pkd1

CID-797718 is a protein kinase D1 (PKD1) inhibitor.

CID755673 is an effective and specific cell-active inhibitor for PKD (IC50: 182 nM); exhibits selective PKD1 inhibition when compared with PLK1, AKT, CAMKIIα, CAK, and PKC isoforms.

CRT0066101 dihydrochloride is an effective and selective PKD inhibitor (IC50s: 1, 2.5 and 2 nM for PKD1, 2, and 3).

N-Cyclohexyl-4-[1-(1-piperazinyl)-2,6-naphthyridin-3-yl]-2-pyridinamine is a novel 2,6-naphthyridine identified by high throughput screen (HTS) as a dual protein kinase C D (PKC PKD) inhibitor[1].

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

CCT245737 is an orally active, selective Chk1 inhibitor with an IC50 of 1.3 nM, and is >1,000-fold selective over CHK2 and CDK1.

kb-NB77-78 is an analog of CID797718, which is a by-product of the synthesis of the parental compound, CID755673(PKD1 inhibitor).

CID 2011756 is an ATP-competitive and specific PKD1 inhibitor.

BRD4 Inhibitor-40 (Compound 23) functions as an inhibitor of BRD, effectively targeting BRD4-BD1, BRD4-BD2, BRD2-BD1, and BRD2-BD2, with IC50 values of 16.1, 142.18, 29.35, and 302.35 nM, respectively. It modulates the expression of c-Myc and p21, induces cell cycle arrest in the G1 phase, and inhibits Pkd1-deficient (PN) renal cystic epithelial cells. Additionally, it prevents renal cyst formation in both Madin-Darby canine kidney and embryonic kidney cyst models, and demonstrates renal cyst inhibition activity in mouse models.

kb NB 142-70 is a selective protein kinase D (PKD) inhibitor with IC50 values of 28.3 nM, 58.7 nM, and 53.2 nM for PKD1, PKD2, and PKD3 respectively.

CRT5, a pyrazine benzamide, is a potent and selective PKD inhibitor. It inhibits VEGF-induced phosphorylation of three PKD substrates (IC50s = 1, 2, and 1.5 nM for PKD1, PKD2, and PKD3, respectively), histone deacetylase 5, CREB (cAMP-response-element-binding protein), and HSP27 (heat-shock protein 27) at Ser82. Additionally, CRT5 decreases VEGF-induced endothelial migration, proliferation, and tubulogenesis[1].

BPKDi is a potent and selective inhibitor of PKD (protein kinase D).

1-Naphthyl PP1 (1-NA-PP 1) is a selective Src inhibitor, targeting v-Src and c-Fyn, c-Abl, CDK2, and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18, and 22 μM, respectively.

3-IN-PP1, a potent protein kinase D (PKD) inhibitor, exhibits pan-PKD inhibitory activity with IC50 values of 108 nM for PKD1, 94 nM for PKD2, and 108 nM for PKD3. Additionally, it serves as a broad-spectrum anticancer agent by inhibiting the growth of various tumor cells. 3-IN-PP1 is utilized in cancer research [1].

Protein kinase D inhibitor 1 (compound 17m) is a potent pan-PKD inhibitor with IC50 values between 17 and 35 nM, demonstrating inhibitory activity in the low nanomolar range. By inhibiting protein kinase D, it effectively suppresses PKD-dependent cortactin phosphorylation [1].

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

Protein kinase D (PKD), a serine threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.

CRT0066101 is a potent, orally active PKD inhibitor with IC 50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively [1]. Additionally, it inhibits PIM2 with an IC 50 of approximately 135.7 nM and demonstrates anticancer effects [2].