144	Relationship of JNK, p38 MAPK, and PI3K activation in TNF-α-induced signaling. Western blot analysis of the effect of another p38 MAPK inhibitor, LY2228820, on TNF-α signaling. HUVECs were pretreated with LY2228820 (10 umol/L) or wortmannin (1 umol/L) for 1 h, followed by stimulation with TNF-α (5 ng/mL) for 15 min (n=2).
S5967^新	Berberine chloride hydrate Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201
S6920^新	SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S6005	VX-702 VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.	Cancers (Basel), 2021, 13(6)1205 Int J Mol Sci, 2021, 22(9)4960 Cell, 2020, 182(3):685-712.e19	Reduction of IL-10 expression due to p38 inhibition is observed also in CpG-stimulated B cells and using VX-702. B cells were pre-treated with 10 uM of VX-702 for 1 h and stimulated with LPS or CpG for 24 or 48 h. Bar graphs indicate mean (±SEM) IL-10 concentrations at 48 h from n = 4 (LPS) and n = 3 (CpG) experiments. Significant differences against the no inhibitor condition were calculated using a paired Student's t-test and indicated as follows: p < 0.05, **p < 0.001.
S2726	PH-797804 PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.	Aging (Albany NY), 2021, 13(5):6346-6358 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	Effect of MEK inhibitor PH-797804 in A549 cells. A549 cells were incubated with increasing concentrations of PH-797804 for 2 h. The cell lysates were harvested and phosphorylation of indicated proteins was determined by Western blotting.
S1458	Neflamapimod (VX-745) Neflamapimod (VX-745) is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.	EMBO J, 2021, e106188 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19	A) TRAP staining of BMMs cultured with M-CSF and RANKL for 7 d in the presence of SB203580 (50 nM) or VX-745 (50 nM). B) Bone slice assay indicated the effects of compounds on bone resorption.
S2928	TAK-715 TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.	Oncogene, 2021, 10.1038/s41388-020-01628-x Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
S3940	3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies.
S8125	Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.	J Leukoc Biol, 2020, 10.1002/JLB.3A0120-379RR J Pharmacol Exp Ther, 2020, 374(3):489-498 Nat Commun, 2019, 10(1):688
S6502	SD 0006 SD0006 is an inhibitor of p38 kinase-alpha (p38alpha) with IC50 values of 0.016 μM and 0.677 μM for p38α and p38β. It is selective for p38α kinase over 50 other kinases screened (including p38γ and p38δ with modest selectivity over p38β).	Eur Rev Med Pharmacol Sci, 2020, 24(21):10966-10974
S7741	SB239063 SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.	EBioMedicine, 2021, 66:103290 Biomed Pharmacother, 2021, 134:111155 J Agric Food Chem, 2021, 10.1021/acs.jafc.1c00199	KLF4 protein half-life is elongated under p38 inhibition. MCF7 cells plated in six-well plate were treated with DMSO or p38 inhibitors (SB203580 and SB239063) for 6 h. Then CHX was added 0, 2, 4 or 6 h before harvest. KLF4 protein level was tested by immunoblotting
S7214	Skepinone-L Skepinone-L (CBS3830) is a selective p38α-MAPK inhibitor with IC50 of 5 nM.	Am J Physiol Renal Physiol, 2020, 318(2):F322-F328 Mol Cancer Ther, 2019, 18(9):1506-1519 Cancer Res, 2018, 78(5):1275-1292	TLR4/MAPK pathway regulated macrophage polarization towards M1 phenotype. LPS/INF-γ induced macrophages were cultured in the absence or presence of siTLR4, SP600125(an inhibitor of JNK), SCH772984(an inhibitor of ERK) and Skepinone-L(an inhibitor of p38) respectively for 24h. Then, all the cells were harvested for western blot assay.
S0752	AUDA AUDA (compound 43) is a potent inhibitor of soluble epoxide hydrolase (sEH) with IC50 of 18 nM and 69 nM for the mouse sEH and human sEH, respectively. AUDA has anti-inflammatory activity that reduces the protein expression of MMP-9, IL-1β, TNF-α and TGF-β. AUDA downregulates Smad3 and p38 signaling pathways.
S0542	R1487 R1487 is an orally bioavailable and highly selective inhibitor of p38α with an ic50 value of 10 nM.	Drug Test Anal, 2020, 10.1002/dta.2917
S4884	Trans-Zeatin Trans-Zeatina ((E)-Zeatin) is the member of the plant growth hormone family known as cytokinins, which regulate cell division, development, and nutrient processing. Trans-Zeatin inhibits UVB-induced MMP-1 expression, c-Jun activation and phosphorylation of ERK, JNK and p38 MAP kinases (MAPKs) dose-dependently.
S9315	Praeruptorin A Praeruptorin A, a naturally existing pyranocumarin, is isolated from the dried root of Peucedanum praeruptorum Dunn. Praeruptorin A inhibits p38/Akt-c-Fos-NFATc1 signaling and PLCγ-independent Ca2+ oscillation. Praeruptorin A can significantly upregulates multidrug resistance-associated protein 2 expression via the constitutive androstane receptor-mediated pathway in vitro, and this should be taken as an herb-drug interaction.
S9075	Mulberroside A Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S8124	BMS-582949 BMS-582949 (PS540446) is a potent and selective p38 mitogen-activated protein kinase (p38 MAPK) inhibitor with IC50 of 13nM,inhibiting both p38 kinase activity and activation of p38.	EMBO J, 2021, e107182 Cell, 2020, 182(3):685-712.e19 Cell, 2020, 182(3):685-712.e19
S7799	Pexmetinib (ARRY-614) Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.	Theranostics, 2021, 11(4):1626-1640 Sci Rep, 2021, 11(1):5752 J Pharmacol Exp Ther, 2019, 370(2):219-230
S6807	TA-02 TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. TA-02 especially inhibits TGFBR-2.
S8706	UM-164 UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
S5183	PD 169316 PD 169316 is a potent, selective and cell-permeable p38 MAP kinase inhibitor with IC50 of 89 nM. PD169316 abrogates signaling initiated by both TGFbeta and Activin A. PD169316 shows antiviral activity against Enterovirus71.	PLoS One, 2021, 16(5):e0252541

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S1950	Metformin HCl Metformin HCl (1,1-Dimethylbiguanide HCl) decreases hyperglycemia in hepatocytes primarily by suppressing glucose production by the liver (hepatic gluconeogenesis). Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.	Immunity, 2021, S1074-7613(21)00210-7 Mol Cell, 2021, S1097-2765(21)00232-X Autophagy, 2021, 1-22	Cropped immunoblot analyses for downstream effector proteins of the MAPK and PI3K/AKT/mTOR signaling pathways for NRASQ61 mutant lung carcinoma and neuroblastoma cell lines. Dual pathway inhibition can be achieved by combining metformin and trametinib, as evidenced by the abolishment of p-ERK and p-S6.
S5958^新	Metformin Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells through activating JNK/p38 MAPK pathway and GADD153.	J Cell Mol Med, 2021, 10.1111/jcmm.16742 Oncotarget, 2021, 12(7):674-685
S2266	Asiatic Acid Asiatic acid (Dammarolic acid, Asiantic acid) is the aglycone of asiaticoside isolated from the plant Centella asiatica, commonly used in wound healing.	J Mater Chem B, 2019, 7(40):6125-6138 Molecules, 2019, 24(12) J Med Virol, 2019, 91(8):1440-1447
S2271	Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Pharmacol, 2021, 12:632201 Molecules, 2021, 26(5)1210 Biology (Basel), 2021, 10(3)250
S7686	ML141 ML141 (CID-2950007) is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis.	Cell Rep, 2021, 36(1):109254 FASEB J, 2021, 35(5):e21598 Sci Rep, 2021, 11(1):8168	(A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.

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S6347^新	5'-N-Ethylcarboxamidoadenosine (NECA) 5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.

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S6347^新

5'-N-Ethylcarboxamidoadenosine (NECA)

5'-N-Ethylcarboxamidoadenosine (NECA, 5'-(N-Ethylcarboxamido)adenosine, Adenosine-5'N-ethylcarboxamide, 5'-Ethylcarboxamidoadenosine) is a stable, nonselective adenosine receptor agonist. 5'-N-Ethylcarboxamidoadenosine acts via multiple mechanisms including: reducing diabetes-induced oxidative stress, inhibiting gene expression of IL-18, TNF-α and ICAM-1 (intercellular adhesion molecule 1 (CD54)), and blocking activation of the JNK-MAPK pathway.

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S9514	Rotundic acid Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.

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S9514

Rotundic acid

Rotundic acid (Rutundic acid), a natural compound, exhibit cytotoxic activities toward human hepatocellular carcinoma (HepG2), malignant melanoma (A375), SCLC (NCI-H446), breast cancer (MCF-7), and colon cancer (HT-29) cell lines.RA induces cell cycle arrest, DNA damage, and apoptosis by modulating the AKT/mTOR and MAPK pathways.